General Information of the Protein
Protein ID
PT01105
Protein Name
Sodium channel protein type 5 subunit alpha
Secondarily
Protein Name
Sodium channel protein cardiac muscle subunit alpha
Sodium channel protein type V subunit alpha
Voltage-gated sodium channel subunit alpha Nav1.5
hH1
Gene Name
SCN5A
Sequence
MANFLLPRGTSSFRRFTRESLAAIEKRMAEKQARGSTTLQESREGLPEEEAPRPQLDLQASKKLPDLYGNPPQELIGEPLEDLDPFYSTQKTFIVLNKGKTIFRFSATNALYVLSPFHPIRRAAVKILVHSLFNMLIMCTILTNCVFMAQHDPPPWTKYVEYTFTAIYTFESLVKILARGFCLHAFTFLRDPWNWLDFSVIIMAYTTEFVDLGNVSALRTFRVLRALKTISVISGLKTIVGALIQSVKKLADVMVLTVFCLSVFALIGLQLFMGNLRHKCVRNFTALNGTNGSVEADGLVWESLDLYLSDPENYLLKNGTSDVLLCGNSSDAGTCPEGYRCLKAGENPDHGYTSFDSFAWAFLALFRLMTQDCWERLYQQTLRSAGKIYMIFFMLVIFLGSFYLVNLILAVVAMAYEEQNQATIAETEEKEKRFQEAMEMLKKEHEALTIRGVDTVSRSSLEMSPLAPVNSHERRSKRRKRMSSGTEECGEDRLPKSDSEDGPRAMNHLSLTRGLSRTSMKPRSSRGSIFTFRRRDLGSEADFADDENSTAGESESHHTSLLVPWPLRRTSAQGQPSPGTSAPGHALHGKKNSTVDCNGVVSLLGAGDPEATSPGSHLLRPVMLEHPPDTTTPSEEPGGPQMLTSQAPCVDGFEEPGARQRALSAVSVLTSALEELEESRHKCPPCWNRLAQRYLIWECCPLWMSIKQGVKLVVMDPFTDLTITMCIVLNTLFMALEHYNMTSEFEEMLQVGNLVFTGIFTAEMTFKIIALDPYYYFQQGWNIFDSIIVILSLMELGLSRMSNLSVLRSFRLLRVFKLAKSWPTLNTLIKIIGNSVGALGNLTLVLAIIVFIFAVVGMQLFGKNYSELRDSDSGLLPRWHMMDFFHAFLIIFRILCGEWIETMWDCMEVSGQSLCLLVFLLVMVIGNLVVLNLFLALLLSSFSADNLTAPDEDREMNNLQLALARIQRGLRFVKRTTWDFCCGLLRQRPQKPAALAAQGQLPSCIATPYSPPPPETEKVPPTRKETRFEEGEQPGQGTPGDPEPVCVPIAVAESDTDDQEEDEENSLGTEEESSKQQESQPVSGGPEAPPDSRTWSQVSATASSEAEASASQADWRQQWKAEPQAPGCGETPEDSCSEGSTADMTNTAELLEQIPDLGQDVKDPEDCFTEGCVRRCPCCAVDTTQAPGKVWWRLRKTCYHIVEHSWFETFIIFMILLSSGALAFEDIYLEERKTIKVLLEYADKMFTYVFVLEMLLKWVAYGFKKYFTNAWCWLDFLIVDVSLVSLVANTLGFAEMGPIKSLRTLRALRPLRALSRFEGMRVVVNALVGAIPSIMNVLLVCLIFWLIFSIMGVNLFAGKFGRCINQTEGDLPLNYTIVNNKSQCESLNLTGELYWTKVKVNFDNVGAGYLALLQVATFKGWMDIMYAAVDSRGYEEQPQWEYNLYMYIYFVIFIIFGSFFTLNLFIGVIIDNFNQQKKKLGGQDIFMTEEQKKYYNAMKKLGSKKPQKPIPRPLNKYQGFIFDIVTKQAFDVTIMFLICLNMVTMMVETDDQSPEKINILAKINLLFVAIFTGECIVKLAALRHYYFTNSWNIFDFVVVILSIVGTVLSDIIQKYFFSPTLFRVIRLARIGRILRLIRGAKGIRTLLFALMMSLPALFNIGLLLFLVMFIYSIFGMANFAYVKWEAGIDDMFNFQTFANSMLCLFQITTSAGWDGLLSPILNTGPPYCDPTLPNSNGSRGDCGSPAVGILFFTTYIIISFLIVVNMYIAIILENFSVATEESTEPLSEDDFDMFYEIWEKFDPEATQFIEYSVLSDFADALSEPLRIAKPNQISLINMDLPMVSGDRIHCMDILFAFTKRVLGESGEMDALKIQMEEKFMAANPSKISYEPITTTLRRKHEEVSAMVIQRAFRRHLLQRSLKHASFLFRQQAGSGLSEEDAPEREGLIAYVMSENFSRPLGPPSSSSISSTSFPPSYDSVTRATSDNLQVRGSDYSHSEDLADFPPSPDRDRESIV
