Target Information

Target General Infomation
Target ID
T69051
Former ID
TTDR00237
Target Name
PN3 Na+ channel
Gene Name
Scn10a
Synonyms
PN3; Peripheral nerve sodium channel 3; Sensory neuron sodium channel; Sodium channel protein type 10 subunit alpha; Sodium channel protein type X subunit alpha; Voltage-gated sodium channel subunit alpha Nav1.8; Scn10a
Target Type
Research
Function
Tetrodotoxin-resistant channel that mediates 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 channelthrough which sodium ions may pass in accordance with their electrochemical gradient. Plays a role in neuropathic pain mechanisms.
BioChemical Class
Voltage-gated ion channel
Target Validation
T69051
UniProt ID
Q62968
Sequence
MELPFASVGTTNFRRFTPESLAEIEKQIAAHRAAKKARTKHRGQEDKGEKPRPQLDLKAC
NQLPKFYGELPAELVGEPLEDLDPFYSTHRTFMVLNKSRTISRFSATWALWLFSPFNLIR
RTAIKVSVHSWFSIFITITILVNCVCMTRTDLPEKVEYVFTVIYTFEALIKILARGFCLN
EFTYLRDPWNWLDFSVITLAYVGAAIDLRGISGLRTFRVLRALKTVSVIPGLKVIVGALI
HSVRKLADVTILTVFCLSVFALVGLQLFKGNLKNKCIRNGTDPHKADNLSSEMAEYIFIK
PGTTDPLLCGNGSDAGHCPGGYVCLKTPDNPDFNYTSFDSFAWAFLSLFRLMTQDSWERL
YQQTLRASGKMYMVFFVLVIFLGSFYLVNLILAVVTMAYEEQSQATIAEIEAKEKKFQEA
LEVLQKEQEVLAALGIDTTSLQSHSGSPLASKNANERRPRVKSRVSEGSTDDNRSPQSDP
YNQRRMSFLGLSSGRRRASHGSVFHFRAPSQDISFPDGITDDGVFHGDQESRRGSILLGR
GAGQTGPLPRSPLPQSPNPGRRHGEEGQLGVPTGELTAGAPEGPALDTTGQKSFLSAGYL
NEPFRAQRAMSVVSIMTSVIEELEESKLKCPPCLISFAQKYLIWECCPKWRKFKMALFEL
VTDPFAELTITLCIVVNTVFMAMEHYPMTDAFDAMLQAGNIVFTVFFTMEMAFKIIAFDP
YYYFQKKWNIFDCVIVTVSLLELSASKKGSLSVLRTFRLLRVFKLAKSWPTLNTLIKIIG
NSVGALGNLTFILAIIVFIFALVGKQLLSEDYGCRKDGVSVWNGEKLRWHMCDFFHSFLV
VFRILCGEWIENMWVCMEVSQKSICLILFLTVMVLGNLVVLNLFIALLLNSFSADNLTAP
EDDGEVNNLQLALARIQVLGHRASRAIASYISSHCRFRWPKVETQLGMKPPLTSSEAKNH
IATDAVSAAVGNLTKPALSSPKENHGDFITDPNVWVSVPIAEGESDLDELEEDMEQASQS
SWQEEDPKGQQEQLPQVQKCENHQAARSPASMMSSEDLAPYLGESWKRKDSPQVPAEGVD
DTSSSEGSTVDCPDPEEILRKIPELADDLDEPDDCFTEGCTRRCPCCNVNTSKSPWATGW
QVRKTCYRIVEHSWFESFIIFMILLSSGALAFEDNYLEEKPRVKSVLEYTDRVFTFIFVF
EMLLKWVAYGFKKYFTNAWCWLDFLIVNISLTSLIAKILEYSDVASIKALRTLRALRPLR
ALSRFEGMRVVVDALVGAIPSIMNVLLVCLIFWLIFSIMGVNLFAGKFSKCVDTRNNPFS
NVNSTMVNNKSECHNQNSTGHFFWVNVKVNFDNVAMGYLALLQVATFKGWMDIMYAAVDS
GEINSQPNWENNLYMYLYFVVFIIFGGFFTLNLFVGVIIDNFNQQKKKLGGQDIFMTEEQ
KKYYNAMKKLGSKKPQKPIPRPLNKYQGFVFDIVTRQAFDIIIMVLICLNMITMMVETDE
QGEEKTKVLGRINQFFVAVFTGECVMKMFALRQYYFTNGWNVFDFIVVILSIGSLLFSAI
LKSLENYFSPTLFRVIRLARIGRILRLIRAAKGIRTLLFALMMSLPALFNIGLLLFLVMF
IYSIFGMASFANVVDEAGIDDMFNFKTFGNSMLCLFQITTSAGWDGLLSPILNTGPPYCD
PNLPNSNGSRGNCGSPAVGIIFFTTYIIISFLIVVNMYIAVILENFNVATEESTEPLSED
DFDMFYETWEKFDPEATQFIAFSALSDFADTLSGPLRIPKPNQNILIQMDLPLVPGDKIH
CLDILFAFTKNVLGESGELDSLKTNMEEKFMATNLSKASYEPIATTLRWKQEDLSATVIQ
KAYRSYMLHRSLTLSNTLHVPRAEEDGVSLPGEGYVTFMANSGLPDKSETASATSFPPSY
DSVTRGLSDRANINPSSSMQNEDEVAAKEGNSPGPQ
Inhibitor 1-[5-(4-Chlorophenyl)-2-furoyl]piperazine Drug Info [529491]
5-(4-chlorophenyl)-N-(2-methylbenzyl)nicotinamide Drug Info [531169]
N-(2-chlorobenzyl)-5-(4-chlorophenyl)nicotinamide Drug Info [531169]
N-benzyl-5-(4-chlorophenyl)nicotinamide Drug Info [531169]
PD-32577 Drug Info [525576]
Binder New analgesic drugs Drug Info [534980]
References
Ref 525576Bioorg Med Chem Lett. 1999 Aug 16;9(16):2447-52.Synthesis and biological activity of substituted bis-(4-hydroxyphenyl)methanes as N-type calcium channel blockers.
Ref 529491Bioorg 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 531169Bioorg Med Chem Lett. 2010 Nov 15;20(22):6812-5. Epub 2010 Sep 18.Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives.
Ref 534980Pathobiology of visceral pain: molecular mechanisms and therapeutic implications. II. Genetic approaches to pain therapy. Am J Physiol Gastrointest Liver Physiol. 2000 Apr;278(4):G507-12.

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