LY395756 [Ligand Id: 11614] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL192051 |
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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 | Displacement of [3H]-341495 binding to membranes expressing recombinant human Metabotropic glutamate receptor 2 | B | 6.39 | pKi | 409 | nM | Ki | J Med Chem (2005) 48: 3605-3612 [PMID:15887967] |
| GtoPdb | - | - | 6.78 | pKi | 165 | nM | Ki | Exp Neurol (2015) 273: 190-201 [PMID:26341392] |
| ChEMBL | Displacement of [3H]-341495 binding to membranes expressing recombinant human Metabotropic glutamate receptor 2 | B | 6.78 | pKi | 165 | nM | Ki | J Med Chem (2005) 48: 3605-3612 [PMID:15887967] |
| ChEMBL | Evaluation of the functional effect on cAMP responses in RGT cells expressing human mGlu2 receptor | F | 6.4 | pEC50 | 397 | nM | EC50 | J Med Chem (2005) 48: 3605-3612 [PMID:15887967] |
| ChEMBL | Evaluation of the functional effect on cAMP responses in RGT cells expressing human mGlu2 receptor | F | 6.79 | pEC50 | 161 | nM | EC50 | J Med Chem (2005) 48: 3605-3612 [PMID:15887967] |
| ChEMBL | Agonist activity at human mGlu2 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assay | B | 7.2 | pEC50 | 63.6 | nM | EC50 | J Med Chem (2013) 56: 4442-4455 [PMID:23675965] |
| mGlu3 receptor/Metabotropic glutamate receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2888] [GtoPdb: 291] [UniProtKB: Q14832] | ||||||||
| ChEMBL | Displacement of [3H]-341495 binding to membranes expressing recombinant human Metabotropic glutamate receptor 3 | B | 6.24 | pKi | 570 | nM | Ki | J Med Chem (2005) 48: 3605-3612 [PMID:15887967] |
| ChEMBL | Displacement of [3H]-341495 binding to membranes expressing recombinant human Metabotropic glutamate receptor 3 | B | 6.52 | pKi | 302 | nM | Ki | J Med Chem (2005) 48: 3605-3612 [PMID:15887967] |
| GtoPdb | - | - | 6.52 | pKi | 302 | nM | Ki | Exp Neurol (2015) 273: 190-201 [PMID:26341392] |
| ChEMBL | Antagonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by HTRF assay | F | 5.47 | pIC50 | 3420 | nM | IC50 | J Med Chem (2013) 56: 4442-4455 [PMID:23675965] |
| ChEMBL | Evaluation of the functional effect on cAMP responses in RGT cells expressing human mGlu3 receptor | F | 5.53 | pIC50 | 2940 | nM | IC50 | J Med Chem (2005) 48: 3605-3612 [PMID:15887967] |
| ChEMBL | Evaluation of the functional effect on cAMP responses in RGT cells expressing human mGlu3 receptor | F | 5.98 | pIC50 | 1050 | nM | IC50 | J Med Chem (2005) 48: 3605-3612 [PMID:15887967] |
| mGlu6 receptor/Metabotropic glutamate receptor 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4573] [GtoPdb: 294] [UniProtKB: O15303] | ||||||||
| ChEMBL | Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay | B | 5.12 | pEC50 | 7540 | nM | EC50 | J Med Chem (2013) 56: 4442-4455 [PMID:23675965] |
| mGlu8 receptor/Metabotropic glutamate receptor 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3228] [GtoPdb: 296] [UniProtKB: O00222] | ||||||||
| ChEMBL | Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay | B | 4.6 | pEC50 | >25000 | nM | EC50 | J Med Chem (2013) 56: 4442-4455 [PMID:23675965] |
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]
