ChEMBL ligand: CHEMBL3183409 (Apalutamide, Arn-509, ARN-509, Erleada, JNJ-56021927)
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!

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	Displacement of [3H]-mibolerone from recombinant wild-type GST-tagged androgen receptor LBD (unknown origin) after 16 hrs by scintillation counting analysis	B	5.84	pKi	1452	nM	Ki	J Med Chem (2019) 62: 491-511 [PMID:30525603]
ChEMBL	Inhibition of androgen receptor (unknown origin)	B	7.03	pKi	93	nM	Ki	Eur J Med Chem (2020) 205: 112667-112667 [PMID:32911308]
ChEMBL	Antagonist activity at androgen receptor (unknown origin)	B	7.46	pKi	34.7	nM	Ki	Eur. J. Med. Chem. (2015) 99: 51-66 [PMID:26046313]
ChEMBL	Inhibition of androgen receptor (unknown origin)	B	6.7	pIC50	200	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..	-	6.7	pIC50	200	nM	IC50	Sci Rep (2015) 5: 12007 [PMID:26137992]
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	6.8	pIC50	160	nM	IC50	J Med Chem (2020) 63: 12642-12665 [PMID:33095584]
GtoPdb	-	-	6.91	pIC50	122	nM	IC50	J Med Chem (2010) 53: 2779-96 [PMID:20218717]
ChEMBL	Displacement of [3H]-R1881 from AR in human LNCaP cells preincubated for 30 mins followed by [3H]-R1881 addition measured after 30 mins by microbeta scintillation counter method	B	7.79	pIC50	16.25	nM	IC50	Bioorg Med Chem Lett (2017) 27: 2803-2806 [PMID:28478926]
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	7.8	pIC50	16	nM	IC50	J Med Chem (2019) 62: 491-511 [PMID:30525603]
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	5.84	pKi	1452	nM	Ki	J Med Chem (2020) 63: 12642-12665 [PMID:33095584]
GtoPdb	Binding affinity measured in competition with [3H]mibolerone using wtAR isolated from rat ventral prostates.	-	7.03	pKi	93	nM	Ki	Sci Rep (2015) 5: 12007 [PMID:26137992]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]