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

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ChEMBL ligand: CHEMBL3286869
  • GluN1/GluN2A/Glutamate NMDA receptor; Grin1/Grin2a in Rat [ChEMBL: CHEMBL2096680] [GtoPdb: 455456] [UniProtKB: P35439Q00959]
  • This target only has 0 pki data point
  • 0
1 CHEMBL3286869_lig_chart_1 Glutamate NMDA receptor; Grin1/Grin2a Rat
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  • GluA1/Glutamate receptor ionotropic, AMPA 1 in Rat [ChEMBL: CHEMBL3753] [GtoPdb: 444] [UniProtKB: P19490]
  • This target only has 0 pki data point
  • 0
2 CHEMBL3286869_lig_chart_2 Glutamate receptor ionotropic, AMPA 1 Rat
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  • TRPV1 in Rat [GtoPdb: 507] [UniProtKB: O35433]
  • This target only has 1 pki data point
  • 6.5
3 CHEMBL3286869_lig_chart_3 TRPV1 Rat
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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 28:

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]