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ChEMBL ligand: CHEMBL22055 (Sufugolix, Tak-013, TAK-013) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]