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Target
Sodium channel protein type 10 subunit alpha
Ligand
BDBM50330932
Substrate
n/a
Meas. Tech.
ChEMBL_684074 (CHEMBL1286451)
IC50
480±n/a nM
Citation
 Scanio, MJ; Shi, L; Drizin, I; Gregg, RJ; Atkinson, RN; Thomas, JB; Johnson, MS; Chapman, ML; Liu, D; Krambis, MJ; Liu, Y; Shieh, CC; Zhang, X; Simler, GH; Joshi, S; Honore, P; Marsh, KC; Knox, A; Werness, S; Antonio, B; Krafte, DS; Jarvis, MF; Faltynek, CR; Marron, BE; Kort, 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 Chem 18:7816-25 (2010) [PubMed]  Article 
Target
Name:
Sodium channel protein type 10 subunit alpha
Synonyms:
SCNAA_MOUSE | Scn10a | Sns | Sodium channel protein type 10 subunit alpha | Sodium channel protein type X alpha subunit
Type:
PROTEIN
Mol. Mass.:
220545.77
Organism:
Mus musculus
Description:
ChEMBL_675096
Residue:
1958
Sequence:
MEFPFGSVGTTNFRRFTPESLAEIEKQIAAHRAAKKGRPKQRGQKDKSEKPRPQLDLKACNQLPRFYGELPAELVGEPLEDLDPFYSTHRTFIVLDKSRTISRFSATWALWLFSPFNLIRRTAIKVSVHSWFSIFITVTILVNCVCMTRTDLPEKLEYAFTVVYTFEALIKILARGFCLNEFTYLRDPWNWLDFSVITLAYVGAAIDLRGISGLRTFRVLRALKTVSVIPGLKVIVGALIHSVRKLADVTILTVFCLSVFALVGLQLFKGNLKNKCIKNGTDPHKADNLSSEMAGDIFIKPGTTDPLLCGNGSDAGHCPNDYVCRKTSDNPDFNYTSFDSFAWAFLSLFRLMTQDSWERLYQQTLRASGKMYMVFFVLVIFLGSFYLVNLILAVVTMAYEEQSQATIAEIEAKEKKFKEALEVLQKEQEVLAALGIDTTSLYSHNGSPLAPKNANERRPRVKSRMSEGSTDDNRSLQSDPYNQRRMSFLGLSSGRRRASHSSVFHFRAPSQDVSFPDGILDDGVFHGDQESRRSSILLGRGAGQAGPLPRSPLPQSPNPGPRRGEEGQRGVPTGELATGAPEGPALDAAGQKNFLSADYLNEPFRAQRAMSVVSIMTSVIEELEESKLKCPPCLISLAQKYLIWECCPKWKKFKMVLFELVTDPFAELTITLCIVVNTVFMAMEHYPMTDAFDAMLQAGNIVFTVFFTMEMAFKIIAFDPYYYFQKKWNIFDCVIVTVSLLELSTSKKGSLSVLRTFRLLRVFKLAKSWPTLNMLIKIIGNSVGALGNLTFILAIIVFIFALVGKQLLSENYGCRRDGISVWNGERLRWHMCDFFHSFLVVFRILCGEWIENMWVCMEVSQDYICLTLFLTVMVLGNLVVLNLFIALLLNSFSADNLTAPEDDGEVNNLQVALARIQVFGHRASRAITSYIRSHCRLRWPKVETQLGMKPPLTSCKAENHIATDAVNAAVGNLAKPALGGPKENHGDFITDPNVWVSVPIAEGESDLDELEEDVEHASQSSWQEESPKGQQELLQQVQKCEDHQAARSPPSGMSSEDLAPYLGERWQREESPRVPAEGVDDTSSSEGSTVDCPDPEEILRKIPELAEELDEPDDCFPEGCTRRCPCCKVNTSKFPWATGWQVRKTCYRIVEHSWFESFIIFMILLSSGALAFEDNYLEEKPRVKSVLEYTDRVFTFIFVFEMLLKWVAYGFKKYFTNAWCWLDFLIVNISLTSLIAKILEYSDVASIKALRTLRALRPLRALSRFEGMRVVVDALVGAIPSIMNVLLVCLIFWLIFSIMGVNLFAGKFSRCVDTRSNPFSVVNSTFVTNKSDCYNQNNTGHFFWVNVKVNFDNVAMGYLALLQVATFKGWMDIMYAAVDSRDINSQPNWEESLYMYLYFVVFIIFGGFFTLNLFVGVIIDNFNQQKKKLGGQDIFMTEEQKKYYNAMKKLGSKKPQKPIPRPLNKYQGFVFDIVTRQAFDIIIMALICLNMITMMVETDNQSEEKTKVLGRINQFFVAVFTGECVMKMFALRQYYFTNGWNVFDFIVVILSISSLLFSAILSSLESYFSPTLLRVIRLARIGRILRLIRAAKGIRTLLFALMMSLPALFNIGLLLFLVMFIYSIFGMASFANVIDEAGIDDMFNFKTFGNSMLCLFQITTSAGWDGLLSPILNTGPPYCDPNRPNSNGSKGNCGSPAVGILFFTTYIIISFLIVVNMYIAVILENFNVATEESTEPLSEDDFDMFYETWEKFDPEATQFIAFSALSDFADTLSGPLRIPKPNQNILIQMDLPLVPGDKIHCLDILFAFTKNVLGESGELDSLKTNMEEKFMATNLSKASYEPIATTLRCKQEDISATIIQKAYRNYMLQRSLMLSNPLHVPRAEEDGVSLPREGYVTFMANDNGGLPDKSETASATSFPPSYDSVTRGLSDRANISTSSSMQNEDEVTAKEGKSPGPQ
  
Inhibitor
Name:
BDBM50330932
Synonyms:
CHEMBL1276882 | N-((2-Morpholin-4-yl-pyridin-3-yl)methyl)-6-(4-cyanophenyl)-pyrazine-2-carboxamide
Type:
Small organic molecule
Emp. Form.:
C22H20F3N5O3
Mol. Mass.:
459.4211
SMILES:
FC(F)(F)Oc1ccc(cc1)-c1cncc(n1)C(=O)NCc1cccnc1N1CCOCC1
Structure:
Search PDB for entries with ligand similarity: