sufugolix [Ligand Id: 1185] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL22055 (Sufugolix, Tak-013, TAK-013)
  • Gonadotropin-releasing hormone receptor in Rhesus macaque [ChEMBL: CHEMBL5647] [UniProtKB: Q8SPZ1]
  • 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]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Gonadotropin-releasing hormone receptor in Rhesus macaque (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5647] [UniProtKB: Q8SPZ1]
ChEMBL Binding affinity at monkey GnRH receptor B 9.22 pIC50 0.6 nM IC50 J Med Chem (2008) 51: 3331-3348 [PMID:18419112]
GnRH1 receptor/Gonadotropin-releasing hormone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1855] [GtoPdb: 256] [UniProtKB: P30968]
ChEMBL Binding affinity towards human gonadotropin-releasing hormone receptor B 9.7 pKi 0.2 nM Ki Bioorg Med Chem Lett (2003) 13: 3617-3622 [PMID:14505682]
GtoPdb - - 10 pKi - - - J Med Chem (2003) 46: 113-24 [PMID:12502365]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118N B 5.97 pIC50 1070 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121A B 6.33 pIC50 470 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
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 6.57 pIC50 270 nM IC50 J Med Chem (2011) 54: 4998-5012 [PMID:21657270]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306K B 6.62 pIC50 242 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24A B 6.62 pIC50 240 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24T B 6.71 pIC50 193 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302A B 6.72 pIC50 192 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells B 6.72 pIC50 190 nM IC50 J Med Chem (2006) 49: 6170-6176 [PMID:17034124]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302Q B 6.83 pIC50 148 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells B 6.92 pIC50 120 nM IC50 J Med Chem (2006) 49: 6170-6176 [PMID:17034124]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302N B 6.94 pIC50 115 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells B 6.96 pIC50 110 nM IC50 J Med Chem (2006) 49: 6170-6176 [PMID:17034124]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24I B 6.97 pIC50 108 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells B 7 pIC50 100 nM IC50 J Med Chem (2006) 49: 6170-6176 [PMID:17034124]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306E B 7.02 pIC50 94.9 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313L B 7.61 pIC50 24.4 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells B 7.62 pIC50 24 nM IC50 J Med Chem (2006) 49: 6170-6176 [PMID:17034124]
ChEMBL Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells B 7.62 pIC50 24 nM IC50 J Med Chem (2006) 49: 6170-6176 [PMID:17034124]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306A B 7.63 pIC50 23.4 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284L B 7.92 pIC50 12.1 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells B 7.92 pIC50 12 nM IC50 J Med Chem (2006) 49: 6170-6176 [PMID:17034124]
ChEMBL Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells B 8 pIC50 10 nM IC50 J Med Chem (2006) 49: 6170-6176 [PMID:17034124]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309Q B 8 pIC50 10 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Tested for inhibition of arachidonic acid(AA) release from CHO cells in Monkey F 8 pIC50 10 nM IC50 J Med Chem (2003) 46: 113-124 [PMID:12502365]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208D B 8.01 pIC50 9.7 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27E B 8.07 pIC50 8.5 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309L B 8.2 pIC50 6.3 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells B 8.22 pIC50 6 nM IC50 J Med Chem (2006) 49: 6170-6176 [PMID:17034124]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300K B 8.28 pIC50 5.2 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305D B 8.37 pIC50 4.3 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305K B 8.52 pIC50 3 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHR B 8.6 pIC50 2.5 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280F B 8.64 pIC50 2.3 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293K B 8.7 pIC50 2 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112K B 8.72 pIC50 1.9 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells B 8.72 pIC50 1.9 nM IC50 J Med Chem (2006) 49: 6170-6176 [PMID:17034124]
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 8.72 pIC50 1.9 nM IC50 J Med Chem (2011) 54: 4998-5012 [PMID:21657270]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300A B 8.72 pIC50 1.9 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300V B 8.74 pIC50 1.8 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