    Show/Hide
Organism
Homo sapiens, Human
Protein Classification
Ion channel
>
Voltage-gated ion channel
>
Voltage-gated sodium channel
Function
This protein mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical gradient (PubMed:1309946, PubMed:21447824, PubMed:25370050, PubMed:23420830, PubMed:23085483, PubMed:26279430, PubMed:26392562, PubMed:26776555). It is a tetrodotoxin-resistant Na(+) channel isoform (PubMed:1309946). This channel is responsible for the initial upstroke of the action potential. Channel inactivation is regulated by intracellular calcium levels (PubMed:19074138).
    Show/Hide
Uniprot ID
Primary ID:
Q14524

Secondarily ID:
A5H1P8
A6N922
A6N923
B2RTU0
E7ET19
E9PEF3
E9PEK2
E9PFW7
Q59H93
Q75RX9
Q75RY0
Q86UR3
Q8IZC9
Q96J69
    Show/Hide
HGNC ID
HGNC:10593
Subcellular Location
Cell membrane
Cytoplasm
Perinuclear region
Cell membrane
Sarcolemma
T-tubule
Cell junction
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000011 , CHO
Compound ID Compound Name Compound Formula
CP0375108
4-butoxy-N-[N'-(4-phenylbutyl)carbamimidoyl]benzamide
   Show/Hide
C22H29N3O2
 1
1
IC50 = 560 nM
   TI
   LI
   LO
   TS
CP0444107
4-ethoxy-N-[N'-(4-phenylbutyl)carbamimidoyl]benzamide
   Show/Hide
C20H25N3O2
 1
1
IC50 = 1100 nM
   TI
   LI
   LO
   TS
CP0391416
3,4,5-trimethoxy-N-[N'-(4-phenylbutyl)carbamimidoyl]benzamide
   Show/Hide
C21H27N3O4
 1
1
IC50 = 1510 nM
   TI
   LI
   LO
   TS
CP0453500
2-methyl-N-[N'-(4-phenylbutyl)carbamimidoyl]benzamide
   Show/Hide
C19H23N3O
 1
1
IC50 = 1750 nM
   TI
   LI
   LO
   TS
CP0430912
N-[N'-[2-(5-methoxy-1H-indol-3-yl)ethyl]carbamimidoyl]-4-methylbenzamide
   Show/Hide
C20H22N4O2
 1
1
IC50 = 1760 nM
   TI
   LI
   LO
   TS
CP0452262
N-[(3S)-5-(4-methylpiperazin-1-yl)-3,4-dihydro-2H-chromen-3-yl]-4-(trifluoromethoxy)benzamide
   Show/Hide
C22H24F3N3O3
 1
1
IC50 = 1995.26 nM
   TI
   LI
   LO
   TS
CP0453220
4-methoxy-N-[N'-(4-phenylbutyl)carbamimidoyl]benzamide
   Show/Hide
C19H23N3O2
 1
1
IC50 = 2100 nM
   TI
   LI
   LO
   TS
CP0437894
N-[N'-(4-phenylbutyl)carbamimidoyl]thiophene-2-carboxamide
   Show/Hide
C16H19N3OS
 1
1
IC50 = 2350 nM
   TI
   LI
   LO
   TS
CP0493834
2-(2,4-dimethylphenyl)-5-methyl-N-[(3S)-5-(4-methylpiperazin-1-yl)-3,4-dihydro-2H-chromen-3-yl]triazole-4-carboxamide
   Show/Hide
C26H32N6O2
 1
1
IC50 = 2511.89 nM
   TI
   LI
   LO
   TS
CP0375122
2,3-dichloro-N-[N'-(4-phenylbutyl)carbamimidoyl]benzamide
   Show/Hide
C18H19Cl2N3O
 1
1
IC50 = 2710 nM
   TI
   LI
   LO
   TS
CP0453181
4-methyl-N-[N'-(4-phenylbutyl)carbamimidoyl]benzamide
   Show/Hide
C19H23N3O
 1
1
IC50 = 2850 nM
   TI
   LI
   LO
   TS
CP0377581
N-[(3S)-5-pyridin-4-yl-3,4-dihydro-2H-chromen-3-yl]-6-(2,2,2-trifluoroethoxy)pyridine-3-carboxamide
   Show/Hide
C22H18F3N3O3
 1
1
IC50 = 3162.28 nM
   TI
   LI
   LO
   TS
CP0452264
N-[(3S)-5-pyridin-3-yl-3,4-dihydro-2H-chromen-3-yl]-6-(2,2,2-trifluoroethoxy)pyridine-3-carboxamide
   Show/Hide
C22H18F3N3O3
 1
1
IC50 = 3162.28 nM
   TI
   LI
   LO
   TS
CP0506417
N-[(3S)-5-pyridin-3-yl-3,4-dihydro-2H-chromen-3-yl]-4-(trifluoromethoxy)benzamide
   Show/Hide
C22H17F3N2O3
 1
1
IC50 = 3162.28 nM
   TI
   LI
   LO
   TS
CP0011846
1-(2-(2-hydroxy-3-(propylamino)propoxy)phenyl)-3-phenylpropan-1-one
   Show/Hide
C21H27NO3
 2
1
IC50 = 3300 nM
   TI
   LI
   LO
   TS
2
IC50 > 5000 nM
   TI
   LI
   LO
   TS
CP0414861
4-methyl-N-[N'-(5-phenylpentyl)carbamimidoyl]benzamide
   Show/Hide
C20H25N3O
 1
1
IC50 = 3600 nM
   TI
   LI
   LO
   TS
CP0440191
4-chloro-N-[N'-(4-phenylbutyl)carbamimidoyl]benzamide
   Show/Hide
C18H20ClN3O
 1
1
IC50 = 3600 nM
   TI
   LI
   LO
   TS
CP0434432
N-[N'-[2-(4-methoxy-1H-indol-3-yl)ethyl]carbamimidoyl]-4-methylbenzamide
   Show/Hide
C20H22N4O2
 1
1
IC50 = 3920 nM
   TI
   LI
   LO
   TS
CP0377578
N-[(3S)-5-pyridin-4-yl-3,4-dihydro-2H-chromen-3-yl]-4-(trifluoromethoxy)benzamide
   Show/Hide
C22H17F3N2O3
 1
1
IC50 = 3981.07 nM
   TI
   LI
   LO
   TS
CP0416294
N-[(3S)-5-pyrimidin-5-yl-3,4-dihydro-2H-chromen-3-yl]-6-(3,3,3-trifluoropropoxy)pyridine-3-carboxamide
   Show/Hide
C22H19F3N4O3
 1
1
IC50 = 3981.07 nM
   TI
   LI
   LO
   TS
CP0436277
N-[(3S)-5-(5-fluoro-6-methoxypyridin-3-yl)-3,4-dihydro-2H-chromen-3-yl]-6-(2,2,2-trifluoroethoxy)pyridine-3-carboxamide
   Show/Hide
C23H19F4N3O4
 1
1
IC50 = 3981.07 nM
   TI
   LI
   LO
   TS
CP0452260
N-[(3S)-5-(2-methoxypyrimidin-5-yl)-3,4-dihydro-2H-chromen-3-yl]-6-(3,3,3-trifluoropropoxy)pyridine-3-carboxamide
   Show/Hide
C23H21F3N4O4
 1
1
IC50 = 3981.07 nM
   TI
   LI
   LO
   TS
CP0492729
N-[N'-(4-phenylbutyl)carbamimidoyl]naphthalene-1-carboxamide
   Show/Hide
C22H23N3O
 1
1
IC50 = 4100 nM
   TI
   LI
   LO
   TS
CP0409607
4-methyl-N-[N'-(2-propan-2-ylphenyl)carbamimidoyl]benzamide
   Show/Hide
C18H21N3O
 1
1
IC50 = 4500 nM
   TI
   LI
   LO
   TS
CP0478841
[(3aS,4R,10aS)-2,6-diamino-10,10-dihydroxy-3a,4,8,9-tetrahydro-1H-pyrrolo[1,2-c]purin-4-yl]methyl acetate
   Show/Hide
C11H18N6O4
 1
1
IC50 = 4566 nM
   TI
   LI
   LO
   TS
CP0377579
5-methyl-N-[(3S)-5-(4-methylpiperazin-1-yl)-3,4-dihydro-2H-chromen-3-yl]-2-phenyltriazole-4-carboxamide
   Show/Hide
C24H28N6O2
 1
1
IC50 = 5011.87 nM
   TI
   LI
   LO
   TS
CP0416296
N-[(3S)-5-(2-methylpyrimidin-5-yl)-3,4-dihydro-2H-chromen-3-yl]-6-(2,2,2-trifluoroethoxy)pyridine-3-carboxamide
   Show/Hide
C22H19F3N4O3
 1
1
IC50 = 5011.87 nM
   TI
   LI
   LO
   TS
CP0443557
N-[(3S)-5-(4-methylpiperazin-1-yl)-3,4-dihydro-2H-chromen-3-yl]-6-(3,3,3-trifluoropropoxy)pyridine-3-carboxamide
   Show/Hide
C23H27F3N4O3
 1
1
IC50 = 5011.87 nM
   TI
   LI
   LO
   TS
CP0452263
N-[(3S)-5-(4-methylpiperazin-1-yl)-3,4-dihydro-2H-chromen-3-yl]-6-(2,2,2-trifluoroethoxy)pyridine-3-carboxamide
   Show/Hide
C22H25F3N4O3
 1
1
IC50 = 5011.87 nM
   TI
   LI
   LO
   TS
CP0452265
N-[(3S)-5-[6-(hydroxymethyl)-5-methylpyridin-3-yl]-3,4-dihydro-2H-chromen-3-yl]-6-[2-(2,2,2-trifluoroethoxy)ethoxy]pyridine-3-carboxamide
   Show/Hide
C26H26F3N3O5
 1
1
IC50 = 5011.87 nM
   TI
   LI
   LO
   TS
CP0454740
4-methyl-N-[N'-(3-phenylpropyl)carbamimidoyl]benzamide
   Show/Hide
C18H21N3O
 1
1
IC50 = 5250 nM
   TI
   LI
   LO
   TS
CP0427278
2,6-dichloro-N-[N'-(4-phenylbutyl)carbamimidoyl]benzamide
   Show/Hide
C18H19Cl2N3O
 1
1
IC50 = 5400 nM
   TI
   LI
   LO
   TS
CP0453499
4-methyl-N-[N'-(3-phenoxypropyl)carbamimidoyl]benzamide
   Show/Hide
C18H21N3O2
 1
1
IC50 = 5600 nM
   TI
   LI
   LO
   TS
CP0526927
4-methyl-N-[N'-(2-phenylethyl)carbamimidoyl]benzamide
   Show/Hide
C17H19N3O
 1
1
IC50 = 5650 nM
   TI
   LI
   LO
   TS
CP0501921
4-methyl-N-[N'-(4-propan-2-yloxyphenyl)carbamimidoyl]benzamide
   Show/Hide
C18H21N3O2
 1
1
IC50 = 5750 nM
   TI
   LI
   LO
   TS
CP0076201
N-[(3S)-5-[6-(hydroxymethyl)pyridin-3-yl]-3,4-dihydro-2H-chromen-3-yl]-6-(2,2,2-trifluoroethoxy)pyridine-3-carboxamide
   Show/Hide
C23H20F3N3O4
 1
1
IC50 = 6309.57 nM
   TI
   LI
   LO
   TS
CP0416293
N-[(3S)-5-[2-(hydroxymethyl)pyridin-4-yl]-3,4-dihydro-2H-chromen-3-yl]-6-(2,2,2-trifluoroethoxy)pyridine-3-carboxamide
