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 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]
