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 |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
C[C@H]1CC2(CCN(c3ccc(N4CCC(CN5CC6(CCC7(CC6)COc6c7ccc7c6CN(C6CCC(=O)NC6=O)C7=O)C5)CC4)cc3)CC2)CN1c1ccc(C#N)c(Cl)c1 | 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-28UKSX | 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 | 1,087 | 63 |
C[C@H]1CC2(CCN(c3ccc(N4CCC(CN5CCC6(CC5)CCC5(CC6)COc6c5ccc5c6CN(C6CCC(=O)NC6=O)C5=O)CC4)cc3)CC2)CN1c1ccc(C#N)c(Cl)c1 | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | 29.5 | 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-P6YOLK | 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 | 1,088 | 0 |
C[C@H]1CC2(CCN(c3ccc(N4CCC(CN5CCC6(CC5)COc5ccc7c(c56)n(C)c(=O)n7C5CCC(=O)NC5=O)CC4)cc3)CC2)CN1c1ccc(C#N)c(Cl)c1 | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | 56.5 | 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-KTFTYK | 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 | 1,089 | 63 |
C[C@H]1CC2(CCN(c3ccc(N4CCC(CN5CCC6(CC5)COc5ccc7c(c56)n(C)c(=O)n7C5CCC(=O)NC5=O)CC4)cc3)CC2)CN1c1ccc(C#N)c(Cl)c1 | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | -12.5 | 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-KTFTYK | 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 | 1,089 | 63 |
C[C@H]1CC2(CCN(c3ccc(N4CCC(CN5CCC6(CCc7cc(C(=O)N[C@H]8CCC(=O)NC8=O)c(F)cc7O6)CC5)CC4)cc3)CC2)CN1c1ccc(C#N)c(Cl)c1 | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | 60.5 | 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-Y866J5 | 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 | 938 | 63 |
C[C@H]1CC2(CCN(c3ccc(N4CCC(CN5CCC6(CCc7cc(C(=O)N[C@H]8CCC(=O)NC8=O)c(F)cc7O6)CC5)CC4)cc3)CC2)CN1c1ccc(C#N)c(Cl)c1 | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | -22 | 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-Y866J5 | 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 | 938 | 63 |
C[C@H]1CC2(CCN(c3ccc(N4CCC(CN5CCN6c7ccc(C(=O)N[C@H]8CCC(=O)NC8=O)c(F)c7OC[C@H]6C5)CC4)cc3)CC2)CN1c1ccc(C#N)c(Cl)c1 | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | 51.5 | 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-T0WFS3 | 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 |
C[C@H]1CC2(CCN(c3ccc(N4CCC(CN5CCN6c7ccc(C(=O)N[C@H]8CCC(=O)NC8=O)cc7OC[C@@H]6C5)CC4)cc3)CC2)CN1c1ccc(C#N)c(Cl)c1 | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | 57.5 | 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-1ZK0N9 | 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 | 1,090 | 63 |
C[C@H]1CC2(CCN(c3ccc(N4CCC(CN5CCN6c7ccc(C(=O)N[C@H]8CCC(=O)NC8=O)cc7OC[C@@H]6C5)CC4)cc3)CC2)CN1c1ccc(C#N)c(Cl)c1 | 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-1ZK0N9 | 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 | 1,090 | 63 |
C[C@H]1CC2(CCN(c3ccc(N4CCC(CN5CCN6c7ccc(C(=O)N[C@H]8CCC(=O)NC8=O)cc7OC[C@H]6C5)CC4)cc3)CC2)CN1c1ccc(C#N)c(Cl)c1 | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP clone FGC | Dmax | % | 75 | 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-Z2F58H | 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 | 1,090 | 63 |
C[C@H]1CC2(CCN(c3ccc(N4CCC(CN5CCN6c7ccc(C(=O)N[C@H]8CCC(=O)NC8=O)cc7OC[C@H]6C5)CC4)cc3)CC2)CN1c1ccc(C#N)c(Cl)c1 | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | VCaP | Dmax | % | 24.5 | 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-Z2F58H | 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 | 1,090 | 63 |
C[C@H]1CC2(CCN(c3cnc(C(=O)N4CCC(CN5CCN(c6cccc(NC7CCC(=O)NC7=O)c6)CC5)CC4)cn3)CC2)CN1c1ccc(C#N)c(Cl)c1 | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP | DC50 | nM | 3 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0395 | Homo sapiens | CHIMERIC COMPOUND FOR TARGETED DEGRADATION OF ANDROGEN RECEPTOR PROTEIN, PREPARATION METHOD THEREFOR, AND MEDICAL USE THEREOF (patent) | Degradation of the Androgen Receptor in LNCaP Cells by Compounds of the Disclosure
The following in vitro cell-based assay measures the degradation activity of test compounds against the androgen receptor (AR) in human prostate cancer cell lines. The activity is expressed as a DC50 value. On the first day of the experi... | TPDdb | ELISA | TPD-FEZE1I | Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*01
Instable (MSI).
Metastatic; Left supraclavicular lymph node;
Caucasian.
Space-flown cell line (cellonaut).
Cancer cell line | 16 | false | 1,091 | 117 |
C[C@H]1CCCN1Cc1nc2ccc(NC(=O)c3ccc4c(cnn4CCCCCCCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)c3)cc2[nH]1 | ENL | MDNQCTVQVRLELGHRAQLRKKPTTEGFTHDWMVFVRGPEQCDIQHFVEKVVFWLHDSFPKPRRVCKEPPYKVEESGYAGFIMPIEVHFKNKEEPRKVCFTYDLFLNLEGNPPVNHLRCEKLTFNNPTTEFRYKLLRAGGVMVMPEGADTVSRPSPDYPMLPTIPLSAFSDPKKTKPSHGSKDANKESSKTSKPHKVTKEHRERPRKDSESKSSSKELEREQAKSSKDTSRKLGEGRLPKEEKAPPPKAAFKEPKMALKETKLESTSPKGGPPPPPPPPPRASSKRPATADSPKPSAKKQKKSSSKGSRSAPGTSPRTSS... | CRBN | MV4-11 | DC50 | nM | 37 | null | null | null | null | 24 | null | null | null | PROteolysis-TArgeting Chimera (PROTAC) | Q03111 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0064 | Homo sapiens | 10.1186/s13045-022-01258-8 | Degradation of ENL in MV4;11 cells after 24 h treatment | PROTAC-DB | null | null | African=0.59%; Native American=0%; East Asian, North=0.34%; East Asian, South=0%; South Asian=2.57%; European, North=67.58%; European, South=28.91%.
48,XY,t(4;11)(q21;q23),+8,+19 (ATCC=CRL-9591).
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC
CSF2 and IL3 dependent.
A*03 A*03
Stable (MSS) (Sanger).
In situ; Peripheral bl... | -1 | false | 1,092 | 0 |
C[C@H]1CCCN1Cc1nc2ccc(NC(=O)c3ccc4c(cnn4CCCCCCCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)c3)cc2[nH]1 | ENL | MDNQCTVQVRLELGHRAQLRKKPTTEGFTHDWMVFVRGPEQCDIQHFVEKVVFWLHDSFPKPRRVCKEPPYKVEESGYAGFIMPIEVHFKNKEEPRKVCFTYDLFLNLEGNPPVNHLRCEKLTFNNPTTEFRYKLLRAGGVMVMPEGADTVSRPSPDYPMLPTIPLSAFSDPKKTKPSHGSKDANKESSKTSKPHKVTKEHRERPRKDSESKSSSKELEREQAKSSKDTSRKLGEGRLPKEEKAPPPKAAFKEPKMALKETKLESTSPKGGPPPPPPPPPRASSKRPATADSPKPSAKKQKKSSSKGSRSAPGTSPRTSS... | CRBN | MV4-11 | Dmax | % | 95 | null | null | null | null | 24 | null | null | null | PROteolysis-TArgeting Chimera (PROTAC) | Q03111 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0064 | Homo sapiens | 10.1186/s13045-022-01258-8 | Degradation of ENL in MV4;11 cells after 24 h treatment | PROTAC-DB | null | null | African=0.59%; Native American=0%; East Asian, North=0.34%; East Asian, South=0%; South Asian=2.57%; European, North=67.58%; European, South=28.91%.
48,XY,t(4;11)(q21;q23),+8,+19 (ATCC=CRL-9591).
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC
CSF2 and IL3 dependent.
A*03 A*03
Stable (MSS) (Sanger).
In situ; Peripheral bl... | -1 | false | 1,092 | 0 |
C[C@H]1CCCN1Cc1nc2ccc(NC(=O)c3ccc4c(cnn4CCCCCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)c3)cc2[nH]1 | ENL | MDNQCTVQVRLELGHRAQLRKKPTTEGFTHDWMVFVRGPEQCDIQHFVEKVVFWLHDSFPKPRRVCKEPPYKVEESGYAGFIMPIEVHFKNKEEPRKVCFTYDLFLNLEGNPPVNHLRCEKLTFNNPTTEFRYKLLRAGGVMVMPEGADTVSRPSPDYPMLPTIPLSAFSDPKKTKPSHGSKDANKESSKTSKPHKVTKEHRERPRKDSESKSSSKELEREQAKSSKDTSRKLGEGRLPKEEKAPPPKAAFKEPKMALKETKLESTSPKGGPPPPPPPPPRASSKRPATADSPKPSAKKQKKSSSKGSRSAPGTSPRTSS... | CRBN | MV4-11 | DC50 | nM | 50 | null | null | null | null | 24 | null | null | null | PROteolysis-TArgeting Chimera (PROTAC) | Q03111 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0064 | Homo sapiens | 10.1186/s13045-022-01258-8 | Degradation of ENL in MV4;11 cells after 24 h treatment | PROTAC-DB | null | null | African=0.59%; Native American=0%; East Asian, North=0.34%; East Asian, South=0%; South Asian=2.57%; European, North=67.58%; European, South=28.91%.
48,XY,t(4;11)(q21;q23),+8,+19 (ATCC=CRL-9591).
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC
CSF2 and IL3 dependent.
A*03 A*03
Stable (MSS) (Sanger).
In situ; Peripheral bl... | -1 | false | 1,093 | 0 |
C[C@H]1CCCN1Cc1nc2ccc(NC(=O)c3ccc4c(cnn4CCCCCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)c3)cc2[nH]1 | ENL | MDNQCTVQVRLELGHRAQLRKKPTTEGFTHDWMVFVRGPEQCDIQHFVEKVVFWLHDSFPKPRRVCKEPPYKVEESGYAGFIMPIEVHFKNKEEPRKVCFTYDLFLNLEGNPPVNHLRCEKLTFNNPTTEFRYKLLRAGGVMVMPEGADTVSRPSPDYPMLPTIPLSAFSDPKKTKPSHGSKDANKESSKTSKPHKVTKEHRERPRKDSESKSSSKELEREQAKSSKDTSRKLGEGRLPKEEKAPPPKAAFKEPKMALKETKLESTSPKGGPPPPPPPPPRASSKRPATADSPKPSAKKQKKSSSKGSRSAPGTSPRTSS... | CRBN | MV4-11 | Dmax | % | 68 | null | null | null | null | 24 | null | null | null | PROteolysis-TArgeting Chimera (PROTAC) | Q03111 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0064 | Homo sapiens | 10.1186/s13045-022-01258-8 | Degradation of ENL in MV4;11 cells after 24 h treatment | PROTAC-DB | null | null | African=0.59%; Native American=0%; East Asian, North=0.34%; East Asian, South=0%; South Asian=2.57%; European, North=67.58%; European, South=28.91%.
48,XY,t(4;11)(q21;q23),+8,+19 (ATCC=CRL-9591).
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC
CSF2 and IL3 dependent.
A*03 A*03
Stable (MSS) (Sanger).
In situ; Peripheral bl... | -1 | false | 1,093 | 0 |
C[C@H]1CCCN1Cc1nc2ccc(NC(=O)c3ccc4c(cnn4CCCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)c3)cc2[nH]1 | ENL | MDNQCTVQVRLELGHRAQLRKKPTTEGFTHDWMVFVRGPEQCDIQHFVEKVVFWLHDSFPKPRRVCKEPPYKVEESGYAGFIMPIEVHFKNKEEPRKVCFTYDLFLNLEGNPPVNHLRCEKLTFNNPTTEFRYKLLRAGGVMVMPEGADTVSRPSPDYPMLPTIPLSAFSDPKKTKPSHGSKDANKESSKTSKPHKVTKEHRERPRKDSESKSSSKELEREQAKSSKDTSRKLGEGRLPKEEKAPPPKAAFKEPKMALKETKLESTSPKGGPPPPPPPPPRASSKRPATADSPKPSAKKQKKSSSKGSRSAPGTSPRTSS... | CRBN | MV4-11 | DC50 | nM | 72 | null | null | null | null | 24 | null | null | null | PROteolysis-TArgeting Chimera (PROTAC) | Q03111 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0064 | Homo sapiens | 10.1186/s13045-022-01258-8 | Degradation of ENL in MV4;11 cells after 24 h treatment | PROTAC-DB | null | null | African=0.59%; Native American=0%; East Asian, North=0.34%; East Asian, South=0%; South Asian=2.57%; European, North=67.58%; European, South=28.91%.
48,XY,t(4;11)(q21;q23),+8,+19 (ATCC=CRL-9591).
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC
CSF2 and IL3 dependent.
A*03 A*03
Stable (MSS) (Sanger).
In situ; Peripheral bl... | -1 | false | 1,094 | 133 |
C[C@H]1CCCN1Cc1nc2ccc(NC(=O)c3ccc4c(cnn4CCCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)c3)cc2[nH]1 | ENL | MDNQCTVQVRLELGHRAQLRKKPTTEGFTHDWMVFVRGPEQCDIQHFVEKVVFWLHDSFPKPRRVCKEPPYKVEESGYAGFIMPIEVHFKNKEEPRKVCFTYDLFLNLEGNPPVNHLRCEKLTFNNPTTEFRYKLLRAGGVMVMPEGADTVSRPSPDYPMLPTIPLSAFSDPKKTKPSHGSKDANKESSKTSKPHKVTKEHRERPRKDSESKSSSKELEREQAKSSKDTSRKLGEGRLPKEEKAPPPKAAFKEPKMALKETKLESTSPKGGPPPPPPPPPRASSKRPATADSPKPSAKKQKKSSSKGSRSAPGTSPRTSS... | CRBN | MV4-11 | Dmax | % | 89 | null | null | null | null | 24 | null | null | null | PROteolysis-TArgeting Chimera (PROTAC) | Q03111 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0064 | Homo sapiens | 10.1186/s13045-022-01258-8 | Degradation of ENL in MV4;11 cells after 24 h treatment | PROTAC-DB | null | null | African=0.59%; Native American=0%; East Asian, North=0.34%; East Asian, South=0%; South Asian=2.57%; European, North=67.58%; European, South=28.91%.
48,XY,t(4;11)(q21;q23),+8,+19 (ATCC=CRL-9591).
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC
CSF2 and IL3 dependent.
A*03 A*03
Stable (MSS) (Sanger).
In situ; Peripheral bl... | -1 | false | 1,094 | 133 |
C[C@H]1CN(C2CN(C3CCN(c4ccc5c(c4)C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)C2)CCN1c1ccc(Nc2cc(-c3ccnc(N4CCn5c(cc6c5CC(C)(C)C6)C4=O)c3CO)cn(C)c2=O)nc1 | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | Ramos | DC50 | nM | 0.612 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q06187 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0597 | Homo sapiens | NITROGEN-CONTAINING TRICYCLIC BIFUNCTIONAL COMPOUND, PREPARATION METHOD THEREFOR, AND APPLICATION THEREOF (patent) | Evaluation of Compounds' BTK Protein Degradation Activity in Ramos Cells
Experimental Methods:
1. RAMOS cells were seeded in 96-well U-bottom cell culture plates, with 80 μL of cell suspension per well (50,000 RAMOS cells per well). The plates were placed in a CO2 incubator and incubated overnight at 37°C.
2. The test ... | TPDdb | HTRF | TPD-WD3OQQ | EBV-negative.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC
A*03 A*03 A*03 A*03
Stable (MSS).
In situ; Ascites;
Caucasian.
B-cell; CL=CL_0000236.
Cancer cell line | 31 | false | 1,095 | 50 |
C[C@H]1CN(C2CN(CC3CCN(c4ccc5c(c4)C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)C2)CCN1c1ccc(Nc2cc(-c3ccnc(N4CCn5c(cc6c5CC(C)(C)C6)C4=O)c3CO)cn(C)c2=O)nc1 | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | Ramos | DC50 | nM | 0.512 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q06187 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0597 | Homo sapiens | NITROGEN-CONTAINING TRICYCLIC BIFUNCTIONAL COMPOUND, PREPARATION METHOD THEREFOR, AND APPLICATION THEREOF (patent) | Evaluation of Compounds' BTK Protein Degradation Activity in Ramos Cells
Experimental Methods:
1. RAMOS cells were seeded in 96-well U-bottom cell culture plates, with 80 μL of cell suspension per well (50,000 RAMOS cells per well). The plates were placed in a CO2 incubator and incubated overnight at 37°C.
2. The test ... | TPDdb | HTRF | TPD-P32ZJE | EBV-negative.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC
A*03 A*03 A*03 A*03
Stable (MSS).
In situ; Ascites;
Caucasian.
B-cell; CL=CL_0000236.
Cancer cell line | 31 | false | 1,096 | 0 |
C[C@H]1CN(C2CN(c3ccc4c(c3)C(=O)N(C3CCC(=O)NC3=O)C4=O)C2)CCN1c1ccc(Nc2cc(-c3ccnc(N4CCn5c(cc6c5CC(C)(C)C6)C4=O)c3CO)cn(C)c2=O)nc1 | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | Ramos | DC50 | nM | 0.785 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q06187 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0597 | Homo sapiens | NITROGEN-CONTAINING TRICYCLIC BIFUNCTIONAL COMPOUND, PREPARATION METHOD THEREFOR, AND APPLICATION THEREOF (patent) | Evaluation of Compounds' BTK Protein Degradation Activity in Ramos Cells
Experimental Methods:
1. RAMOS cells were seeded in 96-well U-bottom cell culture plates, with 80 μL of cell suspension per well (50,000 RAMOS cells per well). The plates were placed in a CO2 incubator and incubated overnight at 37°C.
2. The test ... | TPDdb | HTRF | TPD-NS5P5F | EBV-negative.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC
A*03 A*03 A*03 A*03
Stable (MSS).
In situ; Ascites;
Caucasian.
B-cell; CL=CL_0000236.
Cancer cell line | 31 | true | -1 | -1 |
C[C@H]1CN(CC2CCN(c3ccc4c(c3)C(=O)N(C3CCC(=O)NC3=O)C4)CC2)CCN1c1ccc(Nc2cc(-c3ccnc(N4CCn5c(cc6c5CC(C)(C)C6)C4=O)c3CO)cn(C)c2=O)nc1 | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | Ramos | DC50 | nM | 3.069 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q06187 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0597 | Homo sapiens | NITROGEN-CONTAINING TRICYCLIC BIFUNCTIONAL COMPOUND, PREPARATION METHOD THEREFOR, AND APPLICATION THEREOF (patent) | Evaluation of Compounds' BTK Protein Degradation Activity in Ramos Cells
Experimental Methods:
1. RAMOS cells were seeded in 96-well U-bottom cell culture plates, with 80 μL of cell suspension per well (50,000 RAMOS cells per well). The plates were placed in a CO2 incubator and incubated overnight at 37°C.
2. The test ... | TPDdb | HTRF | TPD-5HGR7P | EBV-negative.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC
A*03 A*03 A*03 A*03
Stable (MSS).
In situ; Ascites;
Caucasian.
B-cell; CL=CL_0000236.
Cancer cell line | 31 | false | 1,097 | 165 |
C[C@H]1CN(CC2CCN(c3ccc4c(c3)C(=O)N(C3CCC(=O)NC3=O)C4=O)C2)CCN1c1ccc(Nc2cc(-c3ccnc(N4CCn5c(cc6c5CC(C)(C)C6)C4=O)c3CO)cn(C)c2=O)nc1 | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | Ramos | DC50 | nM | 2.276 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q06187 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0597 | Homo sapiens | NITROGEN-CONTAINING TRICYCLIC BIFUNCTIONAL COMPOUND, PREPARATION METHOD THEREFOR, AND APPLICATION THEREOF (patent) | Evaluation of Compounds' BTK Protein Degradation Activity in Ramos Cells
Experimental Methods:
1. RAMOS cells were seeded in 96-well U-bottom cell culture plates, with 80 μL of cell suspension per well (50,000 RAMOS cells per well). The plates were placed in a CO2 incubator and incubated overnight at 37°C.
2. The test ... | TPDdb | HTRF | TPD-8U99RT | EBV-negative.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC
A*03 A*03 A*03 A*03
Stable (MSS).
In situ; Ascites;
Caucasian.
B-cell; CL=CL_0000236.
Cancer cell line | 31 | false | 1,098 | 50 |
C[C@H]1CN(CC2CCN(c3ccc4c(c3)C(=O)N(C3CCC(=O)NC3=O)C4=O)CC2)CCN1c1ccc(Nc2cc(-c3ccnc(N4CCn5c(cc6c5CC(C)(C)C6)C4=O)c3CO)cn(C)c2=O)nc1 | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | Ramos | DC50 | nM | 1.103 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q06187 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0597 | Homo sapiens | NITROGEN-CONTAINING TRICYCLIC BIFUNCTIONAL COMPOUND, PREPARATION METHOD THEREFOR, AND APPLICATION THEREOF (patent) | Evaluation of Compounds' BTK Protein Degradation Activity in Ramos Cells
Experimental Methods:
1. RAMOS cells were seeded in 96-well U-bottom cell culture plates, with 80 μL of cell suspension per well (50,000 RAMOS cells per well). The plates were placed in a CO2 incubator and incubated overnight at 37°C.
