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ChEMBL ligand: CHEMBL409 (Bicalutamide, Calutide, Casodex, Cosudex, ICI 176,334, ICI-176334, ICI176,334-1, Kalumid, NSC-759816) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Androgen receptor/Androgen Receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275] | ||||||||
ChEMBL | Antagonist activity at androgen receptor (unknown origin) | B | 6.8 | pKi | 160.2 | nM | Ki | Eur J Med Chem (2015) 99: 51-66 [PMID:26046313] |
ChEMBL | Binding affinity to human androgen receptor expressed in CV1 cells | B | 6.82 | pKi | 151 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 1523-1526 [PMID:17257838] |
ChEMBL | Displacement of [3H]DHT from human Androgen receptor in human MDA-MB-453 cells | B | 6.82 | pKi | 151 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 2967-2971 [PMID:18400499] |
ChEMBL | Binding affinity to human androgen receptor expressed in monkey COS7 cells by whole cell binding assay | B | 6.82 | pKi | 151 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 3431-3435 [PMID:18442912] |
ChEMBL | Binding affinity for human androgen receptor in transiently-transfected COS-1 cells. | B | 6.93 | pKi | 117 | nM | Ki | J Med Chem (1998) 41: 623-639 [PMID:9484511] |
ChEMBL | Binding affinity for human androgen receptor transfected into mammalian COS-1 cells | B | 6.93 | pKi | 117 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 411-414 [PMID:10743937] |
ChEMBL | Binding affinity against Androgen receptor transfected into COS cells | B | 7.09 | pKi | 82 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 745-750 [PMID:9871534] |
ChEMBL | Displacement of [3H]DHT from androgen receptor of human MDA-453 cells | B | 7.19 | pKi | 65 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 6107-6111 [PMID:15546739] |
ChEMBL | Displacement of [3H]-DHT from androgen receptor in human MDA-MB-453 cells after 90 mins by TopCount analysis | B | 7.19 | pKi | 64 | nM | Ki | ACS Med Chem Lett (2015) 6: 908-912 [PMID:26288692] |
ChEMBL | Inhibition of [3H]DHT binding to androgen receptor of MDA-453 cells | B | 7.19 | pKi | 64 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 389-393 [PMID:15603960] |
ChEMBL | Binding affinity for androgen receptor in human MDA-453 cells | B | 7.19 | pKi | 64 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 271-276 [PMID:15603938] |
ChEMBL | Displacement of [3H]DHT from human androgen receptor in MDA453 cells | B | 7.19 | pKi | 64 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 1910-1915 [PMID:18291644] |
ChEMBL | Displacement of [3H]DHT from AR in human MDA-MB-453 cells | B | 7.19 | pKi | 64 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 4491-4495 [PMID:20584610] |
ChEMBL | Inhibition of [3H]-DHT binding to T877A androgen receptor of LNCaP cells | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 389-393 [PMID:15603960] |
ChEMBL | Binding affinity for mutant T877A Androgen receptor in human LNCaP cells | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 271-276 [PMID:15603938] |
GtoPdb | - | - | 7.72 | pKi | 19 | nM | Ki | J Med Chem (2006) 49: 716-26 [PMID:16420057] |
ChEMBL | Inhibition of human AR | B | 7.72 | pKi | 19 | nM | Ki | J Med Chem (2006) 49: 716-726 [PMID:16420057] |
ChEMBL | Inhibition of BF3 site of androgen receptor in enzalutamide-resistant human LNCAP cells assessed as reduction in PSA level after 3 days | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2013) 56: 1136-1148 [PMID:23301637] |
ChEMBL | Antagonist activity at AR T877A mutant in human LNCAP cells assessed as inhibition of DHT-induced proliferation after 48 hrs by MTT assay | B | 4.35 | pIC50 | 44260 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 1199-1204 [PMID:28162857] |
ChEMBL | Antagonist activity at human androgen receptor W741C mutant expressed in COS7 cells assessed as inhibition of DHT-induced luciferase activity after 24 hrs by reporter gene assay | F | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem (2012) 20: 422-434 [PMID:22094279] |
ChEMBL | Antagonist activity at androgen receptor H874Y mutant (unknown origin) expressed in human 22Rv1 cells assessed as inhibition of DHT-induced cell growth after 3 days by WST-8 assay | B | 5.34 | pIC50 | 4600 | nM | IC50 | ACS Med Chem Lett (2013) 4: 937-941 [PMID:24900588] |
GtoPdb | - | - | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (2010) 53: 2779-96 [PMID:20218717] |
ChEMBL | Antagonist activity at androgen receptor T877A mutant (unknown origin) expressed in human LNCAP cells assessed as inhibition of DHT-induced cell growth after 6 days by WST-8 assay | B | 6.03 | pIC50 | 940 | nM | IC50 | ACS Med Chem Lett (2013) 4: 937-941 [PMID:24900588] |
ChEMBL | Inhibition of AR mediated transcriptional activation using reporter assay | F | 6.05 | pIC50 | 890 | nM | IC50 | J Med Chem (2006) 49: 716-726 [PMID:16420057] |
ChEMBL | Reporter Assay: The compounds were subjected to tests using an artificial AR response reporter system in a hormone refractory prostate cancer cell line. In this system, the prostate cancer LNCaP cells were engineered to stably express about 5-fold higher level of AR than endogenous level. The exogenous AR has similar properties to endogenous AR in that both are stabilized by a synthetic androgen R1881. The AR-over expressed cells were also engineered to stably incorporate an AR response reporter and the reporter activity of these cells shows features of hormone refractory prostate cancer. | B | 6.05 | pIC50 | 889 | nM | IC50 | US-9126941-B2. Treatment of hyperproliferative disorders with diarylhydantoin compounds (2015) |
ChEMBL | Inhibition of L701H/T877A mutant androgen receptor of human prostate cancer MDAMB-PCa2b cell proliferation | F | 6.14 | pIC50 | 725 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 389-393 [PMID:15603960] |
ChEMBL | Inhibition of androgen dependent human prostate cancer cell MDA-MB-PCa2b proliferation | F | 6.14 | pIC50 | 725 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 271-276 [PMID:15603938] |
ChEMBL | Antagonist activity at AR in human bicalutamide-resistant LNCAP cells assessed as inhibition of cell proliferation after 6 days | F | 6.22 | pIC50 | 600 | nM | IC50 | Bioorg Med Chem (2010) 18: 8150-8157 [PMID:21050768] |
ChEMBL | Antagonist activity at AR in bicalutamide-resistant human LNCAP cells assessed as effect on cell proliferation after 6 days | F | 6.26 | pIC50 | 550 | nM | IC50 | Bioorg Med Chem (2010) 18: 3159-3168 [PMID:20381361] |
ChEMBL | Antagonist activity at Androgen receptor T877A mutant (unknown origin) expressed in human Cos-7 cells co-expressing pGL3-MMTV-luc vector assessed as luciferase activity by reporter gene assay | B | 6.33 | pIC50 | 470 | nM | IC50 | Bioorg Med Chem (2013) 21: 70-83 [PMID:23199477] |
ChEMBL | Antagonist activity at androgen receptor T877A mutant expressed in Cos7 cells assessed as inhibition of dihydrotestosterone-induced luciferase activity after 24 hrs by reporter gene assay | F | 6.33 | pIC50 | 470 | nM | IC50 | Bioorg Med Chem (2012) 20: 2338-2352 [PMID:22391033] |
ChEMBL | Antagonist activity at human androgen receptor T877A mutant expressed in COS7 cells assessed as inhibition of DHT-induced luciferase activity after 24 hrs by reporter gene assay | F | 6.33 | pIC50 | 470 | nM | IC50 | Bioorg Med Chem (2012) 20: 422-434 [PMID:22094279] |
ChEMBL | In vitro antagonistic activity against mutant androgen receptor of LNCap cells | F | 6.4 | pIC50 | 400 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 6107-6111 [PMID:15546739] |
