T-98475 [Ligand Id: 1184] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL71917 (T-98475)
  • 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 8.4 pIC50 4 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]
ChEMBL Displacement of [125I]leuprorelin from human GnRHR expressed in CHO cell membranes after 60 mins by gamma-ray counting method B 9.7 pKi 0.2 nM Ki Medchemcomm (2017) 8: 1965-1969 [PMID:30108717]
ChEMBL Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay F 10 pKi 0.1 nM Ki Medchemcomm (2017) 8: 1965-1969 [PMID:30108717]
ChEMBL Inhibition of Human gonadotropin-releasing hormone receptor B 7.22 pIC50 60 nM IC50 J Med Chem (2005) 48: 1169-1178 [PMID:15715483]
ChEMBL Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay F 8.3 pIC50 5.01 nM IC50 Medchemcomm (2017) 8: 1965-1969 [PMID:30108717]
ChEMBL Inhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptor B 8.4 pIC50 4 nM IC50 J Med Chem (2006) 49: 3809-3825 [PMID:16789738]
ChEMBL Inhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cells B 8.7 pIC50 2 nM IC50 J Med Chem (2006) 49: 3809-3825 [PMID:16789738]
ChEMBL Inhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptor F 9.22 pIC50 0.6 nM IC50 J Med Chem (2006) 49: 3809-3825 [PMID:16789738]
ChEMBL Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated B 9.7 pIC50 0.2 nM IC50 Bioorg Med Chem Lett (2002) 12: 2179-2183 [PMID:12127532]
ChEMBL Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells B 9.7 pIC50 0.2 nM IC50 J Med Chem (2006) 49: 3809-3825 [PMID:16789738]
ChEMBL Binding affinity at human GnRH receptor B 9.7 pIC50 0.2 nM IC50 J Med Chem (2008) 51: 3331-3348 [PMID:18419112]
ChEMBL Inhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligand B 9.7 pIC50 0.2 nM IC50 Bioorg Med Chem Lett (2002) 12: 399-402 [PMID:11814806]
GtoPdb - - 9.7 pIC50 - - - J Med Chem (1998) 41: 4190-5 [PMID:9784092]
GnRH1 receptor/Gonadotropin-releasing hormone receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3066] [GtoPdb: 256] [UniProtKB: P30969]
ChEMBL Binding affinity towards rat Gonadotropin-releasing hormone receptor B 7.22 pKi 60 nM Ki Bioorg Med Chem Lett (2003) 13: 3617-3622 [PMID:14505682]
ChEMBL Binding affinity against gonadotropin-releasing hormone receptor of rat B 7.22 pIC50 60 nM IC50 Bioorg Med Chem Lett (2002) 12: 399-402 [PMID:11814806]
ChEMBL Inhibition of Rat gonadotropin-releasing hormone receptor(moderate affinity) B 7.22 pIC50 60 nM IC50 J Med Chem (2005) 48: 1169-1178 [PMID:15715483]
ChEMBL Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor B 7.22 pIC50 60 nM IC50 J Med Chem (2006) 49: 3809-3825 [PMID:16789738]
ChEMBL Binding affinity at rat GnRH receptor B 7.22 pIC50 60 nM IC50 J Med Chem (2008) 51: 3331-3348 [PMID:18419112]
ChEMBL Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluated B 9.22 pIC50 0.6 nM IC50 Bioorg Med Chem Lett (2002) 12: 2179-2183 [PMID:12127532]

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]