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 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]