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TargetVoltage-gated sodium channel subunit alpha Nav1.8
LigandBDBM50031299
Substrate/Competitorn/a
Meas. Tech.ChEMBL_552562
IC50 25000±n/a nM
Citation Drizin IGregg RJScanio MJShi LGross MFAtkinson RNThomas JBJohnson MSCarroll WAMarron BEChapman MLLiu DKrambis MJShieh CCZhang XHernandez GGauvin DMMikusa JPZhu CZJoshi SHonore PMarsh KCRoeloffs RWerness SKrafte DSJarvis MFFaltynek CRKort ME Discovery of potent furan piperazine sodium channel blockers for treatment of neuropathic pain. Bioorg Med Chem 16:6379-86 (2008) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Voltage-gated sodium channel subunit alpha Nav1.8
Name:Voltage-gated sodium channel subunit alpha Nav1.8
Synonyms:Sodium Channel | Sodium channel protein type X alpha subunit
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:
BDBM50031299
n/a
NameBDBM50031299
Synonyms:6-(2,3-Dichloro-phenyl)-[1,2,4]triazine-3,5-diamine | 6-(2,3-Dichloro-phenyl)-[1,2,4]triazine-3,5-diamine(lamotrigine) | 6-(2,3-dichlorophenyl)-1,2,4-triazine-3,5-diamine | BW-430C | CHEMBL741 | LAMOTRIGINE | Lamictal | Lamictal cd
TypeSmall organic molecule
Emp. Form.C9H7Cl2N5
Mol. Mass.256.091
SMILESNc1nnc(c(N)n1)-c1cccc(Cl)c1Cl
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: