abiraterone acetate [Ligand Id: 9288] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL271227 (Abiraterone acetate, Abiraterone krka, CB-7630, CB7630, NSC-748121, NSC-749227, Yonsa, Zytiga)
  • Androgen receptor/Androgen Receptor in Human [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275]
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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 full length human androgen receptor expressed in mammalian expression system measured after 22 to 24 hrs by luciferase reporter gene assay B 4.77 pEC50 17050 nM EC50 Bioorg Med Chem Lett (2017) 27: 2216-2220 [PMID:28385503]
CYP17A1/Cytochrome P450 17A1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3522] [GtoPdb: 1361] [UniProtKB: P05093]
ChEMBL Ability to inhibit the Steroid 17-alpha-hydroxylase/17,20 lyase enzyme by 50%. B 7.74 pIC50 18 nM IC50 J Med Chem (1995) 38: 2463-2471 [PMID:7608911]
ChEMBL Ability to inhibit the C17,20-lyase enzyme by 50% using 17-alpha-hydroxyprogesterone as substrate. B 7.77 pIC50 17 nM IC50 J Med Chem (1995) 38: 2463-2471 [PMID:7608911]

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]