SMILES stringlengths 71 300 | POI_Name stringclasses 164
values | POI_Sequence stringclasses 133
values | Ligase_Name stringclasses 9
values | Cell_Line stringclasses 155
values | Value_Type stringclasses 2
values | Value_Unit stringclasses 2
values | Value float64 -53.5 100k | Value_Error float64 1 81.3 ⌀ | Value_Range_Min float64 0.1 1.49k ⌀ | Value_Range_Max float64 0.76 1.99k ⌀ | Value_Concentration float64 0.1 100 ⌀ | Assay_Time float64 2 96 ⌀ | Value_Operator stringclasses 5
values | Value_Category stringclasses 2
values | Value_Concentration_Unit stringclasses 2
values | Modality stringclasses 1
value | POI_UniProt stringclasses 131
values | Ligase_UniProt stringclasses 11
values | Ligase_Sequence stringclasses 11
values | Cell_Line_ID stringclasses 154
values | Cell_Line_Species stringclasses 4
values | Reference stringclasses 367
values | Description stringclasses 501
values | Database stringclasses 6
values | Assay stringclasses 21
values | TPD_ID stringlengths 10 10 ⌀ | Cell_Line_Description stringclasses 151
values | POI_Cluster int64 -1 37 | SMILES_Held_Out bool 2
classes | SMILES_Scaffold_Cluster int64 -1 2.35k | SMILES_Butina_Cluster int64 -1 278 |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
COc1cc(OC2C(C)(C)C(NC(=O)c3ccc(N4CCC(CN5CCC6(CC5)COc5cc7c(cc56)n(C)c(=O)n7C5CCC(=O)NC5=O)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | 25 | null | null | null | 100 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1379 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of compounds against AR protein in LNCaP cells. AR-positive human prostate cancer cells (LNCaP FGC) were seeded into six-well microplates in RPMI 1640 containing 10% FBS to a concentration of 1.5×10?/well. After the cells were cultured overnight in a carbon dioxi... | TPDdb | Western Blot | TPD-EWXDAI | African=2.89%; Native American=0.31%; East Asian, North=0%; East Asian, South=2.4%; South Asian=8.61%; European, North=28.39%; European, South=57.41%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Instable (MSI-high).
CVCL_0395 ! LNCaP
Metastatic; Left supraclavicular lymph node;
... | 16 | false | 884 | 74 |
COc1cc(OC2C(C)(C)C(NC(=O)c3ccc(N4CCC(CN5CCC6(CC5)COc5cc7c(cc56)n(C)c(=O)n7C5CCC(=O)NC5=O)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 77.5 | null | null | null | 5 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of AR protein in VCAP cells. AR-positive human prostate cancer cells VCaP were seeded in DMEM containing 10% FBS to a density of 3×105/well in a six-well microplate. After being cultured overnight in a carbon dioxide incubator (ESCO), the prepared compound of the... | TPDdb | Western Blot | TPD-EWXDAI | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 884 | 74 |
COc1cc(OC2C(C)(C)C(NC(=O)c3ccc(N4CCC(F)(CN5CCC6(CCc7cc(F)c(C(=O)N[C@H]8CCC(=O)NC8=O)cc7O6)CC5)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | -34 | null | null | null | 100 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1379 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of compounds against AR protein in LNCaP cells. AR-positive human prostate cancer cells (LNCaP FGC) were seeded into six-well microplates in RPMI 1640 containing 10% FBS to a concentration of 1.5×10?/well. After the cells were cultured overnight in a carbon dioxi... | TPDdb | Western Blot | TPD-Q2GYI6 | African=2.89%; Native American=0.31%; East Asian, North=0%; East Asian, South=2.4%; South Asian=8.61%; European, North=28.39%; European, South=57.41%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Instable (MSI-high).
CVCL_0395 ! LNCaP
Metastatic; Left supraclavicular lymph node;
... | 16 | false | 885 | 0 |
COc1cc(OC2C(C)(C)C(NC(=O)c3ccc(N4CCC(F)(CN5CCC6(CCc7cc(F)c(C(=O)N[C@H]8CCC(=O)NC8=O)cc7O6)CC5)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 15.5 | null | null | null | 5 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of AR protein in VCAP cells. AR-positive human prostate cancer cells VCaP were seeded in DMEM containing 10% FBS to a density of 3×105/well in a six-well microplate. After being cultured overnight in a carbon dioxide incubator (ESCO), the prepared compound of the... | TPDdb | Western Blot | TPD-Q2GYI6 | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 885 | 0 |
COc1cc(OC2C(C)(C)C(NC(=O)c3ccc(N4CCC(N5CCC6(CC5)COc5cc7c(cc56)n(C)c(=O)n7C5CCC(=O)NC5=O)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | 47 | null | null | null | 100 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1379 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of compounds against AR protein in LNCaP cells. AR-positive human prostate cancer cells (LNCaP FGC) were seeded into six-well microplates in RPMI 1640 containing 10% FBS to a concentration of 1.5×10?/well. After the cells were cultured overnight in a carbon dioxi... | TPDdb | Western Blot | TPD-D976CA | African=2.89%; Native American=0.31%; East Asian, North=0%; East Asian, South=2.4%; South Asian=8.61%; European, North=28.39%; European, South=57.41%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Instable (MSI-high).
CVCL_0395 ! LNCaP
Metastatic; Left supraclavicular lymph node;
... | 16 | false | 886 | 97 |
COc1cc(OC2C(C)(C)C(NC(=O)c3ccc(N4CCC(N5CCC6(CC5)COc5cc7c(cc56)n(C)c(=O)n7C5CCC(=O)NC5=O)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 69.5 | null | null | null | 5 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of AR protein in VCAP cells. AR-positive human prostate cancer cells VCaP were seeded in DMEM containing 10% FBS to a density of 3×105/well in a six-well microplate. After being cultured overnight in a carbon dioxide incubator (ESCO), the prepared compound of the... | TPDdb | Western Blot | TPD-D976CA | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 886 | 97 |
COc1cc(OC2C(C)(C)C(NC(=O)c3ccc(N4CCC5(CC4)CC(N4CCC6(CC4)COc4cc7c(cc46)n(C)c(=O)n7C4CCC(=O)NC4=O)C5)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | 53.5 | null | null | null | 100 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1379 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of compounds against AR protein in LNCaP cells. AR-positive human prostate cancer cells (LNCaP FGC) were seeded into six-well microplates in RPMI 1640 containing 10% FBS to a concentration of 1.5×10?/well. After the cells were cultured overnight in a carbon dioxi... | TPDdb | Western Blot | TPD-L2M7OD | African=2.89%; Native American=0.31%; East Asian, North=0%; East Asian, South=2.4%; South Asian=8.61%; European, North=28.39%; European, South=57.41%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Instable (MSI-high).
CVCL_0395 ! LNCaP
Metastatic; Left supraclavicular lymph node;
... | 16 | false | 887 | 97 |
COc1cc(OC2C(C)(C)C(NC(=O)c3ccc(N4CCC5(CC4)CC(N4CCC6(CC4)COc4cc7c(cc46)n(C)c(=O)n7C4CCC(=O)NC4=O)C5)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 64 | null | null | null | 5 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of AR protein in VCAP cells. AR-positive human prostate cancer cells VCaP were seeded in DMEM containing 10% FBS to a density of 3×105/well in a six-well microplate. After being cultured overnight in a carbon dioxide incubator (ESCO), the prepared compound of the... | TPDdb | Western Blot | TPD-L2M7OD | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 887 | 97 |
COc1cc(OC2C(C)(C)C(NC(=O)c3ccc(N4CCC5(CC4)CC(N4CCC6(CC4)COc4cc7c(cc46)n(C)c(=O)n7C4CCC(=O)NC4=O)C5)nn3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | 34 | null | null | null | 100 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1379 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of compounds against AR protein in LNCaP cells. AR-positive human prostate cancer cells (LNCaP FGC) were seeded into six-well microplates in RPMI 1640 containing 10% FBS to a concentration of 1.5×10?/well. After the cells were cultured overnight in a carbon dioxi... | TPDdb | Western Blot | TPD-BITELX | African=2.89%; Native American=0.31%; East Asian, North=0%; East Asian, South=2.4%; South Asian=8.61%; European, North=28.39%; European, South=57.41%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Instable (MSI-high).
CVCL_0395 ! LNCaP
Metastatic; Left supraclavicular lymph node;
... | 16 | true | -1 | -1 |
COc1cc(OC2C(C)(C)C(NC(=O)c3ccc(N4CCC5(CC4)CC(N4CCC6(CC4)COc4cc7c(cc46)n(C)c(=O)n7C4CCC(=O)NC4=O)C5)nn3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 72.5 | null | null | null | 5 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of AR protein in VCAP cells. AR-positive human prostate cancer cells VCaP were seeded in DMEM containing 10% FBS to a density of 3×105/well in a six-well microplate. After being cultured overnight in a carbon dioxide incubator (ESCO), the prepared compound of the... | TPDdb | Western Blot | TPD-BITELX | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | true | -1 | -1 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(C)(CN5CC6(CCC7(CC6)COc6c7ccc7c6CN(C6CCC(=O)NC6=O)C7=O)C5)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | 78.5 | null | null | null | 100 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1379 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of compounds against AR protein in LNCaP cells. AR-positive human prostate cancer cells (LNCaP FGC) were seeded into six-well microplates in RPMI 1640 containing 10% FBS to a concentration of 1.5×10?/well. After the cells were cultured overnight in a carbon dioxi... | TPDdb | Western Blot | TPD-RNRC80 | African=2.89%; Native American=0.31%; East Asian, North=0%; East Asian, South=2.4%; South Asian=8.61%; European, North=28.39%; European, South=57.41%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Instable (MSI-high).
CVCL_0395 ! LNCaP
Metastatic; Left supraclavicular lymph node;
... | 16 | false | 888 | 0 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(C)(CN5CC6(CCC7(CC6)COc6c7ccc7c6CN(C6CCC(=O)NC6=O)C7=O)C5)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 64 | null | null | null | 5 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of AR protein in VCAP cells. AR-positive human prostate cancer cells VCaP were seeded in DMEM containing 10% FBS to a density of 3×105/well in a six-well microplate. After being cultured overnight in a carbon dioxide incubator (ESCO), the prepared compound of the... | TPDdb | Western Blot | TPD-RNRC80 | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 888 | 0 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(C)(CN5CCC6(CC5)COc5c6ccc(C(=O)N[C@H]6CCC(=O)NC6=O)c5F)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | 23.5 | null | null | null | 100 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1379 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of compounds against AR protein in LNCaP cells. AR-positive human prostate cancer cells (LNCaP FGC) were seeded into six-well microplates in RPMI 1640 containing 10% FBS to a concentration of 1.5×10?/well. After the cells were cultured overnight in a carbon dioxi... | TPDdb | Western Blot | TPD-4KTJ90 | African=2.89%; Native American=0.31%; East Asian, North=0%; East Asian, South=2.4%; South Asian=8.61%; European, North=28.39%; European, South=57.41%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Instable (MSI-high).
CVCL_0395 ! LNCaP
Metastatic; Left supraclavicular lymph node;
... | 16 | false | 889 | 97 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(C)(CN5CCC6(CC5)COc5c6ccc(C(=O)N[C@H]6CCC(=O)NC6=O)c5F)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 26 | null | null | null | 5 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of AR protein in VCAP cells. AR-positive human prostate cancer cells VCaP were seeded in DMEM containing 10% FBS to a density of 3×105/well in a six-well microplate. After being cultured overnight in a carbon dioxide incubator (ESCO), the prepared compound of the... | TPDdb | Western Blot | TPD-4KTJ90 | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 889 | 97 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(C)(CN5CCC6(CC5)COc5cc7c(cc56)n(C)c(=O)n7C5CCC(=O)NC5=O)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | 39 | null | null | null | 100 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1379 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of compounds against AR protein in LNCaP cells. AR-positive human prostate cancer cells (LNCaP FGC) were seeded into six-well microplates in RPMI 1640 containing 10% FBS to a concentration of 1.5×10?/well. After the cells were cultured overnight in a carbon dioxi... | TPDdb | Western Blot | TPD-VF8Z3P | African=2.89%; Native American=0.31%; East Asian, North=0%; East Asian, South=2.4%; South Asian=8.61%; European, North=28.39%; European, South=57.41%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Instable (MSI-high).
CVCL_0395 ! LNCaP
Metastatic; Left supraclavicular lymph node;
... | 16 | false | 884 | 97 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(C)(CN5CCC6(CC5)COc5cc7c(cc56)n(C)c(=O)n7C5CCC(=O)NC5=O)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 74.5 | null | null | null | 5 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of AR protein in VCAP cells. AR-positive human prostate cancer cells VCaP were seeded in DMEM containing 10% FBS to a density of 3×105/well in a six-well microplate. After being cultured overnight in a carbon dioxide incubator (ESCO), the prepared compound of the... | TPDdb | Western Blot | TPD-VF8Z3P | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 884 | 97 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(C)(CN5CCC6(CCc7cc(C(=O)N[C@H]8CCC(=O)NC8=O)c(F)cc7O6)CC5)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | 59 | null | null | null | 100 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1379 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of compounds against AR protein in LNCaP cells. AR-positive human prostate cancer cells (LNCaP FGC) were seeded into six-well microplates in RPMI 1640 containing 10% FBS to a concentration of 1.5×10?/well. After the cells were cultured overnight in a carbon dioxi... | TPDdb | Western Blot | TPD-4K1D18 | African=2.89%; Native American=0.31%; East Asian, North=0%; East Asian, South=2.4%; South Asian=8.61%; European, North=28.39%; European, South=57.41%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Instable (MSI-high).
CVCL_0395 ! LNCaP
Metastatic; Left supraclavicular lymph node;
... | 16 | false | 397 | 74 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(C)(CN5CCC6(CCc7cc(C(=O)N[C@H]8CCC(=O)NC8=O)c(F)cc7O6)CC5)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 14 | null | null | null | 5 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of AR protein in VCAP cells. AR-positive human prostate cancer cells VCaP were seeded in DMEM containing 10% FBS to a density of 3×105/well in a six-well microplate. After being cultured overnight in a carbon dioxide incubator (ESCO), the prepared compound of the... | TPDdb | Western Blot | TPD-4K1D18 | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 397 | 74 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(C)(CN5CCC6(CCc7cc(C(=O)N[C@H]8CCC(=O)NC8=O)c(F)cc7O6)CC5)CC4)cn3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | 21.5 | null | null | null | 100 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1379 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of compounds against AR protein in LNCaP cells. AR-positive human prostate cancer cells (LNCaP FGC) were seeded into six-well microplates in RPMI 1640 containing 10% FBS to a concentration of 1.5×10?/well. After the cells were cultured overnight in a carbon dioxi... | TPDdb | Western Blot | TPD-AK6RYG | African=2.89%; Native American=0.31%; East Asian, North=0%; East Asian, South=2.4%; South Asian=8.61%; European, North=28.39%; European, South=57.41%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Instable (MSI-high).
CVCL_0395 ! LNCaP
Metastatic; Left supraclavicular lymph node;
... | 16 | false | 890 | 74 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(C)(CN5CCC6(CCc7cc(C(=O)N[C@H]8CCC(=O)NC8=O)c(F)cc7O6)CC5)CC4)cn3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 32.5 | null | null | null | 5 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of AR protein in VCAP cells. AR-positive human prostate cancer cells VCaP were seeded in DMEM containing 10% FBS to a density of 3×105/well in a six-well microplate. After being cultured overnight in a carbon dioxide incubator (ESCO), the prepared compound of the... | TPDdb | Western Blot | TPD-AK6RYG | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 890 | 74 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(C)(CN5CCC6(CCc7cc(C(=O)N[C@H]8CCC(=O)NC8=O)c(F)cc7O6)CC5)CC4)nc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | 55 | null | null | null | 100 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1379 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of compounds against AR protein in LNCaP cells. AR-positive human prostate cancer cells (LNCaP FGC) were seeded into six-well microplates in RPMI 1640 containing 10% FBS to a concentration of 1.5×10?/well. After the cells were cultured overnight in a carbon dioxi... | TPDdb | Western Blot | TPD-IF08QI | African=2.89%; Native American=0.31%; East Asian, North=0%; East Asian, South=2.4%; South Asian=8.61%; European, North=28.39%; European, South=57.41%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Instable (MSI-high).
CVCL_0395 ! LNCaP
Metastatic; Left supraclavicular lymph node;
... | 16 | true | -1 | -1 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(C)(CN5CCC6(CCc7cc(C(=O)N[C@H]8CCC(=O)NC8=O)c(F)cc7O6)CC5)CC4)nc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 15 | null | null | null | 5 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of AR protein in VCAP cells. AR-positive human prostate cancer cells VCaP were seeded in DMEM containing 10% FBS to a density of 3×105/well in a six-well microplate. After being cultured overnight in a carbon dioxide incubator (ESCO), the prepared compound of the... | TPDdb | Western Blot | TPD-IF08QI | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | true | -1 | -1 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(C)(CN5CCC6(CCc7cc(C(=O)N[C@H]8CCC(=O)NC8=O)c(F)cc7O6)CC5)CC4)nn3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | 54 | null | null | null | 100 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1379 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of compounds against AR protein in LNCaP cells. AR-positive human prostate cancer cells (LNCaP FGC) were seeded into six-well microplates in RPMI 1640 containing 10% FBS to a concentration of 1.5×10?/well. After the cells were cultured overnight in a carbon dioxi... | TPDdb | Western Blot | TPD-TQIHMG | African=2.89%; Native American=0.31%; East Asian, North=0%; East Asian, South=2.4%; South Asian=8.61%; European, North=28.39%; European, South=57.41%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Instable (MSI-high).
CVCL_0395 ! LNCaP
Metastatic; Left supraclavicular lymph node;
... | 16 | true | -1 | -1 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(C)(CN5CCC6(CCc7cc(C(=O)N[C@H]8CCC(=O)NC8=O)c(F)cc7O6)CC5)CC4)nn3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | -12 | null | null | null | 5 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of AR protein in VCAP cells. AR-positive human prostate cancer cells VCaP were seeded in DMEM containing 10% FBS to a density of 3×105/well in a six-well microplate. After being cultured overnight in a carbon dioxide incubator (ESCO), the prepared compound of the... | TPDdb | Western Blot | TPD-TQIHMG | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | true | -1 | -1 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(C)(CN5CCC6(CCc7cc(F)c(C(=O)N[C@H]8CCC(=O)NC8=O)cc7O6)CC5)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | -1 | null | null | null | 100 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1379 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of compounds against AR protein in LNCaP cells. AR-positive human prostate cancer cells (LNCaP FGC) were seeded into six-well microplates in RPMI 1640 containing 10% FBS to a concentration of 1.5×10?/well. After the cells were cultured overnight in a carbon dioxi... | TPDdb | Western Blot | TPD-JL2PW1 | African=2.89%; Native American=0.31%; East Asian, North=0%; East Asian, South=2.4%; South Asian=8.61%; European, North=28.39%; European, South=57.41%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Instable (MSI-high).
CVCL_0395 ! LNCaP
Metastatic; Left supraclavicular lymph node;
... | 16 | false | 885 | 0 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(C)(CN5CCC6(CCc7cc(F)c(C(=O)N[C@H]8CCC(=O)NC8=O)cc7O6)CC5)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | -13 | null | null | null | 5 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of AR protein in VCAP cells. AR-positive human prostate cancer cells VCaP were seeded in DMEM containing 10% FBS to a density of 3×105/well in a six-well microplate. After being cultured overnight in a carbon dioxide incubator (ESCO), the prepared compound of the... | TPDdb | Western Blot | TPD-JL2PW1 | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 885 | 0 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5CC6(CCC7(CC6)COc6c7ccc7c6CN(C6CCC(=O)NC6=O)C7=O)C5)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | 64.5 | null | null | null | 100 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1379 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of compounds against AR protein in LNCaP cells. AR-positive human prostate cancer cells (LNCaP FGC) were seeded into six-well microplates in RPMI 1640 containing 10% FBS to a concentration of 1.5×10?/well. After the cells were cultured overnight in a carbon dioxi... | TPDdb | Western Blot | TPD-BI17H4 | African=2.89%; Native American=0.31%; East Asian, North=0%; East Asian, South=2.4%; South Asian=8.61%; European, North=28.39%; European, South=57.41%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Instable (MSI-high).
CVCL_0395 ! LNCaP
Metastatic; Left supraclavicular lymph node;
... | 16 | false | 888 | 0 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5CC6(CCC7(CC6)COc6c7ccc7c6CN(C6CCC(=O)NC6=O)C7=O)C5)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 70 | null | null | null | 5 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of AR protein in VCAP cells. AR-positive human prostate cancer cells VCaP were seeded in DMEM containing 10% FBS to a density of 3×105/well in a six-well microplate. After being cultured overnight in a carbon dioxide incubator (ESCO), the prepared compound of the... | TPDdb | Western Blot | TPD-BI17H4 | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 888 | 0 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5CCC6(CC5)COc5c6ccc(C(=O)N[C@H]6CCC(=O)NC6=O)c5F)(OC)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | 38 | null | null | null | 100 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1379 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of compounds against AR protein in LNCaP cells. AR-positive human prostate cancer cells (LNCaP FGC) were seeded into six-well microplates in RPMI 1640 containing 10% FBS to a concentration of 1.5×10?/well. After the cells were cultured overnight in a carbon dioxi... | TPDdb | Western Blot | TPD-8VWIDM | African=2.89%; Native American=0.31%; East Asian, North=0%; East Asian, South=2.4%; South Asian=8.61%; European, North=28.39%; European, South=57.41%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Instable (MSI-high).
CVCL_0395 ! LNCaP
Metastatic; Left supraclavicular lymph node;
... | 16 | false | 889 | 74 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5CCC6(CC5)COc5c6ccc(C(=O)N[C@H]6CCC(=O)NC6=O)c5F)(OC)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | -14.5 | null | null | null | 5 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of AR protein in VCAP cells. AR-positive human prostate cancer cells VCaP were seeded in DMEM containing 10% FBS to a density of 3×105/well in a six-well microplate. After being cultured overnight in a carbon dioxide incubator (ESCO), the prepared compound of the... | TPDdb | Western Blot | TPD-8VWIDM | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 889 | 74 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5CCC6(CC5)COc5c6ccc(C(=O)N[C@H]6CCC(=O)NC6=O)c5F)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | 53 | null | null | null | 100 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1379 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of compounds against AR protein in LNCaP cells. AR-positive human prostate cancer cells (LNCaP FGC) were seeded into six-well microplates in RPMI 1640 containing 10% FBS to a concentration of 1.5×10?/well. After the cells were cultured overnight in a carbon dioxi... | TPDdb | Western Blot | TPD-T8009T | African=2.89%; Native American=0.31%; East Asian, North=0%; East Asian, South=2.4%; South Asian=8.61%; European, North=28.39%; European, South=57.41%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Instable (MSI-high).
CVCL_0395 ! LNCaP
Metastatic; Left supraclavicular lymph node;
... | 16 | false | 889 | 74 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5CCC6(CC5)COc5c6ccc(C(=O)N[C@H]6CCC(=O)NC6=O)c5F)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 51 | null | null | null | 5 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of AR protein in VCAP cells. AR-positive human prostate cancer cells VCaP were seeded in DMEM containing 10% FBS to a density of 3×105/well in a six-well microplate. After being cultured overnight in a carbon dioxide incubator (ESCO), the prepared compound of the... | TPDdb | Western Blot | TPD-T8009T | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 889 | 74 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5CCC6(CC5)COc5c6ccc(C(=O)N[C@H]6CCC(=O)NC6=O)c5OC)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | 6 | null | null | null | 100 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1379 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of compounds against AR protein in LNCaP cells. AR-positive human prostate cancer cells (LNCaP FGC) were seeded into six-well microplates in RPMI 1640 containing 10% FBS to a concentration of 1.5×10?/well. After the cells were cultured overnight in a carbon dioxi... | TPDdb | Western Blot | TPD-S5YGG3 | African=2.89%; Native American=0.31%; East Asian, North=0%; East Asian, South=2.4%; South Asian=8.61%; European, North=28.39%; European, South=57.41%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Instable (MSI-high).
CVCL_0395 ! LNCaP
Metastatic; Left supraclavicular lymph node;
... | 16 | false | 889 | 74 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5CCC6(CC5)COc5c6ccc6c5n(C)c(=O)n6C5CCC(=O)NC5=O)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | 48 | null | null | null | 100 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1379 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of compounds against AR protein in LNCaP cells. AR-positive human prostate cancer cells (LNCaP FGC) were seeded into six-well microplates in RPMI 1640 containing 10% FBS to a concentration of 1.5×10?/well. After the cells were cultured overnight in a carbon dioxi... | TPDdb | Western Blot | TPD-57NYNE | African=2.89%; Native American=0.31%; East Asian, North=0%; East Asian, South=2.4%; South Asian=8.61%; European, North=28.39%; European, South=57.41%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Instable (MSI-high).
CVCL_0395 ! LNCaP
Metastatic; Left supraclavicular lymph node;
... | 16 | false | 891 | 74 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5CCC6(CC5)COc5c6ccc6c5n(C)c(=O)n6C5CCC(=O)NC5=O)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 80 | null | null | null | 5 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of AR protein in VCAP cells. AR-positive human prostate cancer cells VCaP were seeded in DMEM containing 10% FBS to a density of 3×105/well in a six-well microplate. After being cultured overnight in a carbon dioxide incubator (ESCO), the prepared compound of the... | TPDdb | Western Blot | TPD-57NYNE | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 891 | 74 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5CCC6(CC5)COc5c6ccc6c5n(C)c(=O)n6C5CCC(=O)NC5=O)CC4)nn3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | 43 | null | null | null | 100 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1379 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of compounds against AR protein in LNCaP cells. AR-positive human prostate cancer cells (LNCaP FGC) were seeded into six-well microplates in RPMI 1640 containing 10% FBS to a concentration of 1.5×10?/well. After the cells were cultured overnight in a carbon dioxi... | TPDdb | Western Blot | TPD-H8QLWE | African=2.89%; Native American=0.31%; East Asian, North=0%; East Asian, South=2.4%; South Asian=8.61%; European, North=28.39%; European, South=57.41%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Instable (MSI-high).
CVCL_0395 ! LNCaP
Metastatic; Left supraclavicular lymph node;
... | 16 | true | -1 | -1 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5CCC6(CC5)COc5c6ccc6c5n(C)c(=O)n6C5CCC(=O)NC5=O)CC4)nn3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 79 | null | null | null | 5 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of AR protein in VCAP cells. AR-positive human prostate cancer cells VCaP were seeded in DMEM containing 10% FBS to a density of 3×105/well in a six-well microplate. After being cultured overnight in a carbon dioxide incubator (ESCO), the prepared compound of the... | TPDdb | Western Blot | TPD-H8QLWE | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | true | -1 | -1 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5CCC6(CCc7cc(C(=O)N[C@H]8CCC(=O)NC8=O)c(F)cc7O6)CC5)(OC)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | 61 | null | null | null | 100 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1379 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of compounds against AR protein in LNCaP cells. AR-positive human prostate cancer cells (LNCaP FGC) were seeded into six-well microplates in RPMI 1640 containing 10% FBS to a concentration of 1.5×10?/well. After the cells were cultured overnight in a carbon dioxi... | TPDdb | Western Blot | TPD-17KNTK | African=2.89%; Native American=0.31%; East Asian, North=0%; East Asian, South=2.4%; South Asian=8.61%; European, North=28.39%; European, South=57.41%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Instable (MSI-high).
CVCL_0395 ! LNCaP
Metastatic; Left supraclavicular lymph node;
... | 16 | false | 397 | 74 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5CCC6(CCc7cc(C(=O)N[C@H]8CCC(=O)NC8=O)c(F)cc7O6)CC5)(OC)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 27 | null | null | null | 5 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of AR protein in VCAP cells. AR-positive human prostate cancer cells VCaP were seeded in DMEM containing 10% FBS to a density of 3×105/well in a six-well microplate. After being cultured overnight in a carbon dioxide incubator (ESCO), the prepared compound of the... | TPDdb | Western Blot | TPD-17KNTK | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 397 | 74 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5CCC6(CCc7cc(C(=O)N[C@H]8CCC(=O)NC8=O)c(F)cc7O6)CC5)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | 59.5 | null | null | null | 100 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1379 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of compounds against AR protein in LNCaP cells. AR-positive human prostate cancer cells (LNCaP FGC) were seeded into six-well microplates in RPMI 1640 containing 10% FBS to a concentration of 1.5×10?/well. After the cells were cultured overnight in a carbon dioxi... | TPDdb | Western Blot | TPD-LY4LCY | African=2.89%; Native American=0.31%; East Asian, North=0%; East Asian, South=2.4%; South Asian=8.61%; European, North=28.39%; European, South=57.41%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Instable (MSI-high).
CVCL_0395 ! LNCaP
Metastatic; Left supraclavicular lymph node;
... | 16 | false | 397 | 74 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5CCC6(CCc7cc(C(=O)N[C@H]8CCC(=O)NC8=O)c(F)cc7O6)CC5)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 53.5 | null | null | null | 5 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of AR protein in VCAP cells. AR-positive human prostate cancer cells VCaP were seeded in DMEM containing 10% FBS to a density of 3×105/well in a six-well microplate. After being cultured overnight in a carbon dioxide incubator (ESCO), the prepared compound of the... | TPDdb | Western Blot | TPD-LY4LCY | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 397 | 74 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5CCC6(CCc7cc(C(=O)N[C@H]8CCC(=O)NC8=O)c(F)cc7O6)CC5)CC4)nc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | 84.5 | null | null | null | 100 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1379 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of compounds against AR protein in LNCaP cells. AR-positive human prostate cancer cells (LNCaP FGC) were seeded into six-well microplates in RPMI 1640 containing 10% FBS to a concentration of 1.5×10?/well. After the cells were cultured overnight in a carbon dioxi... | TPDdb | Western Blot | TPD-3ZVLNO | African=2.89%; Native American=0.31%; East Asian, North=0%; East Asian, South=2.4%; South Asian=8.61%; European, North=28.39%; European, South=57.41%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Instable (MSI-high).
CVCL_0395 ! LNCaP
Metastatic; Left supraclavicular lymph node;
... | 16 | true | -1 | -1 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5CCC6(CCc7cc(C(=O)N[C@H]8CCC(=O)NC8=O)c(F)cc7O6)CC5)CC4)nc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 70 | null | null | null | 5 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of AR protein in VCAP cells. AR-positive human prostate cancer cells VCaP were seeded in DMEM containing 10% FBS to a density of 3×105/well in a six-well microplate. After being cultured overnight in a carbon dioxide incubator (ESCO), the prepared compound of the... | TPDdb | Western Blot | TPD-3ZVLNO | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | true | -1 | -1 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5CCC6(CCc7cc(C(=O)N[C@H]8CCC(=O)NC8=O)c(F)cc7O6)CC5)CC4)nn3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | 78.5 | null | null | null | 100 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1379 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of compounds against AR protein in LNCaP cells. AR-positive human prostate cancer cells (LNCaP FGC) were seeded into six-well microplates in RPMI 1640 containing 10% FBS to a concentration of 1.5×10?/well. After the cells were cultured overnight in a carbon dioxi... | TPDdb | Western Blot | TPD-GWVUR7 | African=2.89%; Native American=0.31%; East Asian, North=0%; East Asian, South=2.4%; South Asian=8.61%; European, North=28.39%; European, South=57.41%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Instable (MSI-high).
CVCL_0395 ! LNCaP
Metastatic; Left supraclavicular lymph node;
... | 16 | true | -1 | -1 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5CCC6(CCc7cc(C(=O)N[C@H]8CCC(=O)NC8=O)c(F)cc7O6)CC5)CC4)nn3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 23.5 | null | null | null | 5 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of AR protein in VCAP cells. AR-positive human prostate cancer cells VCaP were seeded in DMEM containing 10% FBS to a density of 3×105/well in a six-well microplate. After being cultured overnight in a carbon dioxide incubator (ESCO), the prepared compound of the... | TPDdb | Western Blot | TPD-GWVUR7 | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | true | -1 | -1 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5CCC6(CCc7cc(F)c(C(=O)N[C@H]8CCC(=O)NC8=O)cc7O6)CC5)(OC)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | 36 | null | null | null | 100 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1379 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of compounds against AR protein in LNCaP cells. AR-positive human prostate cancer cells (LNCaP FGC) were seeded into six-well microplates in RPMI 1640 containing 10% FBS to a concentration of 1.5×10?/well. After the cells were cultured overnight in a carbon dioxi... | TPDdb | Western Blot | TPD-DKLW1W | African=2.89%; Native American=0.31%; East Asian, North=0%; East Asian, South=2.4%; South Asian=8.61%; European, North=28.39%; European, South=57.41%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Instable (MSI-high).
CVCL_0395 ! LNCaP
Metastatic; Left supraclavicular lymph node;
... | 16 | false | 885 | 74 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5CCC6(CCc7cc(F)c(C(=O)N[C@H]8CCC(=O)NC8=O)cc7O6)CC5)(OC)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 1 | null | null | null | 5 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of AR protein in VCAP cells. AR-positive human prostate cancer cells VCaP were seeded in DMEM containing 10% FBS to a density of 3×105/well in a six-well microplate. After being cultured overnight in a carbon dioxide incubator (ESCO), the prepared compound of the... | TPDdb | Western Blot | TPD-DKLW1W | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 885 | 74 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5CCC6(CCc7cc(F)c(C(=O)N[C@H]8CCC(=O)NC8=O)cc7O6)CC5)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | 30.5 | null | null | null | 100 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1379 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of compounds against AR protein in LNCaP cells. AR-positive human prostate cancer cells (LNCaP FGC) were seeded into six-well microplates in RPMI 1640 containing 10% FBS to a concentration of 1.5×10?/well. After the cells were cultured overnight in a carbon dioxi... | TPDdb | Western Blot | TPD-4KMUUR | African=2.89%; Native American=0.31%; East Asian, North=0%; East Asian, South=2.4%; South Asian=8.61%; European, North=28.39%; European, South=57.41%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Instable (MSI-high).
CVCL_0395 ! LNCaP
Metastatic; Left supraclavicular lymph node;
... | 16 | false | 885 | 0 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5CCC6(CCc7cc(F)c(C(=O)N[C@H]8CCC(=O)NC8=O)cc7O6)CC5)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 1.5 | null | null | null | 5 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of AR protein in VCAP cells. AR-positive human prostate cancer cells VCaP were seeded in DMEM containing 10% FBS to a density of 3×105/well in a six-well microplate. After being cultured overnight in a carbon dioxide incubator (ESCO), the prepared compound of the... | TPDdb | Western Blot | TPD-4KMUUR | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 885 | 0 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5CCN6c7cc(F)c(C(=O)N[C@H]8CCC(=O)NC8=O)cc7OC[C@H]6C5)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | 47.5 | null | null | null | 100 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1379 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of compounds against AR protein in LNCaP cells. AR-positive human prostate cancer cells (LNCaP FGC) were seeded into six-well microplates in RPMI 1640 containing 10% FBS to a concentration of 1.5×10?/well. After the cells were cultured overnight in a carbon dioxi... | TPDdb | Western Blot | TPD-KUUB56 | African=2.89%; Native American=0.31%; East Asian, North=0%; East Asian, South=2.4%; South Asian=8.61%; European, North=28.39%; European, South=57.41%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Instable (MSI-high).
CVCL_0395 ! LNCaP
Metastatic; Left supraclavicular lymph node;
... | 16 | false | 383 | 74 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5CCN6c7ccc(C(=O)N[C@H]8CCC(=O)NC8=O)cc7OC[C@@H]6C5)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | 70 | null | null | null | 100 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1379 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of compounds against AR protein in LNCaP cells. AR-positive human prostate cancer cells (LNCaP FGC) were seeded into six-well microplates in RPMI 1640 containing 10% FBS to a concentration of 1.5×10?/well. After the cells were cultured overnight in a carbon dioxi... | TPDdb | Western Blot | TPD-ZT4S7K | African=2.89%; Native American=0.31%; East Asian, North=0%; East Asian, South=2.4%; South Asian=8.61%; European, North=28.39%; European, South=57.41%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Instable (MSI-high).
CVCL_0395 ! LNCaP
Metastatic; Left supraclavicular lymph node;
... | 16 | false | 383 | 0 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5CCN6c7ccc(C(=O)N[C@H]8CCC(=O)NC8=O)cc7OC[C@@H]6C5)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 45 | null | null | null | 5 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of AR protein in VCAP cells. AR-positive human prostate cancer cells VCaP were seeded in DMEM containing 10% FBS to a density of 3×105/well in a six-well microplate. After being cultured overnight in a carbon dioxide incubator (ESCO), the prepared compound of the... | TPDdb | Western Blot | TPD-ZT4S7K | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 383 | 0 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5CCN6c7ccc(N[C@H]8CCC(=O)NC8=O)cc7OC[C@@H]6C5)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | 24.5 | null | null | null | 100 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1379 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of compounds against AR protein in LNCaP cells. AR-positive human prostate cancer cells (LNCaP FGC) were seeded into six-well microplates in RPMI 1640 containing 10% FBS to a concentration of 1.5×10?/well. After the cells were cultured overnight in a carbon dioxi... | TPDdb | Western Blot | TPD-8G1T2A | African=2.89%; Native American=0.31%; East Asian, North=0%; East Asian, South=2.4%; South Asian=8.61%; European, North=28.39%; European, South=57.41%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Instable (MSI-high).
CVCL_0395 ! LNCaP
Metastatic; Left supraclavicular lymph node;
... | 16 | false | 892 | 74 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5CCN6c7ccc(N[C@H]8CCC(=O)NC8=O)cc7OC[C@@H]6C5)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 0.5 | null | null | null | 5 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of AR protein in VCAP cells. AR-positive human prostate cancer cells VCaP were seeded in DMEM containing 10% FBS to a density of 3×105/well in a six-well microplate. After being cultured overnight in a carbon dioxide incubator (ESCO), the prepared compound of the... | TPDdb | Western Blot | TPD-8G1T2A | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 892 | 74 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5CCc6c(ccc7c(C8CCC(=O)NC8=O)noc67)C5)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | DC50 | nM | 5 | null | null | null | null | null | < | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CYCLOBUTYL-CONTAINING COMPOUNDS (patent) | Compounds' Effects on AR Degradation in Cells
1.1 Assay for AR Degradation in VCaP Cells
Detection was performed using the HTRF Human Androgen Receptor Detection Kit. 4× Supplemented Lysis Buffer was prepared using 100× Blocking Reagent Stock Solution and 4× Lysis Buffer Stock Solution. 1× Supplemented Lysis Buffer was... | TPDdb | HTRF | TPD-21G322 | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 893 | 74 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5CCc6c(ccc7c(C8CCC(=O)NC8=O)noc67)C5)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 75 | null | null | null | null | null | > | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CYCLOBUTYL-CONTAINING COMPOUNDS (patent) | Compounds' Effects on AR Degradation in Cells
1.1 Assay for AR Degradation in VCaP Cells
Detection was performed using the HTRF Human Androgen Receptor Detection Kit. 4× Supplemented Lysis Buffer was prepared using 100× Blocking Reagent Stock Solution and 4× Lysis Buffer Stock Solution. 1× Supplemented Lysis Buffer was... | TPDdb | HTRF | TPD-21G322 | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 893 | 74 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5CCc6c(ccc7c(C8CCC(=O)NC8=O)noc67)C5)CC4)nc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | DC50 | nM | 5 | null | null | null | null | null | < | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CYCLOBUTYL-CONTAINING COMPOUNDS (patent) | Compounds' Effects on AR Degradation in Cells
1.1 Assay for AR Degradation in VCaP Cells
Detection was performed using the HTRF Human Androgen Receptor Detection Kit. 4× Supplemented Lysis Buffer was prepared using 100× Blocking Reagent Stock Solution and 4× Lysis Buffer Stock Solution. 1× Supplemented Lysis Buffer was... | TPDdb | HTRF | TPD-XB6XKK | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 894 | 166 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5CCc6c(ccc7c(C8CCC(=O)NC8=O)noc67)C5)CC4)nc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 75 | null | null | null | null | null | > | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CYCLOBUTYL-CONTAINING COMPOUNDS (patent) | Compounds' Effects on AR Degradation in Cells
1.1 Assay for AR Degradation in VCaP Cells
Detection was performed using the HTRF Human Androgen Receptor Detection Kit. 4× Supplemented Lysis Buffer was prepared using 100× Blocking Reagent Stock Solution and 4× Lysis Buffer Stock Solution. 1× Supplemented Lysis Buffer was... | TPDdb | HTRF | TPD-XB6XKK | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 894 | 166 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5CCc6c(ccc7c(C8CCC(=O)NC8=O)noc67)C5)CC4)nn3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | DC50 | nM | 5 | null | null | null | null | null | < | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CYCLOBUTYL-CONTAINING COMPOUNDS (patent) | Compounds' Effects on AR Degradation in Cells
1.1 Assay for AR Degradation in VCaP Cells
Detection was performed using the HTRF Human Androgen Receptor Detection Kit. 4× Supplemented Lysis Buffer was prepared using 100× Blocking Reagent Stock Solution and 4× Lysis Buffer Stock Solution. 1× Supplemented Lysis Buffer was... | TPDdb | HTRF | TPD-HNNRVB | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 895 | 166 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5CCc6c(ccc7c(C8CCC(=O)NC8=O)noc67)C5)CC4)nn3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 75 | null | null | null | null | null | > | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CYCLOBUTYL-CONTAINING COMPOUNDS (patent) | Compounds' Effects on AR Degradation in Cells
1.1 Assay for AR Degradation in VCaP Cells
Detection was performed using the HTRF Human Androgen Receptor Detection Kit. 4× Supplemented Lysis Buffer was prepared using 100× Blocking Reagent Stock Solution and 4× Lysis Buffer Stock Solution. 1× Supplemented Lysis Buffer was... | TPDdb | HTRF | TPD-HNNRVB | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 895 | 166 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5CCc6ccc7c(C8CCC(=O)NC8=O)noc7c6CC5)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | DC50 | nM | 5 | null | null | null | null | null | < | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CYCLOBUTYL-CONTAINING COMPOUNDS (patent) | Compounds' Effects on AR Degradation in Cells
1.1 Assay for AR Degradation in VCaP Cells
Detection was performed using the HTRF Human Androgen Receptor Detection Kit. 4× Supplemented Lysis Buffer was prepared using 100× Blocking Reagent Stock Solution and 4× Lysis Buffer Stock Solution. 1× Supplemented Lysis Buffer was... | TPDdb | HTRF | TPD-ZXCJFU | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 896 | 74 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5CCc6ccc7c(C8CCC(=O)NC8=O)noc7c6CC5)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 75 | null | null | null | null | null | > | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CYCLOBUTYL-CONTAINING COMPOUNDS (patent) | Compounds' Effects on AR Degradation in Cells
1.1 Assay for AR Degradation in VCaP Cells
Detection was performed using the HTRF Human Androgen Receptor Detection Kit. 4× Supplemented Lysis Buffer was prepared using 100× Blocking Reagent Stock Solution and 4× Lysis Buffer Stock Solution. 1× Supplemented Lysis Buffer was... | TPDdb | HTRF | TPD-ZXCJFU | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 896 | 74 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5CCc6ccc7c(C8CCC(=O)NC8=O)noc7c6CC5)CC4)nc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | DC50 | nM | 5 | null | null | null | null | null | < | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CYCLOBUTYL-CONTAINING COMPOUNDS (patent) | Compounds' Effects on AR Degradation in Cells
1.1 Assay for AR Degradation in VCaP Cells
Detection was performed using the HTRF Human Androgen Receptor Detection Kit. 4× Supplemented Lysis Buffer was prepared using 100× Blocking Reagent Stock Solution and 4× Lysis Buffer Stock Solution. 1× Supplemented Lysis Buffer was... | TPDdb | HTRF | TPD-OS0HLB | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 897 | 166 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5CCc6ccc7c(C8CCC(=O)NC8=O)noc7c6CC5)CC4)nc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 75 | null | null | null | null | null | > | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CYCLOBUTYL-CONTAINING COMPOUNDS (patent) | Compounds' Effects on AR Degradation in Cells
1.1 Assay for AR Degradation in VCaP Cells
Detection was performed using the HTRF Human Androgen Receptor Detection Kit. 4× Supplemented Lysis Buffer was prepared using 100× Blocking Reagent Stock Solution and 4× Lysis Buffer Stock Solution. 1× Supplemented Lysis Buffer was... | TPDdb | HTRF | TPD-OS0HLB | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 897 | 166 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5Cc6ccc7c(C8CCC(=O)NC8=O)noc7c6C5)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | DC50 | nM | 5 | null | null | null | null | null | < | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CYCLOBUTYL-CONTAINING COMPOUNDS (patent) | Compounds' Effects on AR Degradation in Cells
1.1 Assay for AR Degradation in VCaP Cells
Detection was performed using the HTRF Human Androgen Receptor Detection Kit. 4× Supplemented Lysis Buffer was prepared using 100× Blocking Reagent Stock Solution and 4× Lysis Buffer Stock Solution. 1× Supplemented Lysis Buffer was... | TPDdb | HTRF | TPD-5E6GME | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 898 | 74 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5Cc6ccc7c(C8CCC(=O)NC8=O)noc7c6C5)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 75 | null | null | null | null | null | > | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CYCLOBUTYL-CONTAINING COMPOUNDS (patent) | Compounds' Effects on AR Degradation in Cells
1.1 Assay for AR Degradation in VCaP Cells
Detection was performed using the HTRF Human Androgen Receptor Detection Kit. 4× Supplemented Lysis Buffer was prepared using 100× Blocking Reagent Stock Solution and 4× Lysis Buffer Stock Solution. 1× Supplemented Lysis Buffer was... | TPDdb | HTRF | TPD-5E6GME | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 898 | 74 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5Cc6ccc7c(C8CCC(=O)NC8=O)noc7c6C5)CC4)nc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | DC50 | nM | 5 | null | null | null | null | null | < | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CYCLOBUTYL-CONTAINING COMPOUNDS (patent) | Compounds' Effects on AR Degradation in Cells
1.1 Assay for AR Degradation in VCaP Cells
Detection was performed using the HTRF Human Androgen Receptor Detection Kit. 4× Supplemented Lysis Buffer was prepared using 100× Blocking Reagent Stock Solution and 4× Lysis Buffer Stock Solution. 1× Supplemented Lysis Buffer was... | TPDdb | HTRF | TPD-MT4CJH | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 899 | 166 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(CN5Cc6ccc7c(C8CCC(=O)NC8=O)noc7c6C5)CC4)nc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 75 | null | null | null | null | null | > | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CYCLOBUTYL-CONTAINING COMPOUNDS (patent) | Compounds' Effects on AR Degradation in Cells
1.1 Assay for AR Degradation in VCaP Cells
Detection was performed using the HTRF Human Androgen Receptor Detection Kit. 4× Supplemented Lysis Buffer was prepared using 100× Blocking Reagent Stock Solution and 4× Lysis Buffer Stock Solution. 1× Supplemented Lysis Buffer was... | TPDdb | HTRF | TPD-MT4CJH | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 899 | 166 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(F)(CN5CC6(CCC7(CC6)COc6c7ccc7c6CN(C6CCC(=O)NC6=O)C7=O)C5)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | 52.5 | null | null | null | 100 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1379 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of compounds against AR protein in LNCaP cells. AR-positive human prostate cancer cells (LNCaP FGC) were seeded into six-well microplates in RPMI 1640 containing 10% FBS to a concentration of 1.5×10?/well. After the cells were cultured overnight in a carbon dioxi... | TPDdb | Western Blot | TPD-UF4E1Q | African=2.89%; Native American=0.31%; East Asian, North=0%; East Asian, South=2.4%; South Asian=8.61%; European, North=28.39%; European, South=57.41%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Instable (MSI-high).
CVCL_0395 ! LNCaP
Metastatic; Left supraclavicular lymph node;
... | 16 | false | 888 | 0 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(F)(CN5CC6(CCC7(CC6)COc6c7ccc7c6CN(C6CCC(=O)NC6=O)C7=O)C5)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 55.5 | null | null | null | 5 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of AR protein in VCAP cells. AR-positive human prostate cancer cells VCaP were seeded in DMEM containing 10% FBS to a density of 3×105/well in a six-well microplate. After being cultured overnight in a carbon dioxide incubator (ESCO), the prepared compound of the... | TPDdb | Western Blot | TPD-UF4E1Q | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 888 | 0 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(F)(CN5CCC6(CC5)COc5cc7c(cc56)n(C)c(=O)n7C5CCC(=O)NC5=O)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | 33.5 | null | null | null | 100 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1379 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of compounds against AR protein in LNCaP cells. AR-positive human prostate cancer cells (LNCaP FGC) were seeded into six-well microplates in RPMI 1640 containing 10% FBS to a concentration of 1.5×10?/well. After the cells were cultured overnight in a carbon dioxi... | TPDdb | Western Blot | TPD-XV6OIA | African=2.89%; Native American=0.31%; East Asian, North=0%; East Asian, South=2.4%; South Asian=8.61%; European, North=28.39%; European, South=57.41%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Instable (MSI-high).
CVCL_0395 ! LNCaP
Metastatic; Left supraclavicular lymph node;
... | 16 | false | 884 | 97 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(F)(CN5CCC6(CC5)COc5cc7c(cc56)n(C)c(=O)n7C5CCC(=O)NC5=O)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 60.5 | null | null | null | 5 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of AR protein in VCAP cells. AR-positive human prostate cancer cells VCaP were seeded in DMEM containing 10% FBS to a density of 3×105/well in a six-well microplate. After being cultured overnight in a carbon dioxide incubator (ESCO), the prepared compound of the... | TPDdb | Western Blot | TPD-XV6OIA | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 884 | 97 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(F)(CN5CCC6(CCc7cc(C(=O)N[C@H]8CCC(=O)NC8=O)c(F)cc7O6)CC5)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | -16.5 | null | null | null | 100 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1379 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of compounds against AR protein in LNCaP cells. AR-positive human prostate cancer cells (LNCaP FGC) were seeded into six-well microplates in RPMI 1640 containing 10% FBS to a concentration of 1.5×10?/well. After the cells were cultured overnight in a carbon dioxi... | TPDdb | Western Blot | TPD-KXEE4Z | African=2.89%; Native American=0.31%; East Asian, North=0%; East Asian, South=2.4%; South Asian=8.61%; European, North=28.39%; European, South=57.41%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Instable (MSI-high).
CVCL_0395 ! LNCaP
Metastatic; Left supraclavicular lymph node;
... | 16 | false | 397 | 74 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(F)(CN5CCC6(CCc7cc(C(=O)N[C@H]8CCC(=O)NC8=O)c(F)cc7O6)CC5)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 6.5 | null | null | null | 5 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of AR protein in VCAP cells. AR-positive human prostate cancer cells VCaP were seeded in DMEM containing 10% FBS to a density of 3×105/well in a six-well microplate. After being cultured overnight in a carbon dioxide incubator (ESCO), the prepared compound of the... | TPDdb | Western Blot | TPD-KXEE4Z | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 397 | 74 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(F)(CN5CCCOc6c(ccc(C(=O)N[C@H]7CCC(=O)NC7=O)c6F)CC5)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | 13.5 | null | null | null | 100 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1379 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of compounds against AR protein in LNCaP cells. AR-positive human prostate cancer cells (LNCaP FGC) were seeded into six-well microplates in RPMI 1640 containing 10% FBS to a concentration of 1.5×10?/well. After the cells were cultured overnight in a carbon dioxi... | TPDdb | Western Blot | TPD-QZODOU | African=2.89%; Native American=0.31%; East Asian, North=0%; East Asian, South=2.4%; South Asian=8.61%; European, North=28.39%; European, South=57.41%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Instable (MSI-high).
CVCL_0395 ! LNCaP
Metastatic; Left supraclavicular lymph node;
... | 16 | false | 900 | 0 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(F)(CN5CCCOc6c(ccc(C(=O)N[C@H]7CCC(=O)NC7=O)c6F)CC5)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | -15.5 | null | null | null | 5 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of AR protein in VCAP cells. AR-positive human prostate cancer cells VCaP were seeded in DMEM containing 10% FBS to a density of 3×105/well in a six-well microplate. After being cultured overnight in a carbon dioxide incubator (ESCO), the prepared compound of the... | TPDdb | Western Blot | TPD-QZODOU | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 900 | 0 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(N5CC6(CCC7(CC6)COc6c7ccc7c6CN(C6CCC(=O)NC6=O)C7=O)C5)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | 0.5 | null | null | null | 100 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1379 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of compounds against AR protein in LNCaP cells. AR-positive human prostate cancer cells (LNCaP FGC) were seeded into six-well microplates in RPMI 1640 containing 10% FBS to a concentration of 1.5×10?/well. After the cells were cultured overnight in a carbon dioxi... | TPDdb | Western Blot | TPD-KZ81OM | African=2.89%; Native American=0.31%; East Asian, North=0%; East Asian, South=2.4%; South Asian=8.61%; European, North=28.39%; European, South=57.41%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Instable (MSI-high).
CVCL_0395 ! LNCaP
Metastatic; Left supraclavicular lymph node;
... | 16 | false | 901 | 0 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(N5CC6(CCC7(CC6)COc6c7ccc7c6CN(C6CCC(=O)NC6=O)C7=O)C5)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 66.5 | null | null | null | 5 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of AR protein in VCAP cells. AR-positive human prostate cancer cells VCaP were seeded in DMEM containing 10% FBS to a density of 3×105/well in a six-well microplate. After being cultured overnight in a carbon dioxide incubator (ESCO), the prepared compound of the... | TPDdb | Western Blot | TPD-KZ81OM | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 901 | 0 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(N5CCC6(CC5)COc5c6ccc6c5n(C)c(=O)n6C5CCC(=O)NC5=O)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | -10.5 | null | null | null | 100 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1379 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of compounds against AR protein in LNCaP cells. AR-positive human prostate cancer cells (LNCaP FGC) were seeded into six-well microplates in RPMI 1640 containing 10% FBS to a concentration of 1.5×10?/well. After the cells were cultured overnight in a carbon dioxi... | TPDdb | Western Blot | TPD-8KOAKK | African=2.89%; Native American=0.31%; East Asian, North=0%; East Asian, South=2.4%; South Asian=8.61%; European, North=28.39%; European, South=57.41%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Instable (MSI-high).
CVCL_0395 ! LNCaP
Metastatic; Left supraclavicular lymph node;
... | 16 | false | 902 | 97 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3ccc(N4CCC(N5CCC6(CC5)COc5c6ccc6c5n(C)c(=O)n6C5CCC(=O)NC5=O)CC4)cc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 69 | null | null | null | 5 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of AR protein in VCAP cells. AR-positive human prostate cancer cells VCaP were seeded in DMEM containing 10% FBS to a density of 3×105/well in a six-well microplate. After being cultured overnight in a carbon dioxide incubator (ESCO), the prepared compound of the... | TPDdb | Western Blot | TPD-8KOAKK | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 902 | 97 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3cnc(N4CCC(CN5CCc6c(ccc7c(C8CCC(=O)NC8=O)noc67)C5)CC4)cn3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | DC50 | nM | 5 | null | null | null | null | null | < | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CYCLOBUTYL-CONTAINING COMPOUNDS (patent) | Compounds' Effects on AR Degradation in Cells
1.1 Assay for AR Degradation in VCaP Cells
Detection was performed using the HTRF Human Androgen Receptor Detection Kit. 4× Supplemented Lysis Buffer was prepared using 100× Blocking Reagent Stock Solution and 4× Lysis Buffer Stock Solution. 1× Supplemented Lysis Buffer was... | TPDdb | HTRF | TPD-XB6KYR | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 903 | 166 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3cnc(N4CCC(CN5CCc6c(ccc7c(C8CCC(=O)NC8=O)noc67)C5)CC4)cn3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 75 | null | null | null | null | null | > | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CYCLOBUTYL-CONTAINING COMPOUNDS (patent) | Compounds' Effects on AR Degradation in Cells
1.1 Assay for AR Degradation in VCaP Cells
Detection was performed using the HTRF Human Androgen Receptor Detection Kit. 4× Supplemented Lysis Buffer was prepared using 100× Blocking Reagent Stock Solution and 4× Lysis Buffer Stock Solution. 1× Supplemented Lysis Buffer was... | TPDdb | HTRF | TPD-XB6KYR | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 903 | 166 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3cnc(N4CCC(CN5CCc6c(ccc7c(C8CCC(=O)NC8=O)noc67)C5)CC4)nc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | DC50 | nM | 5 | null | null | null | null | null | < | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CYCLOBUTYL-CONTAINING COMPOUNDS (patent) | Compounds' Effects on AR Degradation in Cells
1.1 Assay for AR Degradation in VCaP Cells
Detection was performed using the HTRF Human Androgen Receptor Detection Kit. 4× Supplemented Lysis Buffer was prepared using 100× Blocking Reagent Stock Solution and 4× Lysis Buffer Stock Solution. 1× Supplemented Lysis Buffer was... | TPDdb | HTRF | TPD-WL030A | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 904 | 166 |
COc1cc(O[C@H]2C(C)(C)[C@H](NC(=O)c3cnc(N4CCC(CN5CCc6c(ccc7c(C8CCC(=O)NC8=O)noc67)C5)CC4)nc3)C2(C)C)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 75 | null | null | null | null | null | > | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CYCLOBUTYL-CONTAINING COMPOUNDS (patent) | Compounds' Effects on AR Degradation in Cells
1.1 Assay for AR Degradation in VCaP Cells
Detection was performed using the HTRF Human Androgen Receptor Detection Kit. 4× Supplemented Lysis Buffer was prepared using 100× Blocking Reagent Stock Solution and 4× Lysis Buffer Stock Solution. 1× Supplemented Lysis Buffer was... | TPDdb | HTRF | TPD-WL030A | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 904 | 166 |
COc1cc(O[C@H]2CC[C@H](NC(=O)C3=NNC(N4CCC(CN5CCC6(CC5)COc5c6ccc6c5n(C)c(=O)n6C5CCC(=O)NC5=O)CC4)C=C3)CC2)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | 36.5 | null | null | null | 100 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1379 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of compounds against AR protein in LNCaP cells. AR-positive human prostate cancer cells (LNCaP FGC) were seeded into six-well microplates in RPMI 1640 containing 10% FBS to a concentration of 1.5×10?/well. After the cells were cultured overnight in a carbon dioxi... | TPDdb | Western Blot | TPD-7GJ4M6 | African=2.89%; Native American=0.31%; East Asian, North=0%; East Asian, South=2.4%; South Asian=8.61%; European, North=28.39%; European, South=57.41%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Instable (MSI-high).
