4-MPPTS [Ligand Id: 1402] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL108939 (LY-487379) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| mGlu2 receptor/Metabotropic glutamate receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416] | ||||||||
| ChEMBL | Ability to displace [3H]LY-341,495 at glutamate-site on Metabotropic glutamate receptor 2; No significant displacement | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2003) 46: 3189-3192 [PMID:12852748] |
| GtoPdb | - | - | 5.8 | pIC50 | - | - | - |
J Med Chem (2003) 46: 3189-92 [PMID:12852748]; Mol Pharmacol (2003) 64: 798-810 [PMID:14500736]; Psychopharmacology (Berl.) (2005) 179: 271-83 [PMID:15717213]; Bioorg Med Chem Lett (2004) 14: 3099-102 [PMID:15149652] |
| ChEMBL | Binding affinity towards human metabotropic glutamate receptor 2 determined by [35S]GTP gamma S binding assay | F | 5.77 | pEC50 | 1700 | nM | EC50 | Bioorg Med Chem Lett (2004) 14: 5867-5872 [PMID:15501058] |
| ChEMBL | Effective concentration for binding to human metabotropic glutamate receptor 2 as determined by GTPgammaS assay | B | 5.77 | pEC50 | 1700 | nM | EC50 | Bioorg Med Chem Lett (2004) 14: 5329-5332 [PMID:15454221] |
| ChEMBL | Effective concentration against Metabotropic glutamate receptor 2 | B | 6.57 | pEC50 | 270 | nM | EC50 | J Med Chem (2003) 46: 3189-3192 [PMID:12852748] |
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]
