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Target
Sodium channel protein type 10 subunit alpha
Ligand
BDBM560175
Substrate
n/a
Meas. Tech.
Biological Assay
IC50
6.60±n/a nM
Citation
 Arasappan, A; Bell, IM; Breslin, MJ; Bungard, CJ; Burgey, CS; Chobanian, HR; Cox, JM; Ginnetti, AT; Guiadeen, DG; Jones, KL; Layton, ME; Liu, H; Liu, J; Perkins, JJ; Stachel, SJ; Suen-Lai, LM; Wu, Z 2-amino-n-heteroaryl-nicotinamides as Nav1.8 inhibitors US Patent  US11377438 Publication Date 7/5/2022 
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:
BDBM560175
Synonyms:
US11377438, Example 215
Type:
Small organic molecule
Emp. Form.:
C20H25ClN4O3S
Mol. Mass.:
436.956
SMILES:
CC1CCC(CC1)c1nc(C)c(Cl)c(C)c1C(=O)Nc1ccnc(c1)S(N)(=O)=O |(2.67,-3.85,;1.33,-3.08,;,-3.85,;-1.33,-3.08,;-1.33,-1.54,;,-.77,;1.33,-1.54,;-2.67,-.77,;-4,-1.54,;-5.33,-.77,;-6.67,-1.54,;-5.33,.77,;-6.67,1.54,;-4,1.54,;-4,3.08,;-2.67,.77,;-1.33,1.54,;-1.33,3.08,;,.77,;1.33,1.54,;1.33,3.08,;2.67,3.85,;4,3.08,;4,1.54,;2.67,.77,;5.33,.77,;6.67,1.54,;4.56,-.56,;6.1,-.56,)|
Structure:
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