LY2389575 [Ligand Id: 9694] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2204436 (LY-2389575) |
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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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
