SCN10A

gene
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Also known as Nav1.8hPN3SNSPN3

Summary

SCN10A (sodium voltage-gated channel alpha subunit 10, HGNC:10582) is a protein-coding gene on chromosome 3p22.2, encoding Sodium channel protein type 10 subunit alpha (Q9Y5Y9). Tetrodotoxin-resistant channel that mediates the voltage-dependent sodium ion permeability of excitable membranes.

The protein encoded by this gene is a tetrodotoxin-resistant voltage-gated sodium channel alpha subunit. The properties of the channel formed by the encoded transmembrane protein can be altered by interaction with different beta subunits. This protein may be involved in the onset of pain associated with peripheral neuropathy. Alternative splicing results in multiple transcript variants.

Source: NCBI Gene 6336 — RefSeq curated summary.

At a glance

  • Gene–disease (curated): episodic pain syndrome, familial, 2 (Strong, GenCC) — +2 more curated relationships
  • GWAS associations: 119
  • Clinical variants (ClinVar): 2,320 total — 2 likely-pathogenic
  • Phenotypes (HPO): 40
  • Druggable target: yes — 21 molecules with ChEMBL bioactivity
  • MANE Select transcript: NM_006514

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:10582
Approved symbolSCN10A
Namesodium voltage-gated channel alpha subunit 10
Location3p22.2
Locus typegene with protein product
StatusApproved
AliasesNav1.8, hPN3, SNS, PN3
Ensembl geneENSG00000185313
Ensembl biotypeprotein_coding
OMIM604427
Entrez6336

Gene structure

Transcript identifiers

Ensembl transcripts: 3 — 3 protein_coding

ENST00000449082, ENST00000643924, ENST00000655275

RefSeq mRNA: 3 — MANE Select: NM_006514 NM_001293306, NM_001293307, NM_006514

CCDS: CCDS33736, CCDS87064

Canonical transcript exons

ENST00000449082 — 28 exons

ExonStartEnd
ENSE000012927503875667438756871
ENSE000012934793878895638789036
ENSE000012949633871865338718826
ENSE000012970753870183938702109
ENSE000012979263871216138712445
ENSE000013012493872660638727052
ENSE000013012713872343038723553
ENSE000013026233873951538739688
ENSE000013034983875007338750184
ENSE000013046523875578838755958
ENSE000013052103877127938771407
ENSE000013075253876119238761383
ENSE000013128473875701838757159
ENSE000013157473871395838714080
ENSE000013163353872225838722412
ENSE000013205013875221938752512
ENSE000013211483874229138742529
ENSE000013223753876068138760747
ENSE000013290923872517438725314
ENSE000013294823876350538763596
ENSE000013308553872854238728901
ENSE000015069533870947838709615
ENSE000015069543879205038792168
ENSE000016609063870727938707383
ENSE000017123343869680738698562
ENSE000017596613871084438710897
ENSE000038223893881603738816217
ENSE000038255393879374138794042

Expression profiles

Bgee: expression breadth broad, 21 present calls, max score 94.07.

Top tissues by expression

227 total, by Bgee expression score (0-100, higher = more expressed):

TissueAnatomy IDExpression scoreQuality
type B pancreatic cellCL:000016994.07silver quality
olfactory bulbUBERON:000226493.90silver quality
diaphragmUBERON:000110392.14silver quality
hair follicleUBERON:000207386.37silver quality
pancreatic ductal cellCL:000207981.91silver quality
mucosa of paranasal sinusUBERON:000503080.57gold quality
mucosa of urinary bladderUBERON:000125980.22silver quality
orbitofrontal cortexUBERON:000416777.95gold quality
cervix squamous epitheliumUBERON:000692277.77silver quality
tongue squamous epitheliumUBERON:000691977.43silver quality
superficial temporal arteryUBERON:000161477.28gold quality
thymusUBERON:000237076.33gold quality
upper arm skinUBERON:000426375.68gold quality
germinal epithelium of ovaryUBERON:000130474.99gold quality
tibialis anteriorUBERON:000138574.21silver quality
gingival epitheliumUBERON:000194971.84gold quality
ileal mucosaUBERON:000033171.66gold quality
lower lobe of lungUBERON:000894970.78silver quality
deltoidUBERON:000147668.45silver quality
choroid plexus epitheliumUBERON:000391167.43silver quality
dorsal motor nucleus of vagus nerveUBERON:000287067.39gold quality
inferior olivary complexUBERON:000212767.31gold quality
skeletal muscle tissue of rectus abdominisUBERON:000451166.36gold quality
epithelium of nasopharynxUBERON:000195165.90gold quality
Brodmann (1909) area 46UBERON:000648365.71gold quality
triceps brachiiUBERON:000150965.33gold quality
gluteal muscleUBERON:000200065.19gold quality
deciduaUBERON:000245064.54gold quality
epithelium of mammary glandUBERON:000324464.50gold quality
layer of synovial tissueUBERON:000761664.02gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 1.

ExperimentMarker?Max mean expression
E-ANND-3yes6.22

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): ESR1, ESR2, IL10, TNF

Literature-anchored findings (GeneRIF, showing 40)

  • A high capacity assay is sensitive to known state-dependent NaV1 modulators and can be used to identify novel and selective inhibitors. (PMID:16506887)
  • calmodulin associates with a sodium channel, Nav1.8, in native neurons, and demonstrates a regulation of Nav1.8 currents that can significantly affect electrogenesis of DRG neurons in which Nav1.8 is normally expressed (PMID:16598065)
  • Chimeras containing the N-terminal half of Na(v)1.8 exhibited a large response similar to wild-type Na(v)1.8, indicating that the region conferring high sensitivity to ciguatoxin action is located in the D1 or D2 domains. (PMID:19164297)
  • Data suggest differing, but partially overlapping, areas of binding of A-803467 and tetracaine in the Na(V)1.8 sodium channel. (PMID:19233853)
  • activation of NK-1 receptor potentiates Na(v)1.8 sodium current via PKCepsilon-dependent signaling pathway, probably participating in the generation of inflammatory hyperalgesia (PMID:19563686)
  • In trigeminal neuralgia (TN) there is a reduction in the expression of Nav1.7 and an increase in the expression of Nav1.3, Nav1.8 expression not significantly different; TN can be, at least in part, a channelopathy. (PMID:19699781)
  • Nav1.8 downregulation may be one of the pathophysiological mechanisms involved in limb lengthening-induced neuropathy. (PMID:19877286)
  • Data describe alternative splicing in a NAGNAG tandem acceptor in SCN10A that results in isoforms including/lacking glutamine 1030, which is conserved among rodents and humans but its alternative usage apparently occurs with species-specific abundance. (PMID:19953341)
  • Aquaporin-1 tunes pain perception by interaction with Na(v)1.8 Na+ channels in dorsal root ganglion neurons. (PMID:20018876)
  • SCN10A is expressed in mouse and human heart tissue and that PR interval is shorter in Scn10a(-/-) mice than in wild-type mice. (PMID:20062061)
  • Ret-Na(v)1.8 conditional knockout mice have increased sensitivity to cold and increased formalin-induced pain, demonstrating that Ret signaling modulates the function of nociceptors in vivo. (PMID:20237269)
  • Transmembrane segments prevent surface expression of sodium channel Nav1.8 and promote calnexin-dependent channel degradation (PMID:20720009)
  • sodium channel Na(v)1.8 is present in sensory nerves and cardiomyocytes of human heart (PMID:21646736)
  • We found that SCN10A 3218 CC homozygosity with the 2884 G and 3275 C alleles was significantly associated with a reduced risk for the development of functional dyspepsia. (PMID:22618805)
  • Single nucleotide polymorphism of TRPV1 315G>C, rs5981521 of pri-miR-325 and SCN10A is related to the development of functional dyspepsia. This involvement differed between Helicobater pylori-positive and -negative patients. (PMID:23047628)
  • Mutations of Na(v)1.8 contribute to painful peripheral neuropathy. (PMID:23115331)
  • Common variants at SCN5A-SCN10A and HEY2 are associated with Brugada syndrome, a rare disease with high risk of sudden cardiac death. (PMID:23872634)
  • I1706V mutation associated with small-fiber neuropathy decreases current threshold and increases the firing frequency of evoked action potentials within small DRG neurons. (PMID:23986244)
  • This study reports a mutation of NaV1.8 which impairs inactivation, in patients with painful idiopathic small fibre neuropathy. (PMID:24006052)
  • SCN10A SNPs modulate PR interval and heart rate response during atrial fibrillation. (PMID:24072447)
  • Results verify that the Na+ channel Na v1.8 is present in human sperm cells and participates in the regulation of sperm function. (PMID:24086692)
  • The results demonstrate that Nav1.8 and Nav1.9 are present in human lingual nerve neuromas, with significant correlations between the level of expression of Nav1.8 and symptoms of pain. (PMID:24144460)
  • A single-nucleotide polymorphism (SNP) associated with alterations in cardiac conduction patterns affects the transcriptional regulation of the sodium channel genes, SCN5A and SCN10A, predisposing for cardiac arrhythmias. (PMID:24360055)
  • SCN10A variant rs6801957, which correlated with slowed cardiac conduction, was associated with reduced SCN5A expression. (PMID:24642470)
  • A novel splice variant of SCN10A lacking exon 11 was found in human but not detected in mouse or rat. (PMID:24763188)
  • As a major susceptibility gene for Brugada syndrome (BrS), SCN10A greatly enhances the genotyping and risk stratifying of probands and BrS family members. (PMID:24998131)
  • Rare SCN10A variants may contribute to atrial fibrillation susceptibility. (PMID:25053638)
  • The common SNP SCN10A V1073 was strongly associated with Brugada syndrome and demonstrated loss of NaV1.8 function, as did rare variants in isolated patients. (PMID:25691538)
  • study suggests that SCN10A variations are involved in the genesis of AF. (PMID:25691686)
  • The results demonstrate distinct properties of human Na(v)1.8, which contribute to the firing properties of human DRG neurons. (PMID:25787950)
  • Compared with Brugada syndrome (BrS) patients carrying SCN5A or CACNA1C mutations, symptomatic patients in the SCN10A group tended to be older than those in the other gene groups. In six BrS probands who carried SCN10A variants, most experienced severe arrhythmic attacks. (PMID:25842276)
  • SCN10A gene mutations that reduce sodium channel current may provide a mechanistic link between Atrioventricular nodal reentrant tachycardia and Brugada syndrome and predispose to expression of both phenotypes. (PMID:25998140)
  • The rs6795970 in the SCN10A gene, which is reported to carry a high risk of heart block, might be associated with cardiac conduction abnormalities in Hypertrophic Cardiomyopathy patients. (PMID:26104176)
  • SCN10A mutations do not play primary role in arrhythmogenic right ventricular dysplasia/cardiomyopathy. (PMID:26733327)
  • SCN10A genetic variation substantially influences functional status in patients with multiple sclerosis. (PMID:26740675)
  • We investigated the association of SCN10A gene variants with 105 sporadic sudden unexplained nocturnal death syndrome victims. A total of 6 rare mutations and 16 polymorphisms were detected in SUNDS victims. This is the first report of common and rare variants of SCN10A gene in the Chinese Han population, which provides the genetic epidemiological evidence that SCN10A may be a novel susceptibility gene. (PMID:27272739)
  • This study demonstrated that at the association and mechanistic levels, the SCN10A single nucleotide polymorphism rs6795970 biases human pain sensitivity. (PMID:27590072)
  • The p.M650K mutation shifted steady-state fast inactivation of Nav1.8 (SCN10A)to more hyperpolarized potentials and did not significantly alter any other tested gating behaviors. The AP half-width was significantly broader and the stimulated action potential firing rate was reduced for M650K transfected DRGs compared to WT. (PMID:27598514)
  • The possible involvement of the SCN10A variant in AF development in Chinese Han populations. (PMID:27725708)
  • Our findings suggest that there are interaction effects of DM and SCN10A (rs7375036) that influence the development of CAN. (PMID:27729462)

Cross-species orthologs

4 orthologs

OrganismSymbolGene ID
danio_rerioscn12aaENSDARG00000090724
danio_rerioscn5labENSDARG00000102312
mus_musculusScn10aENSMUSG00000034533
rattus_norvegicusScn10aENSRNOG00000032473

