Target Information
Target General Infomation | |||||
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Target ID |
T39078
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Former ID |
TTDS00145
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Target Name |
Calcium-activated potassium channel
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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
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Target Type |
Successful
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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.
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BioChemical Class |
Ion transport
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Target Validation |
T39078
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Drugs and Mode of Action | |||||
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 536237 | Reversible 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 538167 | FDA 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 529274 | J 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 530011 | Bioorg 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. |
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