[3H]UBP310 [Ligand Id: 4092] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL373428
  • GluA2/Glutamate receptor ionotropic, AMPA 2 in Human [ChEMBL: CHEMBL4016] [GtoPdb: 445] [UniProtKB: P42262]
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  • GluK1 in Human [GtoPdb: 450] [UniProtKB: P39086]
  • GluK1/Glutamate receptor ionotropic kainate 1 in Rat [ChEMBL: CHEMBL2919] [GtoPdb: 450] [UniProtKB: P22756]
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  • GluK2/Glutamate receptor ionotropic kainate 2 in Human [ChEMBL: CHEMBL3683] [GtoPdb: 451] [UniProtKB: Q13002]
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  • GluK3 in Human [GtoPdb: 452] [UniProtKB: Q13003]
  • GluK3/Glutamate receptor ionotropic kainate 3 in Rat [ChEMBL: CHEMBL3744] [GtoPdb: 452] [UniProtKB: P42264]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GluA2/Glutamate receptor ionotropic, AMPA 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4016] [GtoPdb: 445] [UniProtKB: P42262]
ChEMBL Antagonist activity at human recombinant GLUA2-AMPA receptor expressed in HEK293 cells assessed as inhibition of glutamate-stimulated calcium influx by FLIPR assay F 4 pIC50 >100000 nM IC50 J Med Chem (2007) 50: 1558-1570 [PMID:17348638]
GluK1 in Human [GtoPdb: 450] [UniProtKB: P39086]
GtoPdb - - 7.7 pKd 21 nM Kd Mol Pharmacol (2010) 78: 1036-45 [PMID:20837679]
GluK1/Glutamate receptor ionotropic kainate 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2919] [GtoPdb: 450] [UniProtKB: P22756]
ChEMBL Activity at native GLUK5 kainate receptor assessed as antagonism of kainite-induced depolarization of neonatal anaesthetised rat dorsal root fibres F 7.74 pKd 18 nM Kd J Med Chem (2007) 50: 1558-1570 [PMID:17348638]
GluK2/Glutamate receptor ionotropic kainate 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3683] [GtoPdb: 451] [UniProtKB: Q13002]
ChEMBL Antagonist activity at human recombinant GLUK6 expressed in HEK293 cells assessed as inhibition of glutamate-stimulated calcium influx by FLIPR assay F 4 pIC50 >100000 nM IC50 J Med Chem (2007) 50: 1558-1570 [PMID:17348638]
GluK3 in Human [GtoPdb: 452] [UniProtKB: Q13003]
GtoPdb - - 6.3 pKd 560 nM Kd Mol Pharmacol (2010) 78: 1036-45 [PMID:20837679]
GluK3/Glutamate receptor ionotropic kainate 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3744] [GtoPdb: 452] [UniProtKB: P42264]
ChEMBL Displacement of [3H]SYM2081 from rat GluK3 expressed in Sf9 cells B 7.64 pKi 23 nM Ki J Med Chem (2011) 54: 4793-4805 [PMID:21619066]

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]