2. The test ... | TPDdb | HTRF | TPD-EJ6CYL | EBV-negative.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC
A*03 A*03 A*03 A*03
Stable (MSS).
In situ; Ascites;
Caucasian.
B-cell; CL=CL_0000236.
Cancer cell line | 31 | false | 1,099 | 50 |
C[C@H]1CN(CCC2CCN(c3ccc4c(c3)C(=O)N(C3CCC(=O)NC3=O)C4=O)CC2)CCN1c1ccc(Nc2cc(-c3ccnc(N4CCn5c(cc6c5CC(C)(C)C6)C4=O)c3CO)cn(C)c2=O)nc1 | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | Ramos | DC50 | nM | 1.127 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q06187 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0597 | Homo sapiens | NITROGEN-CONTAINING TRICYCLIC BIFUNCTIONAL COMPOUND, PREPARATION METHOD THEREFOR, AND APPLICATION THEREOF (patent) | Evaluation of Compounds' BTK Protein Degradation Activity in Ramos Cells
Experimental Methods:
1. RAMOS cells were seeded in 96-well U-bottom cell culture plates, with 80 μL of cell suspension per well (50,000 RAMOS cells per well). The plates were placed in a CO2 incubator and incubated overnight at 37°C.
2. The test ... | TPDdb | HTRF | TPD-2K8JE6 | EBV-negative.
Gene fusion; HGNC; HGNC Mutation; HGNC; HGNC
A*03 A*03 A*03 A*03
Stable (MSS).
In situ; Ascites;
Caucasian.
B-cell; CL=CL_0000236.
Cancer cell line | 31 | false | 1,100 | 50 |
C[C@H]1CN(c2ccc(C#N)c(C(F)(F)F)c2)CCN1c1ccc(OCCCCN2CCN(c3ccc4c(c3)CN(C3CCC(=O)NC3=O)C4=O)CC2)cc1 | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP | DC50 | nM | 6.4 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0395 | Homo sapiens | COMPOUNDS AND THEIR USE IN TREATING CANCER (patent) | LNCaP Androgen Receptor Imaging Assay
This cell-based imaging assay uses immuno-fluorescence to measure both cell number and endogenous nuclear AR staining in the prostate cancer cell line LNCaP (expressing AR-full length). The purpose of the assay is to identify compounds that regulate AR protein level according to th... | TPDdb | Fluorescence Imaging Assay | TPD-M7V4GI | Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*01
Instable (MSI).
Metastatic; Left supraclavicular lymph node;
Caucasian.
Space-flown cell line (cellonaut).
Cancer cell line | 16 | true | -1 | -1 |
C[C@H]1CN(c2ccc(C#N)c(C(F)(F)F)c2)CCN1c1ccc(OCCCCN2CCN(c3ccc4c(c3)CN(C3CCC(=O)NC3=O)C4=O)CC2)cc1 | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP | Dmax | % | 87 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0395 | Homo sapiens | COMPOUNDS AND THEIR USE IN TREATING CANCER (patent) | LNCaP Androgen Receptor Imaging Assay
This cell-based imaging assay uses immuno-fluorescence to measure both cell number and endogenous nuclear AR staining in the prostate cancer cell line LNCaP (expressing AR-full length). The purpose of the assay is to identify compounds that regulate AR protein level according to th... | TPDdb | Fluorescence Imaging Assay | TPD-M7V4GI | Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*01
Instable (MSI).
Metastatic; Left supraclavicular lymph node;
Caucasian.
Space-flown cell line (cellonaut).
Cancer cell line | 16 | true | -1 | -1 |
C[C@H]1CN(c2ccc3c(c2)C(=O)N(C2CCC(=O)N=NC2=O)C3=O)CCN1C[C@H]1CC[C@H](NC(=O)c2ccc(Nc3ncnc4c3CCN(c3ccc(C#N)c(Cl)c3)C4)nc2F)CC1 | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP | DC50 | nM | 9.1 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0395 | Homo sapiens | DEGRADATION OF ANDROGEN RECEPTOR (AR) BY CONJUGATION OF AR ANTAGONISTS WITH E3 LIGASE LIGAND AND METHODS OF USE (patent) | Cell Degradation
Cell treatment
LNCaP Cells are collected by TrypLE and washed once and resuspended in assay medium (RPMI1640 +5%CSS) , 5×10 4/well/50μl, seed in 96-well plate , starve for 48h.
LNCaP cells are treated with compounds diluted in 0.2%DMSO and 0.1nM DHT, dilution is done according to the following protocol... | TPDdb | ELISA | TPD-W9ORP2 | Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*01
Instable (MSI).
Metastatic; Left supraclavicular lymph node;
Caucasian.
Space-flown cell line (cellonaut).
Cancer cell line | 16 | false | 1,045 | 39 |
C[C@]1(c2nc3c(C(N)=O)cccc3[nH]2)CCCN1CCOCCOCCOCCOCCOCCOCCNc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O | PARP2 | MAARRRRSTGGGRARALNESKRVNNGNTAPEDSSPAKKTRRCQRQESKKMPVAGGKANKDRTEDKQDGMPGRSWASKRVSESVKALLLKGKAPVDPECTAKVGKAHVYCEGNDVYDVMLNQTNLQFNNNKYYLIQLLEDDAQRNFSVWMRWGRVGKMGQHSLVACSGNLNKAKEIFQKKFLDKTKNNWEDREKFEKVPGKYDMLQMDYATNTQDEEETKKEESLKSPLKPESQLDLRVQELIKLICNVQAMEEMMMEMKYNTKKAPLGKLTVAQIKAGYQSLKKIEDCIRAGQHGRALMEACNEFYTRIPHDFGLRTPPL... | CRBN | HeLa | DC50 | nM | 62.8 | null | null | null | null | 24 | null | null | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9UGN5 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0030 | Homo sapiens | 10.1038/s41589-019-0379-2 | Degradation of PARP2 in HeLa cells after 24 h treatment | PROTAC-DB | 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).... | 8 | false | 1,101 | 24 |
Cc1c(-c2ccc(N3CCc4cccc(C(=O)Nc5nc6ccccc6s5)c4C3)nc2C(=O)NS(=O)(=O)CCCCCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc3c(c2)OCc2ncsc2-3)C(C)(C)C)cnn1CC1CCCCC1 | BCL2L1 | MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK | VHL | MOLT-4 | DC50 | nM | 1.44 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q07817 | P40337 | MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD | CVCL_0013 | Homo sapiens | CHIMERIC COMPOUND USED FOR TARGETED DEGRADATION OF BCL-2 PROTEIN, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL APPLICATION THEREOF (patent) | MOLT-4 cells were cultured in complete medium (RPMI1640 medium containing 10% FBS) and passaged 2-3 times a week at a passage ratio of 1:5. During passage, the cells were transferred to a centrifuge tube, centrifuged at 1200 rpm for 3 minutes, the supernatant medium was discarded, and the cells were resuspended in comp... | TPDdb | ELISA | TPD-T31S4K | African=0.38%; Native American=0%; East Asian, North=1.74%; East Asian, South=0%; South Asian=0.94%; European, North=68.08%; European, South=28.87%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*01 A*01 A*01
Instable (MSI-high).
In situ; ... | 5 | false | 1,102 | 0 |
Cc1c(-c2nc(-c3ccccn3)no2)ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CC5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)CC5)CC4)cc2CC3)c1F | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 2.33 | 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-KL7Y1I | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 1,103 | 15 |
Cc1c(-c2nc(C(N)=O)c3n2CCc2cc(OCCCOc4ccc(N5CCC(=O)NC5=O)cc4)ccc2N3)cccc1N1CCn2c(cc3c2CC(C)(C)C3)C1=O | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 2.76 | 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-7SR6AF | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 1,104 | 217 |
Cc1c(-c2ncnc3[nH]c(-c4ccc(C5CCN(CC6CCN(c7ccc(N8CCC(=O)NC8=O)cc7)CC6)CC5)cc4)cc23)cccc1N1CCn2c(cc3c2CC(C)(C)C3)C1=O | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | null | DC50 | nM | 7.2 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q06187 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | null | Homo sapiens | DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHODS OF USE (patent) | HTFR assay
After 6h treatment, add 10μl 4xlysis buffer to each well; seal the plate and incubate 30min at room temperature on a plate shaker; Once the cells are lysed, 16 μL of cell lysate are transferred to a PE 384-well HTRF detection plate; 4 μL of pre-mixed HTRF antibodies are added to each well; Cover the plate wi... | TPDdb | HTRF | TPD-6RF99A | null | 31 | false | 1,105 | 0 |
Cc1c(-c2ncnc3[nH]c(-c4ccc(N5CCN(CC6CCN(c7ccc(N8CCC(=O)NC8=O)cc7)CC6)CC5)cc4)cc23)cccc1N1CCn2c(cc3c2CC(C)(C)C3)C1=O | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | null | DC50 | nM | 4.7 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q06187 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | null | Homo sapiens | DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHODS OF USE (patent) | HTFR assay
After 6h treatment, add 10μl 4xlysis buffer to each well; seal the plate and incubate 30min at room temperature on a plate shaker; Once the cells are lysed, 16 μL of cell lysate are transferred to a PE 384-well HTRF detection plate; 4 μL of pre-mixed HTRF antibodies are added to each well; Cover the plate wi... | TPDdb | HTRF | TPD-V59RPN | null | 31 | false | 1,106 | 0 |
Cc1c(-c2ncnc3[nH]c(-c4ccc(N5CCN(CC6CCN(c7ccc(N8CCC(=O)NC8=O)cc7)CC6)CC5)nc4)cc23)cccc1N1CCn2c(cc3c2CC(C)(C)C3)C1=O | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | null | DC50 | nM | 3.4 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q06187 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | null | Homo sapiens | DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHODS OF USE (patent) | HTFR assay
After 6h treatment, add 10μl 4xlysis buffer to each well; seal the plate and incubate 30min at room temperature on a plate shaker; Once the cells are lysed, 16 μL of cell lysate are transferred to a PE 384-well HTRF detection plate; 4 μL of pre-mixed HTRF antibodies are added to each well; Cover the plate wi... | TPDdb | HTRF | TPD-0BNKRQ | null | 31 | false | 367 | 0 |
Cc1c(C#N)c(-c2ccc(C#N)cc2)c(C)n1Cc1ccc(C(=O)NCCOCCOCCOCCNC(=O)[C@H](CC(C)C)NC(=O)[C@@H](O)[C@H](N)Cc2ccccc2)cc1 | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | cIAP1 | 22Rv1 | DC50 | nM | 21,600 | null | null | null | null | 6 | null | null | null | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q13490 | MHKTASQRLFPGPSYQNIKSIMEDSTILSDWTNSNKQKMKYDFSCELYRMSTYSTFPAGVPVSERSLARAGFYYTGVNDKVKCFCCGLMLDNWKLGDSPIQKHKQLYPSCSFIQNLVSASLGSTSKNTSPMRNSFAHSLSPTLEHSSLFSGSYSSLSPNPLNSRAVEDISSSRTNPYSYAMSTEEARFLTYHMWPLTFLSPSELARAGFYYIGPGDRVACFACGGKLSNWEPKDDAMSEHRRHFPNCPFLENSLETLRFSISNLSMQTHAARMRTFMYWPSSVPVQPEQLASAGFYYVGRNDDVKCFCCDGGLRCWESGD... | CVCL_1045 | Homo sapiens | 10.1021/acs.jmedchem.7b00168 | Degradation of AR in 22Rv1 cells after 6 h treatment | PROTAC-DB | null | null | African=0.89%; Native American=0.23%; East Asian, North=0.52%; East Asian, South=0%; South Asian=0.27%; European, North=67.46%; European, South=30.62%.
Contains at least 10 integrated copies of xenotropic murine leukemia virus-related virus (XMRV) genome and produces a high titer of the virus.
Mutation; HGNC; HGNC Muta... | 16 | false | 1,107 | 132 |
Cc1c(C(=O)Nc2cc(C(F)(F)F)ccn2)ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CC5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)CC5)CC4)cc2CC3)c1F | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 0.415 | 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-YA2U8Y | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 481 | 15 |
Cc1c(C(=O)Nc2cc(C)n(C)n2)ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CC5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)CC5)CC4)cc2CC3)c1F | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 4.37 | 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-B30O21 | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 1,108 | 15 |
Cc1c(C(=O)Nc2cc(N3CCCC3)ccn2)ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CC5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)CC5)CC4)cc2CC3)c1F | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 1.9 | 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-K0YOI4 | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 1,109 | 15 |
Cc1c(C(=O)Nc2ccc3[nH]ccc3n2)ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CC5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)CC5)CC4)cc2CC3)c1F | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 0.543 | 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-9Z79WK | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 1,110 | 15 |
Cc1c(C(=O)Nc2cccc(-c3ccccc3)n2)ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CC5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)CC5)CC4)cc2CC3)c1F | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 15 | 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-K6VL61 | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 1,111 | 15 |
Cc1c(C(=O)Nc2ccn(C)n2)ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CC5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)CC5)CC4)cc2CC3)c1F | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 4.1 | 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-ACOAUW | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 1,108 | 15 |
Cc1c(C(=O)Nc2cn(C)cn2)ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(C(=O)C5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)CC5)CC4)cc2CC3)c1F | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 1.36 | 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-K2DJ6G | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 1,112 | 15 |
Cc1c(C(=O)Nc2cn(C)cn2)ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CC5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)CC5)CC4)cc2CC3)c1F | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 0.591 | 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-YH2U1M | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 1,113 | 15 |
Cc1c(C(=O)Nc2cn(C)cn2)ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CCc5cc(F)c(C6CCC(=O)NC6=O)c(F)c5)CC4)cc2CC3)c1F | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 1.63 | 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-G7TCNU | 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 |
Cc1c(C(=O)Nc2cn(C)cn2)ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CCc5cc(F)c([C@H]6CCC(=O)NC6=O)c(F)c5)CC4)cc2CC3)c1F | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 0.414 | 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-9H32M1 | 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 |
Cc1c(C(=O)Nc2cn(C)cn2)ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CCc5cccc6c5oc(=O)n6C5CCC(=O)NC5=O)CC4)cc2CC3)c1F | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 0.706 | 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-8BSYXG | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 1,114 | 15 |
Cc1c(C(=O)Nc2cn(C)cn2)ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(C[C@H]5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)C5)CC4)cc2CC3)c1F | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 1.86 | 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-KG3ROD | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 1,115 | 15 |
Cc1c(C(=O)Nc2cn(C3CCC4(CC3)CCN(CC3CC(OCC#Cc5cccc6c5n(C)c(=O)n6C5CCC(=O)NC5=O)C3)CC4)nc2C(F)F)cnn1/C=C\C(=N)N1C[C@H]2C[C@@H]1CO2 | IRAK4 | MNKPITPSTYVRCLNVGLIRKLSDFIDPQEGWKKLAVAIKKPSGDDRYNQFHIRRFEALLQTGKSPTSELLFDWGTTNCTVGDLVDLLIQNEFFAPASLLLPDAVPKTANTLPSKEAITVQQKQMPFCDKDRTLMTPVQNLEQSYMPPDSSSPENKSLEVSDTRFHSFSFYELKNVTNNFDERPISVGGNKMGEGGFGVVYKGYVNNTTVAVKKLAAMVDITTEELKQQFDQEIKVMAKCQHENLVELLGFSSDGDDLCLVYVYMPNGSLLDRLSCLDGTPPLSWHMRCKIAQGAANGINFLHENHHIHRDIKSANILLD... | CRBN | SU-DHL-2 | DC50 | nM | 33 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q9NWZ3 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_9550 | Homo sapiens | IRAK4 DEGRADER AND USE THEREOF (patent) | Degradation of IRAK4 by Compounds in SU-DHL-2 and OCI-LY3 Cells
(1) Experimental Purpose
Flow cytometry was used to detect the degradation level of IRAK4 protein in SU-DHL-2 cell lines.
Experimental Methods
Step 1: SU-DHL-2 cell lines were cultured in RPMI 1640 medium supplemented with 10% fetal bovine serum and 1% dou... | TPDdb | Flow Cytometry | TPD-QUIA54 | Mutation; HGNC; HGNC
In situ; Pleural effusion;
Caucasian.
Cancer cell line | 25 | false | 1,116 | 0 |
Cc1c(C(=O)Nc2cnc3ccccc3n2)ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CC5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)CC5)CC4)cc2CC3)c1F | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 1.69 | 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-U9YKZI | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 1,117 | 15 |
Cc1c(C(=O)Nc2cscn2)ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(C(=O)C5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)CC5)CC4)cc2CC3)c1F | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 1.1 | 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-3VTYHA | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 1,118 | 15 |
Cc1c(C(=O)Nc2cscn2)ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(C5CC(c6ccc(N[C@@H]7CCC(=O)NC7=O)cc6)C5)CC4)cc2CC3)c1F | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 2.14 | 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-XXBD6E | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 1,119 | 116 |
Cc1c(C(=O)Nc2cscn2)ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(C5CC(c6ccc(N[C@H]7CCC(=O)NC7=O)cc6)C5)CC4)cc2CC3)c1F | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 2.42 | 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-NK7VFR | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 1,119 | 116 |
Cc1c(C(=O)Nc2cscn2)ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CC5CCN(c6ccc(CN7CCC(=O)NC7=O)cc6)CC5)CC4)cc2CC3)c1F | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 1.1 | 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-A6WDLH | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 1,120 | 15 |
Cc1c(C(=O)Nc2cscn2)ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CC5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)CC5)CC4)cc2CC3)c1F | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 0.378 | 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-BGCUTN | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 1,121 | 15 |
Cc1c(C(=O)Nc2cscn2)ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CC5CCN(c6cccc(CN7CCC(=O)NC7=O)c6)CC5)CC4)cc2CC3)c1F | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 2.72 | 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-TIIISA | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 1,122 | 15 |
Cc1c(C(=O)Nc2cscn2)ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CC5CN(c6ccc(N7CCC(=O)NC7=O)cc6)C5)CC4)cc2CC3)c1F | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 2.11 | 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-GYSLII | 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 |
Cc1c(C(=O)Nc2cscn2)ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CCc5cc(F)c([C@H]6CCC(=O)NC6=O)c(F)c5)CC4)cc2CC3)c1F | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 1.7 | 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-LILPF4 | 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 |
Cc1c(C(=O)Nc2cscn2)ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CCc5cccc6c5oc(=O)n6C5CCC(=O)NC5=O)CC4)cc2CC3)c1F | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 0.586 | 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-Y4ODIZ | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 1,123 | 15 |
Cc1c(C(=O)Nc2cscn2)ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(C[C@H]5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)C5)CC4)cc2CC3)c1F | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 3.3 | 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-S8164J | 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 |
Cc1c(C(=O)Nc2nc(C(F)(F)F)n[nH]2)ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CC5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)CC5)CC4)cc2CC3)c1F | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 1.87 | 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-ONQLFB | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 1,124 | 15 |
Cc1c(C(=O)Nc2nccs2)ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CC5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)CC5)CC4)cc2CC3)c1F | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 2.9 | 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-QE7ZW2 | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 1,125 | 15 |
Cc1c(C(=O)Nc2ncn(C)n2)ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CC5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)CC5)CC4)cc2CC3)c1F | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 2.32 | 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-0W7M1N | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 1,126 | 15 |
Cc1c(C(=O)Nc2ncnn2C)ccc(-c2nn3c(c2C(N)=O)Nc2ccc(N4CCN(CC5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)CC5)CC4)cc2CC3)c1F | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | TMD8 | DC50 | nM | 3.77 | 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-WDY5N9 | Mutation; HGNC; HGNC Mutation; HGNC; HGNC
Genetically heterogeneous, consists of 3 subclones.
A*02
In situ; Bone marrow;
Japanese.
Cancer cell line | 31 | false | 1,124 | 15 |
Cc1c(F)cc2[nH]ncc2c1-c1c(C2CC2)cc2c(N3CC(C#N)C3)nc(OCC(C)(C)CN(C)C)nc2c1OCc1ccc(C(=O)N2CCN(Cc3ccc4c(N5CCC(=O)NC5=O)nn(C)c4c3)C[C@@H]2C)cc1 | KRAS | MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM | CRBN | PaTu 8902 | DC50 | nM | 11 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P01116 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1845 | Homo sapiens | HETEROCYCLIC COMPOUND FOR INDUCING DEGRADATION OF G12V MUTANT KRAS PROTEIN (patent) | Test Example 1 Evaluation of RAS G12V degrading effect on human KRAS G12V mutation-positive pancreatic cancer line PA-TU-8902 The RAS G12V degrading effect of the test compound was evaluated by measuring the RAS G12V expression level by Cell ELISA method.
36 μL of PA-TU-8902 cells were seeded in a 384-well plate at 1.5... | TPDdb | ELISA | TPD-VFPYPP | African=0%; Native American=0.21%; East Asian, North=1.73%; East Asian, South=0%; South Asian=0%; European, North=62.61%; European, South=35.45%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*02
Stable (MSS) (Sanger).
In situ; Pancreas;
Caucasian.
Cancer cell line | -1 | false | 773 | 57 |
Cc1c(F)cc2[nH]ncc2c1-c1c(C2CC2)cc2c(N3CC(C#N)C3)nc(OCC(C)(C)CN(C)C)nc2c1OCc1ccc(C(=O)N2CCN(Cc3ccc4c(N5CCC(=O)NC5=O)nn(C)c4c3)C[C@@H]2C)cc1 | KRAS | MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM | CRBN | PaTu 8902 | Dmax | % | 88 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P01116 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1845 | Homo sapiens | HETEROCYCLIC COMPOUND FOR INDUCING DEGRADATION OF G12V MUTANT KRAS PROTEIN (patent) | Test Example 1 Evaluation of RAS G12V degrading effect on human KRAS G12V mutation-positive pancreatic cancer line PA-TU-8902 The RAS G12V degrading effect of the test compound was evaluated by measuring the RAS G12V expression level by Cell ELISA method.
36 μL of PA-TU-8902 cells were seeded in a 384-well plate at 1.5... | TPDdb | ELISA | TPD-VFPYPP | African=0%; Native American=0.21%; East Asian, North=1.73%; East Asian, South=0%; South Asian=0%; European, North=62.61%; European, South=35.45%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*02
Stable (MSS) (Sanger).
In situ; Pancreas;
Caucasian.
Cancer cell line | -1 | false | 773 | 57 |
Cc1c(F)cc2[nH]ncc2c1-c1c(C2CC2)cc2c(N3CC(C#N)C3)nc(OCC(C)(C)CN(C)C)nc2c1OCc1ccc(C(=O)N2CCN(Cc3ccc4c(c3)n(C)c(=O)n4C3CCC(=O)NC3=O)C[C@@H]2C)cc1 | KRAS | MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM | CRBN | PaTu 8902 | DC50 | nM | 6 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P01116 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1845 | Homo sapiens | HETEROCYCLIC COMPOUND FOR INDUCING DEGRADATION OF G12V MUTANT KRAS PROTEIN (patent) | Test Example 1 Evaluation of RAS G12V degrading effect on human KRAS G12V mutation-positive pancreatic cancer line PA-TU-8902 The RAS G12V degrading effect of the test compound was evaluated by measuring the RAS G12V expression level by Cell ELISA method.
36 μL of PA-TU-8902 cells were seeded in a 384-well plate at 1.5... | TPDdb | ELISA | TPD-9VTWWV | African=0%; Native American=0.21%; East Asian, North=1.73%; East Asian, South=0%; South Asian=0%; European, North=62.61%; European, South=35.45%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*02
Stable (MSS) (Sanger).
In situ; Pancreas;
Caucasian.
Cancer cell line | -1 | false | 774 | 0 |
Cc1c(F)cc2[nH]ncc2c1-c1c(C2CC2)cc2c(N3CC(C#N)C3)nc(OCC(C)(C)CN(C)C)nc2c1OCc1ccc(C(=O)N2CCN(Cc3ccc4c(c3)n(C)c(=O)n4C3CCC(=O)NC3=O)C[C@@H]2C)cc1 | KRAS | MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM | CRBN | PaTu 8902 | Dmax | % | 88 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P01116 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1845 | Homo sapiens | HETEROCYCLIC COMPOUND FOR INDUCING DEGRADATION OF G12V MUTANT KRAS PROTEIN (patent) | Test Example 1 Evaluation of RAS G12V degrading effect on human KRAS G12V mutation-positive pancreatic cancer line PA-TU-8902 The RAS G12V degrading effect of the test compound was evaluated by measuring the RAS G12V expression level by Cell ELISA method.
36 μL of PA-TU-8902 cells were seeded in a 384-well plate at 1.5... | TPDdb | ELISA | TPD-9VTWWV | African=0%; Native American=0.21%; East Asian, North=1.73%; East Asian, South=0%; South Asian=0%; European, North=62.61%; European, South=35.45%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*02
Stable (MSS) (Sanger).
In situ; Pancreas;
Caucasian.
Cancer cell line | -1 | false | 774 | 0 |
Cc1c(F)cc2[nH]ncc2c1-c1c(C2CC2)cc2c(N3CCOCC3)nc(OCC(C)(C)CN(C)C)nc2c1OCc1ccc(C(=O)N2CCN(Cc3ccc4c(c3)n(C)c(=O)n4C3CCC(=O)NC3=O)C[C@@H]2C)cc1 | KRAS | MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM | CRBN | PaTu 8902 | DC50 | nM | 6 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P01116 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1845 | Homo sapiens | HETEROCYCLIC COMPOUND FOR INDUCING DEGRADATION OF G12V MUTANT KRAS PROTEIN (patent) | Test Example 1 Evaluation of RAS G12V degrading effect on human KRAS G12V mutation-positive pancreatic cancer line PA-TU-8902 The RAS G12V degrading effect of the test compound was evaluated by measuring the RAS G12V expression level by Cell ELISA method.
36 μL of PA-TU-8902 cells were seeded in a 384-well plate at 1.5... | TPDdb | ELISA | TPD-KLUID1 | African=0%; Native American=0.21%; East Asian, North=1.73%; East Asian, South=0%; South Asian=0%; European, North=62.61%; European, South=35.45%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*02
Stable (MSS) (Sanger).
In situ; Pancreas;
Caucasian.
Cancer cell line | -1 | false | 1,127 | 0 |
Cc1c(F)cc2[nH]ncc2c1-c1c(C2CC2)cc2c(N3CCOCC3)nc(OCC(C)(C)CN(C)C)nc2c1OCc1ccc(C(=O)N2CCN(Cc3ccc4c(c3)n(C)c(=O)n4C3CCC(=O)NC3=O)C[C@@H]2C)cc1 | KRAS | MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM | CRBN | PaTu 8902 | Dmax | % | 88 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P01116 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1845 | Homo sapiens | HETEROCYCLIC COMPOUND FOR INDUCING DEGRADATION OF G12V MUTANT KRAS PROTEIN (patent) | Test Example 1 Evaluation of RAS G12V degrading effect on human KRAS G12V mutation-positive pancreatic cancer line PA-TU-8902 The RAS G12V degrading effect of the test compound was evaluated by measuring the RAS G12V expression level by Cell ELISA method.
36 μL of PA-TU-8902 cells were seeded in a 384-well plate at 1.5... | TPDdb | ELISA | TPD-KLUID1 | African=0%; Native American=0.21%; East Asian, North=1.73%; East Asian, South=0%; South Asian=0%; European, North=62.61%; European, South=35.45%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*02
Stable (MSS) (Sanger).
In situ; Pancreas;
Caucasian.
Cancer cell line | -1 | false | 1,127 | 0 |
Cc1c(F)cc2[nH]ncc2c1-c1c(C2CC2)cc2c(N3CC[C@H]3C(N)=O)nc(OCC(C)(C)CN(C)C)nc2c1OCc1ccc(C(=O)N2CCN(Cc3ccc4c(c3)n(C)c(=O)n4C3CCC(=O)NC3=O)C[C@@H]2C)cc1 | KRAS | MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM | CRBN | PaTu 8902 | DC50 | nM | 14 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P01116 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1845 | Homo sapiens | HETEROCYCLIC COMPOUND FOR INDUCING DEGRADATION OF G12V MUTANT KRAS PROTEIN (patent) | Test Example 1 Evaluation of RAS G12V degrading effect on human KRAS G12V mutation-positive pancreatic cancer line PA-TU-8902 The RAS G12V degrading effect of the test compound was evaluated by measuring the RAS G12V expression level by Cell ELISA method.
36 μL of PA-TU-8902 cells were seeded in a 384-well plate at 1.5... | TPDdb | ELISA | TPD-QM0YY7 | African=0%; Native American=0.21%; East Asian, North=1.73%; East Asian, South=0%; South Asian=0%; European, North=62.61%; European, South=35.45%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*02
Stable (MSS) (Sanger).
In situ; Pancreas;
Caucasian.
Cancer cell line | -1 | false | 774 | 89 |
Cc1c(F)cc2[nH]ncc2c1-c1c(C2CC2)cc2c(N3CC[C@H]3C(N)=O)nc(OCC(C)(C)CN(C)C)nc2c1OCc1ccc(C(=O)N2CCN(Cc3ccc4c(c3)n(C)c(=O)n4C3CCC(=O)NC3=O)C[C@@H]2C)cc1 | KRAS | MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM | CRBN | PaTu 8902 | Dmax | % | 99 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P01116 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1845 | Homo sapiens | HETEROCYCLIC COMPOUND FOR INDUCING DEGRADATION OF G12V MUTANT KRAS PROTEIN (patent) | Test Example 1 Evaluation of RAS G12V degrading effect on human KRAS G12V mutation-positive pancreatic cancer line PA-TU-8902 The RAS G12V degrading effect of the test compound was evaluated by measuring the RAS G12V expression level by Cell ELISA method.
36 μL of PA-TU-8902 cells were seeded in a 384-well plate at 1.5... | TPDdb | ELISA | TPD-QM0YY7 | African=0%; Native American=0.21%; East Asian, North=1.73%; East Asian, South=0%; South Asian=0%; European, North=62.61%; European, South=35.45%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*02
Stable (MSS) (Sanger).
In situ; Pancreas;
Caucasian.
Cancer cell line | -1 | false | 774 | 89 |
Cc1c(F)cc2[nH]ncc2c1-c1c(C2CC2)cc2c(N3CC[C@H]3C(N)=O)nc(OC[C@@H]3CCN(C)C3)nc2c1OCc1ccc(C(=O)N2CCN(Cc3ccc4c(N5CCC(=O)NC5=O)nn(C)c4c3)C[C@@H]2C)cc1 | KRAS | MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM | CRBN | PaTu 8902 | DC50 | nM | 38 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P01116 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1845 | Homo sapiens | HETEROCYCLIC COMPOUND FOR INDUCING DEGRADATION OF G12V MUTANT KRAS PROTEIN (patent) | Test Example 1 Evaluation of RAS G12V degrading effect on human KRAS G12V mutation-positive pancreatic cancer line PA-TU-8902 The RAS G12V degrading effect of the test compound was evaluated by measuring the RAS G12V expression level by Cell ELISA method.
36 μL of PA-TU-8902 cells were seeded in a 384-well plate at 1.5... | TPDdb | ELISA | TPD-RH5RU7 | African=0%; Native American=0.21%; East Asian, North=1.73%; East Asian, South=0%; South Asian=0%; European, North=62.61%; European, South=35.45%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*02
Stable (MSS) (Sanger).
In situ; Pancreas;
Caucasian.
Cancer cell line | -1 | false | 1,128 | 57 |
Cc1c(F)cc2[nH]ncc2c1-c1c(C2CC2)cc2c(N3CC[C@H]3C(N)=O)nc(OC[C@@H]3CCN(C)C3)nc2c1OCc1ccc(C(=O)N2CCN(Cc3ccc4c(N5CCC(=O)NC5=O)nn(C)c4c3)C[C@@H]2C)cc1 | KRAS | MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM | CRBN | PaTu 8902 | Dmax | % | 103 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P01116 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1845 | Homo sapiens | HETEROCYCLIC COMPOUND FOR INDUCING DEGRADATION OF G12V MUTANT KRAS PROTEIN (patent) | Test Example 1 Evaluation of RAS G12V degrading effect on human KRAS G12V mutation-positive pancreatic cancer line PA-TU-8902 The RAS G12V degrading effect of the test compound was evaluated by measuring the RAS G12V expression level by Cell ELISA method.
36 μL of PA-TU-8902 cells were seeded in a 384-well plate at 1.5... | TPDdb | ELISA | TPD-RH5RU7 | African=0%; Native American=0.21%; East Asian, North=1.73%; East Asian, South=0%; South Asian=0%; European, North=62.61%; European, South=35.45%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*02
Stable (MSS) (Sanger).
In situ; Pancreas;
Caucasian.
Cancer cell line | -1 | false | 1,128 | 57 |
Cc1c(F)cc2[nH]ncc2c1-c1c(C2CC2)cc2c(NC3CN(c4ncccn4)C3)nc(OCC(C)(C)CN(C)C)nc2c1OCc1ccc(C(=O)N2CCN(Cc3ccc4c(c3)n(C)c(=O)n4C3CCC(=O)NC3=O)C[C@@H]2C)cc1 | KRAS | MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM | CRBN | PaTu 8902 | DC50 | nM | 5 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P01116 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1845 | Homo sapiens | HETEROCYCLIC COMPOUND FOR INDUCING DEGRADATION OF G12V MUTANT KRAS PROTEIN (patent) | Test Example 1 Evaluation of RAS G12V degrading effect on human KRAS G12V mutation-positive pancreatic cancer line PA-TU-8902 The RAS G12V degrading effect of the test compound was evaluated by measuring the RAS G12V expression level by Cell ELISA method.
36 μL of PA-TU-8902 cells were seeded in a 384-well plate at 1.5... | TPDdb | ELISA | TPD-FJRQU1 | African=0%; Native American=0.21%; East Asian, North=1.73%; East Asian, South=0%; South Asian=0%; European, North=62.61%; European, South=35.45%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*02
Stable (MSS) (Sanger).
In situ; Pancreas;
Caucasian.
Cancer cell line | -1 | false | 1,129 | 0 |
Cc1c(F)cc2[nH]ncc2c1-c1c(C2CC2)cc2c(NC3CN(c4ncccn4)C3)nc(OCC(C)(C)CN(C)C)nc2c1OCc1ccc(C(=O)N2CCN(Cc3ccc4c(c3)n(C)c(=O)n4C3CCC(=O)NC3=O)C[C@@H]2C)cc1 | KRAS | MTEYKLVVVGAGGVGKSALTIQLIQNHFVDEYDPTIEDSYRKQVVIDGETCLLDILDTAGQEEYSAMRDQYMRTGEGFLCVFAINNTKSFEDIHHYREQIKRVKDSEDVPMVLVGNKCDLPSRTVDTKQAQDLARSYGIPFIETSAKTRQRVEDAFYTLVREIRQYRLKKISKEEKTPGCVKIKKCIIM | CRBN | PaTu 8902 | Dmax | % | 81 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P01116 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1845 | Homo sapiens | HETEROCYCLIC COMPOUND FOR INDUCING DEGRADATION OF G12V MUTANT KRAS PROTEIN (patent) | Test Example 1 Evaluation of RAS G12V degrading effect on human KRAS G12V mutation-positive pancreatic cancer line PA-TU-8902 The RAS G12V degrading effect of the test compound was evaluated by measuring the RAS G12V expression level by Cell ELISA method.
36 μL of PA-TU-8902 cells were seeded in a 384-well plate at 1.5... | TPDdb | ELISA | TPD-FJRQU1 | African=0%; Native American=0.21%; East Asian, North=1.73%; East Asian, South=0%; South Asian=0%; European, North=62.61%; European, South=35.45%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*02
Stable (MSS) (Sanger).
In situ; Pancreas;
Caucasian.
Cancer cell line | -1 | false | 1,129 | 0 |
Cc1c(N2CCC3(CCN(c4ccc(C(=O)N5CCC(CN6CCN(c7cccc(NC8CCC(=O)NC8=O)c7)CC6)CC5)cc4)CC3)C2)ccc(C#N)c1Cl | AR | MEVQLGLGRVYPRPPSKTYRGAFQNLFQSVREVIQNPGPRHPEAASAAPPGASLLLLQQQQQQQQQQQQQQQQQQQQQQQETSPRQQQQQQGEDGSPQAHRRGPTGYLVLDEEQQPSQPQSALECHPERGCVPEPGAAVAASKGLPQQLPAPPDEDDSAAPSTLSLLGPTFPGLSSCSADLKDILSEASTMQLLQQQQQEAVSEGSSSGRAREASGAPTSSKDNYLGGTSTISDNAKELCKAVSVSMGLGVEALEHLSPGEQLRGDCMYAPLLGVPPAVRPTPCAPLAECKGSLLDDSAGKSTEDTAEYSPFKGGYTKGL... | CRBN | LNCaP | DC50 | nM | 11.7 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | P10275 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0395 | Homo sapiens | CHIMERIC COMPOUND FOR TARGETED DEGRADATION OF ANDROGEN RECEPTOR PROTEIN, PREPARATION METHOD THEREFOR, AND MEDICAL USE THEREOF (patent) | Degradation of the Androgen Receptor in LNCaP Cells by Compounds of the Disclosure
The following in vitro cell-based assay measures the degradation activity of test compounds against the androgen receptor (AR) in human prostate cancer cell lines. The activity is expressed as a DC50 value. On the first day of the experi... | TPDdb | ELISA | TPD-05FFW0 | Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*01
Instable (MSI).
Metastatic; Left supraclavicular lymph node;
Caucasian.
Space-flown cell line (cellonaut).
Cancer cell line | 16 | false | 1,070 | 117 |
Cc1c(NC(=O)c2ccc(C(C)(C)O)cc2F)cc(F)cc1-c1ncnc2[nH]c(-c3ccc(C4CCN(CC5CCN(c6ccc(N7CCC(=O)NC7=O)cc6)CC5)CC4)cc3)cc12 | BTK | MAAVILESIFLKRSQQKKKTSPLNFKKRLFLLTVHKLSYYEYDFERGRRGSKKGSIDVEKITCVETVVPEKNPPPERQIPRRGEESSEMEQISIIERFPYPFQVVYDEGPLYVFSPTEELRKRWIHQLKNVIRYNSDLVQKYHPCFWIDGQYLCCSQTAKNAMGCQILENRNGSLKPGSSHRKTKKPLPPTPEEDQILKKPLPPEPAAAPVSTSELKKVVALYDYMPMNANDLQLRKGDEYFILEESNLPWWRARDKNGQEGYIPSNYVTEAEDSIEMYEWYSKHMTRSQAEQLLKQEGKEGGFIVRDSSKAGKYTVSVF... | CRBN | null | DC50 | nM | 1.5 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q06187 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | null | Homo sapiens | DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHODS OF USE (patent) | HTFR assay
After 6h treatment, add 10μl 4xlysis buffer to each well; seal the plate and incubate 30min at room temperature on a plate shaker; Once the cells are lysed, 16 μL of cell lysate are transferred to a PE 384-well HTRF detection plate; 4 μL of pre-mixed HTRF antibodies are added to each well; Cover the plate wi... | TPDdb | HTRF | TPD-2YKC9C | null | 31 | false | 35 | 49 |
Cc1c(Nc2nc3ccccc3s2)nnc2c1CCCN2c1ccc(-c2cnn(CC34CC5(C)CC(C)(C3)CC(OCCN(C)CCCCCC(=O)N3CCC(c6ccc7c(c6)CN(C6CCC(=O)NC6=O)C7=O)CC3)(C5)C4)c2C)c(C(=O)O)n1 | BCL2L1 | MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK | CRBN | HCT 116 | DC50 | nM | 316 | null | null | null | null | null | > | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q07817 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0291 | Homo sapiens | SELECTIVE BCL-XL PROTAC COMPOUNDS AND METHODS OF USE (patent) | HCT116 cells were purchased from ATCC and cultivated in RPMI 1640 supplemented with 10% heat inactivated fetal bovine serum, penicillin (100 IU/ml), streptomycin (100 μg/ml) and L-glutamine (2 mM). Cells were cultured at 37°C in a humidified atmosphere containing 5% CO2.
Cells were seeded in 96 microwell plates, 24 h ... | TPDdb | Automated Capillary Electrophoresis Immunoassay | TPD-D5U24J | African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut... | 5 | false | 1,130 | 0 |
Cc1c(Nc2nc3ccccc3s2)nnc2c1CCCN2c1ccc(-c2cnn(CC34CC5(C)CC(C)(C3)CC(OCCN(C)CCCCCCCC(=O)N3CCC(c6ccc7c(c6)CN(C6CCC(=O)NC6=O)C7=O)CC3)(C5)C4)c2C)c(C(=O)O)n1 | BCL2L1 | MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK | CRBN | HCT 116 | DC50 | nM | 316 | null | null | null | null | null | > | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q07817 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0291 | Homo sapiens | SELECTIVE BCL-XL PROTAC COMPOUNDS AND METHODS OF USE (patent) | HCT116 cells were purchased from ATCC and cultivated in RPMI 1640 supplemented with 10% heat inactivated fetal bovine serum, penicillin (100 IU/ml), streptomycin (100 μg/ml) and L-glutamine (2 mM). Cells were cultured at 37°C in a humidified atmosphere containing 5% CO2.
Cells were seeded in 96 microwell plates, 24 h ... | TPDdb | Automated Capillary Electrophoresis Immunoassay | TPD-0P2CNP | African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut... | 5 | false | 1,131 | 0 |
Cc1c(Nc2nc3ccccc3s2)nnc2c1CCCN2c1ccc(-c2cnn(CC34CC5(C)CC(C)(C3)CC(OCCN(C)CCCCCCCCC(=O)N3CCC(c6ccc7c(c6)CN(C6CCC(=O)NC6=O)C7=O)CC3)(C5)C4)c2C)c(C(=O)O)n1 | BCL2L1 | MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK | CRBN | HCT 116 | DC50 | nM | 316 | null | null | null | null | null | > | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q07817 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0291 | Homo sapiens | SELECTIVE BCL-XL PROTAC COMPOUNDS AND METHODS OF USE (patent) | HCT116 cells were purchased from ATCC and cultivated in RPMI 1640 supplemented with 10% heat inactivated fetal bovine serum, penicillin (100 IU/ml), streptomycin (100 μg/ml) and L-glutamine (2 mM). Cells were cultured at 37°C in a humidified atmosphere containing 5% CO2.
Cells were seeded in 96 microwell plates, 24 h ... | TPDdb | Automated Capillary Electrophoresis Immunoassay | TPD-HBCJT7 | African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut... | 5 | false | 1,132 | 0 |
Cc1c(Nc2nc3ccccc3s2)nnc2c1CCCN2c1ccc(-c2cnn(CC34CC5(C)CC(C)(C3)CC(OCCN(C)CCCCCCCCCCCC(=O)N3CCC(c6ccc7c(c6)CN(C6CCC(=O)NC6=O)C7=O)CC3)(C5)C4)c2C)c(C(=O)O)n1 | BCL2L1 | MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK | CRBN | HCT 116 | DC50 | nM | 0.711 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q07817 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0291 | Homo sapiens | SELECTIVE BCL-XL PROTAC COMPOUNDS AND METHODS OF USE (patent) | HCT116 cells were purchased from ATCC and cultivated in RPMI 1640 supplemented with 10% heat inactivated fetal bovine serum, penicillin (100 IU/ml), streptomycin (100 μg/ml) and L-glutamine (2 mM). Cells were cultured at 37°C in a humidified atmosphere containing 5% CO2.
