General Information of the Protein
Protein ID
PT02752
Protein Name
Sodium channel protein type 10 subunit alpha
Secondarily
Protein Name
Peripheral nerve sodium channel 3
Sodium channel protein type X subunit alpha
Voltage-gated sodium channel subunit alpha Nav1.8
Gene Name
SCN10A
Sequence
MEFPIGSLETNNFRRFTPESLVEIEKQIAAKQGTKKAREKHREQKDQEEKPRPQLDLKACNQLPKFYGELPAELIGEPLEDLDPFYSTHRTFMVLNKGRTISRFSATRALWLFSPFNLIRRTAIKVSVHSWFSLFITVTILVNCVCMTRTDLPEKIEYVFTVIYTFEALIKILARGFCLNEFTYLRDPWNWLDFSVITLAYVGTAIDLRGISGLRTFRVLRALKTVSVIPGLKVIVGALIHSVKKLADVTILTIFCLSVFALVGLQLFKGNLKNKCVKNDMAVNETTNYSSHRKPDIYINKRGTSDPLLCGNGSDSGHCPDGYICLKTSDNPDFNYTSFDSFAWAFLSLFRLMTQDSWERLYQQTLRTSGKIYMIFFVLVIFLGSFYLVNLILAVVTMAYEEQNQATTDEIEAKEKKFQEALEMLRKEQEVLAALGIDTTSLHSHNGSPLTSKNASERRHRIKPRVSEGSTEDNKSPRSDPYNQRRMSFLGLASGKRRASHGSVFHFRSPGRDISLPEGVTDDGVFPGDHESHRGSLLLGGGAGQQGPLPRSPLPQPSNPDSRHGEDEHQPPPTSELAPGAVDVSAFDAGQKKTFLSAEYLDEPFRAQRAMSVVSIITSVLEELEESEQKCPPCLTSLSQKYLIWDCCPMWVKLKTILFGLVTDPFAELTITLCIVVNTIFMAMEHHGMSPTFEAMLQIGNIVFTIFFTAEMVFKIIAFDPYYYFQKKWNIFDCIIVTVSLLELGVAKKGSLSVLRSFRLLRVFKLAKSWPTLNTLIKIIGNSVGALGNLTIILAIIVFVFALVGKQLLGENYRNNRKNISAPHEDWPRWHMHDFFHSFLIVFRILCGEWIENMWACMEVGQKSICLILFLTVMVLGNLVVLNLFIALLLNSFSADNLTAPEDDGEVNNLQVALARIQVFGHRTKQALCSFFSRSCPFPQPKAEPELVVKLPLSSSKAENHIAANTARGSSGGLQAPRGPRDEHSDFIANPTVWVSVPIAEGESDLDDLEDDGGEDAQSFQQEVIPKGQQEQLQQVERCGDHLTPRSPGTGTSSEDLAPSLGETWKDESVPQVPAEGVDDTSSSEGSTVDCLDPEEILRKIPELADDLEEPDDCFTEGCIRHCPCCKLDTTKSPWDVGWQVRKTCYRIVEHSWFESFIIFMILLSSGSLAFEDYYLDQKPTVKALLEYTDRVFTFIFVFEMLLKWVAYGFKKYFTNAWCWLDFLIVNISLISLTAKILEYSEVAPIKALRTLRALRPLRALSRFEGMRVVVDALVGAIPSIMNVLLVCLIFWLIFSIMGVNLFAGKFWRCINYTDGEFSLVPLSIVNNKSDCKIQNSTGSFFWVNVKVNFDNVAMGYLALLQVATFKGWMDIMYAAVDSREVNMQPKWEDNVYMYLYFVIFIIFGGFFTLNLFVGVIIDNFNQQKKKLGGQDIFMTEEQKKYYNAMKKLGSKKPQKPIPRPLNKFQGFVFDIVTRQAFDITIMVLICLNMITMMVETDDQSEEKTKILGKINQFFVAVFTGECVMKMFALRQYYFTNGWNVFDFIVVVLSIASLIFSAILKSLQSYFSPTLFRVIRLARIGRILRLIRAAKGIRTLLFALMMSLPALFNIGLLLFLVMFIYSIFGMSSFPHVRWEAGIDDMFNFQTFANSMLCLFQITTSAGWDGLLSPILNTGPPYCDPNLPNSNGTRGDCGSPAVGIIFFTTYIIISFLIMVNMYIAVILENFNVATEESTEPLSEDDFDMFYETWEKFDPEATQFITFSALSDFADTLSGPLRIPKPNRNILIQMDLPLVPGDKIHCLDILFAFTKNVLGESGELDSLKANMEEKFMATNLSKSSYEPIATTLRWKQEDISATVIQKAYRSYVLHRSMALSNTPCVPRAEEEAASLPDEGFVAFTANENCVLPDKSETASATSFPPSYESVTRGLSDRVNMRTSSSIQNEDEATSMELIAPGP
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Organism
Homo sapiens, Human
Protein Classification
Ion channel
>
Voltage-gated ion channel
>
Voltage-gated sodium channel
Function
Tetrodotoxin-resistant channel that 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 sodium ions may pass in accordance with their electrochemical gradient. Plays a role in neuropathic pain mechanisms.
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Uniprot ID
Primary ID:
Q9Y5Y9

Secondarily ID:
A6NDQ1
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HGNC ID
HGNC:10582
Subcellular Location
Cell membrane
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
CP0421283
4-(5-Chloro-6-((1-Methylcyclopropyl)Methoxy)Pyridin-3-yl)-2-Fluoro-5-Methoxy-N-(Methylsulfonyl)Benzamide
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C20H14ClF3N2O5S
 1
1
IC50 = 15600 nM
   TI
   LI
   LO
   TS
CP0348250
US9012443, 261
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C19H13F3N4O3S2
 1
1
IC50 > 30000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0051021
5-(4-chlorophenyl)-N-(3,5-dimethoxyphenyl)furan-2-carboxamide
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C19H16ClNO4
 1
1 IC50 = 8 nM
CP0126707
N-(3,5-dimethylphenyl)-6-[4-(trifluoromethoxy)phenyl]pyrazine-2-carboxamide
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C20H16F3N3O2
 1
1 IC50 = 21 nM
CP0243027
N-[(2-morpholin-4-ylpyridin-3-yl)methyl]-6-[4-(trifluoromethoxy)phenyl]pyrazine-2-carboxamide
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C22H20F3N5O3
 1
1 IC50 = 30 nM
Clinical Information about the Protein
Target 1 ( Voltage-gated sodium channel alpha Nav1.8 (SCN10A) )
Target Type Successful Target
Disease 6 Target-related Diseases  6
1 Anaesthesia [ICD-11: 9A78.6]
2 Human immunodeficiency virus infection [ICD-11: 1C62]
3 Spinal anesthesia [ICD-11: MB40.3]
4 Alcohol dependence [ICD-11: 6C40.2]
5 Pain [ICD-11: MG30-MG3Z]
6 Neurological disorder [ICD-11: 6B60]
Approved Drug(s) 6 Approved Drugs  6
1 Bupivacaine Approved
Anaesthesia
2 Proparacaine Approved
Anaesthesia
3 Rilpivirine Approved
Human immunodeficiency virus infection
4 Ropivacaine Approved
Anaesthesia
5 Tetracaine Approved
Spinal anesthesia
6 Tiapride Approved
Alcohol dependence
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 PF-01247324 Phase 1
Pain
Discontinued Drug(s) 1 Discontinued Drug  1
1 SIPATRIGINE Discontinued in Phase 2
Neurological disorder
Investigative Drug(s) 1 Investigative Drug  1
1 A-803467 Investigative
Pain