[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]
  • This target only has 0 pki data point
  • 0
1 CHEMBL373428_lig_chart_1 Glutamate receptor ionotropic, AMPA 2 Human
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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]
  • This target only has 0 pki data point
  • 0
2 CHEMBL373428_lig_chart_2 GluK1 HumanRat
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  • GluK2/Glutamate receptor ionotropic kainate 2 in Human [ChEMBL: CHEMBL3683] [GtoPdb: 451] [UniProtKB: Q13002]
  • This target only has 0 pki data point
  • 0
3 CHEMBL373428_lig_chart_3 Glutamate receptor ionotropic kainate 2 Human
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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]
  • This target only has 1 pki data point
  • 7.64
4 CHEMBL373428_lig_chart_4 GluK3 HumanRat
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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 28:

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]