Target
Sodium channel protein type 2 subunit alpha
Ligand
BDBM50031299
Substrate
n/a
Meas. Tech.
ChEMBL_552564 (CHEMBL954008)
IC50
10000±n/a nM
Citation
 Drizin, IGregg, RJScanio, MJShi, LGross, MFAtkinson, RNThomas, JBJohnson, MSCarroll, WAMarron, BEChapman, MLLiu, DKrambis, MJShieh, CCZhang, XHernandez, GGauvin, DMMikusa, JPZhu, CZJoshi, SHonore, PMarsh, KCRoeloffs, RWerness, SKrafte, DSJarvis, MFFaltynek, CRKort, ME Discovery of potent furan piperazine sodium channel blockers for treatment of neuropathic pain. Bioorg Med Chem 16:6379-86 (2008) [PubMed]  Article 
Target
Name:
Sodium channel protein type 2 subunit alpha
Synonyms:
HBSC II | NAC2 | SCN2A | SCN2A1 | SCN2A2 | SCN2A_HUMAN | Sodium (Site 2) | Sodium channel protein brain II subunit alpha | Sodium channel protein type 2 alpha subunit | Sodium channel protein type II alpha subunit | Voltage-gated sodium channel subunit alpha Nav1.2
Type:
Enzyme
Mol. Mass.:
227954.68
Organism:
Homo sapiens (Human)
Description:
Q99250
Residue:
2005
Sequence:
MAQSVLVPPGPDSFRFFTRESLAAIEQRIAEEKAKRPKQERKDEDDENGPKPNSDLEAGKSLPFIYGDIPPEMVSVPLEDLDPYYINKKTFIVLNKGKAISRFSATPALYILTPFNPIRKLAIKILVHSLFNMLIMCTILTNCVFMTMSNPPDWTKNVEYTFTGIYTFESLIKILARGFCLEDFTFLRDPWNWLDFTVITFAYVTEFVDLGNVSALRTFRVLRALKTISVIPGLKTIVGALIQSVKKLSDVMILTVFCLSVFALIGLQLFMGNLRNKCLQWPPDNSSFEINITSFFNNSLDGNGTTFNRTVSIFNWDEYIEDKSHFYFLEGQNDALLCGNSSDAGQCPEGYICVKAGRNPNYGYTSFDTFSWAFLSLFRLMTQDFWENLYQLTLRAAGKTYMIFFVLVIFLGSFYLINLILAVVAMAYEEQNQATLEEAEQKEAEFQQMLEQLKKQQEEAQAAAAAASAESRDFSGAGGIGVFSESSSVASKLSSKSEKELKNRRKKKKQKEQSGEEEKNDRVRKSESEDSIRRKGFRFSLEGSRLTYEKRFSSPHQSLLSIRGSLFSPRRNSRASLFSFRGRAKDIGSENDFADDEHSTFEDNDSRRDSLFVPHRHGERRHSNVSQASRASRVLPILPMNGKMHSAVDCNGVVSLVGGPSTLTSAGQLLPEGTTTETEIRKRRSSSYHVSMDLLEDPTSRQRAMSIASILTNTMEELEESRQKCPPCWYKFANMCLIWDCCKPWLKVKHLVNLVVMDPFVDLAITICIVLNTLFMAMEHYPMTEQFSSVLSVGNLVFTGIFTAEMFLKIIAMDPYYYFQEGWNIFDGFIVSLSLMELGLANVEGLSVLRSFRLLRVFKLAKSWPTLNMLIKIIGNSVGALGNLTLVLAIIVFIFAVVGMQLFGKSYKECVCKISNDCELPRWHMHDFFHSFLIVFRVLCGEWIETMWDCMEVAGQTMCLTVFMMVMVIGNLVVLNLFLALLLSSFSSDNLAATDDDNEMNNLQIAVGRMQKGIDFVKRKIREFIQKAFVRKQKALDEIKPLEDLNNKKDSCISNHTTIEIGKDLNYLKDGNGTTSGIGSSVEKYVVDESDYMSFINNPSLTVTVPIAVGESDFENLNTEEFSSESDMEESKEKLNATSSSEGSTVDIGAPAEGEQPEVEPEESLEPEACFTEDCVRKFKCCQISIEEGKGKLWWNLRKTCYKIVEHNWFETFIVFMILLSSGALAFEDIYIEQRKTIKTMLEYADKVFTYIFILEMLLKWVAYGFQVYFTNAWCWLDFLIVDVSLVSLTANALGYSELGAIKSLRTLRALRPLRALSRFEGMRVVVNALLGAIPSIMNVLLVCLIFWLIFSIMGVNLFAGKFYHCINYTTGEMFDVSVVNNYSECKALIESNQTARWKNVKVNFDNVGLGYLSLLQVATFKGWMDIMYAAVDSRNVELQPKYEDNLYMYLYFVIFIIFGSFFTLNLFIGVIIDNFNQQKKKFGGQDIFMTEEQKKYYNAMKKLGSKKPQKPIPRPANKFQGMVFDFVTKQVFDISIMILICLNMVTMMVETDDQSQEMTNILYWINLVFIVLFTGECVLKLISLRYYYFTIGWNIFDFVVVILSIVGMFLAELIEKYFVSPTLFRVIRLARIGRILRLIKGAKGIRTLLFALMMSLPALFNIGLLLFLVMFIYAIFGMSNFAYVKREVGIDDMFNFETFGNSMICLFQITTSAGWDGLLAPILNSGPPDCDPDKDHPGSSVKGDCGNPSVGIFFFVSYIIISFLVVVNMYIAVILENFSVATEESAEPLSEDDFEMFYEVWEKFDPDATQFIEFAKLSDFADALDPPLLIAKPNKVQLIAMDLPMVSGDRIHCLDILFAFTKRVLGESGEMDALRIQMEERFMASNPSKVSYEPITTTLKRKQEEVSAIIIQRAYRRYLLKQKVKKVSSIYKKDKGKECDGTPIKEDTLIDKLNENSTPEKTDMTPSTTSPPSYDSVTKPEKEKFEKDKSEKEDKGKDIRESKK
  
Inhibitor
Name:
BDBM50031299
Synonyms:
6-(2,3-Dichloro-phenyl)-[1,2,4]triazine-3,5-diamine | 6-(2,3-Dichloro-phenyl)-[1,2,4]triazine-3,5-diamine(lamotrigine) | 6-(2,3-dichlorophenyl)-1,2,4-triazine-3,5-diamine | BW-430C | CHEMBL741 | LAMOTRIGINE | Lamictal | Lamictal cd
Type:
Small organic molecule
Emp. Form.:
C9H7Cl2N5
Mol. Mass.:
256.091
SMILES:
Nc1nnc(c(N)n1)-c1cccc(Cl)c1Cl
Structure:
Search PDB for entries with ligand similarity: