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 552567 | Analysis 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 526204 | Bioorg 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 525961 | J Med Chem. 2001 Jan 18;44(2):115-37.Medicinal chemistry of neuronal voltage-gated sodium channel blockers. | ||||
Ref 552597 | Development and validation of an in silico P450 profiler based on pharmacophore models. Curr Drug Discov Technol. 2006 Mar;3(1):1-48. | ||||
Ref 525961 | J Med Chem. 2001 Jan 18;44(2):115-37.Medicinal chemistry of neuronal voltage-gated sodium channel blockers. | ||||
Ref 552484 | Transport 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 525961 | J Med Chem. 2001 Jan 18;44(2):115-37.Medicinal chemistry of neuronal voltage-gated sodium channel blockers. | ||||
Ref 552838 | Drug target identification using side-effect similarity. Science. 2008 Jul 11;321(5886):263-6. doi: 10.1126/science.1158140. | ||||
Ref 525961 | J Med Chem. 2001 Jan 18;44(2):115-37.Medicinal chemistry of neuronal voltage-gated sodium channel blockers. | ||||
Ref 525961 | J Med Chem. 2001 Jan 18;44(2):115-37.Medicinal chemistry of neuronal voltage-gated sodium channel blockers. | ||||
Ref 526204 | Bioorg 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 529491 | Bioorg 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 525961 | J Med Chem. 2001 Jan 18;44(2):115-37.Medicinal chemistry of neuronal voltage-gated sodium channel blockers. |
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.