VU0463597 [Ligand Id: 6225] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2204445 ((R)-VU0463597)
  • mGlu2 receptor/Metabotropic glutamate receptor 2 in Human [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416]
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  • mGlu3 receptor/Metabotropic glutamate receptor 3 in Human [ChEMBL: CHEMBL2888] [GtoPdb: 291] [UniProtKB: Q14832]
  • 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]
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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 Negative allosteric modulation of mGlu2 by cell-based assay B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2012) 22: 3921-3925 [PMID:22607673]
mGlu3 receptor/Metabotropic glutamate receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2888] [GtoPdb: 291] [UniProtKB: Q14832]
ChEMBL Negative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assay B 5.82 pIC50 1500 nM IC50 Bioorg Med Chem Lett (2012) 22: 3921-3925 [PMID:22607673]
ChEMBL Negative allosteric modulation of mGlu3 assessed as thallium flux through GIRK channels by cell-based assay B 5.83 pIC50 1479.11 nM IC50 Bioorg Med Chem Lett (2012) 22: 3921-3925 [PMID:22607673]
ChEMBL Negative allosteric modulation of mGlu3 assessed as inhibition of glutamate-induced calcium mobilization in presence of Galpha15 by cell based assay F 6.18 pIC50 660 nM IC50 Bioorg Med Chem Lett (2012) 22: 3921-3925 [PMID:22607673]
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 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins F 5 pIC50 >10000 nM IC50 J Med Chem (2013) 56: 5208-5212 [PMID:23718281]
GtoPdb - - 6.2 pIC50 660 nM IC50 Bioorg Med Chem Lett (2012) 22: 3921-5 [PMID:22607673]
mGlu5 receptor/Metabotropic glutamate receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594]
ChEMBL Negative allosteric modulation of mGlu5 assessed as inhibition of glutamate-induced calcium mobilization by cell based assay F 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2012) 22: 3921-3925 [PMID:22607673]
ChEMBL Positive allosteric modulation of mGlu5 assessed as potentiation of glutamate-induced calcium mobilization by cell based assay F 5 pEC50 >10000 nM EC50 Bioorg Med Chem Lett (2012) 22: 3921-3925 [PMID:22607673]

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]