ChEMBL ligand: CHEMBL2105738 (Galeterona, Galeterone, TOK 001, TOK-001, VN 124, VN-124, VN/124, VN/124-1)
Androgen receptor/Androgen Receptor in Human [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275] There should be some charts here, you may need to enable JavaScript!
CYP17A1/Cytochrome P450 17A1 in Human [ChEMBL: CHEMBL3522] [GtoPdb: 1361] [UniProtKB: P05093] 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 DHT-induced Androgen receptor transcriptional activity in human HEK293 cells measured after 24 hrs by Steady-Glo reagent based assay	B	5.96	pIC50	1108	nM	IC50	J Med Chem (2022) 65: 12460-12481 [PMID:36070471]
GtoPdb	-	-	6.42	pIC50	384	nM	IC50	J Med Chem (2005) 48: 2972-84 [PMID:15828836]
ChEMBL	Induction of androgen receptor degradation in human LNCaP cells incubated for 24 hrs by ELISA	B	4.84	pEC50	14400	nM	EC50	J Med Chem (2023) 66: 9972-9991 [PMID:37458396]
ChEMBL	Induction of degradation of full length Androgen receptor (unknown origin)	B	4.98	pEC50	10410	nM	EC50	J Med Chem (2022) 65: 16128-16154 [PMID:36459083]
ChEMBL	Displacement of [3H]R1881 from androgen receptor in human LNCAP cells	B	6.07	pEC50	845	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	6.17	pEC50	670	nM	EC50	J Med Chem (2013) 56: 4880-4898 [PMID:23713567]
ChEMBL	Displacement of [3H]R1881 from androgen receptor in human PC3 cells	B	6.39	pEC50	405	nM	EC50	J Med Chem (2015) 58: 2077-2087 [PMID:25591066]
CYP17A1/Cytochrome P450 17A1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3522] [GtoPdb: 1361] [UniProtKB: P05093]
ChEMBL	Inhibition of human truncated CYP17A1 expressed in Escherichia coli	B	6.12	pIC50	752	nM	IC50	J Med Chem (2013) 56: 4880-4898 [PMID:23713567]
GtoPdb	-	-	6.52	pIC50	300	nM	IC50	J Med Chem (2005) 48: 2972-84 [PMID:15828836]
ChEMBL	Inhibition of human CYP17 expressed in Escherichia coli	B	6.52	pIC50	300	nM	IC50	J Med Chem (2015) 58: 2077-2087 [PMID:25591066]
ChEMBL	Inhibition of human membrane bound C-terminal His4-tagged CYP17A1 delta19H mutant assessed as reduction in progesterone hydroxylation preincubated for 3 mins followed by NADPH addition measured after 10 mins in presence of NADPH-cytochrome p450 reductase by HPLC method	B	6.55	pIC50	282	nM	IC50	US-20160031929-A1. Inhibitors of cyp17a1 (2016)
ChEMBL	Inhibition of CYP17 (unknown origin)	B	6.85	pIC50	140	nM	IC50	ACS Med Chem Lett (2016) 7: 708-713 [PMID:27437082]
ChEMBL	Inhibition of C-terminal His-tagged recombinant human CYP17A1delta19H mutant expressed in Escherichia coli DH5alpha assessed as decrease in progesterone hydroxylation preincubated for 3 mins followed by NADPH addition measured after 10 mins in presence of cytochrome p450 reductase by LC-MS/MS method	B	7.55	pIC50	28.1	nM	IC50	J Med Chem (2018) 61: 4946-4960 [PMID:29792703]

ChEMBL data shown on this page come from version 34:

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]