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Target
Sodium channel protein type 9 subunit alpha
Ligand
BDBM268499
Substrate
n/a
Meas. Tech.
Electrophysiological Assay (EP) (In Vitro Assay)
pH
7.2±n/a
IC50
66.0±n/a nM
Comments
extracted
Citation
 Bichler, PR; Chowdhury, S; Decker, SM; Dehnhardt, CM; Focken, T; Grimwood, ME; Hemeon, IW; Safina, B; Sheng, T; Sun, S; Wilson, MS; Zenova, AY Substituted triazolopyridines and methods of use thereof US Patent  US9550775 Publication Date 1/24/2017 
Target
Name:
Sodium channel protein type 9 subunit alpha
Synonyms:
NENA | Neuroendocrine sodium channel | Peripheral sodium channel 1 | SCN9A | SCN9A_HUMAN | Sodium channel protein type IX alpha subunit | Voltage-gated sodium channel subunit Nav1.7 | Voltage-gated sodium channel subunit alpha Nav1.7 | hNE-Na
Type:
Protein
Mol. Mass.:
226375.97
Organism:
Homo sapiens (Human)
Description:
Q15858
Residue:
1988
Sequence:
MAMLPPPGPQSFVHFTKQSLALIEQRIAERKSKEPKEEKKDDDEEAPKPSSDLEAGKQLPFIYGDIPPGMVSEPLEDLDPYYADKKTFIVLNKGKTIFRFNATPALYMLSPFSPLRRISIKILVHSLFSMLIMCTILTNCIFMTMNNPPDWTKNVEYTFTGIYTFESLVKILARGFCVGEFTFLRDPWNWLDFVVIVFAYLTEFVNLGNVSALRTFRVLRALKTISVIPGLKTIVGALIQSVKKLSDVMILTVFCLSVFALIGLQLFMGNLKHKCFRNSLENNETLESIMNTLESEEDFRKYFYYLEGSKDALLCGFSTDSGQCPEGYTCVKIGRNPDYGYTSFDTFSWAFLALFRLMTQDYWENLYQQTLRAAGKTYMIFFVVVIFLGSFYLINLILAVVAMAYEEQNQANIEEAKQKELEFQQMLDRLKKEQEEAEAIAAAAAEYTSIRRSRIMGLSESSSETSKLSSKSAKERRNRRKKKNQKKLSSGEEKGDAEKLSKSESEDSIRRKSFHLGVEGHRRAHEKRLSTPNQSPLSIRGSLFSARRSSRTSLFSFKGRGRDIGSETEFADDEHSIFGDNESRRGSLFVPHRPQERRSSNISQASRSPPMLPVNGKMHSAVDCNGVVSLVDGRSALMLPNGQLLPEVIIDKATSDDSGTTNQIHKKRRCSSYLLSEDMLNDPNLRQRAMSRASILTNTVEELEESRQKCPPWWYRFAHKFLIWNCSPYWIKFKKCIYFIVMDPFVDLAITICIVLNTLFMAMEHHPMTEEFKNVLAIGNLVFTGIFAAEMVLKLIAMDPYEYFQVGWNIFDSLIVTLSLVELFLADVEGLSVLRSFRLLRVFKLAKSWPTLNMLIKIIGNSVGALGNLTLVLAIIVFIFAVVGMQLFGKSYKECVCKINDDCTLPRWHMNDFFHSFLIVFRVLCGEWIETMWDCMEVAGQAMCLIVYMMVMVIGNLVVLNLFLALLLSSFSSDNLTAIEEDPDANNLQIAVTRIKKGINYVKQTLREFILKAFSKKPKISREIRQAEDLNTKKENYISNHTLAEMSKGHNFLKEKDKISGFGSSVDKHLMEDSDGQSFIHNPSLTVTVPIAPGESDLENMNAEELSSDSDSEYSKVRLNRSSSSECSTVDNPLPGEGEEAEAEPMNSDEPEACFTDGCVWRFSCCQVNIESGKGKIWWNIRKTCYKIVEHSWFESFIVLMILLSSGALAFEDIYIERKKTIKIILEYADKIFTYIFILEMLLKWIAYGYKTYFTNAWCWLDFLIVDVSLVTLVANTLGYSDLGPIKSLRTLRALRPLRALSRFEGMRVVVNALIGAIPSIMNVLLVCLIFWLIFSIMGVNLFAGKFYECINTTDGSRFPASQVPNRSECFALMNVSQNVRWKNLKVNFDNVGLGYLSLLQVATFKGWTIIMYAAVDSVNVDKQPKYEYSLYMYIYFVVFIIFGSFFTLNLFIGVIIDNFNQQKKKLGGQDIFMTEEQKKYYNAMKKLGSKKPQKPIPRPGNKIQGCIFDLVTNQAFDISIMVLICLNMVTMMVEKEGQSQHMTEVLYWINVVFIILFTGECVLKLISLRHYYFTVGWNIFDFVVVIISIVGMFLADLIETYFVSPTLFRVIRLARIGRILRLVKGAKGIRTLLFALMMSLPALFNIGLLLFLVMFIYAIFGMSNFAYVKKEDGINDMFNFETFGNSMICLFQITTSAGWDGLLAPILNSKPPDCDPKKVHPGSSVEGDCGNPSVGIFYFVSYIIISFLVVVNMYIAVILENFSVATEESTEPLSEDDFEMFYEVWEKFDPDATQFIEFSKLSDFAAALDPPLLIAKPNKVQLIAMDLPMVSGDRIHCLDILFAFTKRVLGESGEMDSLRSQMEERFMSANPSKVSYEPITTTLKRKQEDVSATVIQRAYRRYRLRQNVKNISSIYIKDGDRDDDLLNKKDMAFDNVNENSSPEKTDATSSTTSPPSYDSVTKPDKEKYEQDRTEKEDKGKDSKESKK
  
Inhibitor
Name:
BDBM268499
Synonyms:
N-(7-(adamantan-2-yloxy)-6-cyclopropyl-[1,2,4]triazolo-[4,3-a]pyridin-3-yl)cyclopropanesulfonamide | US9550775, 24 | US9550775, 79
Type:
Small organic molecule
Emp. Form.:
C22H28N4O3S
Mol. Mass.:
428.548
SMILES:
O=S(=O)(Nc1nnc2cc(OC3C4CC5CC(C4)CC3C5)c(cn12)C1CC1)C1CC1 |TLB:17:16:20:13.12.11,17:12:20:15.16.18,THB:11:19:15:13.17.12,11:12:15:19.20.18,10:11:20:15.16.18,(5.44,-4.2,;5.04,-2.71,;3.95,-3.8,;3.95,-1.62,;2.46,-2.02,;1.84,-3.42,;.31,-3.26,;-.01,-1.76,;-1.35,-.99,;-1.35,.55,;-2.68,1.32,;-4.01,.55,;-4.01,-.99,;-6.32,-.37,;-8.02,1.32,;-8.02,-.22,;-6.68,-.99,;-5.35,-1.76,;-6.68,1.32,;-5.35,1.32,;-6.68,2.09,;-.01,1.32,;1.32,.55,;1.32,-.99,;-.01,2.86,;.76,4.2,;-.78,4.2,;6.53,-2.31,;8.02,-2.71,;7.62,-1.22,)|
Structure:
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