Therapeutic Targets Database
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TTD Target ID: TTDR01255

Target Information
NameVoltage-gated sodium channel subunit alpha Nav1.3    
Type of targetResearch target    
SynonymsKIAA1356    
NAC3    
SCN3A    
Sodium channel protein type 3 subunit alpha    
Sodium channel protein type III subunit alpha    
Sodium channel protein, brain III subunit alpha    
Voltage-gated sodium channel subtype III    
DiseaseAnalgesics    [1]
Pain, unspecific    [1]
BioChemical ClassVoltage-gated channel    
UniProt IDQ9NY46
PDB Structure1BYY.    
FunctionMediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na+ ions may pass in accordance with their electrochemical gradient.    
SequenceMAQALLVPPGPESFRLFTRESLAAIEKRAAEEKAKKPKKEQDNDDENKPKPNSDLEAGKN LPFIYGDIPPEMVSEPLEDLDPYYINKKTFIVMNKGKAIFRFSATSALYILTPLNPVRKI AIKILVHSLFSMLIMCTILTNCVFMTLSNPPDWTKNVEYTFTGIYTFESLIKILARGFCL EDFTFLRDPWNWLDFSVIVMAYVTEFVSLGNVSALRTFRVLRALKTISVIPGLKTIVGAL IQSVKKLSDVMILTVFCLSVFALIGLQLFMGNLRNKCLQWPPSDSAFETNTTSYFNGTMD SNGTFVNVTMSTFNWKDYIGDDSHFYVLDGQKDPLLCGNGSDAGQCPEGYICVKAGRNPN YGYTSFDTFSWAFLSLFRLMTQDYWENLYQLTLRAAGKTYMIFFVLVIFLGSFYLVNLIL AVVAMAYEEQNQATLEEAEQKEAEFQQMLEQLKKQQEEAQAVAAASAASRDFSGIGGLGE LLESSSEASKLSSKSAKEWRNRRKKRRQREHLEGNNKGERDSFPKSESEDSVKRSSFLFS MDGNRLTSDKKFCSPHQSLLSIRGSLFSPRRNSKTSIFSFRGRAKDVGSENDFADDEHST FEDSESRRDSLFVPHRHGERRNSNVSQASMSSRMVPGLPANGKMHSTVDCNGVVSLVGGP SALTSPTGQLPPEGTTTETEVRKRRLSSYQISMEMLEDSSGRQRAVSIASILTNTMEELE ESRQKCPPCWYRFANVFLIWDCCDAWLKVKHLVNLIVMDPFVDLAITICIVLNTLFMAME HYPMTEQFSSVLTVGNLVFTGIFTAEMVLKIIAMDPYYYFQEGWNIFDGIIVSLSLMELG LSNVEGLSVLRSFRLLRVFKLAKSWPTLNMLIKIIGNSVGALGNLTLVLAIIVFIFAVVG MQLFGKSYKECVCKINDDCTLPRWHMNDFFHSFLIVFRVLCGEWIETMWDCMEVAGQTMC LIVFMLVMVIGNLVVLNLFLALLLSSFSSDNLAATDDDNEMNNLQIAVGRMQKGIDYVKN KMRECFQKAFFRKPKVIEIHEGNKIDSCMSNNTGIEISKELNYLRDGNGTTSGVGTGSSV EKYVIDENDYMSFINNPSLTVTVPIAVGESDFENLNTEEFSSESELEESKEKLNATSSSE GSTVDVVLPREGEQAETEPEEDLKPEACFTEGCIKKFPFCQVSTEEGKGKIWWNLRKTCY SIVEHNWFETFIVFMILLSSGALAFEDIYIEQRKTIKTMLEYADKVFTYIFILEMLLKWV AYGFQTYFTNAWCWLDFLIVDVSLVSLVANALGYSELGAIKSLRTLRALRPLRALSRFEG MRVVVNALVGAIPSIMNVLLVCLIFWLIFSIMGVNLFAGKFYHCVNMTTGNMFDISDVNN LSDCQALGKQARWKNVKVNFDNVGAGYLALLQVATFKGWMDIMYAAVDSRDVKLQPVYEE NLYMYLYFVIFIIFGSFFTLNLFIGVIIDNFNQQKKKFGGQDIFMTEEQKKYYNAMKKLG SKKPQKPIPRPANKFQGMVFDFVTRQVFDISIMILICLNMVTMMVETDDQGKYMTLVLSR INLVFIVLFTGEFVLKLVSLRHYYFTIGWNIFDFVVVILSIVGMFLAEMIEKYFVSPTLF RVIRLARIGRILRLIKGAKGIRTLLFALMMSLPALFNIGLLLFLVMFIYAIFGMSNFAYV KKEAGIDDMFNFETFGNSMICLFQITTSAGWDGLLAPILNSAPPDCDPDTIHPGSSVKGD CGNPSVGIFFFVSYIIISFLVVVNMYIAVILENFSVATEESAEPLSEDDFEMFYEVWEKF DPDATQFIEFSKLSDFAAALDPPLLIAKPNKVQLIAMDLPMVSGDRIHCLDILFAFTKRV LGESGEMDALRIQMEDRFMASNPSKVSYEPITTTLKRKQEEVSAAIIQRNFRCYLLKQRL KNISSNYNKEAIKGRIDLPIKQDMIIDKLNGNSTPEKTDGSSSTTSPPSYDSVTKPDKEK FEKDKPEKESKGKEVRENQK
