LY2389575 [Ligand Id: 9694] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2204436 (LY-2389575)
  • 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]
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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 assessed as thallium flux through GIRK channels by cell-based assay B 4.77 pIC50 17000 nM IC50 Bioorg Med Chem Lett (2012) 22: 3921-3925 [PMID:22607673]
ChEMBL Negative allosteric modulation of human mGlu2 expressed in AV-12 cells in presence of glutamate EC90 concentration by FLIPR assay B 4.9 pIC50 >12500 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 5.38 pIC50 4200 nM IC50 Bioorg Med Chem Lett (2012) 22: 3921-3925 [PMID:22607673]
GtoPdb Assessed in AV-12 cells expressing the human mGlu3, activated by glutamate as agonist. - 6.72 pIC50 190 nM IC50 Bioorg Med Chem Lett (2012) 22: 3921-5 [PMID:22607673]
ChEMBL Negative allosteric modulation of human mGlu3 expressed in AV-12 cells in presence of glutamate EC90 concentration by FLIPR assay B 6.72 pIC50 190 nM IC50 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]