ACPT-I [Ligand Id: 1408] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL285043 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| mGlu4 receptor/Metabotropic glutamate receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2736] [GtoPdb: 292] [UniProtKB: Q14833] | ||||||||
| ChEMBL | Agonist activity against Metabotropic glutamate receptor 4 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulation | F | 5.14 | pEC50 | 7200 | nM | EC50 | J Med Chem (1997) 40: 3119-3129 [PMID:9301676] |
| ChEMBL | Agonistic activity at Metabotropic glutamate receptor 4 expressed in mammalian cells by GTPgammaS binding assay | B | 5.15 | pEC50 | 7000 | nM | EC50 | Bioorg Med Chem Lett (2000) 10: 1447-1450 [PMID:10888329] |
| ChEMBL | Agonist activity at mGlu4 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method | F | 5.77 | pEC50 | 1700 | nM | EC50 | J Med Chem (2018) 61: 1969-1989 [PMID:29397723] |
| mGlu4 receptor/Metabotropic glutamate receptor 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2787] [GtoPdb: 292] [UniProtKB: P31423] | ||||||||
| ChEMBL | Stimulation of [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cells; Active | F | 4 | pEC50 | <100000 | nM | EC50 | J Med Chem (2005) 48: 2534-2547 [PMID:15801843] |
| GtoPdb | - | - | 5.1 | pEC50 | - | - | - | J Med Chem (1997) 40: 3119-29 [PMID:9301676] |
| ChEMBL | Activity at rat mGluR4 receptor measured as intracellular calcium concentration in HEK293 cells | F | 5.14 | pEC50 | 7200 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 4856-4860 [PMID:16828551] |
| ChEMBL | Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting | F | 5.76 | pEC50 | 1740 | nM | EC50 | J Med Chem (2010) 53: 2797-2813 [PMID:20218620] |
| mGlu6 receptor/Metabotropic glutamate receptor 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4573] [GtoPdb: 294] [UniProtKB: O15303] | ||||||||
| ChEMBL | Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method | F | 4.96 | pEC50 | 11000 | nM | EC50 | J Med Chem (2018) 61: 1969-1989 [PMID:29397723] |
| mGlu6 receptor/Metabotropic glutamate receptor 6 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3842] [GtoPdb: 294] [UniProtKB: P35349] | ||||||||
| GtoPdb | - | - | 4.7 | pIC50 | - | - | - | |
| ChEMBL | Activity at rat mGluR6 receptor measured as intracellular calcium concentration in HEK293 cells | F | 4.74 | pEC50 | 18400 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 4856-4860 [PMID:16828551] |
| ChEMBL | Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting | F | 4.97 | pEC50 | 10600 | nM | EC50 | J Med Chem (2010) 53: 2797-2813 [PMID:20218620] |
| mGlu8 receptor/Metabotropic glutamate receptor 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3228] [GtoPdb: 296] [UniProtKB: O00222] | ||||||||
| ChEMBL | Agonist activity at mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method | F | 5.29 | pEC50 | 5100 | nM | EC50 | J Med Chem (2018) 61: 1969-1989 [PMID:29397723] |
| mGlu8 receptor/Metabotropic glutamate receptor 8 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2718] [GtoPdb: 296] [UniProtKB: P70579] | ||||||||
| ChEMBL | Activity at rat mGluR8 receptor measured as intracellular calcium concentration in HEK293 cells | F | 5 | pEC50 | 10100 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 4856-4860 [PMID:16828551] |
| GtoPdb | - | - | 5.1 | pEC50 | - | - | - | Eur J Pharmacol (2000) 394: 17-26 [PMID:10771029] |
| ChEMBL | Agonist activity at rat mGlu8 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting | F | 5.29 | pEC50 | 5100 | nM | EC50 | J Med Chem (2010) 53: 2797-2813 [PMID:20218620] |
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]