CVCL_0395 ! LNCaP
Metastatic; Left supraclavicular lymph node;
... | 16 | true | -1 | -1 |
COc1cc(O[C@H]2CC[C@H](NC(=O)C3=NNC(N4CCC(CN5CCC6(CC5)COc5c6ccc6c5n(C)c(=O)n6C5CCC(=O)NC5=O)CC4)C=C3)CC2)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 76.5 | null | null | null | 5 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of AR protein in VCAP cells. AR-positive human prostate cancer cells VCaP were seeded in DMEM containing 10% FBS to a density of 3×105/well in a six-well microplate. After being cultured overnight in a carbon dioxide incubator (ESCO), the prepared compound of the... | TPDdb | Western Blot | TPD-7GJ4M6 | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | true | -1 | -1 |
COc1cc(O[C@H]2CC[C@H](NC(=O)c3ccc(N4CCC(CN5CCC6(CC5)COc5cc7c(cc56)n(C)c(=O)n7C5CCC(=O)NC5=O)CC4)nn3)CC2)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | -8.5 | null | null | null | 100 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1379 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of compounds against AR protein in LNCaP cells. AR-positive human prostate cancer cells (LNCaP FGC) were seeded into six-well microplates in RPMI 1640 containing 10% FBS to a concentration of 1.5×10?/well. After the cells were cultured overnight in a carbon dioxi... | TPDdb | Western Blot | TPD-INYPO2 | African=2.89%; Native American=0.31%; East Asian, North=0%; East Asian, South=2.4%; South Asian=8.61%; European, North=28.39%; European, South=57.41%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Instable (MSI-high).
CVCL_0395 ! LNCaP
Metastatic; Left supraclavicular lymph node;
... | 16 | false | 905 | 146 |
COc1cc(O[C@H]2CC[C@H](NC(=O)c3ccc(N4CCC(CN5CCC6(CC5)COc5cc7c(cc56)n(C)c(=O)n7C5CCC(=O)NC5=O)CC4)nn3)CC2)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 78 | null | null | null | 5 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of AR protein in VCAP cells. AR-positive human prostate cancer cells VCaP were seeded in DMEM containing 10% FBS to a density of 3×105/well in a six-well microplate. After being cultured overnight in a carbon dioxide incubator (ESCO), the prepared compound of the... | TPDdb | Western Blot | TPD-INYPO2 | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | false | 905 | 146 |
COc1cc(O[C@H]2CC[C@H](NC(=O)c3ccc(N4CCC(N5CCC6(CC5)COc5cc7c(cc56)n(C)c(=O)n7C5CCC(=O)NC5=O)CC4)nn3)CC2)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | 27 | null | null | null | 100 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1379 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of compounds against AR protein in LNCaP cells. AR-positive human prostate cancer cells (LNCaP FGC) were seeded into six-well microplates in RPMI 1640 containing 10% FBS to a concentration of 1.5×10?/well. After the cells were cultured overnight in a carbon dioxi... | TPDdb | Western Blot | TPD-GQ2UGM | African=2.89%; Native American=0.31%; East Asian, North=0%; East Asian, South=2.4%; South Asian=8.61%; European, North=28.39%; European, South=57.41%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Instable (MSI-high).
CVCL_0395 ! LNCaP
Metastatic; Left supraclavicular lymph node;
... | 16 | true | -1 | -1 |
COc1cc(O[C@H]2CC[C@H](NC(=O)c3ccc(N4CCC(N5CCC6(CC5)COc5cc7c(cc56)n(C)c(=O)n7C5CCC(=O)NC5=O)CC4)nn3)CC2)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 74.5 | null | null | null | 5 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_2235 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of AR protein in VCAP cells. AR-positive human prostate cancer cells VCaP were seeded in DMEM containing 10% FBS to a density of 3×105/well in a six-well microplate. After being cultured overnight in a carbon dioxide incubator (ESCO), the prepared compound of the... | TPDdb | Western Blot | TPD-GQ2UGM | African=0%; Native American=0.05%; East Asian, North=1.4%; East Asian, South=0%; South Asian=0.98%; European, North=69.8%; European, South=27.77%.
Contains an integrated xenotropic MuLV-related virus (XMRV) Bxv-1.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Established from a xenograft produced by... | 16 | true | -1 | -1 |
COc1cc(O[C@H]2CC[C@H](NC(=O)c3ccc(N4CCC5(CC4)CC(N4CCC6(CC4)COc4cc7c(cc46)n(C)c(=O)n7C4CCC(=O)NC4=O)C5)nn3)CC2)ccc1C#N | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | 54 | null | null | null | 100 | null | null | numeric | nM | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1379 | Homo sapiens | CEREBELLAR PROTEIN E3 UBIQUITIN LIGASE INHIBITOR AND CHIMERIC COMPOUND TARGETING PROTEIN DEGRADATION (patent) | The present invention discloses the degradation activity of compounds against AR protein in LNCaP cells. AR-positive human prostate cancer cells (LNCaP FGC) were seeded into six-well microplates in RPMI 1640 containing 10% FBS to a concentration of 1.5×10?/well. After the cells were cultured overnight in a carbon dioxi... | TPDdb | Western Blot | TPD-5U467L | African=2.89%; Native American=0.31%; East Asian, North=0%; East Asian, South=2.4%; South Asian=8.61%; European, North=28.39%; European, South=57.41%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Instable (MSI-high).
CVCL_0395 ! LNCaP
Metastatic; Left supraclavicular lymph node;
... | 16 | false | 906 | 146 |
COc1cc(Oc2ccccc2)ccc1-c1nn2c(c1C(N)=O)Nc1ccc(N3CCN(CC4CCN(c5ccc(N6CCC(=O)NC6=O)cc5)CC4)CC3)cc1CC2 | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 3.6 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q06187 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_A442 | Homo sapiens | DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHOD OF USE (patent) | TMVD-8 cells were seeded at 20000 cells/well at a volume of 15 μl/well in cell culture medium [RPMI1640, 10% heat-inactive FBS, 1% PS] in Corning 96 well plate. TMD-8 cells were treated with compounds diluted in 0.2% DMSO, dilution was done according to the following protocol: (1) making 500× stock solution in DMSO fro... | TPDdb | HTRF | TPD-FTEVTA | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | true | -1 | -1 |
COc1cc2c(OC[C@@H]3CCC(=O)N3)ncc(C#CCCCCCCCCCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)c2cc1C(N)=O | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | VHL | PBMC iPSC #1 | DC50 | nM | 3,000 | null | null | null | null | 24 | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | P40337 | MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD | CVCL_WR41 | Homo sapiens | https://pubmed.ncbi.nlm.nih.gov/31312412/ | null | PROTACpedia | null | null | In situ; Peripheral blood;
Induced pluripotent stem cell | 25 | false | 488 | 0 |
COc1cc2c(OC[C@@H]3CCC(=O)N3)ncc(C#CCCCCCCCCCCC(=O)N[C@H](C(=O)N3C[C@H](O)C[C@H]3C(=O)NCc3ccc(-c4scnc4C)cc3)C(C)(C)C)c2cc1C(N)=O | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | VHL | PBMC iPSC #1 | Dmax | % | 50 | null | null | null | null | 24 | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | P40337 | MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD | CVCL_WR41 | Homo sapiens | 10.1021/acsmedchemlett.9b00219; https://pubmed.ncbi.nlm.nih.gov/31312412/ | Degradation of IRAK4 in PBMC cells after 24 h treatment | PROTAC-DB; PROTACpedia | null | null | In situ; Peripheral blood;
Induced pluripotent stem cell | 25 | false | 488 | 0 |
COc1cc2c(Oc3ccc(NC(=O)C4(C(=O)Nc5ccc(F)cc5)CC4)cc3F)ccnc2cc1OCCCCOCCCCOCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(-c2scnc2C)cc1)C(C)(C)C | MAPK14 | MSQERPTFYRQELNKTIWEVPERYQNLSPVGSGAYGSVCAAFDTKTGLRVAVKKLSRPFQSIIHAKRTYRELRLLKHMKHENVIGLLDVFTPARSLEEFNDVYLVTHLMGADLNNIVKCQKLTDDHVQFLIYQILRGLKYIHSADIIHRDLKPSNLAVNEDCELKILDFGLARHTDDEMTGYVATRWYRAPEIMLNWMHYNQTVDIWSVGCIMAELLTGRTLFPGTDHIDQLKLILRLVGTPGAELLKKISSESARNYIQSLTQMPKMNFANVFIGANPLAVDLLEKMLVLDSDKRITAAQALAHAYFAQYHDPDDEPVA... | VHL | HeLa | Dmax | % | 99.6 | 1.1 | null | null | null | 24 | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q16539 | P40337 | MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD | CVCL_0030 | Homo sapiens | https://pubmed.ncbi.nlm.nih.gov/30631068/ | DC50 error ± 1.0 nM. DMAX error ± 1.1 %. | PROTACpedia | null | null | African=64.74%; Native American=0.77%; East Asian, North=2.26%; East Asian, South=0%; South Asian=0%; European, North=19.45%; European, South=12.78%.
