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 33:

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]