Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T42724
|
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| Former ID |
TTDI03310
|
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| Target Name |
KCa3.1
|
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| Gene Name |
KCNN4
|
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| Synonyms |
KCNN4
|
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| Target Type |
Discontinued
|
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| Disease | Hematopoietic [ICD10: D50-D89] | ||||
| UniProt ID | |||||
| Sequence |
MGGDLVLGLGALRRRKRLLEQEKSLAGWALVLAGTGIGLMVLHAEMLWFGGCSWALYLFL
VKCTISISTFLLLCLIVAFHAKEVQLFMTDNGLRDWRVALTGRQAAQIVLELVVCGLHPA PVRGPPCVQDLGAPLTSPQPWPGFLGQGEALLSLAMLLRLYLVPRAVLLRSGVLLNASYR SIGALNQVRFRHWFVAKLYMNTHPGRLLLGLTLGLWLTTAWVLSVAERQAVNATGHLSDT LWLIPITFLTIGYGDVVPGTMWGKIVCLCTGVMGVCCTALLVAVVARKLEFNKAEKHVHN FMMDIQYTKEMKESAARVLQEAWMFYKHTRRKESHAARRHQRKLLAAINAFRQVRLKHRK LREQVNSMVDISKMHMILYDLQQNLSSSHRALEKQIDTLAGKLDALTELLSTALGPRQLP EPSQQSK |
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| Drugs and Mode of Action | |||||
| Drug(s) | ICA-17043 | Drug Info | Discontinued in Phase 2 | Hematopoietic | [1], [2] |
| Blocker (channel blocker) | compound rac-16 | Drug Info | [3] | ||
| TRAM-34 | Drug Info | [4] | |||
| Activator | DC-EBIO | Drug Info | [5] | ||
| EBIO | Drug Info | [6] | |||
| SKA-121 | Drug Info | [7] | |||
| SKA-31 | Drug Info | [8] | |||
| Modulator | ICA-17043 | Drug Info | |||
| References | |||||
| REF 1 | (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: 2331). | ||||
| REF 2 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013404) | ||||
| REF 3 | IKCa-channel blockers. Part 2: discovery of cyclohexadienes. Bioorg Med Chem Lett. 2005 Jan 17;15(2):401-4. | ||||
| REF 4 | Blockade of the intermediate-conductance calcium-activated potassium channel as a new therapeutic strategy for restenosis. Circulation. 2003 Sep 2;108(9):1119-25. Epub 2003 Aug 25. | ||||
| REF 5 | Benzimidazolone activators of chloride secretion: potential therapeutics for cystic fibrosis and chronic obstructive pulmonary disease. J Pharmacol Exp Ther. 2001 Feb;296(2):600-11. | ||||
| REF 6 | Small conductance calcium-activated potassium channels: from structure to function. Prog Neurobiol. 2010 Jul;91(3):242-55. | ||||
| REF 7 | New positive Ca2+-activated K+ channel gating modulators with selectivity for KCa3.1. Mol Pharmacol. 2014 Sep;86(3):342-57. | ||||
| REF 8 | Naphtho[1,2-d]thiazol-2-ylamine (SKA-31), a new activator of KCa2 and KCa3.1 potassium channels, potentiates the endothelium-derived hyperpolarizing factor response and lowers blood pressure. Mol Pharmacol. 2009 Feb;75(2):281-95. | ||||
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