Target
Sodium channel protein type 10 subunit alpha
Ligand
BDBM50233762
Substrate
n/a
Meas. Tech.
ChEMBL_462444 (CHEMBL928309)
IC50
985±n/a nM
Citation
 London, CHoyt, SBParsons, WHWilliams, BSWarren, VATschirret-Guth, RSmith, MMPriest, BTMcGowan, EMartin, WJLyons, KALi, XKaranam, BVJochnowitz, NGarcia, MLFelix, JPDean, BAbbadie, CKaczorowski, GJDuffy, JL Imidazopyridines: a novel class of hNav1.7 channel blockers. Bioorg Med Chem Lett 18:1696-701 (2008) [PubMed]  Article 
Target
Name:
Sodium channel protein type 10 subunit alpha
Synonyms:
PN3 | Peripheral nerve sodium channel 3 | SCN10A | SCNAA_HUMAN | Sodium channel alpha subunit | Sodium channel protein type 10 subunit alpha | Sodium channel protein type X alpha subunit | Voltage-gated sodium channel subunit alpha Nav1.8 | fret-membrane potential nav1.8 | hPN3
Type:
Enzyme
Mol. Mass.:
220609.21
Organism:
Homo sapiens (Human)
Description:
Q9Y5Y9
Residue:
1956
Sequence:
MEFPIGSLETNNFRRFTPESLVEIEKQIAAKQGTKKAREKHREQKDQEEKPRPQLDLKACNQLPKFYGELPAELIGEPLEDLDPFYSTHRTFMVLNKGRTISRFSATRALWLFSPFNLIRRTAIKVSVHSWFSLFITVTILVNCVCMTRTDLPEKIEYVFTVIYTFEALIKILARGFCLNEFTYLRDPWNWLDFSVITLAYVGTAIDLRGISGLRTFRVLRALKTVSVIPGLKVIVGALIHSVKKLADVTILTIFCLSVFALVGLQLFKGNLKNKCVKNDMAVNETTNYSSHRKPDIYINKRGTSDPLLCGNGSDSGHCPDGYICLKTSDNPDFNYTSFDSFAWAFLSLFRLMTQDSWERLYQQTLRTSGKIYMIFFVLVIFLGSFYLVNLILAVVTMAYEEQNQATTDEIEAKEKKFQEALEMLRKEQEVLAALGIDTTSLHSHNGSPLTSKNASERRHRIKPRVSEGSTEDNKSPRSDPYNQRRMSFLGLASGKRRASHGSVFHFRSPGRDISLPEGVTDDGVFPGDHESHRGSLLLGGGAGQQGPLPRSPLPQPSNPDSRHGEDEHQPPPTSELAPGAVDVSAFDAGQKKTFLSAEYLDEPFRAQRAMSVVSIITSVLEELEESEQKCPPCLTSLSQKYLIWDCCPMWVKLKTILFGLVTDPFAELTITLCIVVNTIFMAMEHHGMSPTFEAMLQIGNIVFTIFFTAEMVFKIIAFDPYYYFQKKWNIFDCIIVTVSLLELGVAKKGSLSVLRSFRLLRVFKLAKSWPTLNTLIKIIGNSVGALGNLTIILAIIVFVFALVGKQLLGENYRNNRKNISAPHEDWPRWHMHDFFHSFLIVFRILCGEWIENMWACMEVGQKSICLILFLTVMVLGNLVVLNLFIALLLNSFSADNLTAPEDDGEVNNLQVALARIQVFGHRTKQALCSFFSRSCPFPQPKAEPELVVKLPLSSSKAENHIAANTARGSSGGLQAPRGPRDEHSDFIANPTVWVSVPIAEGESDLDDLEDDGGEDAQSFQQEVIPKGQQEQLQQVERCGDHLTPRSPGTGTSSEDLAPSLGETWKDESVPQVPAEGVDDTSSSEGSTVDCLDPEEILRKIPELADDLEEPDDCFTEGCIRHCPCCKLDTTKSPWDVGWQVRKTCYRIVEHSWFESFIIFMILLSSGSLAFEDYYLDQKPTVKALLEYTDRVFTFIFVFEMLLKWVAYGFKKYFTNAWCWLDFLIVNISLISLTAKILEYSEVAPIKALRTLRALRPLRALSRFEGMRVVVDALVGAIPSIMNVLLVCLIFWLIFSIMGVNLFAGKFWRCINYTDGEFSLVPLSIVNNKSDCKIQNSTGSFFWVNVKVNFDNVAMGYLALLQVATFKGWMDIMYAAVDSREVNMQPKWEDNVYMYLYFVIFIIFGGFFTLNLFVGVIIDNFNQQKKKLGGQDIFMTEEQKKYYNAMKKLGSKKPQKPIPRPLNKFQGFVFDIVTRQAFDITIMVLICLNMITMMVETDDQSEEKTKILGKINQFFVAVFTGECVMKMFALRQYYFTNGWNVFDFIVVVLSIASLIFSAILKSLQSYFSPTLFRVIRLARIGRILRLIRAAKGIRTLLFALMMSLPALFNIGLLLFLVMFIYSIFGMSSFPHVRWEAGIDDMFNFQTFANSMLCLFQITTSAGWDGLLSPILNTGPPYCDPNLPNSNGTRGDCGSPAVGIIFFTTYIIISFLIMVNMYIAVILENFNVATEESTEPLSEDDFDMFYETWEKFDPEATQFITFSALSDFADTLSGPLRIPKPNRNILIQMDLPLVPGDKIHCLDILFAFTKNVLGESGELDSLKANMEEKFMATNLSKSSYEPIATTLRWKQEDISATVIQKAYRSYVLHRSMALSNTPCVPRAEEEAASLPDEGFVAFTANENCVLPDKSETASATSFPPSYESVTRGLSDRVNMRTSSSIQNEDEATSMELIAPGP
  
Inhibitor
Name:
BDBM50233762
Synonyms:
(R)-tert-butyl 1-oxo-1-((3-(1-phenylcyclopropyl)-3H-imidazo[4,5-b]pyridin-2-yl)methylamino)-3-(2-(trifluoromethoxy)phenyl)propan-2-ylcarbamate | CHEMBL253660
Type:
Small organic molecule
Emp. Form.:
C31H32F3N5O4
Mol. Mass.:
595.6121
SMILES:
CC(C)(C)OC(=O)N[C@H](Cc1ccccc1OC(F)(F)F)C(=O)NCc1nc2cccnc2n1C1(CC1)c1ccccc1
Structure:
Search PDB for entries with ligand similarity: