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, Lidocaina, Lidocaine, Lidocainum, Lidocaton, Lidoderm, Lidopen, Lignocaine, Lignocaine Hcl, Lignostab, Lmx 4, NSC-40030, Octocaine, Oraqix, Solarcaine, Vagisil, Xylestesin, Xylocaine, Xylodase, Xylotox, Ztlido) |
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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] |
| 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 35:
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]
