Target Information

Target General Infomation
Target ID
T39078
Former ID
TTDS00145
Target Name
Calcium-activated potassium channel
Synonyms
Ca(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
Target Type
Successful
Disease Acute pain [ICD9: 338,780; ICD10: R52, G89]
Scorpion envenoming syndrome [ICD9: 989.5; ICD10: T63.2]
Function
Forms 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.
BioChemical Class
Ion transport
Target Validation
T39078
Drugs and Mode of Action
Drug(s) Charybdotoxin Drug Info Approved Scorpion envenoming syndrome [536237], [539474]
Chlorzoxazone Drug Info Approved Acute pain [538167], [539469], [551871]
Inhibitor (2-fluorophenyl)-(4-fluorophenyl)phenylacetamide Drug Info [529274]
1-((2-chlorophenyl)diphenylmethyl)-1H-pyrazole Drug Info [530011]
2,2,2-tris-(3-fluorophenyl)-acetamide Drug Info [529274]
2,2,2-tris-(4-fluorophenyl)-acetamide Drug Info [529274]
2,2-bis-(2-fluorophenyl)-2-phenylacetamide Drug Info [529274]
2,2-bis-(3-fluorophenyl)-2-phenylacetamide Drug Info [529274]
2-(2,4-difluorophenyl)-2,2-diphenylacetamide Drug Info [529274]
2-(2-chlorophenyl)-2,2-diphenylethanamide Drug Info [529274]
2-(3,4-Difluorophenyl)-2,2-diphenylacetamide Drug Info [529274]
2-fluorophenyl-2,2-diphenylacetamide Drug Info [529274]
2-trityl-4,5-dihydrooxazole Drug Info [529274]
4-(4-phenoxybutoxy)-7H-furo[3,2-g]chromen-7-one Drug Info [530011]
4-fluorophenyl-2,2-diphenylacetamide Drug Info [529274]
5-tosyl-5H-dibenzo[b,d]azepin-7(6H)-one Drug Info [530011]
Bis(4-fluorophenyl)-2-fluorophenylacetamide Drug Info [529274]
Bis(4-fluorophenyl)phenylacetamide Drug Info [529274]
N,N-dimethyl-2,2,2-triphenylacetamide Drug Info [529274]
N-ethyl-2,2,2-triphenylacetamide Drug Info [529274]
N-methyl-2,2,2-triphenylacetamide Drug Info [529274]
Triphenylacetic acid methyl ester Drug Info [529274]
TRIPHENYLMETHANAMINE Drug Info [529274]
Blocker Charybdotoxin Drug Info [536237]
Activator Chlorzoxazone Drug Info [536253]
References
Ref 536237Reversible inhibition of the platelet procoagulant response through manipulation of the Gardos channel. Blood. 2006 Oct 1;108(7):2223-8. Epub 2006 Jun 1.
Ref 538167FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 040113.
Ref 539469(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2322).
Ref 539474(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2328).
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 529274J 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.
Ref 530011Bioorg 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.
Ref 536237Reversible inhibition of the platelet procoagulant response through manipulation of the Gardos channel. Blood. 2006 Oct 1;108(7):2223-8. Epub 2006 Jun 1.
Ref 536253Chlorzoxazone inhibits contraction of rat thoracic aorta. Eur J Pharmacol. 2006 Sep 18;545(2-3):161-6. Epub 2006 Jun 29.

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