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, Mexiletine, (rs)-mexiletine) |
|---|
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
|
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 | 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] |
| 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 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 33:
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]