Cells were seeded in 96 microwell plates, 24 h ... | TPDdb | Automated Capillary Electrophoresis Immunoassay | TPD-9S05V0 | African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut... | 5 | false | 1,133 | 0 |
Cc1c(Nc2nc3ccccc3s2)nnc2c1CCCN2c1ccc(-c2cnn(CC34CC5(C)CC(C)(C3)CC(OCCN(C)CCCCCCCCCCCCC(=O)N3CCC(c6ccc7c(c6)CN(C6CCC(=O)NC6=O)C7=O)CC3)(C5)C4)c2C)c(C(=O)O)n1 | BCL2L1 | MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK | CRBN | HCT 116 | DC50 | nM | 0.121 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q07817 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0291 | Homo sapiens | SELECTIVE BCL-XL PROTAC COMPOUNDS AND METHODS OF USE (patent) | HCT116 cells were purchased from ATCC and cultivated in RPMI 1640 supplemented with 10% heat inactivated fetal bovine serum, penicillin (100 IU/ml), streptomycin (100 μg/ml) and L-glutamine (2 mM). Cells were cultured at 37°C in a humidified atmosphere containing 5% CO2.
Cells were seeded in 96 microwell plates, 24 h ... | TPDdb | Automated Capillary Electrophoresis Immunoassay | TPD-9TWBZJ | African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut... | 5 | false | 1,134 | 0 |
Cc1c(Nc2nc3ccccc3s2)nnc2c1CCCN2c1ccc(-c2cnn(CC34CC5(C)CC(C)(C3)CC(OCCN(C)CCCCCCCCCCCCCCCC(=O)N3CCC(c6ccc7c(c6)CN(C6CCC(=O)NC6=O)C7=O)CC3)(C5)C4)c2C)c(C(=O)O)n1 | BCL2L1 | MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK | CRBN | HCT 116 | DC50 | nM | 0.133 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q07817 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0291 | Homo sapiens | SELECTIVE BCL-XL PROTAC COMPOUNDS AND METHODS OF USE (patent) | HCT116 cells were purchased from ATCC and cultivated in RPMI 1640 supplemented with 10% heat inactivated fetal bovine serum, penicillin (100 IU/ml), streptomycin (100 μg/ml) and L-glutamine (2 mM). Cells were cultured at 37°C in a humidified atmosphere containing 5% CO2.
Cells were seeded in 96 microwell plates, 24 h ... | TPDdb | Automated Capillary Electrophoresis Immunoassay | TPD-9MM3V3 | African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut... | 5 | false | 1,135 | 0 |
Cc1c(Nc2nc3ccccc3s2)nnc2c1CCCN2c1ccc(-c2cnn(CC34CC5(C)CC(C)(C3)CC(OCCN(C)CCCCCCCCCCCCCCCCOc3ccc6c(c3)C(=O)N(C3CCC(=O)NC3=O)C6=O)(C5)C4)c2C)c(C(=O)O)n1 | BCL2L1 | MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK | CRBN | HCT 116 | DC50 | nM | 316 | null | null | null | null | null | > | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q07817 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0291 | Homo sapiens | SELECTIVE BCL-XL PROTAC COMPOUNDS AND METHODS OF USE (patent) | HCT116 cells were purchased from ATCC and cultivated in RPMI 1640 supplemented with 10% heat inactivated fetal bovine serum, penicillin (100 IU/ml), streptomycin (100 μg/ml) and L-glutamine (2 mM). Cells were cultured at 37°C in a humidified atmosphere containing 5% CO2.
Cells were seeded in 96 microwell plates, 24 h ... | TPDdb | Automated Capillary Electrophoresis Immunoassay | TPD-A077ZM | African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut... | 5 | false | 1,136 | 0 |
Cc1c(Nc2nc3ccccc3s2)nnc2c1CCCN2c1ccc(-c2cnn(CC34CC5(C)CC(C)(C3)CC(OCCN(C)CCCCCCCCCCCCCCCOc3ccc6c(c3)C(=O)N(C3CCC(=O)NC3=O)C6=O)(C5)C4)c2C)c(C(=O)O)n1 | BCL2L1 | MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK | CRBN | HCT 116 | DC50 | nM | 0.681 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q07817 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0291 | Homo sapiens | SELECTIVE BCL-XL PROTAC COMPOUNDS AND METHODS OF USE (patent) | HCT116 cells were purchased from ATCC and cultivated in RPMI 1640 supplemented with 10% heat inactivated fetal bovine serum, penicillin (100 IU/ml), streptomycin (100 μg/ml) and L-glutamine (2 mM). Cells were cultured at 37°C in a humidified atmosphere containing 5% CO2.
Cells were seeded in 96 microwell plates, 24 h ... | TPDdb | Automated Capillary Electrophoresis Immunoassay | TPD-EPGWED | African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut... | 5 | false | 1,137 | 0 |
Cc1c(Nc2nc3ccccc3s2)nnc2c1CCCN2c1ccc(-c2cnn(CC34CC5(C)CC(C)(C3)CC(OCCN(C)CCCCCCCCCCCCCCCOc3ccc6c(c3)C(=O)N(C3CCC(=O)NC3=O)C6=O)(C5)C4)c2C)c(C(=O)O)n1 | BCL2L1 | MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK | CRBN | NCI-H1650 | DC50 | nM | 1,670 | null | null | null | null | null | > | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q07817 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1483 | Homo sapiens | SELECTIVE BCL-XL PROTAC COMPOUNDS AND METHODS OF USE (patent) | The ability of the BCL-xL degrader low molecular weight compounds to inhibit cell proliferation and survival was assessed using the Promega CellTiter-Glo proliferation assay on the EBC-1 lung cancer cell line (RCB1965, obtained from RIKEN). The cells were cultured in media that is optimal for their growth at 5% CO2, 37... | TPDdb | HiBiT | TPD-EPGWED | African=0.57%; Native American=0%; East Asian, North=3.27%; East Asian, South=0%; South Asian=0%; European, North=61.83%; European, South=34.34%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*02
Stable (MSS) (Sanger).
Metastatic; Pleural effusion;
Caucasian.
Cancer cell line | 5 | false | 1,137 | 0 |
Cc1c(Nc2nc3ccccc3s2)nnc2c1CCCN2c1ccc(-c2cnn(CC34CC5(C)CC(C)(C3)CC(OCCN(C)CCCCCCCCCCCCCCOc3ccc6c(c3)C(=O)N(C3CCC(=O)NC3=O)C6=O)(C5)C4)c2C)c(C(=O)O)n1 | BCL2L1 | MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK | CRBN | HCT 116 | DC50 | nM | 0.341 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q07817 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0291 | Homo sapiens | SELECTIVE BCL-XL PROTAC COMPOUNDS AND METHODS OF USE (patent) | HCT116 cells were purchased from ATCC and cultivated in RPMI 1640 supplemented with 10% heat inactivated fetal bovine serum, penicillin (100 IU/ml), streptomycin (100 μg/ml) and L-glutamine (2 mM). Cells were cultured at 37°C in a humidified atmosphere containing 5% CO2.
Cells were seeded in 96 microwell plates, 24 h ... | TPDdb | Automated Capillary Electrophoresis Immunoassay | TPD-CFMZ7X | African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut... | 5 | false | 1,138 | 0 |
Cc1c(Nc2nc3ccccc3s2)nnc2c1CCCN2c1ccc(-c2cnn(CC34CC5(C)CC(C)(C3)CC(OCCN(C)CCCCCCCCCCCCCOc3ccc6c(c3)C(=O)N(C3CCC(=O)NC3=O)C6=O)(C5)C4)c2C)c(C(=O)O)n1 | BCL2L1 | MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK | CRBN | HCT 116 | DC50 | nM | 0.266 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q07817 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0291 | Homo sapiens | SELECTIVE BCL-XL PROTAC COMPOUNDS AND METHODS OF USE (patent) | HCT116 cells were purchased from ATCC and cultivated in RPMI 1640 supplemented with 10% heat inactivated fetal bovine serum, penicillin (100 IU/ml), streptomycin (100 μg/ml) and L-glutamine (2 mM). Cells were cultured at 37°C in a humidified atmosphere containing 5% CO2.
Cells were seeded in 96 microwell plates, 24 h ... | TPDdb | Automated Capillary Electrophoresis Immunoassay | TPD-UJ2ARF | African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut... | 5 | false | 1,139 | 0 |
Cc1c(Nc2nc3ccccc3s2)nnc2c1CCCN2c1ccc(-c2cnn(CC34CC5(C)CC(C)(C3)CC(OCCN(C)CCCCCCCCCCCCOc3ccc6c(c3)C(=O)N(C3CCC(=O)NC3=O)C6=O)(C5)C4)c2C)c(C(=O)O)n1 | BCL2L1 | MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK | CRBN | HCT 116 | DC50 | nM | 3.08 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q07817 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0291 | Homo sapiens | SELECTIVE BCL-XL PROTAC COMPOUNDS AND METHODS OF USE (patent) | HCT116 cells were purchased from ATCC and cultivated in RPMI 1640 supplemented with 10% heat inactivated fetal bovine serum, penicillin (100 IU/ml), streptomycin (100 μg/ml) and L-glutamine (2 mM). Cells were cultured at 37°C in a humidified atmosphere containing 5% CO2.
Cells were seeded in 96 microwell plates, 24 h ... | TPDdb | Automated Capillary Electrophoresis Immunoassay | TPD-GI60ZT | African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut... | 5 | false | 1,140 | 0 |
Cc1c(Nc2nc3ccccc3s2)nnc2c1CCCN2c1ccc(-c2cnn(CC34CC5(C)CC(C)(C3)CC(OCCN(C)CCCCCCCCCCCOc3ccc6c(c3)C(=O)N(C3CCC(=O)NC3=O)C6=O)(C5)C4)c2C)c(C(=O)O)n1 | BCL2L1 | MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK | CRBN | HCT 116 | DC50 | nM | 0.0447 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q07817 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0291 | Homo sapiens | SELECTIVE BCL-XL PROTAC COMPOUNDS AND METHODS OF USE (patent) | HCT116 cells were purchased from ATCC and cultivated in RPMI 1640 supplemented with 10% heat inactivated fetal bovine serum, penicillin (100 IU/ml), streptomycin (100 μg/ml) and L-glutamine (2 mM). Cells were cultured at 37°C in a humidified atmosphere containing 5% CO2.