HeLa has 5 five HPV18 integration sites Not susceptible to infection by SARS coronavirus 2 (SARS-CoV-2) (COVID-19).
A*03,28; B*w15,w35; C*w02,w03. A*03 A*68
Stable (MSS).... | 35 | false | 907 | 0 |
COc1cc2c(Oc3ccc(NC(=O)C4(C(=O)Nc5ccc(F)cc5)CC4)cc3F)ccnc2cc1OCCCCOCCCCOCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(-c2scnc2C)cc1)C(C)(C)C | MAPK14 | MSQERPTFYRQELNKTIWEVPERYQNLSPVGSGAYGSVCAAFDTKTGLRVAVKKLSRPFQSIIHAKRTYRELRLLKHMKHENVIGLLDVFTPARSLEEFNDVYLVTHLMGADLNNIVKCQKLTDDHVQFLIYQILRGLKYIHSADIIHRDLKPSNLAVNEDCELKILDFGLARHTDDEMTGYVATRWYRAPEIMLNWMHYNQTVDIWSVGCIMAELLTGRTLFPGTDHIDQLKLILRLVGTPGAELLKKISSESARNYIQSLTQMPKMNFANVFIGANPLAVDLLEKMLVLDSDKRITAAQALAHAYFAQYHDPDDEPVA... | VHL | MDA-MB-231 | DC50 | nM | 9.5 | 1 | null | null | null | 24 | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q16539 | P40337 | MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD | CVCL_0062 | Homo sapiens | https://pubmed.ncbi.nlm.nih.gov/30631068/ | DC50 error ± 1.0 nM. DMAX error ± 1.1 %. | PROTACpedia | null | null | African=1.95%; Native American=0%; East Asian, North=2.44%; East Asian, South=0%; South Asian=7.42%; European, North=28.16%; European, South=60.03%.
Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*02/28; B*07,08; C*w02,w06. A*02 A... | 35 | false | 907 | 0 |
COc1cc2c(Oc3ccc(NC(=O)C4(C(=O)Nc5ccc(F)cc5)CC4)cc3F)ccnc2cc1OCCCCOCCCCOCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(-c2scnc2C)cc1)C(C)(C)C | P38-alpha | MSQERPTFYRQELNKTIWEVPERYQNLSPVGSGAYGSVCAAFDTKTGLRVAVKKLSRPFQSIIHAKRTYRELRLLKHMKHENVIGLLDVFTPARSLEEFNDVYLVTHLMGADLNNIVKCQKLTDDHVQFLIYQILRGLKYIHSADIIHRDLKPSNLAVNEDCELKILDFGLARHTDDEMTGYVATRWYRAPEIMLNWMHYNQTVDIWSVGCIMAELLTGRTLFPGTDHIDQLKLILRLVGTPGAELLKKISSESARNYIQSLTQMPKMNFANVFIGANPLAVDLLEKMLVLDSDKRITAAQALAHAYFAQYHDPDDEPVA... | VHL | MDA-MB-231 | DC50 | nM | 9.5 | null | null | null | null | null | null | null | null | PROteolysis-TArgeting Chimera (PROTAC) | Q16539 | P40337 | MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD | CVCL_0062 | Homo sapiens | 10.1038/s41467-018-08027-7 | Degradation of p38alpha in MDA-MB-231 cells | PROTAC-DB | null | null | African=1.95%; Native American=0%; East Asian, North=2.44%; East Asian, South=0%; South Asian=7.42%; European, North=28.16%; European, South=60.03%.
Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*02/28; B*07,08; C*w02,w06. A*02 A... | 35 | false | 907 | 0 |
COc1cc2c(Oc3ccc(NC(=O)C4(C(=O)Nc5ccc(F)cc5)CC4)cc3F)ccnc2cc1OCCCCOCCCCOCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(-c2scnc2C)cc1)C(C)(C)C | P38-alpha | MSQERPTFYRQELNKTIWEVPERYQNLSPVGSGAYGSVCAAFDTKTGLRVAVKKLSRPFQSIIHAKRTYRELRLLKHMKHENVIGLLDVFTPARSLEEFNDVYLVTHLMGADLNNIVKCQKLTDDHVQFLIYQILRGLKYIHSADIIHRDLKPSNLAVNEDCELKILDFGLARHTDDEMTGYVATRWYRAPEIMLNWMHYNQTVDIWSVGCIMAELLTGRTLFPGTDHIDQLKLILRLVGTPGAELLKKISSESARNYIQSLTQMPKMNFANVFIGANPLAVDLLEKMLVLDSDKRITAAQALAHAYFAQYHDPDDEPVA... | VHL | MDA-MB-231 | Dmax | % | 99.6 | null | null | null | null | null | null | null | null | PROteolysis-TArgeting Chimera (PROTAC) | Q16539 | P40337 | MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD | CVCL_0062 | Homo sapiens | 10.1038/s41467-018-08027-7 | Degradation of p38alpha in MDA-MB-231 cells | PROTAC-DB | null | null | African=1.95%; Native American=0%; East Asian, North=2.44%; East Asian, South=0%; South Asian=7.42%; European, North=28.16%; European, South=60.03%.
Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*02/28; B*07,08; C*w02,w06. A*02 A... | 35 | false | 907 | 0 |
COc1cc2c(Oc3ccc(NC(=O)C4(C(=O)Nc5ccc(F)cc5)CC4)cc3F)ccnc2cc1OCCCCOCCCCOCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(-c2scnc2C)cc1)C(C)(C)C | P38-delta | MSLIRKKGFYKQDVNKTAWELPKTYVSPTHVGSGAYGSVCSAIDKRSGEKVAIKKLSRPFQSEIFAKRAYRELLLLKHMQHENVIGLLDVFTPASSLRNFYDFYLVMPFMQTDLQKIMGMEFSEEKIQYLVYQMLKGLKYIHSAGVVHRDLKPGNLAVNEDCELKILDFGLARHADAEMTGYVVTRWYRAPEVILSWMHYNQTVDIWSVGCIMAEMLTGKTLFKGKDYLDQLTQILKVTGVPGTEFVQKLNDKAAKSYIQSLPQTPRKDFTQLFPRASPQAADLLEKMLELDVDKRLTAAQALTHPFFEPFRDPEEETEA... | VHL | MDA-MB-231 | DC50 | nM | 1,160 | null | null | null | null | null | null | null | null | PROteolysis-TArgeting Chimera (PROTAC) | O15264 | P40337 | MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD | CVCL_0062 | Homo sapiens | 10.1038/s41467-018-08027-7 | Degradation of p38delta in MDA-MB-231 cells | PROTAC-DB | null | null | African=1.95%; Native American=0%; East Asian, North=2.44%; East Asian, South=0%; South Asian=7.42%; European, North=28.16%; European, South=60.03%.
Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*02/28; B*07,08; C*w02,w06. A*02 A... | 35 | false | 907 | 0 |
COc1cc2c(Oc3ccc(NC(=O)C4(C(=O)Nc5ccc(F)cc5)CC4)cc3F)ccnc2cc1OCCCCOCCCCOCC(=O)N[C@H](C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(-c2scnc2C)cc1)C(C)(C)C | P38-delta | MSLIRKKGFYKQDVNKTAWELPKTYVSPTHVGSGAYGSVCSAIDKRSGEKVAIKKLSRPFQSEIFAKRAYRELLLLKHMQHENVIGLLDVFTPASSLRNFYDFYLVMPFMQTDLQKIMGMEFSEEKIQYLVYQMLKGLKYIHSAGVVHRDLKPGNLAVNEDCELKILDFGLARHADAEMTGYVVTRWYRAPEVILSWMHYNQTVDIWSVGCIMAEMLTGKTLFKGKDYLDQLTQILKVTGVPGTEFVQKLNDKAAKSYIQSLPQTPRKDFTQLFPRASPQAADLLEKMLELDVDKRLTAAQALTHPFFEPFRDPEEETEA... | VHL | MDA-MB-231 | Dmax | % | 25.1 | null | null | null | null | null | null | null | null | PROteolysis-TArgeting Chimera (PROTAC) | O15264 | P40337 | MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD | CVCL_0062 | Homo sapiens | 10.1038/s41467-018-08027-7 | Degradation of p38delta in MDA-MB-231 cells | PROTAC-DB | null | null | African=1.95%; Native American=0%; East Asian, North=2.44%; East Asian, South=0%; South Asian=7.42%; European, North=28.16%; European, South=60.03%.
Gene deletion; HGNC; HGNC Gene deletion; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*02/28; B*07,08; C*w02,w06. A*02 A... | 35 | false | 907 | 0 |
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