argiotoxin [Ligand Id: 4138] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL1098240 (Argiotoxin-636)
There should be some charts here, you may need to enable JavaScript!
  • GluN2A/Glutamate [NMDA] receptor subunit epsilon 1 in Rat [ChEMBL: CHEMBL310] [GtoPdb: 456] [UniProtKB: Q00959]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • GluA1/Glutamate receptor ionotropic, AMPA 1 in Human [ChEMBL: CHEMBL2009] [GtoPdb: 444] [UniProtKB: P42261]
  • GluA1/Glutamate receptor ionotropic, AMPA 1 in Rat [ChEMBL: CHEMBL3753] [GtoPdb: 444] [UniProtKB: P19490]
There should be some charts here, you may need to enable JavaScript!
  • GluA3/Glutamate receptor ionotropic, AMPA 3 in Human [ChEMBL: CHEMBL3595] [GtoPdb: 446] [UniProtKB: P42263]
There should be some charts here, you may need to enable JavaScript!
  • GluA4/Glutamate receptor ionotropic, AMPA 4 in Human [ChEMBL: CHEMBL3190] [GtoPdb: 447] [UniProtKB: P48058]
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GluN1/GluN2A/Glutamate NMDA receptor; Grin1/Grin2a in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096680] [GtoPdb: 455456] [UniProtKB: P35439Q00959]
ChEMBL Inhibition of rat GluN1/2A expressed in xenopus laevis oocytes assessed as inhibition of glycine-evoked current at membrane potential of -60 mV by voltage-clamp electrophysiology B 7.13 pIC50 74 nM IC50 J. Nat. Prod. (2011) 74: 483-486 [PMID:21188966]
ChEMBL Inhibition of rat GluN1/2A receptor expressed in Xenopus laevis oocyte assessed as glutamate and glycine-induced current at holding potentials from -80 to -40 mV by two electrode voltage clamp analysis B 8 pIC50 10 nM IC50 J. Med. Chem. (2013) 56: 1171-1181 [PMID:23320429]
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 6.75 pIC50 177 nM IC50 J. Med. Chem. (2012) 55: 10297-10301 [PMID:23092360]
GluA1/GluA2/Glutamate receptor AMPA 1/2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3883294] [GtoPdb: 444445] [UniProtKB: P42261P42262]
ChEMBL Inhibition of recombinant GluA1A2 receptor flip isoform expressed in Xenopus oocytes assessed as inhibition of 100 uM kainate-induced current by patch clamp electrophysiological assay B 5.26 pIC50 5500 nM IC50 Bioorg. Med. Chem. (2010) 18: 1381-1387 [PMID:20096591]
GluA1/Glutamate receptor ionotropic, AMPA 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2009] [GtoPdb: 444] [UniProtKB: P42261]
ChEMBL Activity at recombinant GluA1 receptor flop isoform expressed in Xenopus oocytes assessed as effect of 100 uM kainate-induced current by patch clamp electrophysiological assay B 5.47 pIC50 3400 nM IC50 Bioorg. Med. Chem. (2010) 18: 1381-1387 [PMID:20096591]
ChEMBL Inhibition of recombinant GluA1 receptor flip isoform expressed in Xenopus oocytes assessed as inhibition of 100 uM kainate-induced current by patch clamp electrophysiological assay B 6.46 pIC50 350 nM IC50 Bioorg. Med. Chem. (2010) 18: 1381-1387 [PMID:20096591]
ChEMBL Inhibition of GluA1 receptor expressed in Xenopus oocytes assessed as inhibition of 100 uM kainate-induced current by patch clamp electrophysiological assay B 6.46 pIC50 350 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 Inhibition of rat recombinant GluA1 receptor flop isoform expressed in Xenopus oocytes assessed as inhibition of 100 uM kainate-induced current B 5.47 pIC50 3400 nM IC50 Bioorg. Med. Chem. (2010) 18: 1381-1387 [PMID:20096591]
ChEMBL Antagonist activity at rat GluA1 receptor expressed in Xenopus oocytes at membrane potential -60 mV by two-electrode voltage-clamp electrophysiology assay F 6.87 pIC50 135 nM IC50 J. Med. Chem. (2012) 55: 10297-10301 [PMID:23092360]
ChEMBL Inhibition of rat GluA1 expressed in xenopus laevis oocytes assessed as inhibition of glutamate-evoked current at membrane potential of -60 mV by voltage-clamp electrophysiology B 7.11 pIC50 77 nM IC50 J. Nat. Prod. (2011) 74: 483-486 [PMID:21188966]
ChEMBL Inhibition of rat GluA1 receptor flip form expressed in Xenopus laevis oocyte assessed as glutamate-induced current at holding potentials from -80 to -40 mV by two electrode voltage clamp analysis B 7.11 pIC50 77 nM IC50 J. Med. Chem. (2013) 56: 1171-1181 [PMID:23320429]
GluA3/Glutamate receptor ionotropic, AMPA 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3595] [GtoPdb: 446] [UniProtKB: P42263]
ChEMBL Inhibition of recombinant GluA3 receptor flip isoform expressed in Xenopus oocytes assessed as inhibition of 100 uM kainate-induced current by patch clamp electrophysiological assay B 6.64 pIC50 230 nM IC50 Bioorg. Med. Chem. (2010) 18: 1381-1387 [PMID:20096591]
ChEMBL Inhibition of GluA3 receptor expressed in Xenopus oocytes assessed as inhibition of 100 uM kainate-induced current by patch clamp electrophysiological assay B 6.64 pIC50 230 nM IC50 Bioorg. Med. Chem. (2010) 18: 1381-1387 [PMID:20096591]
GluA4/Glutamate receptor ionotropic, AMPA 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3190] [GtoPdb: 447] [UniProtKB: P48058]
ChEMBL Inhibition of GluA4 receptor expressed in Xenopus oocytes assessed as inhibition of 100 uM kainate-induced current by patch clamp electrophysiological assay B 6.37 pIC50 430 nM IC50 Bioorg. Med. Chem. (2010) 18: 1381-1387 [PMID:20096591]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]