ChEMBL ligand: CHEMBL409 (Bicalutamide, Calutide, Casodex, Cosudex, ICI 176,334, ICI-176334, ICI176,334-1, Kalumid, NSC-759816)
Androgen receptor/Androgen Receptor in Human [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275] Androgen receptor/Androgen Receptor in Mouse [ChEMBL: CHEMBL3056] [GtoPdb: 628] [UniProtKB: P19091] Androgen receptor/Androgen Receptor in Rat [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207] There should be some charts here, you may need to enable JavaScript!
Estrogen receptor-α/Estrogen receptor alpha in Human [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372] There should be some charts here, you may need to enable JavaScript!
Glucocorticoid receptor in Human [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150] There should be some charts here, you may need to enable JavaScript!
Progesterone receptor in Human [ChEMBL: CHEMBL208] [GtoPdb: 627] [UniProtKB: P06401] Progesterone receptor in Rabbit [ChEMBL: CHEMBL3456] [UniProtKB: P06186] Progesterone receptor in Rat [ChEMBL: CHEMBL2596] [GtoPdb: 627] [UniProtKB: Q63449] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
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]