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Target
Sodium channel protein type 4 subunit alpha
Ligand
BDBM190243
Substrate
n/a
Meas. Tech.
Binding Assay
IC50
87±9 nM
Citation
 Du Bois, J; Mulcahy, J; Andresen, B; Yeomans, DC; Biswal, S Methods and compositions for studying, imaging, and treating pain US Patent  US9174999 Publication Date 11/3/2015 
Target
Name:
Sodium channel protein type 4 subunit alpha
Synonyms:
SCN4A_RAT | Scn4a | Sodium channel protein type IV alpha subunit | Voltage-gated sodium channel subunit alpha Nav1.4 | Voltage-gated sodium channel subunit alpha Nav1.4 (I757A) | Voltage-gated sodium channel subunit alpha Nav1.4 (M1240A)
Type:
Enzyme
Mol. Mass.:
208810.50
Organism:
Rattus norvegicus (Rat)
Description:
P15390
Residue:
1840
Sequence:
MASSSLPNLVPPGPHCLRPFTPESLAAIEQRAVEEEARLQRNKQMEIEEPERKPRSDLEAGKNLPLIYGDPPPEVIGIPLEDLDPYYSDKKTFIVLNKGKAIFRFSATPALYLLSPFSIVRRVAIKVLIHALFSMFIMITILTNCVFMTMSNPPSWSKHVEYTFTGIYTFESLIKMLARGFCIDDFTFLRDPWNWLDFSVITMAYVTEFVDLGNISALRTFRVLRALKTITVIPGLKTIVGALIQSVKKLSDVMILTVFCLSVFALVGLQLFMGNLRQKCVRWPPPMNDTNTTWYGNDTWYSNDTWYGNDTWYINDTWNSQESWAGNSTFDWEAYINDEGNFYFLEGSNDALLCGNSSDAGHCPEGYECIKAGRNPNYGYTSYDTFSWAFLALFRLMTQDYWENLFQLTLRAAGKTYMIFFVVIIFLGSFYLINLILAVVAMAYAEQNEATLAEDQEKEEEFQQMLEKYKKHQEELEKAKAAQALESGEEADGDPTHNKDCNGSLDASGEKGPPRPSCSADSAISDAMEELEEAHQKCPPWWYKCAHKVLIWNCCAPWVKFKHIIYLIVMDPFVDLGITICIVLNTLFMAMEHYPMTEHFDNVLSVGNLVFTGIFTAEMVLKLIAMDPYEYFQQGWNIFDSFIVTLSLVELGLANVQGLSVLRSFRLLRVFKLAKSWPTLNMLIKIIGNSVGALGNLTLVLAIIVFIFAVVGMQLFGKSYKECVCKIASDCNLPRWHMNDFFHSFLIVFRILCGEWIETMWDCMEVAGQAMCLTVFLMVMVIGNLVVLNLFLALLLSSFSADSLAASDEDGEMNNLQIAIGRIKWGIGFAKTFLLGLLRGKILSPKEIILSLGEPGGAGENAEESTPEDEKKEPPPEDKELKDNHILNHVGLTDGPRSSIELDHLNFINNPYLTIQVPIASEESDLEMPTEEETDAFSEPEDIKKPLQPLYDGNSSVCSTADYKPPEEDPEEQAEENPEGEQPEECFTEACVKRCPCLYVDISQGRGKMWWTLRRACFKIVEHNWFETFIVFMILLSSGALAFEDIYIEQRRVIRTILEYADKVFTYIFILEMLLKWVAYGFKVYFTNAWCWLDFLIVDVSIISLVANWLGYSELGPIKSLRTLRALRPLRALSRFEGMRVVVNALLGAIPSIMNVLLVCLIFWLIFSIMGVNLFAGKFYYCVNTTTSERFDISVVNNKSESESLMYTGQVRWMNVKVNYDNVGLGYLSLLQVATFKGWMDIMYAAVDSREKEEQPHYEVNLYMYLYFVIFIIFGSFFTLNLFIGVIIDNFNQQKKKFGGKDIFMTEEQKKYYNAMKKLGSKKPQKPIPRPQNKIQGMVYDFVTKQVFDISIMILICLNMVTMMVETDDQSQLKVDILYNINMVFIIIFTGECVLKMFALRHYYFTIGWNIFDFVVVILSIVGLALSDLIQKYFVSPTLFRVIRLARIGRVLRLIRGAKGIRTLLFALMMSLPALFNIGLLLFLVMFIYSIFGMSNFAYVKKESGIDDMFNFETFGNSIICLFEITTSAGWDGLLNPILNSGPPDCDPTLENPGTNVRGDCGNPSIGICFFCSYIIISFLIVVNMYIAIILENFNVATEESSEPLSEDDFEMFYETWEKFDPDATQFIDYSRLSDFVDTLQEPLKIAKPNKIKLITLDLPMVPGDKIHCLDILFALTKEVLGDSGEMDALKQTMEEKFMAANPSKVSYEPITTTLKRKQEEVCAIKIQRAYRRHLLQRSVKQASYMYRHSQDGNDDGAPEKEGLLANTMNKMYGHEKEGDGVQSQGEEEKASTEDAGPTVEPEPTSSSDTALTPSPPPLPPSSSPPQGQTVRPGVKESLV
  
Inhibitor
Name:
BDBM190243
Synonyms:
US9174999, 12
Type:
Small organic molecule
Emp. Form.:
C27H35N7O6
Mol. Mass.:
553.609
SMILES:
OC1(O)CCCC(=[NH2+])NC(COC(=O)NCCNC(=O)c2ccc(cc2)C(=O)c2ccccc2)C2NC(=[NH2+])NC12
Structure:
Search PDB for entries with ligand similarity: