Ki Summary

Reaction Details

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Target

Sodium channel protein type 5 subunit alpha

Ligand

BDBM343208

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_1662520 (CHEMBL4012201)

IC50

140±n/a nM

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

More Info.:

Get all data from this article, Assay Method

Sodium channel protein type 5 subunit alpha

Name:

Sodium channel protein type 5 subunit alpha

Synonyms:

Type:

Enzyme

Mol. Mass.:

226908.60

Organism:

Homo sapiens (Human)

Description:

Q14524

Residue:

2016

Sequence:

MANFLLPRGTSSFRRFTRESLAAIEKRMAEKQARGSTTLQESREGLPEEEAPRPQLDLQA
SKKLPDLYGNPPQELIGEPLEDLDPFYSTQKTFIVLNKGKTIFRFSATNALYVLSPFHPI
RRAAVKILVHSLFNMLIMCTILTNCVFMAQHDPPPWTKYVEYTFTAIYTFESLVKILARG
FCLHAFTFLRDPWNWLDFSVIIMAYTTEFVDLGNVSALRTFRVLRALKTISVISGLKTIV
GALIQSVKKLADVMVLTVFCLSVFALIGLQLFMGNLRHKCVRNFTALNGTNGSVEADGLV
WESLDLYLSDPENYLLKNGTSDVLLCGNSSDAGTCPEGYRCLKAGENPDHGYTSFDSFAW
AFLALFRLMTQDCWERLYQQTLRSAGKIYMIFFMLVIFLGSFYLVNLILAVVAMAYEEQN
QATIAETEEKEKRFQEAMEMLKKEHEALTIRGVDTVSRSSLEMSPLAPVNSHERRSKRRK
RMSSGTEECGEDRLPKSDSEDGPRAMNHLSLTRGLSRTSMKPRSSRGSIFTFRRRDLGSE
ADFADDENSTAGESESHHTSLLVPWPLRRTSAQGQPSPGTSAPGHALHGKKNSTVDCNGV
VSLLGAGDPEATSPGSHLLRPVMLEHPPDTTTPSEEPGGPQMLTSQAPCVDGFEEPGARQ
RALSAVSVLTSALEELEESRHKCPPCWNRLAQRYLIWECCPLWMSIKQGVKLVVMDPFTD
LTITMCIVLNTLFMALEHYNMTSEFEEMLQVGNLVFTGIFTAEMTFKIIALDPYYYFQQG
WNIFDSIIVILSLMELGLSRMSNLSVLRSFRLLRVFKLAKSWPTLNTLIKIIGNSVGALG
NLTLVLAIIVFIFAVVGMQLFGKNYSELRDSDSGLLPRWHMMDFFHAFLIIFRILCGEWI
ETMWDCMEVSGQSLCLLVFLLVMVIGNLVVLNLFLALLLSSFSADNLTAPDEDREMNNLQ
LALARIQRGLRFVKRTTWDFCCGLLRQRPQKPAALAAQGQLPSCIATPYSPPPPETEKVP
PTRKETRFEEGEQPGQGTPGDPEPVCVPIAVAESDTDDQEEDEENSLGTEEESSKQQESQ
PVSGGPEAPPDSRTWSQVSATASSEAEASASQADWRQQWKAEPQAPGCGETPEDSCSEGS
TADMTNTAELLEQIPDLGQDVKDPEDCFTEGCVRRCPCCAVDTTQAPGKVWWRLRKTCYH
IVEHSWFETFIIFMILLSSGALAFEDIYLEERKTIKVLLEYADKMFTYVFVLEMLLKWVA
YGFKKYFTNAWCWLDFLIVDVSLVSLVANTLGFAEMGPIKSLRTLRALRPLRALSRFEGM
RVVVNALVGAIPSIMNVLLVCLIFWLIFSIMGVNLFAGKFGRCINQTEGDLPLNYTIVNN
KSQCESLNLTGELYWTKVKVNFDNVGAGYLALLQVATFKGWMDIMYAAVDSRGYEEQPQW
EYNLYMYIYFVIFIIFGSFFTLNLFIGVIIDNFNQQKKKLGGQDIFMTEEQKKYYNAMKK
LGSKKPQKPIPRPLNKYQGFIFDIVTKQAFDVTIMFLICLNMVTMMVETDDQSPEKINIL
AKINLLFVAIFTGECIVKLAALRHYYFTNSWNIFDFVVVILSIVGTVLSDIIQKYFFSPT
LFRVIRLARIGRILRLIRGAKGIRTLLFALMMSLPALFNIGLLLFLVMFIYSIFGMANFA
YVKWEAGIDDMFNFQTFANSMLCLFQITTSAGWDGLLSPILNTGPPYCDPTLPNSNGSRG
DCGSPAVGILFFTTYIIISFLIVVNMYIAIILENFSVATEESTEPLSEDDFDMFYEIWEK
FDPEATQFIEYSVLSDFADALSEPLRIAKPNQISLINMDLPMVSGDRIHCMDILFAFTKR
VLGESGEMDALKIQMEEKFMAANPSKISYEPITTTLRRKHEEVSAMVIQRAFRRHLLQRS
LKHASFLFRQQAGSGLSEEDAPEREGLIAYVMSENFSRPLGPPSSSSISSTSFPPSYDSV
TRATSDNLQVRGSDYSHSEDLADFPPSPDRDRESIV

BDBM343208

n/a

Name

BDBM343208

Synonyms:

3-amino-4-(2-chloro-3'-fluoro-5-methoxy-4-biphenylyl)-N-3-isoxazolyl-7-cinnolinesulfonamide | US9776995, Example 446

Type

Small organic molecule

Emp. Form.

C24H17ClFN5O4S

Mol. Mass.

525.939

SMILES

COc1cc(c(Cl)cc1-c1c(N)nnc2cc(ccc12)S(=O)(=O)Nc1ccon1)-c1cccc(F)c1 |(.67,1.54,;-.67,.77,;-.67,-.77,;.67,-1.54,;.67,-3.08,;-.67,-3.85,;-.67,-5.39,;-2,-3.08,;-2,-1.54,;-3.33,-.77,;-4.67,-1.54,;-4.67,-3.08,;-6,-.77,;-6,.77,;-4.67,1.54,;-4.67,3.08,;-3.33,3.85,;-2,3.08,;-2,1.54,;-3.33,.77,;-3.33,5.39,;-4.67,6.16,;-4.67,4.62,;-2,6.16,;-.67,5.39,;.8,5.87,;1.7,4.62,;.8,3.37,;-.67,3.85,;2,-3.85,;2,-5.39,;3.33,-6.16,;4.67,-5.39,;4.67,-3.85,;6,-3.08,;3.33,-3.08,)|

Structure