apalutamide [Ligand Id: 9043] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3183409 (Apalutamide, JNJ-56021927, Erleada, ARN-509)
  • Androgen receptor/Androgen Receptor in Human [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275]
  • Androgen receptor in Rat [GtoPdb: 628] [UniProtKB: P15207]
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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 androgen receptor (unknown origin) B 7.46 pKi 34.7 nM Ki Eur. J. Med. Chem. (2015) 99: 51-66 [PMID:26046313]
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]
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]
Androgen receptor in Rat [GtoPdb: 628] [UniProtKB: P15207]
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 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]