Target Validation Information
Target ID T39716
Target Name Sodium channel protein type 5 subunit alpha
Target Type
Successful
Drug Potency against Target Mexiletine Drug Info IC50 = 130000 nM [552567]
N-Butyl-N'-(4-methyl-benzoyl)-guanidine Drug Info IC50 = 9000 nM [526204]
NS-7 Drug Info IC50 = 1000 nM [525961]
Quinine Drug Info Ki = 43 nM [552597]
Indol-1-yl-propyl-pyridin-4-yl-amine Drug Info IC50 = 5500 nM [525961]
LUBELUZOLE Drug Info IC50 = 280 nM [525961]
Disopyramide Drug Info Ki = 2700 nM [552838]
PD-85639 Drug Info IC50 = 46 nM [525961]
LOMERIZINE Drug Info IC50 = 26 nM [525961]
N-(4-Methyl-benzoyl)-N'-phenethyl-guanidine Drug Info IC50 = 5650 nM [526204]
1-[5-(4-Chlorophenyl)-2-furoyl]piperazine Drug Info IC50 = 4600 nM [529491]
SIPATRIGINE Drug Info IC50 = 5300 nM [525961]
Action against Disease Model Procainamide The 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. [552484] Drug Info
References
Ref 552567Analysis of human Nav1.8 expressed in SH-SY5Y neuroblastoma cells. Eur J Pharmacol. 2005 Dec 28;528(1-3):52-8. Epub 2005 Dec 2.
Ref 526204Bioorg 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.
Ref 525961J Med Chem. 2001 Jan 18;44(2):115-37.Medicinal chemistry of neuronal voltage-gated sodium channel blockers.
Ref 552597Development and validation of an in silico P450 profiler based on pharmacophore models. Curr Drug Discov Technol. 2006 Mar;3(1):1-48.
Ref 525961J Med Chem. 2001 Jan 18;44(2):115-37.Medicinal chemistry of neuronal voltage-gated sodium channel blockers.
Ref 552484Transport of the dopamine D2 agonist pramipexole by rat organic cation transporters OCT1 and OCT2 in kidney. Drug Metab Dispos. 2005 Apr;33(4):495-9. Epub 2005 Jan 7.
Ref 525961J Med Chem. 2001 Jan 18;44(2):115-37.Medicinal chemistry of neuronal voltage-gated sodium channel blockers.
Ref 552838Drug target identification using side-effect similarity. Science. 2008 Jul 11;321(5886):263-6. doi: 10.1126/science.1158140.
Ref 525961J Med Chem. 2001 Jan 18;44(2):115-37.Medicinal chemistry of neuronal voltage-gated sodium channel blockers.
Ref 525961J Med Chem. 2001 Jan 18;44(2):115-37.Medicinal chemistry of neuronal voltage-gated sodium channel blockers.
Ref 526204Bioorg 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.
Ref 529491Bioorg 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.
Ref 525961J Med Chem. 2001 Jan 18;44(2):115-37.Medicinal chemistry of neuronal voltage-gated sodium channel blockers.

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