Target Information
Target General Infomation | |||||
---|---|---|---|---|---|
Target ID |
T39716
|
||||
Former ID |
TTDS00402
|
||||
Target Name |
Sodium channel protein type 5 subunit alpha
|
||||
Gene Name |
SCN5A
|
||||
Synonyms |
HH1; Sodium channel protein cardiac muscle subunit alpha; Sodium channel protein type V subunit alpha; Voltage-gated sodium channel subunit alpha Nav1.5; SCN5A
|
||||
Target Type |
Successful
|
||||
Disease | Angina pectoris [ICD9: 413; ICD10: I20] | ||||
Anesthesia [ICD9: 338; ICD10: R20.0] | |||||
Anesthesia; Hemorrhoids [ICD9:338; ICD10: R20.0, I84] | |||||
Arrhythmia [ICD9: 427; ICD10: I47-I49] | |||||
Bacterial infections [ICD9: 001-009, 010-018, 020-027, 030-041, 080-088, 090-099, 100-104; ICD10: A00-B99] | |||||
Complex partial seizures [ICD9: 345.4; ICD10: G40.2] | |||||
Cough [ICD9: 786.2; ICD10: R05] | |||||
Dysrhythmias [ICD9: 427; ICD10: I47-I49] | |||||
Epilepsy [ICD10: G40] | |||||
Epilepsy; Convulsion [ICD10: G40] | |||||
Heart arrhythmia [ICD10: I47-I49] | |||||
Local anaesthetic [ICD10: R20.0] | |||||
Migraine [ICD9: 346; ICD10: G43] | |||||
Neurological disease [ICD9: 338, 338.2, 410, 782.3,780; ICD10: I21, I22, R52, R52.1-R52.2, R60.9, G89] | |||||
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89] | |||||
Urinary incontinence [ICD9: 788.3; ICD10: N39.3, N39.4, R32] | |||||
Ventricular arrhythmias [ICD9: 427.1; ICD10: I47.2] | |||||
Ventricular tachycardia; Symptomatic premature ventricular beats; Ventricular fibrillation [ICD10: I47.2] | |||||
BioChemical Class |
Voltage-gated ion channel
|
||||
Target Validation |
T39716
|
||||
UniProt ID | |||||
Sequence |
MANFLLPRGTSSFRRFTRESLAAIEKRMAEKQARGSTTLQESREGLPEEEAPRPQLDLQA
SKKLPDLYGNPPQELIGEPLEDLDPFYSTQKTFIVLNKGKTIFRFSATNALYVLSPFHPI RRAAVKILVHSLFNMLIMCTILTNCVFMAQHDPPPWTKYVEYTFTAIYTFESLVKILARG FCLHAFTFLRDPWNWLDFSVIIMAYTTEFVDLGNVSALRTFRVLRALKTISVISGLKTIV GALIQSVKKLADVMVLTVFCLSVFALIGLQLFMGNLRHKCVRNFTALNGTNGSVEADGLV WESLDLYLSDPENYLLKNGTSDVLLCGNSSDAGTCPEGYRCLKAGENPDHGYTSFDSFAW AFLALFRLMTQDCWERLYQQTLRSAGKIYMIFFMLVIFLGSFYLVNLILAVVAMAYEEQN QATIAETEEKEKRFQEAMEMLKKEHEALTIRGVDTVSRSSLEMSPLAPVNSHERRSKRRK RMSSGTEECGEDRLPKSDSEDGPRAMNHLSLTRGLSRTSMKPRSSRGSIFTFRRRDLGSE ADFADDENSTAGESESHHTSLLVPWPLRRTSAQGQPSPGTSAPGHALHGKKNSTVDCNGV VSLLGAGDPEATSPGSHLLRPVMLEHPPDTTTPSEEPGGPQMLTSQAPCVDGFEEPGARQ RALSAVSVLTSALEELEESRHKCPPCWNRLAQRYLIWECCPLWMSIKQGVKLVVMDPFTD LTITMCIVLNTLFMALEHYNMTSEFEEMLQVGNLVFTGIFTAEMTFKIIALDPYYYFQQG WNIFDSIIVILSLMELGLSRMSNLSVLRSFRLLRVFKLAKSWPTLNTLIKIIGNSVGALG NLTLVLAIIVFIFAVVGMQLFGKNYSELRDSDSGLLPRWHMMDFFHAFLIIFRILCGEWI ETMWDCMEVSGQSLCLLVFLLVMVIGNLVVLNLFLALLLSSFSADNLTAPDEDREMNNLQ LALARIQRGLRFVKRTTWDFCCGLLRQRPQKPAALAAQGQLPSCIATPYSPPPPETEKVP PTRKETRFEEGEQPGQGTPGDPEPVCVPIAVAESDTDDQEEDEENSLGTEEESSKQQESQ PVSGGPEAPPDSRTWSQVSATASSEAEASASQADWRQQWKAEPQAPGCGETPEDSCSEGS TADMTNTAELLEQIPDLGQDVKDPEDCFTEGCVRRCPCCAVDTTQAPGKVWWRLRKTCYH IVEHSWFETFIIFMILLSSGALAFEDIYLEERKTIKVLLEYADKMFTYVFVLEMLLKWVA YGFKKYFTNAWCWLDFLIVDVSLVSLVANTLGFAEMGPIKSLRTLRALRPLRALSRFEGM RVVVNALVGAIPSIMNVLLVCLIFWLIFSIMGVNLFAGKFGRCINQTEGDLPLNYTIVNN KSQCESLNLTGELYWTKVKVNFDNVGAGYLALLQVATFKGWMDIMYAAVDSRGYEEQPQW EYNLYMYIYFVIFIIFGSFFTLNLFIGVIIDNFNQQKKKLGGQDIFMTEEQKKYYNAMKK LGSKKPQKPIPRPLNKYQGFIFDIVTKQAFDVTIMFLICLNMVTMMVETDDQSPEKINIL AKINLLFVAIFTGECIVKLAALRHYYFTNSWNIFDFVVVILSIVGTVLSDIIQKYFFSPT LFRVIRLARIGRILRLIRGAKGIRTLLFALMMSLPALFNIGLLLFLVMFIYSIFGMANFA YVKWEAGIDDMFNFQTFANSMLCLFQITTSAGWDGLLSPILNTGPPYCDPTLPNSNGSRG DCGSPAVGILFFTTYIIISFLIVVNMYIAIILENFSVATEESTEPLSEDDFDMFYEIWEK FDPEATQFIEYSVLSDFADALSEPLRIAKPNQISLINMDLPMVSGDRIHCMDILFAFTKR VLGESGEMDALKIQMEEKFMAANPSKISYEPITTTLRRKHEEVSAMVIQRAFRRHLLQRS LKHASFLFRQQAGSGLSEEDAPEREGLIAYVMSENFSRPLGPPSSSSISSTSFPPSYDSV TRATSDNLQVRGSDYSHSEDLADFPPSPDRDRESIV |
||||
Drugs and Mode of Action | |||||
Drug(s) | Benzonatate | Drug Info | Approved | Cough | [538191], [542600] |
Dibucaine | Drug Info | Approved | Anesthesia; Hemorrhoids | [538393], [542167], [551871] | |
Disopyramide | Drug Info | Approved | Ventricular arrhythmias | [538219], [542176] | |
Dyclonine | Drug Info | Approved | Pain | [538425], [542183], [551871] | |
Ethotoin | Drug Info | Approved | Complex partial seizures | [538439], [542194] | |
Fosphenytoin | Drug Info | Approved | Epilepsy; Convulsion | [551871] | |
Hexylcaine | Drug Info | Approved | Local anaesthetic | [551871] | |
Indecainide | Drug Info | Approved | Dysrhythmias | [538531] | |
LOMERIZINE | Drug Info | Approved | Migraine | [545070], [551871] | |
Mephenytoin | Drug Info | Approved | Epilepsy | [538388], [542238] | |
Mexiletine | Drug Info | Approved | Ventricular tachycardia; Symptomatic premature ventricular beats; Ventricular fibrillation | [551871] | |
Moricizine | Drug Info | Approved | Arrhythmia | [551871] | |
Prilocaine | Drug Info | Approved | Pain | [538314], [542296], [551871] | |
Tetrodotoxin | Drug Info | Approved | Bacterial infections | [535573], [539688] | |
F-15845 | Drug Info | Phase 1 | Angina pectoris | [548229] | |
Disopyramide | Drug Info | Withdrawn from market | Urinary incontinence | [542176], [551871] | |
Encainide | Drug Info | Withdrawn from market | Heart arrhythmia | [537733], [551871] | |
Hexylcaine | Drug Info | Withdrawn from market | Anesthesia | [538409], [542208] | |
Moricizine | Drug Info | Withdrawn from market | Heart arrhythmia | [538532], [542261], [551871] | |
LUBELUZOLE | Drug Info | Discontinued in Preregistration | Neurological disease | [545928] | |
SIPATRIGINE | Drug Info | Discontinued in Phase 2 | Neurological disease | [545614] | |
PD-85639 | Drug Info | Terminated | Discovery agent | [545294] | |
Inhibitor | 1-[5-(4-Chlorophenyl)-2-furoyl]piperazine | Drug Info | [529491] | ||
F-15845 | Drug Info | [531108], [532635] | |||
Indol-1-yl-propyl-pyridin-4-yl-amine | Drug Info | [525961] | |||
KC-12291 | Drug Info | [529518] | |||
LOMERIZINE | Drug Info | [525961] | |||
LUBELUZOLE | Drug Info | [525961] | |||
N-(4-Methyl-benzoyl)-N'-phenethyl-guanidine | Drug Info | [526204] | |||
N-Butyl-N'-(4-methyl-benzoyl)-guanidine | Drug Info | [526204] | |||
PD-85639 | Drug Info | [525961] | |||
SIPATRIGINE | Drug Info | [525961] | |||
Blocker | Acetylprocainamide | Drug Info | [538082] | ||
Benzonatate | Drug Info | [536316] | |||
Dibucaine | Drug Info | [535573] | |||
Disopyramide | Drug Info | [535117] | |||
Dyclonine | Drug Info | [538082] | |||
Encainide | Drug Info | [537980] | |||
Ethotoin | Drug Info | [536316] | |||
Fosphenytoin | Drug Info | [537516] | |||
Hexylcaine | Drug Info | [536316] | |||
Indecainide | Drug Info | [537786] | |||
Mephenytoin | Drug Info | [537516] | |||
Mexiletine | Drug Info | [535117] | |||
Moricizine | Drug Info | [537980] | |||
Prilocaine | Drug Info | [538082] | |||
Tetrodotoxin | Drug Info | [535573] | |||
Activator | aconitine | Drug Info | [532584] | ||
batrachotoxin | Drug Info | [532575] | |||
veratridine | Drug Info | [531463] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Adrenergic signaling in cardiomyocytes | ||||
PathWhiz Pathway | Muscle/Heart Contraction | ||||
Reactome | Interaction between L1 and Ankyrins | ||||
WikiPathways | SIDS Susceptibility Pathways | ||||
Cardiac Progenitor Differentiation | |||||
References | |||||
Ref 535573 | Halothane attenuates the cerebroprotective action of several Na+ and Ca2+ channel blockers via reversal of their ion channel blockade. Eur J Pharmacol. 2002 Oct 4;452(2):175-81. | ||||
Ref 537733 | New antiarrhythmic drugs: tocainide, mexiletine, flecainide, encainide, and amiodarone. Mayo Clin Proc. 1987 Nov;62(11):1033-50. | ||||
Ref 538191 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 040587. | ||||
Ref 538219 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 070101. | ||||
Ref 538314 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 076290. | ||||
Ref 538388 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 006008. | ||||
Ref 538393 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 006203. | ||||
Ref 538409 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 008472. | ||||
Ref 538425 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 009925. | ||||
Ref 538439 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 010841. | ||||
Ref 538531 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 019693. | ||||
Ref 538532 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 019753. | ||||
Ref 539688 | (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: 2616). | ||||
Ref 542167 | (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: 7159). | ||||
Ref 542176 | (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: 7167). | ||||
Ref 542183 | (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: 7173). | ||||
Ref 542194 | (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: 7183). | ||||
Ref 542208 | (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: 7196). | ||||