Cells were seeded in 96 microwell plates, 24 h ... | TPDdb | Automated Capillary Electrophoresis Immunoassay | TPD-IBREF0 | African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut... | 5 | false | 1,141 | 0 |
Cc1c(Nc2nc3ccccc3s2)nnc2c1CCCN2c1ccc(-c2cnn(CC34CC5(C)CC(C)(C3)CC(OCCN(C)CCCCCCCCCCOc3ccc6c(c3)C(=O)N(C3CCC(=O)NC3=O)C6=O)(C5)C4)c2C)c(C(=O)O)n1 | BCL2L1 | MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK | CRBN | HCT 116 | DC50 | nM | 0.11 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q07817 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0291 | Homo sapiens | SELECTIVE BCL-XL PROTAC COMPOUNDS AND METHODS OF USE (patent) | HCT116 cells were purchased from ATCC and cultivated in RPMI 1640 supplemented with 10% heat inactivated fetal bovine serum, penicillin (100 IU/ml), streptomycin (100 μg/ml) and L-glutamine (2 mM). Cells were cultured at 37°C in a humidified atmosphere containing 5% CO2.
Cells were seeded in 96 microwell plates, 24 h ... | TPDdb | Automated Capillary Electrophoresis Immunoassay | TPD-YVR69D | African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut... | 5 | false | 1,142 | 0 |
Cc1c(Nc2nc3ccccc3s2)nnc2c1CCCN2c1ccc(-c2cnn(CC34CC5(C)CC(C)(C3)CC(OCCN(C)CCCCCCCCCCOc3ccc6c(c3)C(=O)N(C3CCC(=O)NC3=O)C6=O)(C5)C4)c2C)c(C(=O)O)n1 | BCL2L1 | MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK | CRBN | NCI-H1650 | DC50 | nM | 1,670 | null | null | null | null | null | > | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q07817 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_1483 | Homo sapiens | SELECTIVE BCL-XL PROTAC COMPOUNDS AND METHODS OF USE (patent) | The ability of the BCL-xL degrader low molecular weight compounds to inhibit cell proliferation and survival was assessed using the Promega CellTiter-Glo proliferation assay on the EBC-1 lung cancer cell line (RCB1965, obtained from RIKEN). The cells were cultured in media that is optimal for their growth at 5% CO2, 37... | TPDdb | HiBiT | TPD-YVR69D | African=0.57%; Native American=0%; East Asian, North=3.27%; East Asian, South=0%; South Asian=0%; European, North=61.83%; European, South=34.34%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC
A*02
Stable (MSS) (Sanger).
Metastatic; Pleural effusion;
Caucasian.
Cancer cell line | 5 | false | 1,142 | 0 |
Cc1c(Nc2nc3ccccc3s2)nnc2c1CCCN2c1ccc(-c2cnn(CC34CC5(C)CC(C)(C3)CC(OCCN(C)CCCCCCCCCOc3ccc6c(c3)C(=O)N(C3CCC(=O)NC3=O)C6=O)(C5)C4)c2C)c(C(=O)O)n1 | BCL2L1 | MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK | CRBN | HCT 116 | DC50 | nM | 0.0184 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q07817 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0291 | Homo sapiens | SELECTIVE BCL-XL PROTAC COMPOUNDS AND METHODS OF USE (patent) | HCT116 cells were purchased from ATCC and cultivated in RPMI 1640 supplemented with 10% heat inactivated fetal bovine serum, penicillin (100 IU/ml), streptomycin (100 μg/ml) and L-glutamine (2 mM). Cells were cultured at 37°C in a humidified atmosphere containing 5% CO2.
Cells were seeded in 96 microwell plates, 24 h ... | TPDdb | Automated Capillary Electrophoresis Immunoassay | TPD-LUYXO4 | African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut... | 5 | false | 1,143 | 0 |
Cc1c(Nc2nc3ccccc3s2)nnc2c1CCCN2c1ccc(-c2cnn(CC34CC5(C)CC(C)(C3)CC(OCCN(C)CCCCCCCCOc3ccc6c(c3)C(=O)N(C3CCC(=O)NC3=O)C6=O)(C5)C4)c2C)c(C(=O)O)n1 | BCL2L1 | MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK | CRBN | HCT 116 | DC50 | nM | 316 | null | null | null | null | null | > | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q07817 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0291 | Homo sapiens | SELECTIVE BCL-XL PROTAC COMPOUNDS AND METHODS OF USE (patent) | HCT116 cells were purchased from ATCC and cultivated in RPMI 1640 supplemented with 10% heat inactivated fetal bovine serum, penicillin (100 IU/ml), streptomycin (100 μg/ml) and L-glutamine (2 mM). Cells were cultured at 37°C in a humidified atmosphere containing 5% CO2.
Cells were seeded in 96 microwell plates, 24 h ... | TPDdb | Automated Capillary Electrophoresis Immunoassay | TPD-JTHQJR | African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut... | 5 | false | 1,144 | 0 |
Cc1c(Nc2nc3ccccc3s2)nnc2c1CCCN2c1ccc(-c2cnn(CC34CC5(C)CC(C)(C3)CC(OCCN(C)CCCCCCCCOc3cccc6c3C(=O)N(C3CCC(=O)NC3=O)C6=O)(C5)C4)c2C)c(C(=O)O)n1 | BCL2L1 | MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK | CRBN | HCT 116 | DC50 | nM | 316 | null | null | null | null | null | > | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q07817 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0291 | Homo sapiens | SELECTIVE BCL-XL PROTAC COMPOUNDS AND METHODS OF USE (patent) | HCT116 cells were purchased from ATCC and cultivated in RPMI 1640 supplemented with 10% heat inactivated fetal bovine serum, penicillin (100 IU/ml), streptomycin (100 μg/ml) and L-glutamine (2 mM). Cells were cultured at 37°C in a humidified atmosphere containing 5% CO2.
Cells were seeded in 96 microwell plates, 24 h ... | TPDdb | Automated Capillary Electrophoresis Immunoassay | TPD-DFZFTT | African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut... | 5 | false | 1,145 | 0 |
Cc1c(Nc2nc3ccccc3s2)nnc2c1CCCN2c1ccc(-c2cnn(CC34CC5(C)CC(C)(C3)CC(OCCN(C)CCCCCCCOc3ccc6c(c3)C(=O)N(C3CCC(=O)NC3=O)C6=O)(C5)C4)c2C)c(C(=O)O)n1 | BCL2L1 | MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK | CRBN | HCT 116 | DC50 | nM | 0.211 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q07817 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0291 | Homo sapiens | SELECTIVE BCL-XL PROTAC COMPOUNDS AND METHODS OF USE (patent) | HCT116 cells were purchased from ATCC and cultivated in RPMI 1640 supplemented with 10% heat inactivated fetal bovine serum, penicillin (100 IU/ml), streptomycin (100 μg/ml) and L-glutamine (2 mM). Cells were cultured at 37°C in a humidified atmosphere containing 5% CO2.
Cells were seeded in 96 microwell plates, 24 h ... | TPDdb | Automated Capillary Electrophoresis Immunoassay | TPD-KODQEU | African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut... | 5 | false | 1,146 | 0 |
Cc1c(Nc2nc3ccccc3s2)nnc2c1CCCN2c1ccc(-c2cnn(CC34CC5(C)CC(C)(C3)CC(OCCN(C)CCCCCCOc3cccc6c3C(=O)N(C3CCC(=O)NC3=O)C6=O)(C5)C4)c2C)c(C(=O)O)n1 | BCL2L1 | MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK | CRBN | HCT 116 | DC50 | nM | 316 | null | null | null | null | null | > | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q07817 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0291 | Homo sapiens | SELECTIVE BCL-XL PROTAC COMPOUNDS AND METHODS OF USE (patent) | HCT116 cells were purchased from ATCC and cultivated in RPMI 1640 supplemented with 10% heat inactivated fetal bovine serum, penicillin (100 IU/ml), streptomycin (100 μg/ml) and L-glutamine (2 mM). Cells were cultured at 37°C in a humidified atmosphere containing 5% CO2.
Cells were seeded in 96 microwell plates, 24 h ... | TPDdb | Automated Capillary Electrophoresis Immunoassay | TPD-YUSHSO | African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut... | 5 | false | 1,147 | 0 |
Cc1c(Nc2nc3ccccc3s2)nnc2c1CCCN2c1ccc(-c2cnn(CC34CC5(C)CC(C)(C3)CC(OCCN(C)CCCCCOc3ccc6c(c3)C(=O)N(C3CCC(=O)NC3=O)C6=O)(C5)C4)c2C)c(C(=O)O)n1 | BCL2L1 | MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK | CRBN | HCT 116 | DC50 | nM | 0.739 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q07817 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0291 | Homo sapiens | SELECTIVE BCL-XL PROTAC COMPOUNDS AND METHODS OF USE (patent) | HCT116 cells were purchased from ATCC and cultivated in RPMI 1640 supplemented with 10% heat inactivated fetal bovine serum, penicillin (100 IU/ml), streptomycin (100 μg/ml) and L-glutamine (2 mM). Cells were cultured at 37°C in a humidified atmosphere containing 5% CO2.
Cells were seeded in 96 microwell plates, 24 h ... | TPDdb | Automated Capillary Electrophoresis Immunoassay | TPD-WVARXV | African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut... | 5 | false | 1,148 | 0 |
Cc1c(Nc2nc3ccccc3s2)nnc2c1CCCN2c1ccc(-c2cnn(CC34CC5(C)CC(C)(C3)CC(OCCN(C)CCOCCNc3cccc6c3C(=O)N(C3CCC(=O)NC3=O)C6=O)(C5)C4)c2C)c(C(=O)O)n1 | BCL2L1 | MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLADSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAYQSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEPWIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK | CRBN | HCT 116 | DC50 | nM | 10.5 | null | null | null | null | null | null | numeric | null | PROteolysis-TArgeting Chimera (PROTAC) | Q07817 | Q96SW2 | MAGEGDQQDAAHNMGNHLPLLPAESEEEDEMEVEDQDSKEAKKPNIINFDTSLPTSHTYLGADMEEFHGRTLHDDDSCQVIPVLPQVMMILIPGQTLPLQLFHPQEVSMVRNLIQKDRTFAVLAYSNVQEREAQFGTTAEIYAYREEQDFGIEIVKVKAIGRQRFKVLELRTQSDGIQQAKVQILPECVLPSTMSAVQLESLNKCQIFPSKPVSREDQCSYKWWQKYQKRKFHCANLTSWPRWLYSLYDAETLMDRIKKQLREWDENLKDDSLPSNPIDFSYRVAACLPIDDVLRIQLLKIGSAIQRLRCELDIMNKCTS... | CVCL_0291 | Homo sapiens | SELECTIVE BCL-XL PROTAC COMPOUNDS AND METHODS OF USE (patent) | HCT116 cells were purchased from ATCC and cultivated in RPMI 1640 supplemented with 10% heat inactivated fetal bovine serum, penicillin (100 IU/ml), streptomycin (100 μg/ml) and L-glutamine (2 mM). Cells were cultured at 37°C in a humidified atmosphere containing 5% CO2.
Cells were seeded in 96 microwell plates, 24 h ... | TPDdb | Automated Capillary Electrophoresis Immunoassay | TPD-6KLKKD | African=0%; Native American=0.08%; East Asian, North=1.16%; East Asian, South=0%; South Asian=0.97%; European, North=64.85%; European, South=32.93%.
Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mutation; HGNC; HGNC Mut... | 5 | false | 1,149 | 0 |
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