Target ValidationClick to Find Target Validation Information.    
Inhibitor2- (1-Pentyl-hexyl)-4-phenyl-1H-imidazole[2]
2-Hexyl-4- (4-isobutyl-phenyl)-1H-imidazole[2]
2-Hydroxy-2-phenyl-nonanoic acid amide[3]
4-Biphenyl-4-yl-2- (1-pentyl-hexyl)-1H-imidazole[2]
4-Biphenyl-4-yl-2- (1-propyl-butyl)-1H-imidazole[2]
4-Biphenyl-4-yl-2-cyclohexylmethyl-1H-imidazole[2]
4-Biphenyl-4-yl-2-hexyl-1H-imidazole[2]
4-Biphenyl-4-yl-2-methyl-1H-imidazole[2]
5-Ethyl-3-methyl-5-phenyl-oxazolidine-2,4-dione[4]
5-Heptyl-5-phenyl-imidazolidine-2,4-dione[3]
5-Hexyl-5-phenyl-imidazolidine-2,4-dione[3]
5-Nonyl-5-phenyl-imidazolidine-2,4-dione[3]
BW-202W92[5]
CCNCSSKWCRDHSRCC[6]
L-741742[7]
LIDOFLAZINE[8]
LIFARIZINE[9]
LUBELUZOLE[9]
PD-85639[8]
SIPATRIGINE[9]
U-92032[10]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Challenges in Analgesic Drug Development. Clin Pharmacol Ther. 2009 Aug 12. To Reference
Ref 2Bioorg Med Chem Lett. 2004 Jul 5;14(13):3521-3.2-Alkyl-4-arylimidazoles: structurally novel sodium channel modulators. To Reference
Ref 3J Med Chem. 1999 May 6;42(9):1537-45.Comparative molecular field analysis of hydantoin binding to the neuronal voltage-dependent sodium channel. To Reference
Ref 4J Med Chem. 1989 Jul;32(7):1577-80.Sodium channel binding and anticonvulsant activities for the enantiomers of a bicyclic 2,4-oxazolidinedione and monocyclic models. To Reference
Ref 5J Med Chem. 2009 May 14;52(9):2694-707.Oxadiazolylindazole sodium channel modulators are neuroprotective toward hippocampal neurones. To Reference
Ref 6J Biol Chem. 2007 Oct 19;282(42):30699-706. Epub 2007 Aug 27.Structure/function characterization of micro-conotoxin KIIIA, an analgesic, nearly irreversible blocker of mammalian neuronal sodium channels. To Reference
Ref 7J Med Chem. 1999 Jul 15;42(14):2706-15.1-(3-Cyanobenzylpiperidin-4-yl)-5-methyl-4-phenyl-1, 3-dihydroimidazol-2-one: a selective high-affinity antagonist for the human dopamine D(4) receptor with excellent selectivity over ion channels. To Reference
Ref 8J Med Chem. 1994 Jan 21;37(2):268-74.Synthesis and pharmacological evaluation of phenylacetamides as sodium-channel blockers. To Reference
Ref 9J Med Chem. 2002 Aug 15;45(17):3755-64.Synthesis and structure-activity relationships of 6,7-benzomorphan derivatives as use-dependent sodium channel blockers for the treatment of stroke. To Reference
Ref 10J Med Chem. 2000 Sep 7;43(18):3372-6.Discovery of (2S)-1-(4-amino-2,3,5- trimethylphenoxy)-3-[4-[4-(4- fluorobenzyl)phenyl]-1-piperazinyl]-2-propanol dimethanesulfonate (SUN N8075): a dual Na(+) and Ca(2+) channel blocker with antioxidant activity. To Reference



 

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