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 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]