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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

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]
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
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 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]