IN-3 [Ligand Id: 5584] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL314260 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| GnRH1 receptor/Gonadotropin-releasing hormone receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1855] [GtoPdb: 256] [UniProtKB: P30968] | ||||||||
| ChEMBL | In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor. | F | 8.14 | pIC50 | 7.2 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 2597-2602 [PMID:11551758] |
| GtoPdb | - | - | 9.22 | pIC50 | 0.6 | nM | IC50 |
Bioorg Med Chem Lett (2001) 11: 2597-602 [PMID:11551758]; J Clin Endocrinol Metab (2002) 87: 3255-62 [PMID:12107234] |
| ChEMBL | Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin. | B | 9.22 | pIC50 | 0.6 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 2597-2602 [PMID:11551758] |
| GnRH1 receptor/Gonadotropin-releasing hormone receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3066] [GtoPdb: 256] [UniProtKB: P30969] | ||||||||
| ChEMBL | Binding affinity at rat GnRH receptor by whole cell binding assay | B | 8.77 | pIC50 | 1.7 | nM | IC50 | J Med Chem (2008) 51: 3331-3348 [PMID:18419112] |
| GtoPdb | - | - | 8.77 | pIC50 | 1.7 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 2597-602 [PMID:11551758] |
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]
