ChEMBL ligand: CHEMBL409 (Bicalutamida, Bicalutamide, Calutide, Casodex, Cosudex, ICI 176,334, ICI-176334, ICI176,334-1, Kalumid, NSC-759816)
Androgen receptor in Human [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275] Androgen receptor in Mouse [ChEMBL: CHEMBL3056] [GtoPdb: 628] [UniProtKB: P19091] 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 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 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	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	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 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 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	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	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	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	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	Androgen Receptor Binding Assay: Androgen receptor (AR) binding affinities of test compounds were studied in cytosolic lysates obtained from ventral prostates of castrated rats by competition binding assay (Schilling K. and Liao S., The Prostate, 1984; 5(6):581-588). Cytosol preparations and 1 nM [3H]mibolerone were incubated with increasing concentrations of test compounds. To determine non-specific binding, parallel incubations were carried out using excess of unlabelled testosterone. After incubation, bound and free steroids were separated by treatment with dextran-coated charcoal suspension. Bound radioactivity was determined by counting of supernatant fraction in scintillation fluid. Radioactivity was measured using a Microbeta counter. All data points were done as quadrublicates. Dissociation constant of [3H]mibolerone for rat androgen receptor was determined by saturation binding assay obtained from ventral prostates of castrated rats essentially as described (Isomaa V. et al., Endocrinology, 1982; 111(3):833-843).	B	7.4	pKi	40	nM	Ki	US-11046713-B2. Androgen receptor modulating compounds (2021)
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	Binding affinity to Androgen receptor (unknown origin) assessed as inhibition constant	B	7.96	pKi	11	nM	Ki	Eur J Med Chem (2022) 230: 114119-114119 [PMID:35063736]
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]
ChEMBL	Binding affinity to Androgen receptor (unknown origin)	B	5.89	pIC50	1300	nM	IC50	J Med Chem (2022) 65: 8772-8797 [PMID:35786895]
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 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	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 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	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 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	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	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 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 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 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 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 Androgen receptor in human LNCaP cells assessed as inhibition of Binding Function 3 (BF3) of AR measured by luciferase assay	B	6.57	pIC50	270	nM	IC50	J Med Chem (2022) 65: 8772-8797 [PMID:35786895]
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	AR Antagonism: Antagonism of test compounds for AR was measured by reporter gene assay in human embryonic kidney (HEK293) cells stably transfected with an expression vector encoding full-length human AR and androgen responsive luciferase reporter gene construct (hAR/HEK293 cells). To determine antagonism for hAR, the cells were treated simultaneously with increasing concentrations of the test compound and submaximal concentration of testosterone (usually 0.45 nM). The final DMSO concentration was 1%. All test compounds were studied in triplicates. The cells were incubated for 24 before measurement of luciferase activity using Luciferase Assay System (Promega Corporation).Agonism of test compounds in AR overexpressing cells was measured by reporter gene assay in HEK293 cells stably transfected with an expression vector encoding full-length human AR and androgen responsive luciferase reporter gene construct. A clone expressing high levels of androgen receptor (5 times more than AR levels in AR-HEK293 cells) was selected to study agonism in AR overexpressing cells. To determine agonism, the cells were treated with increasing concentrations of the test compound. The final DMSO concentration was 1%. The test compounds were studied in triplicates and luciferase activity was determined as described above.	B	6.64	pIC50	228	nM	IC50	US-11046713-B2. Androgen receptor modulating compounds (2021)
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	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	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 androgen receptor expressed in CHOK1 cells	B	6.7	pIC50	200	nM	IC50	Bioorg Med Chem (2007) 15: 174-185 [PMID:17064916]
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	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	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	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	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	Antagonist activity at Androgen receptor (unknown origin) in African green monkey COS-1 cells	B	6.92	pIC50	120.23	nM	IC50	J Med Chem (2022) 65: 8772-8797 [PMID:35786895]
ChEMBL	Displacement of [17-alpha-methyl-3H]mibolerone from androgen receptor T877A mutant expressed in HEK293 cells after 3 hrs	B	6.92	pIC50	120	nM	IC50	Bioorg Med Chem (2012) 20: 2338-2352 [PMID:22391033]
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	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	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	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 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]
ChEMBL	Androgen Receptor Assay: Androgen binding is measured using the hydroxylapatite (HAP) assay. In brief, the radioactive steroid [3H]R1881 solubilized in ethanol is diluted with buffer B (10 mM Tris-HCl, 1.5 mM EDTA disodium salt, 10 mM α-monothioglycerol, pH 7.4). Aliquots of the cell or prostate cytosol preparation (0.1 ml) are then incubated with 5 nM [3H]R1881 (0.1 ml, ¿100 000 cpm) in the presence or absence of the indicated concentrations of unlabeled compounds (0.1 ml, prepared in buffer B containing 30% ethanol) for 16-18 h at 0-4° C. Triamcinolone acetonide (TAC; 100 nM) is added to mask progesterone receptors. Unbound steroids are separated by incubation for 40 min at 0-4° C. with 0.3 ml HAP prepared in buffer P (50 mM Tris-HCl, 10 mM KH2PO4, pH 7.4). After incubation with HAP and 10 min of centrifugation at 1000×g, the pellet is washed 3 times with 1 ml of buffer P. Thereafter, the radioactivity is extracted from the pellet by incubation at room temperature for 60 min with 1 ml of ethanol. After centrifugation, the supernatant is decanted into a scintillation vial and the pellet is extracted again with ethanol. After the addition of scintillation liquid, the radioactivity is measured in a liquid scintillation counter.	B	6.72	pIC50	190	nM	IC50	US-9682960-B2. Non-steroidal antiandrogens and selective androgen receptor modulators with a pyridyl moiety (2017)
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 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 36:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]