| Reaction Details |
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 | Report a problem with these data |
| Target | Sodium channel protein type 4 subunit alpha |
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| Ligand | BDBM50257175 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEBML_1689579 |
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| IC50 | >30000±n/a nM |
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| Citation |  Swain, NA; Batchelor, D; Beaudoin, S; Bechle, BM; Bradley, PA; Brown, AD; Brown, B; Butcher, KJ; Butt, RP; Chapman, ML; Denton, S; Ellis, D; Galan, SRG; Gaulier, SM; Greener, BS; de Groot, MJ; Glossop, MS; Gurrell, IK; Hannam, J; Johnson, MS; Lin, Z; Markworth, CJ; Marron, BE; Millan, DS; Nakagawa, S; Pike, A; Printzenhoff, D; Rawson, DJ; Ransley, SJ; Reister, SM; Sasaki, K; Storer, RI; Stupple, PA; West, CW Discovery of Clinical Candidate 4-[2-(5-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-1,3-thiazol-4-ylbenzenesulfonamide (PF-05089771): Design and Optimization of Diaryl Ether Aryl Sulfonamides as Selective Inhibitors of Na J Med Chem60:7029-7042 (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 4 subunit alpha |
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| Name: | Sodium channel protein type 4 subunit alpha |
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| Synonyms: | SCN4A | SCN4A_HUMAN | SkM1 | Sodium channel alpha subunit | Sodium channel protein skeletal muscle subunit alpha | Sodium channel protein type 4 subunit alpha | Sodium channel protein type IV alpha subunit | Sodium channel protein type IV subunit alpha | Voltage-gated sodium channel subunit alpha Nav1.4 | Voltage-gated sodium channel subunit alpha Nav1.4 (Nav1.4) |
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| Type: | Protein |
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| Mol. Mass.: | 208010.01 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P35499 |
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| Residue: | 1836 |
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| Sequence: | MARPSLCTLVPLGPECLRPFTRESLAAIEQRAVEEEARLQRNKQMEIEEPERKPRSDLEA
GKNLPMIYGDPPPEVIGIPLEDLDPYYSNKKTFIVLNKGKAIFRFSATPALYLLSPFSVV
RRGAIKVLIHALFSMFIMITILTNCVFMTMSDPPPWSKNVEYTFTGIYTFESLIKILARG
FCVDDFTFLRDPWNWLDFSVIMMAYLTEFVDLGNISALRTFRVLRALKTITVIPGLKTIV
GALIQSVKKLSDVMILTVFCLSVFALVGLQLFMGNLRQKCVRWPPPFNDTNTTWYSNDTW
YGNDTWYGNEMWYGNDSWYANDTWNSHASWATNDTFDWDAYISDEGNFYFLEGSNDALLC
GNSSDAGHCPEGYECIKTGRNPNYGYTSYDTFSWAFLALFRLMTQDYWENLFQLTLRAAG
KTYMIFFVVIIFLGSFYLINLILAVVAMAYAEQNEATLAEDKEKEEEFQQMLEKFKKHQE
ELEKAKAAQALEGGEADGDPAHGKDCNGSLDTSQGEKGAPRQSSSGDSGISDAMEELEEA
HQKCPPWWYKCAHKVLIWNCCAPWLKFKNIIHLIVMDPFVDLGITICIVLNTLFMAMEHY
PMTEHFDNVLTVGNLVFTGIFTAEMVLKLIAMDPYEYFQQGWNIFDSIIVTLSLVELGLA
NVQGLSVLRSFRLLRVFKLAKSWPTLNMLIKIIGNSVGALGNLTLVLAIIVFIFAVVGMQ
LFGKSYKECVCKIALDCNLPRWHMHDFFHSFLIVFRILCGEWIETMWDCMEVAGQAMCLT
VFLMVMVIGNLVVLNLFLALLLSSFSADSLAASDEDGEMNNLQIAIGRIKLGIGFAKAFL
LGLLHGKILSPKDIMLSLGEADGAGEAGEAGETAPEDEKKEPPEEDLKKDNHILNHMGLA
DGPPSSLELDHLNFINNPYLTIQVPIASEESDLEMPTEEETDTFSEPEDSKKPPQPLYDG
NSSVCSTADYKPPEEDPEEQAEENPEGEQPEECFTEACVQRWPCLYVDISQGRGKKWWTL
RRACFKIVEHNWFETFIVFMILLSSGALAFEDIYIEQRRVIRTILEYADKVFTYIFIMEM
LLKWVAYGFKVYFTNAWCWLDFLIVDVSIISLVANWLGYSELGPIKSLRTLRALRPLRAL
SRFEGMRVVVNALLGAIPSIMNVLLVCLIFWLIFSIMGVNLFAGKFYYCINTTTSERFDI
SEVNNKSECESLMHTGQVRWLNVKVNYDNVGLGYLSLLQVATFKGWMDIMYAAVDSREKE
EQPQYEVNLYMYLYFVIFIIFGSFFTLNLFIGVIIDNFNQQKKKLGGKDIFMTEEQKKYY
NAMKKLGSKKPQKPIPRPQNKIQGMVYDLVTKQAFDITIMILICLNMVTMMVETDNQSQL
KVDILYNINMIFIIIFTGECVLKMLALRQYYFTVGWNIFDFVVVILSIVGLALSDLIQKY
FVSPTLFRVIRLARIGRVLRLIRGAKGIRTLLFALMMSLPALFNIGLLLFLVMFIYSIFG
MSNFAYVKKESGIDDMFNFETFGNSIICLFEITTSAGWDGLLNPILNSGPPDCDPNLENP
GTSVKGDCGNPSIGICFFCSYIIISFLIVVNMYIAIILENFNVATEESSEPLGEDDFEMF
YETWEKFDPDATQFIAYSRLSDFVDTLQEPLRIAKPNKIKLITLDLPMVPGDKIHCLDIL
FALTKEVLGDSGEMDALKQTMEEKFMAANPSKVSYEPITTTLKRKHEEVCAIKIQRAYRR
HLLQRSMKQASYMYRHSHDGSGDDAPEKEGLLANTMSKMYGHENGNSSSPSPEEKGEAGD
AGPTMGLMPISPSDTAWPPAPPPGQTVRPGVKESLV
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| BDBM50257175 |
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| n/a |
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| Name | BDBM50257175 |
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| Synonyms: | CHEMBL2324776 |
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| Type | Small organic molecule |
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| Emp. Form. | C19H10ClF4N5O3S2 |
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| Mol. Mass. | 531.891 |
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| SMILES | Fc1cc(Oc2ccc(cc2-c2ccnnc2)C(F)(F)F)c(Cl)cc1S(=O)(=O)Nc1nncs1 |
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| Structure | 
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