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Target
Sodium channel protein type 10 subunit alpha
Ligand
BDBM50329206
Substrate
n/a
Meas. Tech.
ChEMBL_675099 (CHEMBL1272890)
IC50
32±n/a nM
Citation
 Kort, ME; Atkinson, RN; Thomas, JB; Drizin, I; Johnson, MS; Secrest, MA; Gregg, RJ; Scanio, MJ; Shi, L; Hakeem, AH; Matulenko, MA; Chapman, ML; Krambis, MJ; Liu, D; Shieh, CC; Zhang, X; Simler, G; Mikusa, JP; Zhong, C; Joshi, S; Honore, P; Roeloffs, R; Werness, S; Antonio, B; Marsh, KC; Faltynek, CR; Krafte, DS; Jarvis, MF; Marron, BE Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives. Bioorg Med Chem Lett 20:6812-5 (2010) [PubMed]  Article
Target
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:
MELPFASVGTTNFRRFTPESLAEIEKQIAAHRAAKKARTKHRGQEDKGEKPRPQLDLKACNQLPKFYGELPAELVGEPLEDLDPFYSTHRTFMVLNKSRTISRFSATWALWLFSPFNLIRRTAIKVSVHSWFSIFITITILVNCVCMTRTDLPEKVEYVFTVIYTFEALIKILARGFCLNEFTYLRDPWNWLDFSVITLAYVGAAIDLRGISGLRTFRVLRALKTVSVIPGLKVIVGALIHSVRKLADVTILTVFCLSVFALVGLQLFKGNLKNKCIRNGTDPHKADNLSSEMAEYIFIKPGTTDPLLCGNGSDAGHCPGGYVCLKTPDNPDFNYTSFDSFAWAFLSLFRLMTQDSWERLYQQTLRASGKMYMVFFVLVIFLGSFYLVNLILAVVTMAYEEQSQATIAEIEAKEKKFQEALEVLQKEQEVLAALGIDTTSLQSHSGSPLASKNANERRPRVKSRVSEGSTDDNRSPQSDPYNQRRMSFLGLSSGRRRASHGSVFHFRAPSQDISFPDGITDDGVFHGDQESRRGSILLGRGAGQTGPLPRSPLPQSPNPGRRHGEEGQLGVPTGELTAGAPEGPALDTTGQKSFLSAGYLNEPFRAQRAMSVVSIMTSVIEELEESKLKCPPCLISFAQKYLIWECCPKWRKFKMALFELVTDPFAELTITLCIVVNTVFMAMEHYPMTDAFDAMLQAGNIVFTVFFTMEMAFKIIAFDPYYYFQKKWNIFDCVIVTVSLLELSASKKGSLSVLRTFRLLRVFKLAKSWPTLNTLIKIIGNSVGALGNLTFILAIIVFIFALVGKQLLSEDYGCRKDGVSVWNGEKLRWHMCDFFHSFLVVFRILCGEWIENMWVCMEVSQKSICLILFLTVMVLGNLVVLNLFIALLLNSFSADNLTAPEDDGEVNNLQLALARIQVLGHRASRAIASYISSHCRFRWPKVETQLGMKPPLTSSEAKNHIATDAVSAAVGNLTKPALSSPKENHGDFITDPNVWVSVPIAEGESDLDELEEDMEQASQSSWQEEDPKGQQEQLPQVQKCENHQAARSPASMMSSEDLAPYLGESWKRKDSPQVPAEGVDDTSSSEGSTVDCPDPEEILRKIPELADDLDEPDDCFTEGCTRRCPCCNVNTSKSPWATGWQVRKTCYRIVEHSWFESFIIFMILLSSGALAFEDNYLEEKPRVKSVLEYTDRVFTFIFVFEMLLKWVAYGFKKYFTNAWCWLDFLIVNISLTSLIAKILEYSDVASIKALRTLRALRPLRALSRFEGMRVVVDALVGAIPSIMNVLLVCLIFWLIFSIMGVNLFAGKFSKCVDTRNNPFSNVNSTMVNNKSECHNQNSTGHFFWVNVKVNFDNVAMGYLALLQVATFKGWMDIMYAAVDSGEINSQPNWENNLYMYLYFVVFIIFGGFFTLNLFVGVIIDNFNQQKKKLGGQDIFMTEEQKKYYNAMKKLGSKKPQKPIPRPLNKYQGFVFDIVTRQAFDIIIMVLICLNMITMMVETDEQGEEKTKVLGRINQFFVAVFTGECVMKMFALRQYYFTNGWNVFDFIVVILSIGSLLFSAILKSLENYFSPTLFRVIRLARIGRILRLIRAAKGIRTLLFALMMSLPALFNIGLLLFLVMFIYSIFGMASFANVVDEAGIDDMFNFKTFGNSMLCLFQITTSAGWDGLLSPILNTGPPYCDPNLPNSNGSRGNCGSPAVGIIFFTTYIIISFLIVVNMYIAVILENFNVATEESTEPLSEDDFDMFYETWEKFDPEATQFIAFSALSDFADTLSGPLRIPKPNQNILIQMDLPLVPGDKIHCLDILFAFTKNVLGESGELDSLKTNMEEKFMATNLSKASYEPIATTLRWKQEDLSATVIQKAYRSYMLHRSLTLSNTLHVPRAEEDGVSLPGEGYVTFMANSGLPDKSETASATSFPPSYDSVTRGLSDRANINPSSSMQNEDEVAAKEGNSPGPQ
  
Inhibitor
Name:
BDBM50329206
Synonyms:
5-(4-chlorophenyl)-N-((2-ethoxypyridin-3-yl)methyl)nicotinamide | CHEMBL1270207
Type:
Small organic molecule
Emp. Form.:
C20H18ClN3O2
Mol. Mass.:
367.829
SMILES:
CCOc1ncccc1CNC(=O)c1cncc(c1)-c1ccc(Cl)cc1
Structure:
Search PDB for entries with ligand similarity: