perampanel [Ligand Id: 7050] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1214124 (E2007, E-2007, ER-155055-90, Fycompa, Perampanel)
  • GluA1/Glutamate receptor ionotropic, AMPA 1 in Human [ChEMBL: CHEMBL2009] [GtoPdb: 444] [UniProtKB: P42261]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GluA1/Glutamate receptor ionotropic, AMPA 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2009] [GtoPdb: 444] [UniProtKB: P42261]
ChEMBL Antagonist activity at human iGluA1 receptor flip isoform expressed in CHO-S cells assessed as inhibition of glutamate-induced increase in intracellular calcium levels after 2 mins followed by cyclothiazide/glutamate addition by fluo-4 NW dye based fluorescence imaging plate reader method B 5.19 pIC50 6510 nM IC50 J. Med. Chem. (2016) 59: 4753-4768 [PMID:27067148]
ChEMBL Antagonist activity at human iGluA1 receptor flop isoform expressed in CHO-S cells coexpressing TARP gamma-8 and human EAAT3 assessed as inhibition of glutamate-induced increase in intracellular calcium levels after 2 mins followed by cyclothiazide/glutamate addition by fluo-4 AM dye based fluorescence imaging plate reader method B 5.93 pIC50 1180 nM IC50 J. Med. Chem. (2016) 59: 4753-4768 [PMID:27067148]
ChEMBL Antagonist activity at human iGluA1 receptor flop isoform expressed in CHO-S cells coexpressing TARP gamma-4 assessed as inhibition of glutamate-induced increase in intracellular calcium levels after 2 mins followed by cyclothiazide/glutamate addition by fluorescence imaging plate reader method B 6.21 pIC50 623 nM IC50 J. Med. Chem. (2016) 59: 4753-4768 [PMID:27067148]
ChEMBL Antagonist activity at human iGluA1 receptor flop isoform expressed in CHO-S cells coexpressing TARP gamma-2 assessed as inhibition of glutamate-induced increase in intracellular calcium levels after 2 mins followed by cyclothiazide/glutamate addition by fluo-4 AM dye based fluorescence imaging plate reader method B 6.31 pIC50 485 nM IC50 J. Med. Chem. (2016) 59: 4753-4768 [PMID:27067148]
ChEMBL Antagonist activity at human iGluA1 receptor flop isoform expressed in CHO-S cells coexpressing TARP gamma-3 assessed as inhibition of glutamate-induced increase in intracellular calcium levels after 2 mins followed by cyclothiazide/glutamate addition by fluorescence imaging plate reader method B 6.61 pIC50 243 nM IC50 J. Med. Chem. (2016) 59: 4753-4768 [PMID:27067148]

ChEMBL data shown on this page come from version 31:

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]