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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL79 (ALGRX 3268, ALGRX-3268, Alphacaine, Anestacon, Dentipatch, Embolex, Iontocaine, Lidocaina, 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]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • Nav1.5/Sodium channel protein type V alpha subunit in Human [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
  • Nav1.5 in Rat [GtoPdb: 582] [UniProtKB: P15389]
There should be some charts here, you may need to enable JavaScript!
  • Nav1.2 in Rat [GtoPdb: 579] [UniProtKB: P04775]
There should be some charts here, you may need to enable JavaScript!
  • Nav1.8 in Rat [GtoPdb: 585] [UniProtKB: Q62968]
There should be some charts here, you may need to enable JavaScript!
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]
ChEMBL Inhibition of human Nav1.7 in inactivated condition by automated patch-clamp assay B 4.8 pIC50 16000 nM IC50 RSC Med Chem (2022) 13: 895-920 [PMID:36092147]
Nav1.7 in Rat [GtoPdb: 584] [UniProtKB: O08562]
GtoPdb - - 3.3 pIC50 - - - Br J Pharmacol (2004) 142: 576-84 [PMID:15148257]
Nav1.5/Sodium channel protein type V alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
GtoPdb - - 4.8 pKd - - - J Gen Physiol (1995) 106: 1193-209 [PMID:8786356]
ChEMBL Inhibition of human Nav1.5 in inactivated condition by automated patch-clamp assay B 4.3 pIC50 50000 nM IC50 RSC Med Chem (2022) 13: 895-920 [PMID:36092147]
Nav1.5 in Rat [GtoPdb: 582] [UniProtKB: P15389]
GtoPdb - - 4.2 pIC50 - - - Mol Pharmacol (1989) 36: 150-9 [PMID:2546048]
Nav1.2 in Rat [GtoPdb: 579] [UniProtKB: P04775]
GtoPdb - - 5 pIC50 - - - Proc Natl Acad Sci USA (1996) 93: 9270-5 [PMID:8799190]
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 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]