VU0463597 [Ligand Id: 6225] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2204445 ((R)-VU0463597) |
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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 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]
