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 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]
