LY404187 [Ligand Id: 4249] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL435582
  • GluA1/Glutamate receptor ionotropic, AMPA 1 in Human [ChEMBL: CHEMBL2009] [GtoPdb: 444] [UniProtKB: P42261]
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  • GluA2/Glutamate receptor ionotropic, AMPA 2 in Human [ChEMBL: CHEMBL4016] [GtoPdb: 445] [UniProtKB: P42262]
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  • GluA3/Glutamate receptor ionotropic, AMPA 3 in Human [ChEMBL: CHEMBL3595] [GtoPdb: 446] [UniProtKB: P42263]
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  • GluA4/Glutamate receptor ionotropic, AMPA 4 in Human [ChEMBL: CHEMBL3190] [GtoPdb: 447] [UniProtKB: P48058]
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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 Inhibition of GluR1 expressed in HEK cells B 5.25 pEC50 5650 nM EC50 J. Med. Chem. (2010) 53: 7271-7279 [PMID:20839777]
GtoPdb - - 5.25 pEC50 5650 nM EC50 Neuropharmacology (2001) 40: 976-83 [PMID:11406188]
GluA2/Glutamate receptor ionotropic, AMPA 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4016] [GtoPdb: 445] [UniProtKB: P42262]
ChEMBL Activity against human GLUR2 flop expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay F 5.72 pEC50 1905 nM EC50 Bioorg. Med. Chem. Lett. (2006) 16: 5057-5061 [PMID:16879964]
ChEMBL Inhibition of GluR2 flop expressed in HEK cells B 5.84 pEC50 1440 nM EC50 J. Med. Chem. (2010) 53: 7271-7279 [PMID:20839777]
ChEMBL Activity against human GLUR2 flip expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay F 6.25 pEC50 559 nM EC50 Bioorg. Med. Chem. Lett. (2006) 16: 5057-5061 [PMID:16879964]
GtoPdb - - 6.82 pEC50 150 nM EC50 Neuropharmacology (2001) 40: 976-83 [PMID:11406188]
ChEMBL Agonist activity at GluR2 receptor F 6.82 pEC50 150 nM EC50 J. Med. Chem. (2010) 53: 7271-7279 [PMID:20839777]
GluA3/Glutamate receptor ionotropic, AMPA 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3595] [GtoPdb: 446] [UniProtKB: P42263]
ChEMBL Inhibition of GluR3 expressed in HEK cells B 5.78 pEC50 1660 nM EC50 J. Med. Chem. (2010) 53: 7271-7279 [PMID:20839777]
GtoPdb - - 5.78 pEC50 1660 nM EC50 Neuropharmacology (2001) 40: 976-83 [PMID:11406188]
GluA4/Glutamate receptor ionotropic, AMPA 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3190] [GtoPdb: 447] [UniProtKB: P48058]
ChEMBL Activity against human GLUR4 flop expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay F 5.97 pEC50 1061 nM EC50 Bioorg. Med. Chem. Lett. (2006) 16: 5057-5061 [PMID:16879964]
ChEMBL Activity against human GLUR4 flip expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay F 6.38 pEC50 420 nM EC50 Bioorg. Med. Chem. Lett. (2006) 16: 5057-5061 [PMID:16879964]
ChEMBL Tested for potentiation towards human iGluR4 receptor expressed in HEK293 cells F 6.54 pEC50 290 nM EC50 J. Med. Chem. (2000) 43: 4354-4358 [PMID:11087558]
ChEMBL Potentiation of responses mediated by 100 uM L-glutamate in transfected HEK293 cells expressing human homomeric iGluR4 flip receptors. F 6.54 pEC50 290 nM EC50 J. Med. Chem. (2002) 45: 2101-2111 [PMID:11985477]
ChEMBL Inhibition of GluR4 expressed in HEK293 cells B 6.54 pEC50 290 nM EC50 J. Med. Chem. (2010) 53: 7271-7279 [PMID:20839777]
GtoPdb - - 6.68 pEC50 210 nM EC50 Neuropharmacology (2001) 40: 976-83 [PMID:11406188]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]