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 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]
