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