   Show/Hide
C23H20F3N3O4
 1
1
IC50 = 6309.57 nM
   TI
   LI
   LO
   TS
CP0416295
N-[(3S)-5-(2-methoxypyrimidin-5-yl)-3,4-dihydro-2H-chromen-3-yl]-6-(2,2,2-trifluoroethoxy)pyridine-3-carboxamide
   Show/Hide
C22H19F3N4O4
 1
1
IC50 = 6309.57 nM
   TI
   LI
   LO
   TS
CP0441744
2,5-dichloro-N-[N'-(4-phenylbutyl)carbamimidoyl]benzamide
   Show/Hide
C18H19Cl2N3O
 1
1
IC50 = 7890 nM
   TI
   LI
   LO
   TS
CP0448195
N-[N'-(4-phenylbutyl)carbamimidoyl]furan-2-carboxamide
   Show/Hide
C16H19N3O2
 1
1
IC50 = 7900 nM
   TI
   LI
   LO
   TS
CP0443558
N-[(3S)-5-[6-(hydroxymethyl)pyridin-3-yl]-3,4-dihydro-2H-chromen-3-yl]-6-[2-(2,2,2-trifluoroethoxy)ethoxy]pyridine-3-carboxamide
   Show/Hide
C25H24F3N3O5
 1
1
IC50 = 7943.28 nM
   TI
   LI
   LO
   TS
CP0430923
N-[N'-[2-(4-chlorophenyl)ethyl]carbamimidoyl]-4-methylbenzamide
   Show/Hide
C17H18ClN3O
 1
1
IC50 = 8500 nM
   TI
   LI
   LO
   TS
CP0497887
4-methyl-N-[N'-(naphthalen-1-ylmethyl)carbamimidoyl]benzamide
   Show/Hide
C20H19N3O
 1
1
IC50 = 8850 nM
   TI
   LI
   LO
   TS
CP0381027
N-(N'-butylcarbamimidoyl)-4-methylbenzamide
   Show/Hide
C13H19N3O
 1
1
IC50 = 9000 nM
   TI
   LI
   LO
   TS
CP0406161
4-methyl-N-[N'-methyl-N-(4-phenylbutyl)carbamimidoyl]benzamide
   Show/Hide
C20H25N3O
 1
1
IC50 = 9000 nM
   TI
   LI
   LO
   TS
CP0377577
N-[(3S)-5-[6-(1-hydroxyethyl)pyridin-3-yl]-3,4-dihydro-2H-chromen-3-yl]-6-[2-(2,2,2-trifluoroethoxy)ethoxy]pyridine-3-carboxamide
   Show/Hide
C26H26F3N3O5
 1
1
IC50 = 10000 nM
   TI
   LI
   LO
   TS
CP0433781
N-[(3S)-5-(2-methoxypyrimidin-5-yl)-3,4-dihydro-2H-chromen-3-yl]-6-(2,2,2-trifluoroethoxymethyl)pyridine-3-carboxamide
   Show/Hide
C23H21F3N4O4
 1
1
IC50 = 10000 nM
   TI
   LI
   LO
   TS
CP0400789
(5-chloro-1-methylindol-2-yl)-[6-[(dimethylamino)methyl]-3,4-dihydro-1H-isoquinolin-2-yl]methanone
   Show/Hide
C22H24ClN3O
 1
1
IC50 = 10300 nM
   TI
   LI
   LO
   TS
CP0430694
4-methyl-N-[N'-(2-thiophen-2-ylethyl)carbamimidoyl]benzamide
   Show/Hide
C15H17N3OS
 1
1
IC50 = 10500 nM
   TI
   LI
   LO
   TS
CP0383088
N-[N'-(2-benzylsulfanylethyl)carbamimidoyl]-4-methylbenzamide
   Show/Hide
C18H21N3OS
 1
1
IC50 = 10800 nM
   TI
   LI
   LO
   TS
CP0062157
N-[(3S)-5-(5-methoxypyrazin-2-yl)-3,4-dihydro-2H-chromen-3-yl]-6-(2,2,2-trifluoroethoxymethyl)pyridine-3-carboxamide
   Show/Hide
C23H21F3N4O4
 1
1
IC50 = 12589.25 nM
   TI
   LI
   LO
   TS
CP0383545
4-methyl-N-[N'-(2-phenoxyethyl)carbamimidoyl]benzamide
   Show/Hide
C17H19N3O2
 1
1
IC50 = 14200 nM
   TI
   LI
   LO
   TS
CP0524330
3,4-dichloro-N-[N'-(4-phenylbutyl)carbamimidoyl]benzamide
   Show/Hide
C18H19Cl2N3O
 1
1
IC50 = 15500 nM
   TI
   LI
   LO
   TS
CP0430911
4-methyl-N-[N'-(4-propan-2-ylphenyl)carbamimidoyl]benzamide
   Show/Hide
C18H21N3O
 1
1
IC50 = 19700 nM
   TI
   LI
   LO
   TS
CP0377582
N-[(3S)-5-(5-methylpyrazin-2-yl)-3,4-dihydro-2H-chromen-3-yl]-6-(2,2,2-trifluoroethoxymethyl)pyridine-3-carboxamide
   Show/Hide
C23H21F3N4O3
 1
1
IC50 = 19952.62 nM
   TI
   LI
   LO
   TS
CP0508613
4-methyl-N-[N'-(3,4,5-trimethoxyphenyl)carbamimidoyl]benzamide
   Show/Hide
C18H21N3O4
 1
1
IC50 = 24350 nM
   TI
   LI
   LO
   TS
CP0523038
N-[(3S)-5-(5-methoxypyrazin-2-yl)-3,4-dihydro-2H-chromen-3-yl]-6-(2,2,2-trifluoroethoxy)pyridine-3-carboxamide
   Show/Hide
C22H19F3N4O4
 1
1
IC50 > 25118.86 nM
   TI
   LI
   LO
   TS
CP0271660
(R)-1-(Methylsulfonylamino)-3-[2-(4-methoxyphenyl)ethyl]-4-(4-methoxy-phenyl)-2-imidazolidinone
   Show/Hide
C20H25N3O5S
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0163715
5-chloro-4-[3-oxo-4-[[2-(trifluoromethyl)phenyl]methyl]piperazin-1-yl]-1H-pyridazin-6-one
   Show/Hide
C16H14ClF3N4O2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0372478
N-[(5-chloro-6-oxo-1H-pyridin-3-yl)-(4-fluorophenyl)methyl]-2-[1-[[1-[4-(trifluoromethyl)phenyl]pyrrol-3-yl]methyl]piperidin-4-yl]acetamide
   Show/Hide
C31H29ClF4N4O2
 1
1
IC50 > 31600 nM
   TI
   LI
   LO
   TS
CP0436279
2-(2-methoxyethyl)-5-methyl-N-[(3S)-5-pyridin-3-yl-3,4-dihydro-2H-chromen-3-yl]triazole-4-carboxamide
   Show/Hide
C21H23N5O3
 1
1
IC50 > 31622.78 nM
   TI
   LI
   LO
   TS
CP0437804
5-methyl-2-phenyl-N-[(3S)-5-pyridin-4-yl-3,4-dihydro-2H-chromen-3-yl]triazole-4-carboxamide
   Show/Hide
C24H21N5O2
 1
1
IC50 > 31622.78 nM
   TI
   LI
   LO
   TS
CP0439895
2-(2-methoxyethyl)-5-methyl-N-[(3S)-5-pyridin-4-yl-3,4-dihydro-2H-chromen-3-yl]triazole-4-carboxamide
   Show/Hide
C21H23N5O3
 1
1
IC50 > 31622.78 nM
   TI
   LI
   LO
   TS
CP0452261
5-methyl-2-(2-methylpropyl)-N-[(3S)-5-pyridin-3-yl-3,4-dihydro-2H-chromen-3-yl]triazole-4-carboxamide
   Show/Hide
C22H25N5O2
 1
1
IC50 > 31622.78 nM
   TI
   LI
   LO
   TS
CP0010753
N-[[1-[2-(tert-butylcarbamoylamino)ethyl]-4-(hydroxymethyl)piperidin-4-yl]methyl]-3,5-dichlorobenzamide
   Show/Hide
C21H32Cl2N4O3
 1
1
IC50 > 33000 nM
   TI
   LI
   LO
   TS
CP0053278
(5-bromo-1-methylpyrrolo[2,3-c]pyridin-2-yl)-[6-[(dimethylamino)methyl]-3,4-dihydro-1H-isoquinolin-2-yl]methanone
   Show/Hide
C21H23BrN4O
 1
1
IC50 > 33000 nM
   TI
   LI
   LO
   TS
CP0094025
(5-chloro-1-methylindol-2-yl)-[6-[(dimethylamino)methyl]-7-methyl-3,4-dihydro-1H-isoquinolin-2-yl]methanone
   Show/Hide
C23H26ClN3O
 1
1
IC50 > 33000 nM
   TI
   LI
   LO
   TS
CP0381028
N-(2,3-dihydroindole-1-carboximidoyl)-4-methylbenzamide
   Show/Hide
C17H17N3O
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0436278
N-[(3S)-5-(5-methylpyrazin-2-yl)-3,4-dihydro-2H-chromen-3-yl]-6-(2,2,2-trifluoroethoxy)pyridine-3-carboxamide
   Show/Hide
C22H19F3N4O3
 1
1
IC50 > 3162.28 nM
   TI
   LI
   LO
   TS
CP0637108
rac-1-(2-(2-hydroxy-3-(4-p-tolylpiperazin-1-yl)propoxy)phenyl)-3-phenylpropan-1-one hydrochloride
   Show/Hide
C29H35ClN2O3
 1
1
IC50 > 5000 nM
   TI
   LI
   LO
   TS
CP0636848
rac-1-(2-(2-hydroxy-3-(4-phenylpiperidin-1-yl)propoxy)phenyl)-3-phenylpropan-1-one hydrochloride
   Show/Hide
C29H34ClNO3
 1
1
IC50 > 5000 nM
   TI
   LI
   LO
   TS
CP0637784
rac-1-(2-(3-(4-benzhydrylpiperazin-1-yl)-2-hydroxypropoxy)-5-fluorophenyl)-3-phenylpropan-1-one hydrochloride
   Show/Hide
C35H38ClFN2O3
 1
1
IC50 > 5000 nM
   TI
   LI
   LO
   TS
CP0443560
4-butoxy-N-[(3S)-5-(4-methylpiperazin-1-yl)-3,4-dihydro-2H-chromen-3-yl]benzamide
   Show/Hide
C25H33N3O3
 1
1
IC50 > 6309.57 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0032710
4-[(3S,4S)-3-(3,4-difluorophenyl)-1-(2,2,2-trifluoroethyl)piperidin-4-yl]oxy-3,5-difluoro-N-(6-fluoropyridin-2-yl)benzenesulfonamide
   Show/Hide
C24H19F8N3O3S
 2
1 IC50 = 110 nM
2 Ki = 370 nM
CP0055093
6-[4-(trifluoromethoxy)phenyl]-3-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]pyridine
   Show/Hide
C14H7F6N3O
 1
1 IC50 = 333 nM
CP0303021
US8952169, 6
   Show/Hide
C19H23ClFNO4S
 1
1 IC50 = 1070 nM
CP0076327
1-(2,6-dimethylphenoxy)-2-propanolamine
   Show/Hide
C11H17NO
 1
1 IC50 = 3000 nM
CP0034615
(6-Methoxy-quinolin-4-yl)-(5-vinyl-1-aza-bicyclo[2.2.2]oct-2-yl)-methanol
   Show/Hide
C20H24N2O2
 1
1 IC50 = 6900 nM
CP0189235
CHEBI:87690
   Show/Hide
C24H33N3O4
 1
1 IC50 = 7000 nM
CP0051021
5-(4-chlorophenyl)-N-(3,5-dimethoxyphenyl)furan-2-carboxamide
   Show/Hide
C19H16ClNO4
 2
1 IC50 = 7440 nM
2 IC50 > 2000 nM
CP0069734
2,2-diphenyl-N-[4-(1,3-thiazol-2-ylsulfamoyl)phenyl]acetamide
   Show/Hide
C23H19N3O3S2
 1
1 IC50 = 9200 nM
CP0123958
10-hydroxymethyl-5-imino-(2S)-12,13-dioxa-4,6-diazatetracyclo[7.3.1.13,11.03,8]tetradecane-1,2,7,10,14-pentaol
   Show/Hide
C11H17N3O8
 1
1 IC50 > 30 nM
CP0204850
4-[2-(3-amino-1,2-benzoxazol-5-yl)-4-chlorophenoxy]-2,5-difluoro-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide
   Show/Hide
C21H12ClF2N5O4S2
 1
1 IC50 > 1000 nM
CP0052824
4-[[(3S,4R)-4-(4-chlorophenyl)piperidin-3-yl]methoxy]-2,5-difluoro-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide
   Show/Hide
C20H19ClF2N4O3S2
 1
1 IC50 > 10000 nM
CP0095952
3-cyano-4-[2-(2-methylpyrazol-3-yl)phenoxy]-N-(1,3-thiazol-2-yl)benzenesulfonamide
   Show/Hide
C20H15N5O3S2
 1
1 IC50 > 10000 nM
Clinical Information about the Protein
Target 1 ( Voltage-gated sodium channel alpha Nav1.5 (SCN5A) )
Target Type Successful Target
Disease 12 Target-related Diseases  12
1 Cough [ICD-11: MD12]
2 Anaesthesia [ICD-11: 9A78.6]
3 Ventricular arrhythmias [ICD-11: BC71]
4 Pain [ICD-11: MG30-MG3Z]
5 Complex partial seizure [ICD-11: 8A68.0]
6 Migraine [ICD-11: 8A80]
7 Epilepsy [ICD-11: 8A60-8A68]
8 Ventricular tachycardia [ICD-11: BC71]
9 Arrhythmia [ICD-11: BC9Z]
10 Bacterial infection [ICD-11: 1A00-1C4Z]
11 Neurological disorder [ICD-11: 6B60]
12 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Approved Drug(s) 12 Approved Drugs  12
1 Benzonatate Approved
Cough
2 Dibucaine Approved
Anaesthesia
3 Disopyramide Approved
Ventricular arrhythmias
4 Dyclonine Approved
Pain
5 Ethotoin Approved
Complex partial seizure
6 Hexylcaine Approved
Anaesthesia
7 LOMERIZINE Approved
Migraine
8 Mephenytoin Approved
Epilepsy
9 Mexiletine Approved
Ventricular tachycardia
10 Moricizine Approved
Arrhythmia
11 Prilocaine Approved
Pain
12 Tetrodotoxin Approved
Bacterial infection
Discontinued Drug(s) 3 Discontinued Drugs  3
1 LUBELUZOLE Discontinued in Preregistration
Neurological disorder
2 Acecainide Discontinued in Phase 3
Solid tumour/cancer
3 SIPATRIGINE Discontinued in Phase 2
Neurological disorder