Target Information

Target General Infomation
Target ID
T42724
Former ID
TTDI03310
Target Name
KCa3.1
Gene Name
KCNN4
Synonyms
KCNN4
Target Type
Discontinued
Disease Hematopoietic [ICD10: D50-D89]
UniProt ID
O15554
Sequence
MGGDLVLGLGALRRRKRLLEQEKSLAGWALVLAGTGIGLMVLHAEMLWFGGCSWALYLFL
VKCTISISTFLLLCLIVAFHAKEVQLFMTDNGLRDWRVALTGRQAAQIVLELVVCGLHPA
PVRGPPCVQDLGAPLTSPQPWPGFLGQGEALLSLAMLLRLYLVPRAVLLRSGVLLNASYR
SIGALNQVRFRHWFVAKLYMNTHPGRLLLGLTLGLWLTTAWVLSVAERQAVNATGHLSDT
LWLIPITFLTIGYGDVVPGTMWGKIVCLCTGVMGVCCTALLVAVVARKLEFNKAEKHVHN
FMMDIQYTKEMKESAARVLQEAWMFYKHTRRKESHAARRHQRKLLAAINAFRQVRLKHRK
LREQVNSMVDISKMHMILYDLQQNLSSSHRALEKQIDTLAGKLDALTELLSTALGPRQLP
EPSQQSK
Drugs and Mode of Action
Drug(s) ICA-17043 Drug Info Discontinued in Phase 2 Hematopoietic [539476], [547148]
Blocker (channel blocker) compound rac-16 Drug Info [527341]
TRAM-34 Drug Info [526701]
Activator DC-EBIO Drug Info [525956]
EBIO Drug Info [530822]
SKA-121 Drug Info [532854]
SKA-31 Drug Info [529778]
Modulator ICA-17043 Drug Info
References
Ref 539476(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 547148Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013404)
Ref 525956Benzimidazolone 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 526701Blockade 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 527341IKCa-channel blockers. Part 2: discovery of cyclohexadienes. Bioorg Med Chem Lett. 2005 Jan 17;15(2):401-4.
Ref 529778Naphtho[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.
Ref 530822Small conductance calcium-activated potassium channels: from structure to function. Prog Neurobiol. 2010 Jul;91(3):242-55.
Ref 532854New positive Ca2+-activated K+ channel gating modulators with selectivity for KCa3.1. Mol Pharmacol. 2014 Sep;86(3):342-57.