degarelix [Ligand Id: 5585] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL415606 (Degarelix, FE200486 (AS ACETATE SALT), Firmagon)
  • 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 9.2 pKd 0.63 nM Kd J. Med. Chem. (2001) 44: 453-467 [PMID:11462984]
GtoPdb - - 8.77 pKi 1.7 nM Ki Cancer Manag Res (2010) 2: 39-52 [PMID:21188095]
ChEMBL Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells F 8.06 pIC50 8.8 nM IC50 J. Med. Chem. (2001) 44: 453-467 [PMID:11462984]
ChEMBL Antagonism of GnRH response in HEK293 cells expressing human GnRH receptor F 8.79 pIC50 1.64 nM IC50 J. Med. Chem. (2005) 48: 4851-4860 [PMID:16033265]
ChEMBL Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay F 9.24 pIC50 0.58 nM IC50 J. Med. Chem. (2006) 49: 3536-3543 [PMID:16759096]
ChEMBL Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay F 9.24 pIC50 0.58 nM IC50 J. Med. Chem. (2006) 49: 3536-3543 [PMID:16759096]

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, 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]