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 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]