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 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]