agatoxin 489 [Ligand Id: 2484] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3286869
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  • GluA1/Glutamate receptor ionotropic, AMPA 1 in Rat [ChEMBL: CHEMBL3753] [GtoPdb: 444] [UniProtKB: P19490]
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  • TRPV1 in Rat [GtoPdb: 507] [UniProtKB: O35433]
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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: 455456] [UniProtKB: P35439Q00959]
ChEMBL Inhibition of rat recombinant GluN1/2A expressed in Xenopus oocytes assessed as inhibition of glutamate/glycine-evoked channel current at holding potential of -80 mV by two-electrode voltage clamp technique B 7.92 pIC50 12 nM IC50 J Med Chem (2014) 57: 4940-4949 [PMID:24824658]
GluA1/Glutamate receptor ionotropic, AMPA 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3753] [GtoPdb: 444] [UniProtKB: P19490]
ChEMBL Inhibition of rat recombinant GluA1 expressed in Xenopus oocytes assessed as inhibition of glutamate-induced channel current at holding potential of -80 mV by two-electrode voltage clamp technique B 7.96 pIC50 11 nM IC50 J Med Chem (2014) 57: 4940-4949 [PMID:24824658]
TRPV1 in Rat [GtoPdb: 507] [UniProtKB: O35433]
GtoPdb - - 6.5 pKi - - - Biochemistry (2005) 44: 15544-9 [PMID:16300403]

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]