ChEMBL ligand: CHEMBL1082407 (Enzalutamide, Mdv 3100, MDV-3100, MDV3100, Xtandi)
Androgen receptor/Androgen Receptor in Human [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275] Androgen receptor/Androgen Receptor in Rat [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207] 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!
kallikrein related peptidase 3/Prostate specific antigen in Human [ChEMBL: CHEMBL2099] [GtoPdb: 2373] [UniProtKB: P07288] 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	Binding affinity to human AR LBD (663 to 920 residues) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant by biolayer interferometry assay	B	4.4	pKd	40200	nM	Kd	J Med Chem (2022) 65: 2507-2521 [PMID:35077161]
ChEMBL	Displacement of [3H]-mibolerone from GST-tagged human AR-LBD expressed in HEK293 cells	B	5.44	pKi	3641.29	nM	Ki	Bioorg Med Chem (2020) 28: 115554-115554 [PMID:32546299]
ChEMBL	Displacement of [3H]-mibolerone from recombinant wild-type GST-tagged androgen receptor LBD (unknown origin) after 16 hrs by scintillation counting analysis	B	5.44	pKi	3641	nM	Ki	J Med Chem (2019) 62: 491-511 [PMID:30525603]
ChEMBL	Inhibition of androgen receptor (unknown origin)	B	7.07	pKi	86	nM	Ki	Eur J Med Chem (2020) 205: 112667-112667 [PMID:32911308]
ChEMBL	Antagonist activity at androgen receptor (unknown origin)	B	7.55	pKi	28.2	nM	Ki	Eur J Med Chem (2015) 99: 51-66 [PMID:26046313]
ChEMBL	Binding affinity to wild-type androgen receptor in human LNCaP cells assessed as inhibition constant incubated for 24 hrs by Cheng-Prusoff equation analysis	B	7.77	pKi	17	nM	Ki	J Med Chem (2021) 64: 909-924 [PMID:33470111]
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	Displacement of Fluormone AL Green from androgen receptor ligand binding domain (unknown origin) after 4 hrs by fluorescence polarization assay	B	5.25	pIC50	5600	nM	IC50	J Med Chem (2013) 56: 8280-8297 [PMID:24044500]
ChEMBL	Competitive displacement of [3H]R1881 from human AR-LBD expressed in LNCaP cells incubated for 24 hrs by scintillation counting method based radioligand competitive binding assay	B	5.27	pIC50	5336	nM	IC50	Eur J Med Chem (2019) 171: 265-281 [PMID:30925341]
ChEMBL	Displacement of fluormone-AL green from GST-tagged androgen receptor LBD (unknown origin) measured after 4 hrs by fluorescence polarization assay	B	5.4	pIC50	3970	nM	IC50	Eur J Med Chem (2020) 192: 112156-112156 [PMID:32114360]
ChEMBL	Antagonist activity at Androgen receptor (unknown origin) expressed in COS7 cells by dual luciferase reporter gene assay relative to control	B	5.52	pIC50	3030	nM	IC50	Eur J Med Chem (2020) 192: 112196-112196 [PMID:32169785]
ChEMBL	Antagonist activity at androgen receptor (unknown origin) expressed in African green monkey COS7 cells assessed as inhibition of R1881-induced protein activation after 24 hrs by luciferase reporter gene assay	B	5.9	pIC50	1260	nM	IC50	Eur J Med Chem (2018) 143: 1325-1344 [PMID:29117897]
ChEMBL	Antagonist activity at androgen receptor (unknown origin) expressed in HEK293 cells using DHT as substrate preincubated for 30 mins followed by substrate addition measured after 24 hrs by Steady-Glo luciferase assay	B	6.19	pIC50	646.9	nM	IC50	Bioorg Med Chem (2021) 31: 115953-115953 [PMID:33388655]
ChEMBL	Inhibition of AR transcriptional activity in human LNCaP cells harboring ARR2PB-eGFP assessed as decrease in PSA level	B	6.32	pIC50	480	nM	IC50	J Med Chem (2021) 64: 17221-17238 [PMID:34809430]
ChEMBL	Antagonist activity at GAL4 DBD-fused androgen receptor LBD (unknown origin) transfected in UAS-bla GripTite 293 cells assessed as inhibition of R1881-induced receptor activation after 16 to 24 hrs by beta-lactamase reporter gene assay	B	6.44	pIC50	361	nM	IC50	Bioorg Med Chem Lett (2016) 26: 3636-3640 [PMID:27301368]
ChEMBL	Inhibition of androgen receptor (unknown origin)	B	6.66	pIC50	219	nM	IC50	Eur J Med Chem (2020) 205: 112667-112667 [PMID:32911308]
GtoPdb	Antagonism of testosterone-induced activation of wtAR determined using AR-HEK293 cells and a luciferase reporter system.	-	6.66	pIC50	219	nM	IC50	Sci Rep (2015) 5: 12007 [PMID:26137992]
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	6.67	pIC50	216	nM	IC50	J Med Chem (2021) 64: 11045-11062 [PMID:34269581]
ChEMBL	Antagonist activity at recombinant human AR expressed in HEK293 cells assessed as inhibition of R1881-induced transcriptional activity measured after 24 hrs by dual luciferase reporter gene assay	B	6.67	pIC50	216	nM	IC50	J Med Chem (2020) 63: 12642-12665 [PMID:33095584]
ChEMBL	Antagonist activity at human androgen receptor expressed in HEK293 cells assessed as inhibition of R1881-induced receptor transactivation after 24 hrs by luciferase reporter gene assay	B	6.67	pIC50	216	nM	IC50	J Med Chem (2019) 62: 491-511 [PMID:30525603]
ChEMBL	Antagonist activity at wild type androgen receptor in castration-resistant human LNCaP cells assessed as inhibition of R1881-stimulated receptor transcriptional activation measured after 20 to 24 hrs by Steady-Glo luciferase assay	B	6.93	pIC50	117	nM	IC50	ACS Med Chem Lett (2021) 12: 1245-1252 [PMID:34422225]
ChEMBL	Antagonist activity at AR wild-type (unknown origin) transfected in human LNCAP cells cotransfected with ARE-LUC incubated for 20 to 24 hrs in presence of AR agonist R1881 by steady-glo luciferase reporter gene assay	B	6.93	pIC50	117	nM	IC50	J Med Chem (2021) 64: 909-924 [PMID:33470111]
ChEMBL	Inhibition of R1881-induced full length AR transcriptional activity in human LNCAP cells harboring AR2PB-eGFP construct after 72 hrs by fluorescence assay	B	7.05	pIC50	90	nM	IC50	Eur J Med Chem (2018) 157: 1164-1173 [PMID:30193215]
ChEMBL	Binding affinity to GST-tagged AR ligand binding domain (unknown origin) measured after 4 hrs by fluorescence polarization assay	B	7.1	pIC50	80	nM	IC50	J Med Chem (2021) 64: 17221-17238 [PMID:34809430]
ChEMBL	Antagonist activity at androgen receptor in human LNCaP cells harboring eGFP/ARRIPB incubated for 3 days by fluorescence method	B	7.12	pIC50	75	nM	IC50	J Med Chem (2021) 64: 14968-14982 [PMID:34661404]
ChEMBL	Antagonist activity against human androgen receptor expressed in human LNCap cells trasfected with ARR2PB-eGFP cells incubated for 3 days by fluorescence based AR transcription assay	B	7.15	pIC50	70	nM	IC50	J Med Chem (2022) 65: 2507-2521 [PMID:35077161]
ChEMBL	Inhibition of full length AR transcriptional activity in human LNCAP cells harboring AR2PB-eGFP construct assessed as reduction in R1881-induced secreted PSA level after 72 hrs by fluorescence assay	B	7.3	pIC50	50	nM	IC50	Eur J Med Chem (2018) 157: 1164-1173 [PMID:30193215]
ChEMBL	Displacement of [3H]methyltrienolone from wild-type androgen receptor in human LNCaP cells incubated for 24 hrs by scintillation counting analysis	B	7.42	pIC50	38	nM	IC50	J Med Chem (2021) 64: 909-924 [PMID:33470111]
GtoPdb	-	-	7.44	pIC50	36	nM	IC50	Science (2009) 324: 787-90 [PMID:19359544]
ChEMBL	Antagonist activity at androgen receptor in human LNCaP cells transfected with ARR2 PB-eGFP assessed as inhibition of DHT-induced transcriptional activity measured after 3 days by fluorescence assay	B	7.44	pIC50	36	nM	IC50	Eur J Med Chem (2020) 192: 112156-112156 [PMID:32114360]
ChEMBL	Displacement of [18F]-FDHT from androgen receptor in human LNCAP/AR cells	B	7.68	pIC50	21	nM	IC50	Bioorg Med Chem Lett (2016) 26: 5222-5228 [PMID:27717544]
ChEMBL	Inhibition of AR transcriptional activity in human LNCaP cells harboring ARR2PB-eGFP incubated for 72 hrs by fluorescence assay	B	7.85	pIC50	14	nM	IC50	J Med Chem (2021) 64: 17221-17238 [PMID:34809430]
ChEMBL	Antagonist activity at androgen receptor in human C4-2-PSA-rl cells incubated for 24 hrs in presence of androgen R1881 by dual-glo luciferase reporter gene assay	B	5.96	pEC50	1100	nM	EC50	ACS Med Chem Lett (2016) 7: 785-790 [PMID:27563404]
