dysiherbaine [Ligand Id: 4185] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL221142 (Dysiherbaine)
  • GluK1/Glutamate receptor ionotropic kainate 1 in Human [ChEMBL: CHEMBL1918] [GtoPdb: 450] [UniProtKB: P39086]
  • GluK1 in Rat [GtoPdb: 450] [UniProtKB: P22756]
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  • GluK2/Glutamate receptor ionotropic kainate 2 in Human [ChEMBL: CHEMBL3683] [GtoPdb: 451] [UniProtKB: Q13002]
  • GluK2 in Rat [GtoPdb: 451] [UniProtKB: P42260]
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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 Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1918] [GtoPdb: 450] [UniProtKB: P39086]
ChEMBL Displacement of [3H]kianic acid from recombinant GluK1 kainate receptor (unknown origin) expressed in HEK293 cell membranes measured after 1 hr B 9.13 pKi 0.74 nM Ki Bioorg Med Chem Lett (2016) 26: 5164-5167 [PMID:27720549]
GluK1 in Rat [GtoPdb: 450] [UniProtKB: P22756]
GtoPdb - - 9.13 pKi 0.74 nM Ki J Pharmacol Exp Ther (2001) 296: 650-8 [PMID:11160654]
GluK2/Glutamate receptor ionotropic kainate 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3683] [GtoPdb: 451] [UniProtKB: Q13002]
ChEMBL Displacement of [3H]kianic acid from recombinant GluK2 kainate receptor (unknown origin) expressed in HEK293 cell membranes measured after 1 hr B 8.92 pKi 1.2 nM Ki Bioorg Med Chem Lett (2016) 26: 5164-5167 [PMID:27720549]
GluK2 in Rat [GtoPdb: 451] [UniProtKB: P42260]
GtoPdb - - 8.92 pKi 1.2 nM Ki J Pharmacol Exp Ther (2001) 296: 650-8 [PMID:11160654]

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]