domoic acid [Ligand Id: 4181] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1232313
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  • GluK1/Glutamate receptor ionotropic, kainate 1 in Human [ChEMBL: CHEMBL1918] [GtoPdb: 450] [UniProtKB: P39086]
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  • GluK2/Glutamate receptor ionotropic, kainate 2 in Human [ChEMBL: CHEMBL3683] [GtoPdb: 451] [UniProtKB: Q13002]
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  • GluK3/Glutamate receptor ionotropic, kainate 3 in Human [ChEMBL: CHEMBL3684] [GtoPdb: 452] [UniProtKB: Q13003]
  • GluK3 in Rat [GtoPdb: 452] [UniProtKB: P42264]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GluA4/Glutamate receptor 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3505] [GtoPdb: 447] [UniProtKB: P19493]
ChEMBL Binding affinity to AMPA receptor in rat synaptosomes B 5.05 pIC50 9000 nM IC50 J Med Chem (2024) 67: 14524-14542 [PMID:39133077]
ChEMBL Displacement of [3H]-AMPA from AMPA in rat synaptic membrane B 6.33 pIC50 470 nM IC50 J Med Chem (2024) 67: 14524-14542 [PMID:39133077]
GluK1/Glutamate receptor ionotropic, kainate 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1918] [GtoPdb: 450] [UniProtKB: P39086]
ChEMBL Displacement of [3H](2S, 4R)-4-MeGlu (SYM-2081) from GluK1 (unknown origin) B 8.95 pKi 1.11 nM Ki J Med Chem (2024) 67: 14524-14542 [PMID:39133077]
GluK2/Glutamate receptor ionotropic, kainate 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3683] [GtoPdb: 451] [UniProtKB: Q13002]
GtoPdb Measuring displacement of [3H]Kainate binding by domoate. - 7.74 pKi 18.3 nM Ki J Med Chem (1996) 39: 3617-24 [PMID:8809152]
ChEMBL Displacement of [3H](2S, 4R)-4-MeGlu (SYM-2081) from GluK2 (unknown origin) B 8.22 pKi 6.04 nM Ki J Med Chem (2024) 67: 14524-14542 [PMID:39133077]
GluK3/Glutamate receptor ionotropic, kainate 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3684] [GtoPdb: 452] [UniProtKB: Q13003]
ChEMBL Displacement of [3H](2S, 4R)-4-MeGlu (SYM-2081) from GluK3 (unknown origin) B 8.32 pKi 4.84 nM Ki J Med Chem (2024) 67: 14524-14542 [PMID:39133077]
GluK3 in Rat [GtoPdb: 452] [UniProtKB: P42264]
GtoPdb - - 8.42 pKi 3.84 nM Ki J Med Chem (2008) 51: 4093-103 [PMID:18578478]

ChEMBL data shown on this page come from version 36:

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]