Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDS00145

Target Information
NameCalcium-activated potassium channel    
Type of targetSuccessful target    
SynonymsCa(2+)-activated potassium channel IKCa1    
Ca-activated K channel    
Gardos channel    
HSK4    
IK channel KCNN4    
IK1    
IKCa1    
IKCa1 Ca 2+ -activated K + channel    
Intermediate conductance calcium-activated potassium channel protein 4    
KCNN4    
KCa4    
Putative Gardos channel    
SK4    
DiseaseAnemia, unspecified
[ICD9: 280-285   ICD10: D50-D64]
[1]
Autoimmune diseases
[ICD9: 279.4   ICD10: D84.9, M35.9]
[1]
Cystic fibrosis
[ICD9: 277.0   ICD10: E84]
[1]
Diarrhea (secretory)
[ICD9: 787.91   ICD10: A09, K59.1]
[1]
Graft-versus-host disease, acute
[ICD9: 279.50   ICD10: T86.0]
[1]
Graft-versus-host disease, chronic
[ICD9: 279.50   ICD10: T86.0]
[1]
Sickle cell anemia
[ICD9: 280-285   ICD10: D50-D64]
[2]
Drug(s)CharybdotoxinApprovedScorpion envenoming syndrome[3]
ChlorzoxazoneApprovedAcute painful musculoskeletal conditions[4]
HalofantrineApprovedMalaria[5]
QuinineApprovedMalaria[3]
ICA-17043Phase IIExercise Induced Asthma[2]
AVE0118Phase IObstructive sleep apnea[6]
ICA-17043Terminated in Phase IIISickle cell disease[2]
BioChemical ClassIon transport    
UniProt IDO15554
Q12791
PDB Structure2K44; 3MT5; 3NAF.    
FunctionForms a voltage-independent potassium channel that is activated by intracellular calcium. activation is followed by membrane hyperpolarization which promotes calcium influx. The channel is blocked by clotrimazole and charybdotoxin.    
SequenceMGGDLVLGLGALRRRKRLLEQEKSLAGWALVLAGTGIGLMVLHAEMLWFGGCSWALYLFL VKCTISISTFLLLCLIVAFHAKEVQLFMTDNGLRDWRVALTGRQAAQIVLELVVCGLHPA PVRGPPCVQDLGAPLTSPQPWPGFLGQGEALLSLAMLLRLYLVPRAVLLRSGVLLNASYR SIGALNQVRFRHWFVAKLYMNTHPGRLLLGLTLGLWLTTAWVLSVAERQAVNATGHLSDT LWLIPITFLTIGYGDVVPGTMWGKIVCLCTGVMGVCCTALLVAVVARKLEFNKAEKHVHN FMMDIQYTKEMKESAARVLQEAWMFYKHTRRKESHAARRHQRKLLAAINAFRQVRLKHRK LREQVNSMVDISKMHMILYDLQQNLSSSHRALEKQIDTLAGKLDALTELLSTALGPRQLP EPSQQSK
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
Inhibitor (2-fluorophenyl)-[7]
1- ([8]
2,2,2-tris- (3-fluorophenyl)-acetamide[7]
2,2,2-tris- (4-fluorophenyl)-acetamide[7]
2,2-bis- (2-fluorophenyl)-2-phenylacetamide[7]
2,2-bis- (3-fluorophenyl)-2-phenylacetamide[7]
2- (2,4-difluorophenyl)-2,2-diphenylacetamide[7]
2- (2-chlorophenyl)-2,2-diphenylethanamide[7]
2- (3,4-Difluorophenyl)-2,2-diphenylacetamide[7]
2-fluorophenyl-2,2-diphenylacetamide[7]
2-trityl-4,5-dihydrooxazole[7]
4- (4-phenoxybutoxy)-7H-furo[3,2-g]chromen-7-one[8]
4-fluorophenyl-2,2-diphenylacetamide[7]
5-tosyl-5H-dibenzo[b,d]azepin-7 (6H)-one[8]
N,N-dimethyl-2,2,2-triphenylacetamide[7]
N-ethyl-2,2,2-triphenylacetamide[7]
N-methyl-2,2,2-triphenylacetamide[7]
TRIPHENYLMETHANAMINE[7]
bis (4-fluorophenyl)-2-fluorophenylacetamide[7]
bis (4-fluorophenyl)phenylacetamide[7]
triphenylacetic acid methyl ester[7]
BlockerAVE0118[6]
Charybdotoxin[3]
Halofantrine[5]
ICA-17043[2]
Quinine[3]
ActivatorChlorzoxazone[4]
ModulatorBMS-204352[9]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1The Ca2+-activated K+ channel of intermediate conductance: a molecular target for novel treatments? Curr Drug Targets. 2001 Dec;2(4):401-22. To Reference
Ref 2Sickle cell disease: from membrane pathophysiology to novel therapies for prevention of erythrocyte dehydration. J Pediatr Hematol Oncol. 2003 Dec;25(12):927-33. To Reference
Ref 3Reversible inhibition of the platelet procoagulant response through manipulation of the Gardos channel. Blood. 2006 Oct 1;108(7):2223-8. Epub 2006 Jun 1. To Reference
Ref 4Chlorzoxazone inhibits contraction of rat thoracic aorta. Eur J Pharmacol. 2006 Sep 18;545(2-3):161-6. Epub 2006 Jun 29. To Reference
Ref 5Antimalarial drugs inhibit the acetylcholine-receptor-operated potassium current in atrial myocytes. Heart Lung Circ. 2002;11(2):112-6. To Reference
Ref 6Pharma & Vaccines. Product Development Pipeline. April 29 2009. To Reference
Ref 7J Med Chem. 2008 Feb 28;51(4):976-82. Epub 2008 Jan 31.Novel inhibitors of the Gardos channel for the treatment of sickle cell disease. To Reference
Ref 8Bioorg Med Chem Lett. 2009 Apr 15;19(8):2299-304. Epub 2009 Feb 25.Inhibitors of potassium channels KV1.3 and IK-1 as immunosuppressants. To Reference
Ref 9Current status of neuroprotective agents in the treatment of acute ischemic stroke. Curr Neurol Neurosci Rep. 2001 Jan;1(1):13-8. To Reference



 

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