VU0080241 [Ligand Id: 6227] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL477396 (VU0080241)
  • mGlu1 receptor/Metabotropic glutamate receptor 1 in Rat [ChEMBL: CHEMBL4477] [GtoPdb: 289] [UniProtKB: P23385]
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  • mGlu4 receptor/Metabotropic glutamate receptor 4 in Human [ChEMBL: CHEMBL2736] [GtoPdb: 292] [UniProtKB: Q14833]
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  • 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
mGlu1 receptor/Metabotropic glutamate receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4477] [GtoPdb: 289] [UniProtKB: P23385]
ChEMBL Antagonist activity at rat mGluR1 expressed in Syrian golden hamster BHK cells assessed as potentiation of glutamate-induced calcium flux by fluorescence assay F 5.59 pIC50 2600 nM IC50 Bioorg Med Chem Lett (2008) 18: 5626-5630 [PMID:18793851]
mGlu4 receptor/Metabotropic glutamate receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2736] [GtoPdb: 292] [UniProtKB: Q14833]
GtoPdb - - 5.3 pEC50 4600 nM EC50 Bioorg Med Chem Lett (2008) 18: 5626-30 [PMID:18793851]
ChEMBL Activity at human mGluR4 expressed in CHO coexpressing Gqi5 assessed as potentiation of glutamate-induced calcium flux by fluorescence assay F 5.34 pEC50 4600 nM EC50 Bioorg Med Chem Lett (2008) 18: 5626-5630 [PMID:18793851]
mGlu5 receptor/Metabotropic glutamate receptor 5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2564] [GtoPdb: 293] [UniProtKB: P31424]
ChEMBL Activity at rat mGluR5 expressed in HEK cells assessed as potentiation of glutamate-induced calcium flux by fluorescence assay F 5.3 pEC50 5000 nM EC50 Bioorg Med Chem Lett (2008) 18: 5626-5630 [PMID:18793851]

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]