Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
 

 

Target Validation Information
TTD IDTTDS00402
Target NameSodium channel protein type 5 subunit alpha    
Type of TargetSuccessful target    
Drug Potency against TargetMexiletineIC50 = 130000 nM[1]
DisopyramideKi = 2700 nM[2]
QuinidineKi = 43 nM[3]
EnecadinIC50 = 1000 nM[4]
LOMERIZINEIC50 = 26 nM[4]
LUBELUZOLEIC50 = 280 nM[4]
PD-85639IC50 = 46 nM[4]
1-[5-(4-Chlorophenyl)-2-furoyl]piperazineIC50 = 4600 nM[5]
SIPATRIGINEIC50 = 5300 nM[4]
Indol-1-yl-propyl-pyridin-4-yl-amine(Besipirdine)IC50 = 5500 nM[4]
N-(4-Methyl-benzoyl)-N'-phenethyl-guanidineIC50 = 5650 nM[6]
N-Butyl-N'-(4-methyl-benzoyl)-guanidineIC50 = 9000 nM[6]
Action against Disease ModelProcainamideThe uptake of [14C]pramipexole by rOCT1, rOCT2, and kidney slices was inhibited by procainamide and corticosterone, which are selective inhibitors of rOCT1 and rOCT2, respectively. The IC50 values of procainamide and corticosterone for the uptake of [14C]pramipexole by rOCT1, rOCT2, and kidney slices were 7.7, 167.0, and 47.0 microM and 163.7, 10.7, and 47.7 microM, respectively. These results demonstrate that both rOCT1 and rOCT2 are involved in the renal uptake of pramipexole across the basolateral membrane of the proximal tubular epithelial cells.[7]
Ref 1Eur J Pharmacol. 2005 Dec 28;528(1-3):52-8. Epub 2005 Dec 2.Analysis of human Nav1.8 expressed in SH-SY5Y neuroblastoma cells. To Reference
Ref 2Science. 2008 Jul 11;321(5886):263-6.Drug target identification using side-effect similarity. To Reference
Ref 3Curr Drug Discov Technol. 2006 Mar;3(1):1-48.Development and validation of an in silico P450 profiler based on pharmacophore models. To Reference
Ref 4J Med Chem. 2001 Jan 18;44(2):115-37.Medicinal chemistry of neuronal voltage-gated sodium channel blockers. To Reference
Ref 5Bioorg Med Chem. 2008 Jun 15;16(12):6379-86. Epub 2008 May 6.Discovery of potent furan piperazine sodium channel blockers for treatment of neuropathic pain. To Reference
Ref 6Bioorg Med Chem Lett. 2001 Dec 17;11(24):3151-5.Solution-phase, parallel synthesis and pharmacological evaluation of acylguanidine derivatives as potential sodium channel blockers. To Reference
Ref 7Drug Metab Dispos. 2005 Apr;33(4):495-9. Epub 2005 Jan 7.Transport of the dopamine D2 agonist pramipexole by rat organic cation transporters OCT1 and OCT2 in kidney. To Reference



 

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Professor in Department of Pharmacy
National University of Singapore, Singapore


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