Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDC00303

Target Information
NamePotassium voltage-gated channel subfamily A member 5    
Type of targetClinical trial target    
Synonyms02-Sensitive Potassium Channel Kv1.5    
HK2    
HPCN1    
Potassium channel Kv1.5    
Voltage-gated potassium channel subunit Kv1.5    
DiseaseVascular disease
[ICD9: 325, 430-459   ICD10: G45-G46, I60-I95]
[1]
Drug(s)4-AminopyridinePhase III completedSpinal cord injury[2]
AzimilidePhase III completedAtrial fibrillation[3]
DronedaroneWithdrawn in MAAAtrial fibrillation[3]
BioChemical ClassVoltage-gated channel    
UniProt IDP22460
FunctionMediates the voltage-dependent potassium ion permeability of excitable membranes. assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a potassium-selective channel.    
SequenceMEIALVPLENGGAMTVRGGDEARAGCGQATGGELQCPPTAGLSDGPKEPAPKGRGAQRDA DSGVRPLPPLPDPGVRPLPPLPEELPRPRRPPPEDEEEEGDPGLGTVEDQALGTASLHHQ RVHINISGLRFETQLGTLAQFPNTLLGDPAKRLRYFDPLRNEYFFDRNRPSFDGILYYYQ SGGRLRRPVNVSLDVFADEIRFYQLGDEAMERFREDEGFIKEEEKPLPRNEFQRQVWLIF EYPESSGSARAIAIVSVLVILISIITFCLETLPEFRDERELLRHPPAPHQPPAPAPGANG SGVMAPPSGPTVAPLLPRTLADPFFIVETTCVIWFTFELLVRFFACPSKAGFSRNIMNII DVVAIFPYFITLGTELAEQQPGGGGGGQNGQQAMSLAILRVIRLVRVFRIFKLSRHSKGL QILGKTLQASMRELGLLIFFLFIGVILFSSAVYFAEADNQGTHFSSIPDAFWWAVVTMTT VGYGDMRPITVGGKIVGSLCAIAGVLTIALPVPVIVSNFNYFYHRETDHEEPAVLKEEQG TQSQGPGLDRGVQRKVSGSRGSFCKAGGTLENADSARRGSCPLEKCNVKAKSNVDLRRSL YALCLDTSRETDL
Target ValidationClick to Find Target Validation Information.    
Inhibitor2-amino-2-phenyl-1,1-di (pyridin-3-yl)ethanol[4]
2-morpholino-1,1,2-triphenylethanol[4]
2-morpholino-1,1-di (pyridin-3-yl)hexan-1-ol[4]
2-morpholino-1,1-di (pyridin-3-yl)octan-1-ol[4]
2-morpholino-2-phenyl-1,1-di (pyridin-3-yl)ethanol[4]
2-phenoxy-1- (2-p-tolylthiazolidin-3-yl)ethanone[5]
2-phenyl-1,1-di (pyridin-3-yl)ethanol[4]
3- (4-methoxybenzyloxy)-2-phenylthiazolidin-4-one[5]
3- (benzyloxy)-2-[5]
3-methyl-2-morpholino-1,1-diphenylbutan-1-ol[4]
4- (4-phenoxybutoxy)-7H-furo[3,2-g]chromen-7-one[6]
N-Benzyl-2- (toluene-4-sulfonylamino)-benzamide[7]
N-Phenethyl-2- (toluene-4-sulfonylamino)-benzamide[7]
Blocker4-Aminopyridine[2]
AVE-0118[3]
Azimilide[3]
Dronedarone[3]
NIP-142[3]
RS-100302[3]
S-20951[3]
S-9947[3]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1In vivo gene transfer of the O2-sensitive potassium channel Kv1.5 reduces pulmonary hypertension and restores hypoxic pulmonary vasoconstriction in chronically hypoxic rats. Circulation. 2003 Apr 22;107(15):2037-44. Epub 2003 Apr 14. To Reference
Ref 2Emerging drugs for spinal cord injury. Expert Opin Emerg Drugs. 2008 Mar;13(1):63-80. To Reference
Ref 3New antiarrhythmic agents for atrial fibrillation and atrial flutter. Expert Opin Emerg Drugs. 2005 May;10(2):311-22. To Reference
Ref 4Bioorg Med Chem Lett. 2010 Apr 15;20(8):2493-6. Epub 2010 Mar 4.Discovery of triarylethanolamine inhibitors of the Kv1.5 potassium channel. To Reference
Ref 5Bioorg Med Chem Lett. 2007 Jan 1;17(1):282-4. Epub 2006 Nov 13.Evolution of thiazolidine-based blockers of human Kv1.5 for the treatment of atrial arrhythmias. To Reference
Ref 6Bioorg Med Chem Lett. 2010 Dec 1;20(23):6989-92. Epub 2010 Oct 23.Substituted N-{3-[(1,1-dioxido-1,2-benzothiazol-3-yl)(phenyl)amino]propyl}benzamide analogs as potent Kv1.3 ion channel blockers. Part 2. To Reference
Ref 7Bioorg Med Chem Lett. 2004 Jun 7;14(11):2823-7.Pharmacophore-based search, synthesis, and biological evaluation of anthranilic amides as novel blockers of the Kv1.5 channel. To Reference



 

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