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ChEMBL ligand: CHEMBL71917 (T-98475) |
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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 | 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]