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 8.8 pIC50 1.6 nM IC50 J Med Chem (2011) 54: 4998-5012 [PMID:21657270]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203P B 8.85 pIC50 1.4 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208E B 8.89 pIC50 1.3 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293E B 8.92 pIC50 1.2 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115Q B 8.92 pIC50 1.2 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells B 8.92 pIC50 1.2 nM IC50 J Med Chem (2006) 49: 6170-6176 [PMID:17034124]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315A B 8.92 pIC50 1.2 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290Q B 8.96 pIC50 1.1 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291F B 9.05 pIC50 0.9 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124A B 9.05 pIC50 0.9 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190K B 9.05 pIC50 0.9 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284F B 9.05 pIC50 0.9 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293N B 9.1 pIC50 0.8 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186K B 9.1 pIC50 0.8 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111K B 9.1 pIC50 0.8 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells B 9.1 pIC50 0.8 nM IC50 J Med Chem (2006) 49: 6170-6176 [PMID:17034124]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272L B 9.1 pIC50 0.8 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168I B 9.1 pIC50 0.8 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells B 9.15 pIC50 0.7 nM IC50 J Med Chem (2006) 49: 6170-6176 [PMID:17034124]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189A B 9.15 pIC50 0.7 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189K B 9.15 pIC50 0.7 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27A B 9.15 pIC50 0.7 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315D B 9.15 pIC50 0.7 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189E B 9.22 pIC50 0.6 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295Q B 9.22 pIC50 0.6 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293A B 9.22 pIC50 0.6 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290F B 9.22 pIC50 0.6 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168A B 9.22 pIC50 0.6 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118A B 9.22 pIC50 0.6 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112F B 9.22 pIC50 0.6 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112A B 9.22 pIC50 0.6 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111Q B 9.22 pIC50 0.6 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51A B 9.22 pIC50 0.6 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50T B 9.22 pIC50 0.6 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to LHRH receptor in monkey (chinese hamster ovary (CHO) cells) B 9.22 pIC50 0.6 nM IC50 J Med Chem (2003) 46: 113-124 [PMID:12502365]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203K B 9.3 pIC50 0.5 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191E B 9.3 pIC50 0.5 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203E B 9.3 pIC50 0.5 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290L B 9.3 pIC50 0.5 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells B 9.3 pIC50 0.5 nM IC50 J Med Chem (2006) 49: 6170-6176 [PMID:17034124]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295K B 9.3 pIC50 0.5 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182E B 9.3 pIC50 0.5 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295A B 9.3 pIC50 0.5 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186D B 9.3 pIC50 0.5 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189P B 9.3 pIC50 0.5 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283F B 9.3 pIC50 0.5 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203Q B 9.3 pIC50 0.5 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111A B 9.4 pIC50 0.4 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117A B 9.4 pIC50 0.4 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305A B 9.4 pIC50 0.4 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182A B 9.52 pIC50 0.3 nM IC50 J Med Chem (2006) 49: 637-647 [PMID:16420049]
ChEMBL Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells. B 10 pIC50 0.1 nM IC50 J Med Chem (2003) 46: 113-124 [PMID:12502365]
ChEMBL Binding affinity at human GnRH receptor B 10 pIC50 0.1 nM IC50 J Med Chem (2008) 51: 3331-3348 [PMID:18419112]
ChEMBL Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter B 10 pIC50 0.1 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 10.22 pIC50 0.06 nM IC50 J Med Chem (2011) 54: 4998-5012 [PMID:21657270]
ChEMBL Tested for inhibition of arachidonic acid(AA) release from CHO cells in Human F 10.22 pIC50 0.06 nM IC50 J Med Chem (2003) 46: 113-124 [PMID:12502365]
GnRH1 receptor/Gonadotropin-releasing hormone receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3066] [GtoPdb: 256] [UniProtKB: P30969]
ChEMBL Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to LHRH receptor in rat anterior pituitaries B 6 pIC50 >1000 nM IC50 J Med Chem (2003) 46: 113-124 [PMID:12502365]
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 8.89 pIC50 1.3 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]