Paralogs (26): CACNA1G (ENSG00000006283), SCN4A (ENSG00000007314), CACNA1S (ENSG00000081248), CACNA1I (ENSG00000100346), CACNA1F (ENSG00000102001), NALCN (ENSG00000102452), SCN2A (ENSG00000136531), SCN7A (ENSG00000136546), CACNA1A (ENSG00000141837), SCN1A (ENSG00000144285), CACNA1B (ENSG00000148408), CACNA1C (ENSG00000151067), CATSPER3 (ENSG00000152705), SCN3A (ENSG00000153253), CACNA1D (ENSG00000157388), TPCN2 (ENSG00000162341), CATSPER2 (ENSG00000166762), SCN11A (ENSG00000168356), SCN9A (ENSG00000169432), CATSPER1 (ENSG00000175294), SCN5A (ENSG00000183873), TPCN1 (ENSG00000186815), CATSPER4 (ENSG00000188782), CACNA1H (ENSG00000196557), SCN8A (ENSG00000196876), CACNA1E (ENSG00000198216)

Protein

Protein identifiers

Sodium channel protein type 10 subunit alphaQ9Y5Y9 (reviewed: Q9Y5Y9)

Alternative names: Peripheral nerve sodium channel 3, Sodium channel protein type X subunit alpha, Voltage-gated sodium channel subunit alpha Nav1.8

All UniProt accessions (3): Q9Y5Y9, A0A2R8Y6J6, A0A590UJM0

UniProt curated annotations — full annotation on UniProt →

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.

Subunit / interactions. The channel consists of an ion conducting pore forming alpha-subunit regulated by one or more associated auxiliary subunits SCN1B, SCN2B and SCN3B; electrophysiological properties may vary depending on the type of the associated beta subunits. Found in a number of complexes with PRX, DYNLT1 and PDZD2. Interacts with proteins such as FSTL1, PRX, DYNLT1, PDZD2, S100A10 and many others. Interacts with NEDD4 and NEDD4L.

Subcellular location. Cell membrane.

Tissue specificity. Expressed in the dorsal root ganglia and sciatic nerve.

Post-translational modifications. Ubiquitinated by NEDD4L; which promotes its endocytosis. Phosphorylation at Ser-1451 by PKC in a highly conserved cytoplasmic loop slows inactivation of the sodium channel and reduces peak sodium currents. Lacks the cysteine which covalently binds the conotoxin GVIIJ. This cysteine (position 816) is speculated in other sodium channel subunits alpha to be implied in covalent binding with the sodium channel subunit beta-2 or beta-4.

Disease relevance. Episodic pain syndrome, familial, 2 (FEPS2) [MIM:615551] An autosomal dominant neurologic disorder characterized by adult-onset of paroxysmal pain mainly affecting the distal lower extremities. The disease is caused by variants affecting the gene represented in this entry.

Domain organisation. The sequence contains 4 internal repeats, each with 5 hydrophobic segments (S1, S2, S3, S5, S6) and one positively charged segment (S4). Segments S4 are probably the voltage-sensors and are characterized by a series of positively charged amino acids at every third position.

Similarity. Belongs to the sodium channel (TC 1.A.1.10) family. Nav1.8/SCN10A subfamily.

RefSeq proteins (3): NP_001280235, NP_001280236, NP_006505* (*=MANE)

Domains & families (InterPro)

IDNameType
IPR001696Na_channel_asuFamily
IPR005821Ion_trans_domDomain
IPR010526Na_trans_assoc_domDomain
IPR027359Volt_channel_dom_sfHomologous_superfamily
IPR043203VGCC_Ca_NaFamily
IPR044564Na_chnl_inactivation_gateDomain
IPR058542IQ_SCN5A_CDomain

Pfam: PF00520, PF06512, PF24609

Catalyzed reactions (Rhea), 1 shown:

  • Na(+)(in) = Na(+)(out) (RHEA:34963)

UniProt features (190 total): helix 57, topological domain 29, transmembrane region 24, strand 17, sequence variant 13, turn 13, glycosylation site 9, modified residue 7, region of interest 6, intramembrane region 4, repeat 4, compositionally biased region 3, disulfide bond 2, chain 1, domain 1

Structure

Experimental structures (PDB)

8 structures.

PDBMethodResolution (Å)
7WE4ELECTRON MICROSCOPY2.7
9DBNELECTRON MICROSCOPY2.76
7WFRELECTRON MICROSCOPY3
7WFWELECTRON MICROSCOPY3.1
9DBKELECTRON MICROSCOPY3.12
7WELELECTRON MICROSCOPY3.2
9DBMELECTRON MICROSCOPY3.22
9DBLELECTRON MICROSCOPY3.24

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-Q9Y5Y9-F168.060.12

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Post-translational modifications (7): 441, 444, 467, 479, 612, 615, 1451

Disulfide bonds (2): 276–319, 857–866

Glycosylation sites (9): 284, 288, 312, 335, 819, 1312, 1328, 1336, 1686

Function

Pathways and Gene Ontology

Reactome pathways

8 pathways

IDPathway
R-HSA-445095Interaction between L1 and Ankyrins
R-HSA-5576892Phase 0 - rapid depolarisation
R-HSA-1266738Developmental Biology
R-HSA-373760L1CAM interactions
R-HSA-397014Muscle contraction
R-HSA-422475Axon guidance
R-HSA-5576891Cardiac conduction
R-HSA-9675108Nervous system development

MSigDB gene sets: 214 (showing top): GSE45365_NK_CELL_VS_CD8A_DC_MCMV_INFECTION_DN, GOBP_MEMBRANE_DEPOLARIZATION, GOBP_BUNDLE_OF_HIS_CELL_TO_PURKINJE_MYOCYTE_COMMUNICATION, GOBP_CIRCULATORY_SYSTEM_PROCESS, GOBP_SODIUM_ION_TRANSMEMBRANE_TRANSPORT, GOBP_MEMBRANE_DEPOLARIZATION_DURING_ACTION_POTENTIAL, GOBP_REGULATION_OF_MEMBRANE_DEPOLARIZATION, GOBP_MONOATOMIC_CATION_TRANSPORT, GOBP_CELL_CELL_SIGNALING, GOBP_REGULATION_OF_STRIATED_MUSCLE_CONTRACTION, GOBP_ANIMAL_ORGAN_MORPHOGENESIS, GOBP_REGULATION_OF_MUSCLE_CONTRACTION, GOBP_MUSCLE_CONTRACTION, GOBP_CELL_COMMUNICATION_INVOLVED_IN_CARDIAC_CONDUCTION, GOBP_REGULATION_OF_HEART_RATE

GO Biological Process (17): regulation of heart rate (GO:0002027), sensory perception (GO:0007600), regulation of monoatomic ion transmembrane transport (GO:0034765), sodium ion transmembrane transport (GO:0035725), odontogenesis of dentin-containing tooth (GO:0042475), regulation of cardiac muscle contraction (GO:0055117), regulation of atrial cardiac muscle cell membrane depolarization (GO:0060371), cardiac muscle cell action potential involved in contraction (GO:0086002), membrane depolarization during action potential (GO:0086010), AV node cell action potential (GO:0086016), bundle of His cell action potential (GO:0086043), monoatomic ion transport (GO:0006811), sodium ion transport (GO:0006814), monoatomic ion transmembrane transport (GO:0034220), transmembrane transport (GO:0055085), monoatomic cation transmembrane transport (GO:0098655), regulation of presynaptic membrane potential (GO:0099505)

GO Molecular Function (6): voltage-gated sodium channel activity (GO:0005248), transmembrane transporter binding (GO:0044325), voltage-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potential (GO:0099508), monoatomic ion channel activity (GO:0005216), monoatomic cation channel activity (GO:0005261), sodium channel activity (GO:0005272)

GO Cellular Component (9): voltage-gated sodium channel complex (GO:0001518), plasma membrane (GO:0005886), axon (GO:0030424), presynaptic membrane (GO:0042734), extracellular exosome (GO:0070062), clathrin complex (GO:0071439), glutamatergic synapse (GO:0098978), membrane (GO:0016020), monoatomic ion channel complex (GO:0034702)

Reactome top-level categories

Rollup of top-6 pathways:

CategoryPathways
L1CAM interactions1
Cardiac conduction1
Axon guidance1
Nervous system development1
Muscle contraction1
Developmental Biology1

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
cardiac muscle cell action potential3
regulation of heart contraction2
monoatomic ion transmembrane transport2
transport2
regulation of biological quality1
nervous system process1
regulation of transmembrane transport1
regulation of monoatomic ion transport1
sodium ion transport1
monoatomic cation transmembrane transport1
odontogenesis1
regulation of striated muscle contraction1
cardiac muscle contraction1
regulation of membrane depolarization1
cardiac muscle cell contraction1
action potential1
membrane depolarization1
AV node cell to bundle of His cell signaling1
bundle of His cell to Purkinje myocyte signaling1
metal ion transport1
monoatomic ion transport1
transmembrane transport1
cellular process1
monoatomic cation transport1
regulation of membrane potential1
sodium channel activity1
protein binding1
voltage-gated monoatomic ion channel activity1
presynaptic membrane1
regulation of presynaptic membrane potential1
monoatomic ion transmembrane transporter activity1
channel activity1
monoatomic ion channel activity1
monoatomic cation transmembrane transporter activity1
monoatomic cation channel activity1
sodium ion transmembrane transporter activity1
sodium channel complex1
plasma membrane protein complex1
membrane1
cell periphery1

Protein interactions and networks

STRING

1798 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
SCN10ASCLT1Q96NL6829
SCN10AS100A10P08206824
SCN10AANXA2P07355815
SCN10ATRPV1Q8NER1806
SCN10ATRPA1O75762750
SCN10AKCNK3O14649750
SCN10ASCN4BQ8IWT1747
SCN10AARHGAP24Q8N264740
SCN10ANAV1Q8NEY1726
SCN10AGPD1LQ8N335716
SCN10ASCN1BQ07699708
SCN10ACAV2P51636692
SCN10ATBX5Q99593687
SCN10ATRPM8Q7Z2W7665
SCN10ASCN3BQ9NY72663

IntAct

4 interactions, top by confidence:

ABTypeScore
NEDD4SCN10Apsi-mi:“MI:0407”(direct interaction)0.440
Mpsi-mi:“MI:0914”(association)0.350
ATG16L1psi-mi:“MI:0914”(association)0.350
AFG2BMMP24OSpsi-mi:“MI:0914”(association)0.350

ESM2 similar proteins: A2APX8, A2ASI5, B1AWN6, C9D7C2, D0E0C2, O08562, O35505, O46669, O73700, O88420, O88457, P02719, P04774, P04775, P08104, P0DMA5, P15381, P15389, P15390, P22002, P27732, P35498, P35499, P35500, Q01815, Q07652, Q13936, Q14524, Q15858, Q20JQ7, Q28371, Q28644, Q2XVR3, Q2XVR4, Q2XVR5, Q2XVR6, Q2XVR7, Q62205, Q62968, Q6QIY3

Diamond homologs: A2APX8, A2ASI5, B1AWN6, B1AYL1, D0E0C2, F1LQQ7, O00555, O08562, O46669, O73705, O73706, O73707, O88420, O88457, P02719, P04774, P04775, P08104, P0DMA5, P15389, P15390, P27884, P35498, P35499, P35500, P54282, P56699, P97445, Q01118, Q02789, Q05973, Q14524, Q15858, Q15878, Q20JQ7, Q28371, Q28644, Q2XVR3, Q2XVR4, Q2XVR5

SIGNOR signaling

12 interactions.

AEffectBMechanism
SCN10A“up-regulates quantity”sodium(1+)relocalization
FGF13“down-regulates activity”SCN10Abinding
FGF12“down-regulates activity”SCN10Abinding
FGF14“down-regulates activity”SCN10Abinding
FGF11“down-regulates activity”SCN10Abinding
SCN10Aup-regulatesAction_potential
NEDD4L“down-regulates quantity by destabilization”SCN10Aubiquitination
ESR1“down-regulates quantity by repression”SCN10A“transcriptional regulation”
ESR2“down-regulates quantity by repression”SCN10A“transcriptional regulation”
TNF“up-regulates quantity by expression”SCN10A“transcriptional regulation”
TNF“up-regulates activity”SCN10A
IL10“down-regulates quantity by repression”SCN10A“transcriptional regulation”

Disease & clinical

Clinical variants and AI predictions

ClinVar

2320 variants total. Per-class counts are floors (≥ shown; pagination cap):

ClassificationCount (floor)
Pathogenic0
Likely pathogenic2
Uncertain significance1295
Likely benign750
Benign55

Top pathogenic / likely-pathogenic (2)

Variant IDHGVSClassification
4688148NM_006514.4(SCN10A):c.2231T>A (p.Leu744Gln)Likely pathogenic
560687NM_006514.4(SCN10A):c.4201_4203del (p.Phe1401del)Likely pathogenic

SpliceAI

4736 predictions. Top by Δscore:

VariantEffectΔscore
3:38701834:CTT:Cdonor_loss1.0000
3:38701835:TTA:Tdonor_loss1.0000
3:38701836:TAC:Tdonor_loss1.0000
3:38701837:A:ACdonor_gain1.0000
3:38701837:ACT:Adonor_gain1.0000
3:38701838:C:CAdonor_gain1.0000
3:38701838:CT:Cdonor_gain1.0000
3:38701838:CTC:Cdonor_gain1.0000
3:38701838:CTCG:Cdonor_gain1.0000
3:38701854:C:CTdonor_gain1.0000
3:38701878:T:Adonor_gain1.0000
3:38701902:G:GAdonor_gain1.0000
3:38702105:TTGTT:Tacceptor_gain1.0000
3:38707377:CCC:Cacceptor_gain1.0000
3:38707378:CCC:Cacceptor_gain1.0000
3:38712211:T:Adonor_gain1.0000
3:38712302:T:Adonor_gain1.0000
3:38712334:T:TAdonor_gain1.0000
3:38712335:C:Adonor_gain1.0000
3:38714085:G:GCacceptor_gain1.0000
3:38718645:CCACT:Cdonor_loss1.0000
3:38718646:CACTC:Cdonor_loss1.0000
3:38718647:ACTCA:Adonor_loss1.0000
3:38718648:CTCA:Cdonor_loss1.0000
3:38718649:TCA:Tdonor_loss1.0000
3:38718651:A:ACdonor_gain1.0000
3:38718651:A:ATdonor_loss1.0000
3:38718651:ACATT:Adonor_gain1.0000
3:38718652:C:CTdonor_gain1.0000
3:38718652:CA:Cdonor_gain1.0000

AlphaMissense

12993 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
3:38709524:A:GL1412P0.999
3:38710882:A:GW1369R0.999
3:38710882:A:TW1369R0.999
3:38713992:G:CP1257R0.999
3:38722267:A:CS1166R0.999
3:38722267:A:TS1166R0.999
3:38722269:T:GS1166R0.999
3:38722270:G:CS1165R0.999
3:38722270:G:TS1165R0.999
3:38722272:T:GS1165R0.999
3:38727042:A:GL884P0.999
3:38728634:A:GW850R0.999
3:38728634:A:TW850R0.999
3:38728813:A:GL790P0.999
3:38697978:A:GW1748R0.998
3:38697978:A:TW1748R0.998
3:38712362:G:CS1296R0.998
3:38712362:G:TS1296R0.998
3:38712364:T:GS1296R0.998
3:38712376:A:GW1292R0.998
3:38712376:A:TW1292R0.998
3:38712388:A:GC1288R0.998
3:38713992:G:TP1257Q0.998
3:38728632:C:AW850C0.998
3:38728632:C:GW850C0.998
3:38728694:A:GW830R0.998
3:38728694:A:TW830R0.998
3:38728801:A:GL794P0.998
3:38739575:A:CS740R0.998
3:38739575:A:TS740R0.998

dbSNP variants (sampled 300 via entrez): RS1000006330 (3:38712221 C>G,T), RS1000023396 (3:38730205 G>A), RS1000051769 (3:38704300 G>A,T), RS1000070351 (3:38742187 C>T), RS1000092246 (3:38764520 A>G), RS1000105139 (3:38704017 C>G,T), RS1000136675 (3:38787055 A>T), RS1000159935 (3:38803442 C>T), RS1000172071 (3:38748890 A>G), RS1000211910 (3:38709638 G>A), RS1000263247 (3:38776194 T>C), RS1000304362 (3:38787331 T>C), RS1000310431 (3:38698652 A>G), RS1000311872 (3:38754920 C>G,T), RS1000321735 (3:38747349 T>C)

Disease associations

OMIM: gene MIM:604427 | disease phenotypes: MIM:601144, MIM:615551, MIM:615548, MIM:615552, MIM:613751, MIM:209850, MIM:192500

GenCC curated gene-disease

DiseaseClassificationInheritance
episodic pain syndrome, familial, 2StrongAutosomal dominant
sodium channelopathy-related small fiber neuropathySupportiveAutosomal dominant
Brugada syndromeLimitedUnknown

ClinGen Gene-Disease Validity (1)

Expert-panel classifications — Definitive > Strong > Moderate > Limited > Disputed > Refuted.

DiseaseClassificationInheritance
Brugada syndromeDisputedAD

Mondo (10): Brugada syndrome (MONDO:0015263), episodic pain syndrome, familial, 2 (MONDO:0014246), hereditary sensory and autonomic neuropathy type 7 (MONDO:0014244), familial episodic pain syndrome with predominantly lower limb involvement (MONDO:0014247), heterotaxy, visceral, 4, autosomal (MONDO:0013403), Brugada syndrome 1 (MONDO:0011001), autism (MONDO:0005260), familial long QT syndrome (MONDO:0019171), cardiomyopathy (MONDO:0004994), (MONDO:0017629)

Orphanet (9): Brugada syndrome (Orphanet:130), Hereditary sodium channelopathy-related small fibers neuropathy (Orphanet:306577), Familial episodic pain syndrome (Orphanet:391384), Familial episodic pain syndrome with predominantly lower limb involvement (Orphanet:391392), Hereditary sensory and autonomic neuropathy type 7 (Orphanet:391397), Visceral heterotaxy (Orphanet:450), Romano-Ward syndrome (Orphanet:101016), Congenital long QT syndrome (Orphanet:768), Rare cardiomyopathy (Orphanet:167848)

HPO phenotypes

40 total (30 of 40 shown, HPO-id order):

HPOTerm
HP:0000006Autosomal dominant inheritance
HP:0000365Hearing impairment
HP:0000989Pruritus
HP:0001197Abnormality of prenatal development or birth
HP:0001250Seizure
HP:0001279Syncope
HP:0001645Sudden cardiac death
HP:0001649Tachycardia
HP:0001663Ventricular fibrillation
HP:0001664Torsade de pointes
HP:0001688Sinus bradycardia
HP:0001695Cardiac arrest
HP:0001872Abnormality of thrombocytes
HP:0001909Leukemia
HP:0002019Constipation
HP:0002045Hypothermia
HP:0002205Recurrent respiratory infections
HP:0002633Vasculitis
HP:0002900Hypokalemia
HP:0002936Distal sensory impairment
HP:0003581Adult onset
HP:0004308Ventricular arrhythmia
HP:0004751Paroxysmal ventricular tachycardia
HP:0004755Supraventricular tachycardia
HP:0005135Abnormal T-wave
HP:0005184Prolonged QTc interval
HP:0009830Peripheral neuropathy
HP:0010741Pedal edema
HP:0010783Erythema
HP:0011704Sick sinus syndrome

GWAS associations

119 associations (top):

StudyTraitp-value
GCST000561_2Electrocardiographic traits4.000000e-09
GCST000561_6Electrocardiographic traits1.000000e-58
GCST000562_9PR interval2.000000e-74
GCST000564_1Electrocardiographic traits3.000000e-15
GCST000852_1Atrioventricular conduction5.000000e-07
GCST000872_1QRS duration1.000000e-28
GCST000872_7QRS duration2.000000e-20
GCST000971_2PR interval2.000000e-12
GCST001735_2PR interval9.000000e-09
GCST001795_10Systemic lupus erythematosus7.000000e-06
GCST001893_1Electrocardiographic conduction measures5.000000e-27
GCST002098_2Brugada syndrome1.000000e-68
GCST002456_3PR segment duration7.000000e-41
GCST002457_2P wave duration8.000000e-27
GCST002500_21QT interval2.000000e-11
GCST002500_22QT interval1.000000e-10
GCST002500_32QT interval4.000000e-27
GCST002500_33QT interval2.000000e-11
GCST002500_34QT interval1.000000e-13
GCST002533_6QRS duration2.000000e-06
GCST002535_3PR interval1.000000e-14
GCST002542_9Electrocardiographic traits3.000000e-07
GCST003598_35QRS duration1.000000e-28
GCST003598_8QRS duration2.000000e-30
GCST003844_47QRS duration7.000000e-40
GCST004826_5P wave duration2.000000e-39
GCST005080_6PR interval1.000000e-55
GCST005787_27Heart rate response to exercise5.000000e-08
GCST005788_7Heart rate response to recovery post exercise3.000000e-08
GCST006061_34Atrial fibrillation4.000000e-18

EFO canonical traits (11, from GWAS)

EFO IDTrait name
EFO:0005054QRS complex
EFO:0004462PR interval
EFO:0004327electrocardiography
EFO:0005095PR segment
EFO:0005094P wave duration
EFO:0004682QT interval
EFO:0009184heart rate response to exercise
EFO:0009185heart rate response to recovery post exercise
EFO:0005763pulse pressure measurement
EFO:0008398T wave morphology measurement
EFO:0011014health-related quality of life measurement

MeSH disease descriptors (3)

DescriptorNameTree numbers
D001321Autistic DisorderF03.625.164.113.500
D053840Brugada SyndromeC14.280.067.322; C14.280.123.250; C16.320.100
D009202CardiomyopathiesC14.280.238

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL2331043 (PROTEIN FAMILY), CHEMBL5451 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

21 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 465,529 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

MoleculeNamePhasePatents
CHEMBL11IMIPRAMINE448,893
CHEMBL12713SERTINDOLE48,984
CHEMBL1423PIMOZIDE417,310
CHEMBL193NIFEDIPINE474,353
CHEMBL23DILTIAZEM454,676
CHEMBL45816MIBEFRADIL47,838
CHEMBL54HALOPERIDOL460,883
CHEMBL558MEXILETINE415,463
CHEMBL629AMITRIPTYLINE452,595
CHEMBL633AMIODARONE429,704
CHEMBL71CHLORPROMAZINE445,827
CHEMBL741LAMOTRIGINE428,962
CHEMBL113461TEDISAMIL31,251
CHEMBL475534NITRENDIPINE316,468
CHEMBL5314404AJMALINE3
CHEMBL3544913VIXOTRIGINE3374
CHEMBL3707392ELECLAZINE3111
CHEMBL87045CIFENLINE21,298
CHEMBL3589904PF-045310832320
CHEMBL3707218FUNAPIDE2219
CHEMBL4297317PF-063055911

PharmGKB: 1 entry (VIP=true, CPIC=false)

PharmGKB clinical annotations

1 annotations.

VariantTypeLevelDrugsPhenotypes
rs9825762Toxicity3carboplatin;taxanesOvarian Neoplasms

PharmGKB variants

1 variants.

VariantGenesLevelScore#Clin annotsDrugs
rs9825762SCN10A33.001carboplatin;taxanes

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: vgic — Voltage-gated sodium channels (NaV)

Most potent curated ligand interactions (17 total), top 17:

LigandActionAffinityParameter
A-803467Channel blocker8.1pIC50
A-887826Channel blocker7.96pIC50
VX-150Channel blocker7.82pIC50
LTGO-33Channel blocker7.62pIC50
PF-04885614Inhibition7.28pIC50
suzetrigineBinding7.19pKd
PF-01247324Pore blocker6.71pIC50
AM-6120Inhibition6.0pIC50
cannabidiolChannel blocker5.7pIC50
ABBV-318Inhibition5.42pIC50
funapideInhibition5.32pIC50
cannabigerolChannel blocker5.3pIC50
ANP-230Channel blocker4.94pIC50
cannabinolChannel blocker4.8pIC50
lacosamideAntagonist4.8pIC50
tetrodotoxinPore blocker4.2pIC50
lidocainePore blocker4.0pIC50

Binding affinities (BindingDB)

1702 measured of 1793 human assays (1793 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

LigandMeasureValuePatent
2-(4,4-difluoroazepan-1-yl)-6,7-difluoro-N-(3-sulfamoylphenyl) quinoline-3-carboxamide (KH16)IC500.084 nMUS-20250115578: AROMATIC FUSED RING NAV1.8 INHIBITOR, AND USE THEREOF
2-(4,4-difluoroazepan-1-yl)-6,7-difluoro-N-(2-sulfamoylpyridine-4-yl)quinoline-3-carboxamide (KH17)IC500.095 nMUS-20250115578: AROMATIC FUSED RING NAV1.8 INHIBITOR, AND USE THEREOF
5-cyclopropyl-4-[(3R)-1-[(3,5-dichlorophenyl)methyl]piperidin-3-yl]oxy-2-fluoro-N-methylsulfonylbenzamideIC500.3 nMUS-9694002: Substituted benzamides and methods of use thereof
2-(4,4-difluoroazepan-1-yl)-N-(2-sulfamoylpyridine-4-yl) quinoline-3-carboxamide (KH14)IC500.34 nMUS-20250115578: AROMATIC FUSED RING NAV1.8 INHIBITOR, AND USE THEREOF
N-(3-carbamoyl-4-fluorophenyl)-2-(4,4-difluoroazepan-1-yl)-6,7-difluoroquinoline-3-carboxamide (KH21)IC500.36 nMUS-20250115578: AROMATIC FUSED RING NAV1.8 INHIBITOR, AND USE THEREOF
2-[(2R,3S,4S,5R)-3-(3,4-difluoro-2-methoxyphenyl)-4,5-dimethyl-5-(trifluoromethyl)oxolan-2-yl]-1H-imidazo[4,5-c]pyridine-4-carboximidamideIC500.69 nMUS-20250255878: SMALL MOLECULE INHIBITORS OF NAV1.8 SODIUM CHANNELS FOR PAIN RELIEF
2-(azepan-1-yl)-5-chloro-4,6-dimethyl-N-(3-sulfamoylphenyl)nicotinamideIC500.7 nMUS-12344595
N-(2-carbamoylpyridin-4-yl)-2-(4,4-difluoroazepan-1-yl)-6,7-difluoroquinoline-3-carboxamide (KH10)IC500.784 nMUS-20250115578: AROMATIC FUSED RING NAV1.8 INHIBITOR, AND USE THEREOF
5-cyclopropyl-N-cyclopropylsulfonyl-4-[[1-[(3,5-dichlorophenyl)-phenylmethyl]piperidin-4-yl]methoxy]-2-fluorobenzamideIC500.8 nMUS-9694002: Substituted benzamides and methods of use thereof
4,5-dichloro-2-(4-fluoro-2-methoxyphenoxy)-N-(2-oxopiperidin-4-yl)benzamideIC501 nMUS-9758483: Pyridone amides as modulators of sodium channels
3-(4-fluoro-2-methoxyphenoxy)-N-(3-methylsulfonylphenyl)quinoxaline-2-carboxamideIC501 nMUS-9783501: Substituted quinolines as modulators of sodium channels
N-(3-carbamoyl-4-fluorophenyl)-2-(4,4-difluoroazepan-1-yl)quinoline-3-carboxamideIC501 nMUS-20250115578: AROMATIC FUSED RING NAV1.8 INHIBITOR, AND USE THEREOF
9-Chloro-2,8-difluoro-3-(trifluoromethyl)-10,11,12,13-tetrahydro-19H-5,18-methano-dibenzo[c,f]pyrido[3,2-j][1,5,9]triazacyclotridecine-15,19(14H)-dioneIC501.26 nMUS-20250368647: NITROGEN CONTAINING CONDENSED 2,3-DIHYDROQUINAZOLINONE COMPOUNDS AS NAV1.8 INHIBITORS
4-[(3R)-1-[[3-chloro-5-(trifluoromethoxy)phenyl]methyl]piperidin-3-yl]oxy-5-cyclopropyl-2-fluoro-N-methylsulfonylbenzamideIC501.3 nMUS-9694002: Substituted benzamides and methods of use thereof
3-((2R,3S,4S,5R)-3-(3,4-difluoro-2-methoxyphenyl)-4,5-dimethyl-5-(trifluoromethyl)tetrahydrofuran-2-carboxamido)pyridine 1-oxideIC501.34 nMUS-20250255878: SMALL MOLECULE INHIBITORS OF NAV1.8 SODIUM CHANNELS FOR PAIN RELIEF
2-((2R,3S,4S,5R)-3-(3,4-difluoro-2-methoxyphenyl)-4,5-dimethyl-5-(trifluoromethyl)tetrahydrofuran-2-yl)-5-fluoro-1H-benzo[d]imidazole-4-carboximidamideIC501.47 nMUS-20250255878: SMALL MOLECULE INHIBITORS OF NAV1.8 SODIUM CHANNELS FOR PAIN RELIEF
5-cyclopropyl-4-[[1-[(3,5-dichlorophenyl)-phenylmethyl]piperidin-4-yl]methoxy]-2-fluoro-N-methylsulfonylbenzamideIC501.5 nMUS-9694002: Substituted benzamides and methods of use thereof
N-(2-carbamoylpyridin-4-yl)-2-(4,4-difluoroazepan-1-yl)-7-methylquinoline-3-carboxamide (KH23)IC501.5 nMUS-20250115578: AROMATIC FUSED RING NAV1.8 INHIBITOR, AND USE THEREOF
2-Chloro-8,9-difluoro-3-(trifluoromethyl)-10,11,12,13-tetrahydro-19H-5,18-methanodibenzo[c,f]pyrido[3,2-j][1,5,9]triazacyclotridecine-15,19(14H)-dione hydrochlorideIC501.58 nMUS-20250368647: NITROGEN CONTAINING CONDENSED 2,3-DIHYDROQUINAZOLINONE COMPOUNDS AS NAV1.8 INHIBITORS
5-cyclopropyl-4-[[1-[(2S)-2-(3,5-dichlorophenyl)-1-methoxypropan-2-yl]piperidin-4-yl]methoxy]-2-fluoro-N-methylsulfonylbenzamideIC501.6 nMUS-9694002: Substituted benzamides and methods of use thereof
5-cyclopropyl-4-[[1-[(1S)-1-(3,5-dichlorophenyl)-2-methoxy-2-methylpropyl]piperidin-4-yl]methoxy]-N-ethylsulfonyl-2-fluorobenzamideIC501.6 nMUS-9694002: Substituted benzamides and methods of use thereof
