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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) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 32:
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]