GYKI53655 [Ligand Id: 4209] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL267450 (GYKI-53655)
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  • 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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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GluA1/GluA2/GluA3/GluA4/Glutamate receptor ionotropic, AMPA in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2093871] [GtoPdb: 444, 445, 446, 447] [UniProtKB: P19490, P19491, P19492, P19493]
ChEMBL Inhibitory activity against AMPA receptor currents in rat cortical cells stimulated with 50 uM kainic acid F 6 pIC50 1000 nM IC50 J Med Chem (1996) 39: 343-346 [PMID:8558499]
GluA1/Glutamate receptor ionotropic, AMPA 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2009] [GtoPdb: 444] [UniProtKB: P42261]
ChEMBL Activity at recombinant GluA1 receptor flip isoform expressed in Xenopus oocytes co-expressing gamma2-TARP assessed as effect on glutamate/trichloromethiazide-induced current B 4.55 pEC50 28000 nM EC50 Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591]
GluA2/Glutamate receptor ionotropic, AMPA 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4016] [GtoPdb: 445] [UniProtKB: P42262]
ChEMBL Activity at recombinant GluA2 receptor flip isoform expressed in Xenopus oocytes co-expressing gamma2-TARP assessed as effect on glutamate/trichloromethiazide-induced current B 4 pEC50 100000 nM EC50 Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591]

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]