lidocaine [Ligand Id: 2623] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL79 (ALGRX 3268, ALGRX-3268, Alphacaine, Anestacon, Dentipatch, Embolex, Iontocaine, Lidocaine, Lidocainum, Lidocaton, Lidoderm, Lidopen, Lignocaine, Lignocaine Hcl, Lignostab, Lmx 4, NSC-40030, Octocaine, Oraqix, Solarcaine, Vagisil, Xylestesin, Xylocaine, Xylodase, Xylotox, Ztlido)
  • Nav1.3/Sodium channel protein type III alpha subunit in Human [ChEMBL: CHEMBL5163] [GtoPdb: 580] [UniProtKB: Q9NY46]
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  • Nav1.4/Sodium channel protein type IV alpha subunit in Human [ChEMBL: CHEMBL2072] [GtoPdb: 581] [UniProtKB: P35499]
  • Nav1.4 in Rat [GtoPdb: 581] [UniProtKB: P15390]
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  • Nav1.7/Sodium channel protein type IX alpha subunit in Human [ChEMBL: CHEMBL4296] [GtoPdb: 584] [UniProtKB: Q15858]
  • Nav1.7 in Rat [GtoPdb: 584] [UniProtKB: O08562]
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  • Nav1.2 in Rat [GtoPdb: 579] [UniProtKB: P04775]
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  • Nav1.5 in Human [GtoPdb: 582] [UniProtKB: Q14524]
  • Nav1.5 in Rat [GtoPdb: 582] [UniProtKB: P15389]
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  • Nav1.8 in Rat [GtoPdb: 585] [UniProtKB: Q62968]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Nav1.3/Sodium channel protein type III alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5163] [GtoPdb: 580] [UniProtKB: Q9NY46]
ChEMBL Modulation of human Nav1.3 in open-inactivated state assessed as inhibition of inward current after 4 mins by whole-cell electrophysiology B 4.98 pIC50 10500 nM IC50 Eur. J. Med. Chem. (2014) 74: 23-30 [PMID:24440379]
Nav1.4/Sodium channel protein type IV alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2072] [GtoPdb: 581] [UniProtKB: P35499]
ChEMBL Modulation of human Nav1.4 in open-inactivated state assessed as inhibition of inward current after 4 mins by whole-cell electrophysiology B 5.7 pIC50 2000 nM IC50 Eur. J. Med. Chem. (2014) 74: 23-30 [PMID:24440379]
Nav1.4 in Rat [GtoPdb: 581] [UniProtKB: P15390]
GtoPdb - - 2.7 pIC50 - - - Cardiovasc Res (1999) 42: 503-9 [PMID:10533585]
Nav1.7/Sodium channel protein type IX alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4296] [GtoPdb: 584] [UniProtKB: Q15858]
ChEMBL Modulation of human Nav1.7 in open-inactivated state assessed as inhibition of inward current after 4 mins by whole-cell electrophysiology B 4.54 pIC50 29000 nM IC50 Eur. J. Med. Chem. (2014) 74: 23-30 [PMID:24440379]
Nav1.7 in Rat [GtoPdb: 584] [UniProtKB: O08562]
GtoPdb - - 3.3 pIC50 - - - Br J Pharmacol (2004) 142: 576-84 [PMID:15148257]
Nav1.2 in Rat [GtoPdb: 579] [UniProtKB: P04775]
GtoPdb - - 5 pIC50 - - - Proc Natl Acad Sci USA (1996) 93: 9270-5 [PMID:8799190]
Nav1.5 in Human [GtoPdb: 582] [UniProtKB: Q14524]
GtoPdb - - 4.8 pKd - - - J Gen Physiol (1995) 106: 1193-209 [PMID:8786356]
Nav1.5 in Rat [GtoPdb: 582] [UniProtKB: P15389]
GtoPdb - - 4.2 pIC50 - - - Mol Pharmacol (1989) 36: 150-9 [PMID:2546048]
Nav1.8 in Rat [GtoPdb: 585] [UniProtKB: Q62968]
GtoPdb - - 4 pIC50 - - - Gan To Kagaku Ryoho (1992) 19: 1136-8 [PMID:1514825]

ChEMBL data shown on this page come from version 31:

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]