argiotoxin [Ligand Id: 4138] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1098240 (Argiotoxin-636) |
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| 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: 455, 456] [UniProtKB: P35439, Q00959] | ||||||||
| 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: 444, 445] [UniProtKB: P42261, P42262] | ||||||||
| 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 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]
