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 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]
