VU0092273 [Ligand Id: 6421] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1684241 (VU0092273)
  • mGlu3 receptor/Metabotropic glutamate receptor 3 in Rat [ChEMBL: CHEMBL3067] [GtoPdb: 291] [UniProtKB: P31422]
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  • mGlu5 receptor/Metabotropic glutamate receptor 5 in Human [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594]
  • mGlu5 receptor/Metabotropic glutamate receptor 5 in Rat [ChEMBL: CHEMBL2564] [GtoPdb: 293] [UniProtKB: P31424]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
mGlu3 receptor/Metabotropic glutamate receptor 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3067] [GtoPdb: 291] [UniProtKB: P31422]
ChEMBL Negative allosteric modulation of rat mGlu3 assessed as assessed as thallium flux through GIRK channels by cell-based assay B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 3921-3925 [PMID:22607673]
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 8 pEC50 10 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 1350-1353 [PMID:21315585]
mGlu5 receptor/Metabotropic glutamate receptor 5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2564] [GtoPdb: 293] [UniProtKB: P31424]
GtoPdb - - 5.89 pEC50 1300 nM EC50 Mol Pharmacol (2012) 81: 120-33 [PMID:22021324]
ChEMBL Positive allosteric modulation of rat mGlu5 expressed in HEK293 cells in presence of glutamate EC20 concentration by Fluo-2AM dye based fluorescence analysis B 6.57 pEC50 270 nM EC50 Bioorg. Med. Chem. Lett. (2012) 22: 3921-3925 [PMID:22607673]
GtoPdb - - 7.46 pEC50 35 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]