ChEMBL	Displacement of [3H]R1881 from AR in human LNCaP cells after 2 hrs by scintillation counting analysis	B	6.04	pEC50	915	nM	EC50	J Med Chem (2013) 56: 4880-4898 [PMID:23713567]
ChEMBL	Antagonist activity at full length human androgen receptor expressed in mammalian expression system measured after 22 to 24 hrs by luciferase reporter gene assay	B	6.38	pEC50	420	nM	EC50	Bioorg Med Chem Lett (2017) 27: 2216-2220 [PMID:28385503]
ChEMBL	Inhibition of DHT-induced androgen receptor transactivation in human LNCaP cells after 24 hrs by luciferase reporter gene assay relative to control	B	6.74	pEC50	180	nM	EC50	ACS Med Chem Lett (2016) 7: 708-713 [PMID:27437082]
ChEMBL	Agonist activity at VP16-AR F877L mutant (unknown origin) transfected in human HepG2 cells cotransfected with ARE-LUC incubated for 48 hrs by steady-glo luciferase reporter gene assay	B	7.21	pEC50	61.8	nM	EC50	J Med Chem (2021) 64: 909-924 [PMID:33470111]
ChEMBL	Displacement of [3H]R1881 from AR in human MDA-MB-453 cells	B	7.31	pEC50	49	nM	EC50	J Med Chem (2013) 56: 4880-4898 [PMID:23713567]
Androgen receptor/Androgen Receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
ChEMBL	Displacement of [3H]-MIB from wild-type rat AR LBD measured after 16 hrs by scintillation counting method	B	5.44	pKi	3641	nM	Ki	J Med Chem (2020) 63: 12642-12665 [PMID:33095584]
ChEMBL	Inhibition of [3H] MIB binding to rat prostate androgen receptor LBD by competitive binding assay	B	5.44	pKi	3641	nM	Ki	J Med Chem (2021) 64: 11045-11062 [PMID:34269581]
GtoPdb	Binding affinity measured in competition with [3H]mibolerone using wtAR isolated from rat ventral prostates.	-	7.07	pKi	86	nM	Ki	Sci Rep (2015) 5: 12007 [PMID:26137992]
ChEMBL	Displacement of fluormone-AL Green from His-tagged/GST-fused recombinant rat androgen receptor LBD expressed in insect cells measured after 4 hrs by fluorescence polarization assay	B	5.88	pIC50	1320	nM	IC50	Bioorg Med Chem (2019) 27: 133-143 [PMID:30482547]
ChEMBL	Displacement of fluormone-AL Green from His-tagged/GST-fused recombinant rat androgen receptor LBD expressed in insect cells measured after 4 hrs by fluorescence polarization assay	B	5.88	pIC50	1320	nM	IC50	Bioorg Med Chem (2019) 27: 115081-115081 [PMID:31493989]
ChEMBL	Antagonist activity at rat androgen receptor fused with DNA-binding domain of GAL4 expressed in AR-UAS-bla GripTite 293 cells assessed as inhibition of R1881-induced receptor activation preincubated for 30 mins followed by R1881 addition measured after 16 to 24 hrs by betalactamase reporter gene assay	B	6.44	pIC50	361	nM	IC50	Eur J Med Chem (2016) 118: 230-243 [PMID:27131065]
ChEMBL	Displacement of fluormone-DHT green from His/GST-tagged rat AR ligand binding domain after 4 to 8 hrs by fluorescence polarization assay	B	6.53	pIC50	294	nM	IC50	ACS Med Chem Lett (2016) 7: 1024-1027 [PMID:27994731]
Glucocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150]
ChEMBL	Binding affinity to glucocorticoid receptor in human IM-9 cells assessed as inhibition constant incubated for 6 hrs by Cheng-Prusoff equation analysis	B	4.85	pKi	14000	nM	Ki	J Med Chem (2021) 64: 909-924 [PMID:33470111]
ChEMBL	Displacement of [3H]dexamethasone from glucocorticoid receptor in human IM-9 cells incubated for 6 hrs by scintillation counting analysis	B	4.54	pIC50	29000	nM	IC50	J Med Chem (2021) 64: 909-924 [PMID:33470111]
ChEMBL	Antagonist activity at glucocorticoid receptor in human HeLa cells assessed as reduction in dexamethasone-induced luciferase activity by dual-Glo luciferase assay	B	5	pIC50	>10000	nM	IC50	J Med Chem (2021) 64: 17221-17238 [PMID:34809430]
kallikrein related peptidase 3/Prostate specific antigen in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2099] [GtoPdb: 2373] [UniProtKB: P07288]
ChEMBL	Inhibition of prostate specific antigen in human LNCaP cells	B	6.89	pIC50	130	nM	IC50	Eur J Med Chem (2020) 192: 112156-112156 [PMID:32114360]

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]