Ref 542238 | (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: 7223). | ||||
Ref 542261 | (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: 7244). | ||||
Ref 542296 | (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: 7276). | ||||
Ref 542600 | (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: 7611). | ||||
Ref 545070 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002033) | ||||
Ref 545294 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002730) | ||||
Ref 545614 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003904) | ||||
Ref 545928 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005388) | ||||
Ref 525961 | J Med Chem. 2001 Jan 18;44(2):115-37.Medicinal chemistry of neuronal voltage-gated sodium channel blockers. | ||||
Ref 526204 | Bioorg Med Chem Lett. 2001 Dec 17;11(24):3151-5.Solution-phase, parallel synthesis and pharmacological evaluation of acylguanidine derivatives as potential sodium channel blockers. | ||||
Ref 529491 | Bioorg Med Chem. 2008 Jun 15;16(12):6379-86. Epub 2008 May 6.Discovery of potent furan piperazine sodium channel blockers for treatment of neuropathic pain. | ||||
Ref 529518 | J Med Chem. 2008 Jul 10;51(13):3856-66. Epub 2008 Jun 5.Sodium late current blockers in ischemia reperfusion: is the bullet magic?. | ||||
Ref 531108 | Selective inhibition of persistent sodium current by F 15845 prevents ischaemia-induced arrhythmias. Br J Pharmacol. 2010 Sep;161(1):79-91. | ||||
Ref 531463 | Sodium channel comodification with full activator reveals veratridine reaction dynamics. Mol Pharmacol. 1990 Feb;37(2):144-8. | ||||
Ref 532575 | Binding of [3H]batrachotoxinin A benzoate to specific sites on rat cardiac sodium channels. Mol Pharmacol. 1986 Dec;30(6):617-23. | ||||
Ref 532584 | Properties of aconitine-modified sodium channels in single cells of mouse ventricular myocardium. Gen Physiol Biophys. 1986 Oct;5(5):473-84. | ||||
Ref 532635 | A rare loss-of-function SCN5A variant is associated with lidocaine-induced ventricular fibrillation. Pharmacogenomics J. 2014 Aug;14(4):372-5. | ||||
Ref 535117 | Effect of sodium channel blockers on ST segment, QRS duration, and corrected QT interval in patients with Brugada syndrome. J Cardiovasc Electrophysiol. 2000 Dec;11(12):1320-9. | ||||
Ref 535573 | Halothane attenuates the cerebroprotective action of several Na+ and Ca2+ channel blockers via reversal of their ion channel blockade. Eur J Pharmacol. 2002 Oct 4;452(2):175-81. | ||||
Ref 537516 | Lacosamide: a new approach to target voltage-gated sodium currents in epileptic disorders. CNS Drugs. 2009;23(7):555-68. doi: 10.2165/00023210-200923070-00002. | ||||
Ref 537786 | Electrophysiological studies of indecainide hydrochloride, a new antiarrhythmic agent, in canine cardiac tissues. J Cardiovasc Pharmacol. 1984 Jul-Aug;6(4):614-21. |
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.