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ChEMBL ligand: CHEMBL313747 (Joro Spider Toxin 3) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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GluN2A/Glutamate [NMDA] receptor subunit epsilon 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL310] [GtoPdb: 456] [UniProtKB: Q00959] | ||||||||
ChEMBL | Antagonist activity at rat glutamate N1/2A receptor expressed in Xenopus oocytes at membrane potential -60 mV by two-electrode voltage-clamp electrophysiology assay | F | 5.77 | pIC50 | 1710 | nM | IC50 | J Med Chem (2012) 55: 10297-10301 [PMID:23092360] |
GluA1/Glutamate receptor ionotropic, AMPA 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2009] [GtoPdb: 444] [UniProtKB: P42261] | ||||||||
ChEMBL | Inhibition of recombinant GluA1 receptor flop isoform expressed in Xenopus oocytes assessed as inhibition of 300 uM kainate-induced current by patch clamp electrophysiological assay | B | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
GluA1/Glutamate receptor ionotropic, AMPA 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3753] [GtoPdb: 444] [UniProtKB: P19490] | ||||||||
ChEMBL | Antagonist activity at rat GluA1 receptor expressed in Xenopus oocytes at membrane potential -60 mV by two-electrode voltage-clamp electrophysiology assay | F | 7.19 | pIC50 | 65 | nM | IC50 | J Med Chem (2012) 55: 10297-10301 [PMID:23092360] |
GluA3/Glutamate receptor ionotropic, AMPA 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3595] [GtoPdb: 446] [UniProtKB: P42263] | ||||||||
ChEMBL | Inhibition of recombinant GluA3 receptor flop isoform expressed in Xenopus oocytes assessed as inhibition of 300 uM kainate-induced current by patch clamp electrophysiological assay | B | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem (2010) 18: 1381-1387 [PMID:20096591] |
GluK1/Glutamate receptor ionotropic kainate 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2919] [GtoPdb: 450] [UniProtKB: P22756] | ||||||||
ChEMBL | Antagonist activity at rat GluK1 receptor expressed in Xenopus oocytes at membrane potential -60 mV by two-electrode voltage-clamp electrophysiology assay | F | 7.72 | pIC50 | 19 | nM | IC50 | J Med Chem (2012) 55: 10297-10301 [PMID:23092360] |
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]