ChEMBL | Inhibition of T877A androgen receptor of human prostate cancer cells in reporter gene assay | F | 6.4 | pIC50 | 400 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 389-393 [PMID:15603960] |
ChEMBL | Inhibition of mutant T877A Androgen receptor in human LNCaP cells | B | 6.4 | pIC50 | 400 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 271-276 [PMID:15603938] |
ChEMBL | Antagonist activity at wild type human AR expressed in human LNCAP cells by transactivation assay | F | 6.4 | pIC50 | 400 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 4491-4495 [PMID:20584610] |
ChEMBL | Inhibitory concentration against human androgen receptor (AR) dependent transcriptional activity in co-transfected mammalian CV-1 cells | F | 6.47 | pIC50 | 338 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 411-414 [PMID:10743937] |
ChEMBL | Antagonist activity at wild type Androgen receptor (unknown origin) expressed in human Cos-7 cells co-expressing pGL3-MMTV-luc vector assessed as luciferase activity by reporter gene assay | B | 6.48 | pIC50 | 330 | nM | IC50 | Bioorg Med Chem (2013) 21: 70-83 [PMID:23199477] |
ChEMBL | Antagonist activity at human androgen receptor expressed in COS7 cells assessed as inhibition of DHT-induced luciferase activity after 24 hrs by reporter gene assay | F | 6.48 | pIC50 | 330 | nM | IC50 | Bioorg Med Chem (2012) 20: 422-434 [PMID:22094279] |
ChEMBL | Antagonist activity at androgen receptor expressed in Cos7 cells assessed as inhibition of dihydrotestosterone-induced luciferase activity after 24 hrs by reporter gene assay | F | 6.48 | pIC50 | 330 | nM | IC50 | Bioorg Med Chem (2012) 20: 2338-2352 [PMID:22391033] |
ChEMBL | Antagonist activity at human androgen receptor expressed in human CV1 cells assessed as inhibition of receptor-mediated transactivation by MMTV-luciferase reporter gene assay | F | 6.52 | pIC50 | 300 | nM | IC50 | Bioorg Med Chem (2010) 18: 6960-6969 [PMID:20826091] |
ChEMBL | Inhibition of androgen receptor in human LNCAP cells after 1 day by luciferase reporter gene assay | B | 6.57 | pIC50 | 270 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 3887-3890 [PMID:23727044] |
ChEMBL | Antagonist activity at human androgen receptor expressed in HEK-293 cells harboring GRE-LUC and CMV-renilla luciferase assessed as inhibition of transactivation incubated for 24 hrs in presence of R1881 by dual luciferase assay | B | 6.61 | pIC50 | 248 | nM | IC50 | J Med Chem (2021) 64: 11045-11062 [PMID:34269581] |
ChEMBL | Activity at androgen receptor in human Saos2 cells assessed as IL6 repression | B | 6.63 | pIC50 | 232 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 3431-3435 [PMID:18442912] |
ChEMBL | Displacement of [3H]mibolerone from androgen receptor expressed in CHOK1 cells | B | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem (2007) 15: 174-185 [PMID:17064916] |
ChEMBL | Displacement of [3H]mibolerone from human androgen receptor expressed in CHOK1 cells | B | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 5573-5576 [PMID:17804229] |
ChEMBL | Displacement of [3H]mibolerone from human AR expressed in CHO-K1 cells after 2 hrs by scintillation counting | B | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem (2010) 18: 3159-3168 [PMID:20381361] |
ChEMBL | Antagonist activity at human AR expressed in human HeLa cells co-transfected with MMTV-Luc-Hyg after 48 hrs by transient-luciferase reporter gene assay | F | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem (2010) 18: 8150-8157 [PMID:21050768] |
ChEMBL | Antagonist activity at androgen receptor in human MDA-MB-453 cells assessed as inhibition of DHT-induced PSA expression by alkaline phosphatase reporter gene assay | B | 6.76 | pIC50 | 173 | nM | IC50 | ACS Med Chem Lett (2015) 6: 908-912 [PMID:26288692] |
ChEMBL | Antagonist activity at human wild type AR expressed in human MDA-MB-435 cells by transactivation assay | F | 6.76 | pIC50 | 173 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 4491-4495 [PMID:20584610] |
ChEMBL | Antagonist activity at human androgen receptor in MDA453 cells by alkaline phosphatase reporter gene assay | F | 6.76 | pIC50 | 173 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 1910-1915 [PMID:18291644] |
ChEMBL | Inhibition of human androgen receptor of breast carcinoma MDA-453 cells in reporter gene assay | F | 6.76 | pIC50 | 173 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 389-393 [PMID:15603960] |
ChEMBL | Inhibition of androgen receptor in human MDA-453 cells | B | 6.76 | pIC50 | 173 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 271-276 [PMID:15603938] |
ChEMBL | In vitro antagonistic activity against androgen receptor of MDA-453 cells | F | 6.77 | pIC50 | 170 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 6107-6111 [PMID:15546739] |
ChEMBL | Antagonist activity at human androgen receptor expressed in CV1 cells | F | 6.79 | pIC50 | 162 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 1523-1526 [PMID:17257838] |
ChEMBL | Antagonist activity at human androgen receptor african green monkey CV1 cells by cotransfection assay | F | 6.79 | pIC50 | 162 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 3431-3435 [PMID:18442912] |
ChEMBL | Antagonist activity at human androgen receptor in CV1 cells by transcriptional activation assay | F | 6.79 | pIC50 | 162 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 2967-2971 [PMID:18400499] |
ChEMBL | Antagonistic activity against human androgen receptor (hAR) in co-transfected CV-1 cells. | F | 6.8 | pIC50 | 157 | nM | IC50 | J Med Chem (1998) 41: 623-639 [PMID:9484511] |
ChEMBL | Antagonistic activity (IC50) against human androgen receptor (hAR) in co-transfected CV-1 cell | F | 6.8 | pIC50 | 157 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 745-750 [PMID:9871534] |
ChEMBL | Antagonist activity at human androgen receptor expressed in HeLa cells assessed as inhibition of dihydrotestosterone induced transcriptional activity by reporter gene assay | F | 6.85 | pIC50 | 140 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 5573-5576 [PMID:17804229] |
ChEMBL | Antagonist activity at androgen receptor expressed in HeLa cells assessed as inhibition of dihydrotestosterone-induced transcriptional activity by reporter gene assay | F | 6.85 | pIC50 | 140 | nM | IC50 | Bioorg Med Chem (2007) 15: 174-185 [PMID:17064916] |
ChEMBL | Displacement of [17-alpha-methyl-3H]-mibolerone from human androgen receptor T877A mutant expressed in HEK293 derived FreeStyle293F cells after 3 hrs | B | 6.92 | pIC50 | 120 | nM | IC50 | Bioorg Med Chem (2012) 20: 422-434 [PMID:22094279] |
ChEMBL | Inhibition of Androgen receptor T877A mutant (unknown origin) expressed in Freestyle293F cells | B | 6.92 | pIC50 | 120 | nM | IC50 | Bioorg Med Chem (2013) 21: 70-83 [PMID:23199477] |
ChEMBL | In vitro binding affinity at human androgen receptor transfected into COS cells. | B | 6.93 | pIC50 | 117 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 1003-1008 [PMID:10230628] |
ChEMBL | Antagonist activity against pSG5-tagged human androgen receptor expressed in COS1 cells assessed as reduction in receptor-mediated transcriptional activity by AR-regulated rat probasin promoter fragment driven firefly luciferase reporter assay | B | 7.06 | pIC50 | 86.9 | nM | IC50 | J Med Chem (2015) 58: 1569-1574 [PMID:25646649] |
ChEMBL | Displacement of [3H]R1881 from pSG5-tagged human androgen receptor expressed in COS1 cells assessed as relative binding inhibition | B | 7.06 | pIC50 | 86.9 | nM | IC50 | J Med Chem (2015) 58: 1569-1574 [PMID:25646649] |
ChEMBL | Displacement of [17-alpha-methyl-3H]-mibolerone from human androgen receptor expressed in HEK293 derived FreeStyle293F cells after 3 hrs | B | 7.27 | pIC50 | 54 | nM | IC50 | Bioorg Med Chem (2012) 20: 422-434 [PMID:22094279] |
ChEMBL | Displacement of [17-alpha-methyl-3H]mibolerone from androgen receptor expressed in HEK293 cells after 3 hrs | B | 7.27 | pIC50 | 54 | nM | IC50 | Bioorg Med Chem (2012) 20: 2338-2352 [PMID:22391033] |
ChEMBL | Inhibition of wild type Androgen receptor (unknown origin) expressed in Freestyle293F cells | B | 7.27 | pIC50 | 54 | nM | IC50 | Bioorg Med Chem (2013) 21: 70-83 [PMID:23199477] |
ChEMBL | In vitro agonistic activity against human androgen receptor (hAR) expressed in CV-1 cells; not active | F | 8 | pIC50 | >10 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 1003-1008 [PMID:10230628] |
ChEMBL | Agonist activity at Androgen receptor T877A mutant in human LNCaP-hr cells assessed as prostate specific antigen secretion measured after 3 days by enzyme-immunoassay | B | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem (2013) 21: 70-83 [PMID:23199477] |
ChEMBL | Agonist activity at human androgen receptor african green monkey CV1 cells by cotransfection assay | F | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 3431-3435 [PMID:18442912] |
ChEMBL | Agonist activity at human androgen receptor expressed in COS7 cells assessed as luciferase activity after 24 hrs by reporter gene assay | F | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem (2012) 20: 422-434 [PMID:22094279] |
ChEMBL | Agonist activity at human androgen receptor T877A mutant expressed in COS7 cells assessed as luciferase activity after 24 hrs by reporter gene assay | F | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem (2012) 20: 422-434 [PMID:22094279] |
ChEMBL | Agonist activity at wild type Androgen receptor in human LNCaP-hr cells assessed as prostate specific antigen secretion measured after 3 days by enzyme-immunoassay | B | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem (2013) 21: 70-83 [PMID:23199477] |
ChEMBL | Agonist activity at androgen receptor expressed in Cos7 cells after 24 hrs by luciferase reporter gene assay | F | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem (2012) 20: 2338-2352 [PMID:22391033] |
ChEMBL | Agonist activity at androgen receptor T877A mutant expressed in Cos7 cells after 24 hrs by luciferase reporter gene assay | F | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem (2012) 20: 2338-2352 [PMID:22391033] |
ChEMBL | Displacement of [3H]R1881 from androgen receptor in human PC3 cells | B | 5.37 | pEC50 | 4300 | nM | EC50 | J Med Chem (2015) 58: 2077-2087 [PMID:25591066] |
ChEMBL | Displacement of [3H]R1881 from AR in human LNCaP cells after 2 hrs by scintillation counting analysis | B | 5.85 | pEC50 | 1400 | nM | EC50 | J Med Chem (2013) 56: 4880-4898 [PMID:23713567] |
ChEMBL | Displacement of [3H]R1881 from androgen receptor in human LNCAP cells | B | 6.01 | pEC50 | 971 | nM | EC50 | J Med Chem (2015) 58: 2077-2087 [PMID:25591066] |
ChEMBL | Agonist activity at human androgen receptor W741C mutant expressed in COS7 cells assessed as luciferase activity after 24 hrs by reporter gene assay | F | 6.74 | pEC50 | 180 | nM | EC50 | Bioorg Med Chem (2012) 20: 422-434 [PMID:22094279] |
ChEMBL | In vitro antagonistic activity against human androgen receptor (hAR) expressed in CV-1 cells | F | 6.8 | pEC50 | 157 | nM | EC50 | Bioorg Med Chem Lett (1999) 9: 1003-1008 [PMID:10230628] |
ChEMBL | Displacement of [3H]R1881 from AR in human MDA-MB-453 cells | B | 7.51 | pEC50 | 31 | nM | EC50 | J Med Chem (2013) 56: 4880-4898 [PMID:23713567] |
Androgen receptor/Androgen Receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3056] [GtoPdb: 628] [UniProtKB: P19091] | ||||||||
ChEMBL | Antagonist activity at androgen receptor in androgen-dependent mouse SC3 cells assessed as inhibition of testosterone-induced cell growth after 3 days | B | 5.52 | pIC50 | 3000 | nM | IC50 | Bioorg Med Chem (2013) 21: 1643-1651 [PMID:23462715] |
ChEMBL | Antiandrogen activity against androgen receptor in androgen-dependent mouse SC3 cells assessed as inhibition of testosterone-induced cell proliferation by WST1 assay | B | 6.17 | pIC50 | 670 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 6661-6666 [PMID:20888766] |
Androgen receptor/Androgen Receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207] | ||||||||
ChEMBL | Inhibition of [3H] MIB binding to rat prostate androgen receptor LBD by competitive binding assay | B | 6.29 | pKi | 509 | nM | Ki | J Med Chem (2021) 64: 11045-11062 [PMID:34269581] |
ChEMBL | In vivo binding affinity for rat ventral prostate androgen receptor by displacement of [3H]R-1881 | B | 6.48 | pKi | 330 | nM | Ki | J Med Chem (1992) 35: 1663-1670 [PMID:1588549] |
ChEMBL | Inhibition of rat AR | B | 7.85 | pKi | 14 | nM | Ki | J Med Chem (2006) 49: 716-726 [PMID:16420057] |
ChEMBL | Displacement of [3H]R1881 from rat androgen receptor | B | 5.89 | pIC50 | 1300 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 5646-5649 [PMID:16942875] |
ChEMBL | Inhibition of rat AR-mediated reporter gene expression in COS7 cells | B | 6.07 | pIC50 | 850 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 3233-3237 [PMID:16603353] |
ChEMBL | Antagonist activity at GAL4-DBD fused rat androgen receptor expressed in UAS-bla 293 cells assessed as reduction in R1881-induced activation incubated for 16 hrs followed by fluorescence substrate addition and measured after 2 hrs by beta lactamase reporter gene assay | B | 6.31 | pIC50 | 490 | nM | IC50 | Eur J Med Chem (2019) 180: 1-14 [PMID:31288149] |
ChEMBL | Displacement of [3H]testosterone from Sprague-Dawley rat AR by liquid scintillation counting | B | 7.27 | pIC50 | 54 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1744-1747 [PMID:21349712] |
ChEMBL | Displacement of [3H]testosterone from androgen receptor in Sprague-Dawley rat prostate gland after 2 hrs by liquid scintillation counting | B | 7.6 | pIC50 | 25 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6310-6313 [PMID:21944856] |
Estrogen receptor-α/Estrogen receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372] | ||||||||
ChEMBL | Inhibition of human ERalpha | B | 4 | pKi | >100000 | nM | Ki | J Med Chem (2006) 49: 716-726 [PMID:16420057] |
Glucocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150] | ||||||||
ChEMBL | Inhibition of human GR | B | 4 | pKi | >100000 | nM | Ki | J Med Chem (2006) 49: 716-726 [PMID:16420057] |
Progesterone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL208] [GtoPdb: 627] [UniProtKB: P06401] | ||||||||
ChEMBL | Antagonistic activity against human progesterone receptor B (hPR-B) in co-transfected CV-1 cells. | F | 5.74 | pIC50 | 1819 | nM | IC50 | J Med Chem (1998) 41: 623-639 [PMID:9484511] |
Progesterone receptor in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3456] [UniProtKB: P06186] | ||||||||
ChEMBL | Displacement of [3H]progesterone from rabbit PR by liquid scintillation counting | B | 5.25 | pIC50 | 5600 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1744-1747 [PMID:21349712] |
ChEMBL | Displacement of [3H]progesterone from progesterone receptor in JW rabbit uterus after 2 hrs by liquid scintillation counting | B | 5.25 | pIC50 | 5600 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6310-6313 [PMID:21944856] |
Progesterone receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2596] [GtoPdb: 627] [UniProtKB: Q63449] | ||||||||
ChEMBL | Inhibition of rat PR | B | 5.14 | pKi | 7200 | nM | Ki | J Med Chem (2006) 49: 716-726 [PMID:16420057] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]