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 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]