UBP302 [Ligand Id: 4333] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL372797 (UBP-302)
  • GluK1/Glutamate receptor ionotropic kainate 1 in Rat [ChEMBL: CHEMBL2919] [GtoPdb: 450] [UniProtKB: P22756]
  • This target only has 0 pki data point
  • 0
1 CHEMBL372797_lig_chart_1 Glutamate receptor ionotropic kainate 1 Rat
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  • GluK3/Glutamate receptor ionotropic kainate 3 in Human [ChEMBL: CHEMBL3684] [GtoPdb: 452] [UniProtKB: Q13003]
  • This target only has 0 pki data point
  • 0
2 CHEMBL372797_lig_chart_2 Glutamate receptor ionotropic kainate 3 Human
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  • GluK5/Glutamate receptor ionotropic kainate 5 in Rat [ChEMBL: CHEMBL4041] [GtoPdb: 454] [UniProtKB: Q63273]
  • This target only has 0 pki data point
  • 0
3 CHEMBL372797_lig_chart_3 Glutamate receptor ionotropic kainate 5 Rat
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GluK1/Glutamate receptor ionotropic kainate 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2919] [GtoPdb: 450] [UniProtKB: P22756]
ChEMBL Displacement of [3H]S-glutamate from rat GluR5 S1S2 ligand binding core expressed in Escherichia coli (DE3) B 5.4 pKd 3940 nM Kd Bioorg. Med. Chem. (2009) 17: 6390-6401 [PMID:19656686]
ChEMBL Antagonism on GLUK5 containing kainate induced depolarization of isolated neonatal rat dorsal root C-fibers F 6.4 pKd 402 nM Kd J. Med. Chem. (2005) 48: 7867-7881 [PMID:16302825]
ChEMBL Activity at native GLUK5 kainate receptor assessed as antagonism of kainite-induced depolarization of neonatal anaesthetised rat dorsal root fibres F 6.4 pKd 402 nM Kd J. Med. Chem. (2007) 50: 1558-1570 [PMID:17348638]
GluK3/Glutamate receptor ionotropic kainate 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3684] [GtoPdb: 452] [UniProtKB: Q13003]
ChEMBL Antagonist activity at recombinant GluK3 receptor (unknown origin) expressed in Xenopus oocyte assessed as inhibition of glutamate-induced current amplitude by voltage-clamp method B 5.4 pIC50 4000 nM IC50 Bioorg Med Chem Lett (2016) 26: 5568-5572 [PMID:27765511]
GluK5/Glutamate receptor ionotropic kainate 5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4041] [GtoPdb: 454] [UniProtKB: Q63273]
ChEMBL Antagonist activity against GLUK5-containing kainate receptor by inhibition of kainate-induced depolarization of neonatal rat dorsal root fibers F 6.4 pKd 402 nM Kd J. Med. Chem. (2006) 49: 2579-2592 [PMID:16610801]

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]