abarelix [Ligand Id: 1188] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1252 (R-382, R3827, R-3827, Plenaxis, PPI-149, R382, Abarelix)
  • GnRH1 receptor/Gonadotropin-releasing hormone receptor in Human [ChEMBL: CHEMBL1855] [GtoPdb: 256] [UniProtKB: P30968]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GnRH1 receptor/Gonadotropin-releasing hormone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1855] [GtoPdb: 256] [UniProtKB: P30968]
ChEMBL Competitive antagonism of GnRH-induced response in the reporter gene assay F 9.1 pKd 0.79 nM Kd J. Med. Chem. (2001) 44: 453-467 [PMID:11462984]
GtoPdb - - 9.49 pKi 0.32 nM Ki Endocrinology (2007) 148: 857-67 [PMID:17095587]
ChEMBL Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells F 8.46 pIC50 3.5 nM IC50 J. Med. Chem. (2001) 44: 453-467 [PMID:11462984]

ChEMBL data shown on this page come from version 28:

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]