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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL1252 (R-382, R-3827, Abarelix, Plenaxis, PPI-149, R382)
  • GnRH1 receptor/Gonadotropin-releasing hormone receptor in Human [ChEMBL: CHEMBL1855] [GtoPdb: 256] [UniProtKB: P30968]
  • This target only has 1 pki data point
1 CHEMBL1252_lig_chart_1 Gonadotropin-releasing hormone receptor Human
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
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 27:

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]