relugolix [Ligand Id: 5586] 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: CHEMBL1800159 (Orgovyx, Relugolix, Tak-385, TAK-385)
  • GnRH1 receptor/Gonadotropin-releasing hormone receptor in Human [ChEMBL: CHEMBL1855] [GtoPdb: 256] [UniProtKB: P30968]
  • GnRH1 receptor/Gonadotropin-releasing hormone receptor in Rat [ChEMBL: CHEMBL3066] [GtoPdb: 256] [UniProtKB: P30969]
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 Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay B 9.08 pKd 0.84 nM Kd J Med Chem (2020) 63: 11854-11881 [PMID:32960053]
ChEMBL Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay B 9.43 pKd 0.37 nM Kd J Med Chem (2020) 63: 11854-11881 [PMID:32960053]
ChEMBL Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serum F 7.74 pIC50 18 nM IC50 J Med Chem (2011) 54: 4998-5012 [PMID:21657270]
ChEMBL Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum F 9.09 pIC50 0.82 nM IC50 J Med Chem (2011) 54: 4998-5012 [PMID:21657270]
GtoPdb - - 9.48 pIC50 0.33 nM IC50 J Med Chem (2011) 54: 4998-5012 [PMID:21657270]
ChEMBL Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum B 9.48 pIC50 0.33 nM IC50 J Med Chem (2011) 54: 4998-5012 [PMID:21657270]
ChEMBL Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting F 9.48 pIC50 0.33 nM IC50 J Med Chem (2011) 54: 4998-5012 [PMID:21657270]
ChEMBL Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter B 10.1 pIC50 0.08 nM IC50 J Med Chem (2011) 54: 4998-5012 [PMID:21657270]
GnRH1 receptor/Gonadotropin-releasing hormone receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3066] [GtoPdb: 256] [UniProtKB: P30969]
GtoPdb - - 9.48 pIC50 0.33 nM IC50 J Med Chem (2011) 54: 4998-5012 [PMID:21657270]
ChEMBL Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum B 9.49 pIC50 0.32 nM IC50 J Med Chem (2011) 54: 4998-5012 [PMID:21657270]
ChEMBL Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter B 9.49 pIC50 0.32 nM IC50 J Med Chem (2011) 54: 4998-5012 [PMID:21657270]

ChEMBL data shown on this page come from version 32:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]