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TargetSodium channel protein type 10 subunit alpha
LigandBDBM50330933
Substrate/Competitorn/a
Meas. Tech.ChEMBL_684073 (CHEMBL1286450)
IC50 52±n/a nM
Citation Scanio, MJShi, LDrizin, IGregg, RJAtkinson, RNThomas, JBJohnson, MSChapman, MLLiu, DKrambis, MJLiu, YShieh, CCZhang, XSimler, GHJoshi, SHonore, PMarsh, KCKnox, AWerness, SAntonio, BKrafte, DSJarvis, MFFaltynek, CRMarron, BEKort, ME Discovery and biological evaluation of potent, selective, orally bioavailable, pyrazine-based blockers of the Na(v)1.8 sodium channel with efficacy in a model of neuropathic pain. Bioorg Med Chem18:7816-25 (2010) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Sodium channel protein type 10 subunit alpha
Name:Sodium channel protein type 10 subunit alpha
Synonyms:SCNAA_RAT | Scn10a | Sns | Sodium Channel | Sodium channel protein type X alpha subunit | Voltage-gated sodium channel subunit alpha Nav1.8
Type:Enzyme
Mol. Mass.:219724.17
Organism:Rattus norvegicus (Rat)
Description:Q62968
Residue:1956
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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50330933
n/a
NameBDBM50330933
Synonyms:CHEMBL1277514 | N-(3,5-Dimethylphenyl)-6-(4-chlorophenyl)-pyrazine-2-carboxamide
TypeSmall organic molecule
Emp. Form.C19H16ClN3O
Mol. Mass.337.803
SMILESCc1cc(C)cc(NC(=O)c2cncc(n2)-c2ccc(Cl)cc2)c1
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: