Reaction Details |
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Target | Sodium channel protein type 8 subunit alpha |
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Ligand | BDBM342904 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1662524 (CHEMBL4012205) |
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IC50 | 16000±n/a nM |
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Citation | Weiss, MM; Dineen, TA; Marx, IE; Altmann, S; Boezio, A; Bregman, H; Chu-Moyer, M; DiMauro, EF; Feric Bojic, E; Foti, RS; Gao, H; Graceffa, R; Gunaydin, H; Guzman-Perez, A; Huang, H; Huang, L; Jarosh, M; Kornecook, T; Kreiman, CR; Ligutti, J; La, DS; Lin, MJ; Liu, D; Moyer, BD; Nguyen, HN; Peterson, EA; Rose, PE; Taborn, K; Youngblood, BD; Yu, V; Fremeau, RT Sulfonamides as Selective Na J Med Chem60:5969-5989 (2017) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Sodium channel protein type 8 subunit alpha |
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Name: | Sodium channel protein type 8 subunit alpha |
Synonyms: | MED | SCN8A | SCN8A_HUMAN | Sodium channel protein type 8 alpha subunit | Sodium channel protein type 8 subunit alpha | Sodium channel protein type VIII alpha subunit | Voltage-gated sodium channel subunit alpha Nav1.6 | ep nav1.6 |
Type: | PROTEIN |
Mol. Mass.: | 225271.59 |
Organism: | Homo sapiens (Human) |
Description: | ChEMBL_1516902 |
Residue: | 1980 |
Sequence: | MAARLLAPPGPDSFKPFTPESLANIERRIAESKLKKPPKADGSHREDDEDSKPKPNSDLE
AGKSLPFIYGDIPQGLVAVPLEDFDPYYLTQKTFVVLNRGKTLFRFSATPALYILSPFNL
IRRIAIKILIHSVFSMIIMCTILTNCVFMTFSNPPDWSKNVEYTFTGIYTFESLVKIIAR
GFCIDGFTFLRDPWNWLDFSVIMMAYITEFVNLGNVSALRTFRVLRALKTISVIPGLKTI
VGALIQSVKKLSDVMILTVFCLSVFALIGLQLFMGNLRNKCVVWPINFNESYLENGTKGF
DWEEYINNKTNFYTVPGMLEPLLCGNSSDAGQCPEGYQCMKAGRNPNYGYTSFDTFSWAF
LALFRLMTQDYWENLYQLTLRAAGKTYMIFFVLVIFVGSFYLVNLILAVVAMAYEEQNQA
TLEEAEQKEAEFKAMLEQLKKQQEEAQAAAMATSAGTVSEDAIEEEGEEGGGSPRSSSEI
SKLSSKSAKERRNRRKKRKQKELSEGEEKGDPEKVFKSESEDGMRRKAFRLPDNRIGRKF
SIMNQSLLSIPGSPFLSRHNSKSSIFSFRGPGRFRDPGSENEFADDEHSTVEESEGRRDS
LFIPIRARERRSSYSGYSGYSQGSRSSRIFPSLRRSVKRNSTVDCNGVVSLIGGPGSHIG
GRLLPEATTEVEIKKKGPGSLLVSMDQLASYGRKDRINSIMSVVTNTLVEELEESQRKCP
PCWYKFANTFLIWECHPYWIKLKEIVNLIVMDPFVDLAITICIVLNTLFMAMEHHPMTPQ
FEHVLAVGNLVFTGIFTAEMFLKLIAMDPYYYFQEGWNIFDGFIVSLSLMELSLADVEGL
SVLRSFRLLRVFKLAKSWPTLNMLIKIIGNSVGALGNLTLVLAIIVFIFAVVGMQLFGKS
YKECVCKINQDCELPRWHMHDFFHSFLIVFRVLCGEWIETMWDCMEVAGQAMCLIVFMMV
MVIGNLVVLNLFLALLLSSFSADNLAATDDDGEMNNLQISVIRIKKGVAWTKLKVHAFMQ
AHFKQREADEVKPLDELYEKKANCIANHTGADIHRNGDFQKNGNGTTSGIGSSVEKYIID
EDHMSFINNPNLTVRVPIAVGESDFENLNTEDVSSESDPEGSKDKLDDTSSSEGSTIDIK
PEVEEVPVEQPEEYLDPDACFTEGCVQRFKCCQVNIEEGLGKSWWILRKTCFLIVEHNWF
ETFIIFMILLSSGALAFEDIYIEQRKTIRTILEYADKVFTYIFILEMLLKWTAYGFVKFF
TNAWCWLDFLIVAVSLVSLIANALGYSELGAIKSLRTLRALRPLRALSRFEGMRVVVNAL
VGAIPSIMNVLLVCLIFWLIFSIMGVNLFAGKYHYCFNETSEIRFEIEDVNNKTECEKLM
EGNNTEIRWKNVKINFDNVGAGYLALLQVATFKGWMDIMYAAVDSRKPDEQPKYEDNIYM
YIYFVIFIIFGSFFTLNLFIGVIIDNFNQQKKKFGGQDIFMTEEQKKYYNAMKKLGSKKP
QKPIPRPLNKIQGIVFDFVTQQAFDIVIMMLICLNMVTMMVETDTQSKQMENILYWINLV
FVIFFTCECVLKMFALRHYYFTIGWNIFDFVVVILSIVGMFLADIIEKYFVSPTLFRVIR
LARIGRILRLIKGAKGIRTLLFALMMSLPALFNIGLLLFLVMFIFSIFGMSNFAYVKHEA
GIDDMFNFETFGNSMICLFQITTSAGWDGLLLPILNRPPDCSLDKEHPGSGFKGDCGNPS
VGIFFFVSYIIISFLIVVNMYIAIILENFSVATEESADPLSEDDFETFYEIWEKFDPDAT
QFIEYCKLADFADALEHPLRVPKPNTIELIAMDLPMVSGDRIHCLDILFAFTKRVLGDSG
ELDILRQQMEERFVASNPSKVSYEPITTTLRRKQEEVSAVVLQRAYRGHLARRGFICKKT
TSNKLENGGTHREKKESTPSTASLPSYDSVTKPEKEKQQRAEEGRRERAKRQKEVRESKC
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BDBM342904 |
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n/a |
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Name | BDBM342904 |
Synonyms: | 1-(2-fluoro-5-methoxy-3'-(trifluoromethyl)-4-biphenylyl)-N-3-isoxazolyl-6-isoquinolinesulfonamide | US9776995, Example 115 |
Type | Small organic molecule |
Emp. Form. | C26H17F4N3O4S |
Mol. Mass. | 543.489 |
SMILES | COc1cc(c(F)cc1-c1nccc2cc(ccc12)S(=O)(=O)Nc1ccon1)-c1cccc(c1)C(F)(F)F |
Structure |
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