VU0240382 [Ligand Id: 6422] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1682799
  • mGlu5 receptor/Metabotropic glutamate receptor 5 in Human [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594]
  • mGlu5 receptor in Rat [GtoPdb: 293] [UniProtKB: P31424]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
mGlu5 receptor/Metabotropic glutamate receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594]
ChEMBL Positive allosteric modulation of mGlu5 receptor assessed as calcium mobilization F 7.3 pEC50 50 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 1350-1353 [PMID:21315585]
ChEMBL Positive allosteric modulation of human mGlu4 receptor expressed in human HEK293 cells assessed as potentiation of glutamate-induced calcium mobilization after 1 hr by FLIPR assay F 7.35 pEC50 44.67 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 1402-1406 [PMID:21295468]
ChEMBL Positive allosteric modulation of human mGlu4 receptor expressed in human HEK293 cells assessed as potentiation of glutamate-induced calcium mobilization after 1 hr by FLIPR assay F 7.35 pEC50 44.3 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 1402-1406 [PMID:21295468]
mGlu5 receptor in Rat [GtoPdb: 293] [UniProtKB: P31424]
GtoPdb - - 7.41 pEC50 39 nM EC50 Mol Pharmacol (2012) 81: 120-33 [PMID:22021324]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]