PF0998425 [Ligand Id: 6698] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL458084 (PF-0998425)
  • 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 Androgen receptor in human MDA-kb2 cells B 7.05 pIC50 90 nM IC50 J Med Chem (2022) 65: 8772-8797 [PMID:35786895]
ChEMBL Antagonist activity against human androgen receptor expressed in human MDA-MB-453 cells assessed as inhibition of dihydrotestosterone-induced effect by luciferase receptor gene assay F 7.37 pIC50 43 nM IC50 J Med Chem (2008) 51: 7010-7014 [PMID:18921992]
ChEMBL Displacement of [3H]dihydrotestosterone from human androgen receptor expressed in Sf9 cells B 7.43 pIC50 37 nM IC50 J Med Chem (2008) 51: 7010-7014 [PMID:18921992]
GtoPdb - - 7.5 pIC50 - - - J Med Chem (2008) 51: 7010-4 [PMID:18921992]
ChEMBL Binding affinity to human Androgen receptor B 7.59 pIC50 26 nM IC50 J Med Chem (2022) 65: 8772-8797 [PMID:35786895]
Progesterone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL208] [GtoPdb: 627] [UniProtKB: P06401]
ChEMBL Inhibition of progesterone receptor B 5 pIC50 >10000 nM IC50 J Med Chem (2008) 51: 7010-7014 [PMID:18921992]

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]