mexiletine [Ligand Id: 2629] 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: CHEMBL558 (Dl-mexiletine, Mexiletina, Mexiletine, (rs)-mexiletine)
There should be some charts here, you may need to enable JavaScript!
  • K2P3.1/Potassium channel subfamily K member 3 in Human [ChEMBL: CHEMBL2321613] [GtoPdb: 515] [UniProtKB: O14649]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
There should be some charts here, you may need to enable JavaScript!
  • Nav1.2/Sodium channel protein type II alpha subunit in Human [ChEMBL: CHEMBL4187] [GtoPdb: 579] [UniProtKB: Q99250]
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]
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]
There should be some charts here, you may need to enable JavaScript!
  • Nav1.8/Sodium channel protein type X alpha subunit in Human [ChEMBL: CHEMBL5451] [GtoPdb: 585] [UniProtKB: Q9Y5Y9]
  • Nav1.8/Sodium channel protein type X alpha subunit in Rat [ChEMBL: CHEMBL4017] [GtoPdb: 585] [UniProtKB: Q62968]
There should be some charts here, you may need to enable JavaScript!
  • Nav1.4 in Human [GtoPdb: 581] [UniProtKB: P35499]
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
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG B 5 pIC50 10000 nM IC50 Eur J Med Chem (2011) 46: 618-630 [PMID:21185626]
ChEMBL Inhibition of hERG K channel F 5 pIC50 >10000 nM IC50 Cardiovasc Res (2011) 91: 53-61 [PMID:21300721]
K2P3.1/Potassium channel subfamily K member 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2321613] [GtoPdb: 515] [UniProtKB: O14649]
ChEMBL Inhibition of of TASK1 (unknown origin) expressed in CHO cells assessed as reduction in channel currents B 4.01 pIC50 97300 nM IC50 J Med Chem (2016) 59: 5149-5157 [PMID:26588045]
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 6.14 pKi 724 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 5.94 pIC50 1138 nM IC50 DrugMatrix in vitro pharmacology data
Nav1.2/Sodium channel protein type II alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4187] [GtoPdb: 579] [UniProtKB: Q99250]
ChEMBL Inhibition of human recombinant Nav1.2 channel expressed in HEK293 cells by whole cell voltage clamp technique B 5.54 pIC50 2900 nM IC50 Bioorg Med Chem (2008) 16: 6379-6386 [PMID:18501613]
Nav1.7/Sodium channel protein type IX alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4296] [GtoPdb: 584] [UniProtKB: Q15858]
ChEMBL Binding affinity to inactivated human sodium channel Nav1.7 expressed in human HEK293 cells by patch-clamp electrophysiological assay B 4.89 pKi 13000 nM Ki J Med Chem (2011) 54: 4427-4445 [PMID:21634377]
ChEMBL Antagonist activity at 20% inactivated human sodium channel Nav1.7 expressed in human HEK293 cells by patch-clamp electrophysiological assay F 1.25 pIC50 56000000 nM IC50 Bioorg Med Chem Lett (2012) 22: 1055-1060 [PMID:22209205]
ChEMBL Inhibition of 20% inactivated human sodium channel Nav1.7 expressed in human HEK293 cells by patch-clamp electrophysiological assay B 4.25 pIC50 56000 nM IC50 J Med Chem (2011) 54: 4427-4445 [PMID:21634377]
ChEMBL Blockade of human Nav1.7 channel expressed in HEK293 cells by FRET assay B 4.96 pIC50 11000 nM IC50 Bioorg Med Chem Lett (2008) 18: 1696-1701 [PMID:18243692]
ChEMBL Inhibition of human Nav1.7 in inactivated condition by automated patch-clamp assay B 5.13 pIC50 7400 nM IC50 RSC Med Chem (2022) 13: 895-920 [PMID:36092147]
Nav1.5/Sodium channel protein type V alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
ChEMBL Blockade of human full-length NaV1.5 expressed in HEK293 cells co-transfected with pCD8-IRES-hbeta1 assessed as 10 Hz of use-dependent-induced channel current at -120 mV holding potential after 36 to 72 hrs by patch clamp assay B 4.24 pIC50 58000 nM IC50 J Med Chem (2012) 55: 1418-1422 [PMID:22191686]
ChEMBL Inhibition of human Nav1.5 in inactivated condition by automated patch-clamp assay B 4.82 pIC50 15000 nM IC50 RSC Med Chem (2022) 13: 895-920 [PMID:36092147]
ChEMBL Inhibition of human recombinant Nav1.5 channel expressed in HEK293 cells by whole cell voltage clamp technique B 4.89 pIC50 13000 nM IC50 Bioorg Med Chem (2008) 16: 6379-6386 [PMID:18501613]
ChEMBL Inhibition of Nav1.5 (unknown origin)-mediated late channel current B 5.52 pIC50 3000 nM IC50 Bioorg Med Chem Lett (2021) 45: 128133-128133 [PMID:34044121]
Nav1.8/Sodium channel protein type X alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5451] [GtoPdb: 585] [UniProtKB: Q9Y5Y9]
ChEMBL Inhibition of human recombinant Nav1.8 channel expressed in HEK293 cells by whole cell voltage clamp technique B 4.25 pIC50 56000 nM IC50 Bioorg Med Chem (2008) 16: 6379-6386 [PMID:18501613]
Nav1.8/Sodium channel protein type X alpha subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4017] [GtoPdb: 585] [UniProtKB: Q62968]
ChEMBL Blockade of Nav1.8 channel in rat dorsal root ganglion neurons assessed as inhibition of TTX-R current by whole cell patch clamp technique B 4.51 pIC50 31000 nM IC50 Bioorg Med Chem (2008) 16: 6379-6386 [PMID:18501613]
ChEMBL Inhibition of Nav1.8 channel in rat dorsal root ganglion neurons assessed as blockade of TTX-R current by patch clamp method B 4.52 pIC50 >30000 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 8520-8525 [PMID:17483457]
Nav1.4 in Human [GtoPdb: 581] [UniProtKB: P35499]
GtoPdb - - 3.4 pIC50 - - - J Physiol (Lond.) (2004) 554: 621-33 [PMID:14608007]

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]