ACPT-I [Ligand Id: 1408] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL285043
  • mGlu4 receptor/Metabotropic glutamate receptor 4 in Human [ChEMBL: CHEMBL2736] [GtoPdb: 292] [UniProtKB: Q14833]
  • mGlu4 receptor/Metabotropic glutamate receptor 4 in Rat [ChEMBL: CHEMBL2787] [GtoPdb: 292] [UniProtKB: P31423]
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  • mGlu6 receptor/Metabotropic glutamate receptor 6 in Human [ChEMBL: CHEMBL4573] [GtoPdb: 294] [UniProtKB: O15303]
  • mGlu6 receptor/Metabotropic glutamate receptor 6 in Rat [ChEMBL: CHEMBL3842] [GtoPdb: 294] [UniProtKB: P35349]
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  • mGlu8 receptor/Metabotropic glutamate receptor 8 in Human [ChEMBL: CHEMBL3228] [GtoPdb: 296] [UniProtKB: O00222]
  • mGlu8 receptor/Metabotropic glutamate receptor 8 in Rat [ChEMBL: CHEMBL2718] [GtoPdb: 296] [UniProtKB: P70579]
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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 B 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 B 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 B 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 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]