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ChEMBL ligand: CHEMBL373428 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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/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/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 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]