5-cyclopropyl-4-[[1-[(1S)-1-(3,5-dichloro-2-fluorophenyl)ethyl]piperidin-4-yl]methoxy]-2-fluoro-N-methylsulfonylbenzamideIC501.6 nMUS-9694002: Substituted benzamides and methods of use thereof
4-[[1-[1-(2-chloro-4-fluorophenyl)-2,2,2-trifluoroethyl]piperidin-4-yl]methoxy]-5-cyclopropyl-2-fluoro-N-methylsulfonylbenzamideIC501.6 nMUS-9694002: Substituted benzamides and methods of use thereof
4-[(3R)-1-[(2-chlorophenyl)methyl]piperidin-3-yl]oxy-5-cyclopropyl-N-cyclopropylsulfonyl-2-fluorobenzamideIC501.7 nMUS-9694002: Substituted benzamides and methods of use thereof
5-cyclopropyl-4-[(3R)-1-[(2,4-dichlorophenyl)methyl]piperidin-3-yl]oxy-2-fluoro-N-methylsulfonylbenzamideIC501.7 nMUS-9694002: Substituted benzamides and methods of use thereof
5-cyclopropyl-4-[[1-[(1R)-1-(3,5-dichlorophenyl)-2-methoxy-2-methylpropyl]piperidin-4-yl]methoxy]-N-ethylsulfonyl-2-fluorobenzamideIC501.7 nMUS-9694002: Substituted benzamides and methods of use thereof
5-cyclopropyl-4-[[1-[2-(3,5-dichlorophenyl)propan-2-yl]piperidin-4-yl]methoxy]-2-fluoro-N-methylsulfonylbenzamideIC501.7 nMUS-9694002: Substituted benzamides and methods of use thereof
5-cyclopropyl-4-[[1-[(1S)-1-(3,5-dichlorophenyl)ethyl]-4-methylpiperidin-4-yl]methoxy]-2-fluoro-N-methylsulfonylbenzamideIC501.7 nMUS-9694002: Substituted benzamides and methods of use thereof
5-cyclopropyl-4-[[1-[(1S)-1-(3,5-dichlorophenyl)-2-methoxy-2-methylpropyl]piperidin-4-yl]methoxy]-2-fluoro-N-methylsulfonylbenzamideIC501.8 nMUS-9694002: Substituted benzamides and methods of use thereof
5-cyclopropyl-2-fluoro-4-[(3R)-1-[[4-fluoro-2-(trifluoromethyl)phenyl]methyl]piperidin-3-yl]oxy-N-methylsulfonylbenzamideIC501.9 nMUS-9694002: Substituted benzamides and methods of use thereof
5-cyclopropyl-4-[(3R)-1-[(1S)-1-(3,5-dichlorophenyl)ethyl]piperidin-3-yl]oxy-2-fluoro-N-methylsulfonylbenzamideIC501.9 nMUS-9694002: Substituted benzamides and methods of use thereof
4-[[1-[[3-chloro-5-(trifluoromethoxy)phenyl]methyl]piperidin-4-yl]methoxy]-5-cyclopropyl-2-fluoro-N-methylsulfonylbenzamideIC501.9 nMUS-9694002: Substituted benzamides and methods of use thereof
5-cyclopropyl-4-[[1-[2-(3,5-dichlorophenyl)propan-2-yl]piperidin-4-yl]methoxy]-N-ethylsulfonyl-2-fluorobenzamideIC501.9 nMUS-9694002: Substituted benzamides and methods of use thereof
5-cyclopropyl-4-[[1-[1-(3,5-dichlorophenyl)-2,2,2-trifluoroethyl]piperidin-4-yl]methoxy]-2-fluoro-N-methylsulfonylbenzamideIC501.9 nMUS-9694002: Substituted benzamides and methods of use thereof
N-(azetidin-1-ylsulfonyl)-4-[(3R,6R)-1-[(2-chloro-4-fluorophenyl)methyl]-6-methylpiperidin-3-yl]oxy-5-cyclopropyl-2-fluorobenzamideIC501.9 nMUS-9694002: Substituted benzamides and methods of use thereof
4-[(3R,6R)-1-[(2-chloro-4-fluorophenyl)methyl]-6-methylpiperidin-3-yl]oxy-5-cyclopropyl-N-cyclopropylsulfonyl-2-fluorobenzamideIC501.9 nMUS-9694002: Substituted benzamides and methods of use thereof
2-(4-fluoro-2-methoxyphenoxy)-N-(2-oxopiperidin-4-yl)-4-(trifluoromethyl)benzamideIC502 nMUS-9758483: Pyridone amides as modulators of sodium channels
2-(2-chloro-4-fluorophenoxy)-N-(3-sulfamoylphenyl)quinoline-3-carboxamideIC502 nMUS-9783501: Substituted quinolines as modulators of sodium channels
5-cyclopropyl-4-[[1-[1-(3,5-dichlorophenyl)propyl]piperidin-4-yl]methoxy]-2-fluoro-N-methylsulfonylbenzamideIC502 nMUS-9694002: Substituted benzamides and methods of use thereof
4-[[1-[bis(3-chlorophenyl)methyl]piperidin-4-yl]methoxy]-5-cyclopropyl-2-fluoro-N-methylsulfonylbenzamideIC502 nMUS-9694002: Substituted benzamides and methods of use thereof
4-[[1-[bis(2-chlorophenyl)methyl]piperidin-4-yl]methoxy]-5-cyclopropyl-2-fluoro-N-methylsulfonylbenzamideIC502 nMUS-9694002: Substituted benzamides and methods of use thereof
8,9-Dichloro-2,3-difluoro-10,11,12,13-tetrahydro-19H-5,18-methanodibenzo[c,f]pyrido[3,2-j][1,5,9]triazacyclotridecine-15,19(14H)-dione hydrochlorideIC502 nMUS-20250368647: NITROGEN CONTAINING CONDENSED 2,3-DIHYDROQUINAZOLINONE COMPOUNDS AS NAV1.8 INHIBITORS
US12441703, Compound 117IC502 nMUS-12441703: Carboxamides as modulators of sodium channels
4-[[2-Fluoro-6-[2-Methoxy-4-(Trifluoromethoxy)Phenoxy]-3-(Trifluoromethyl)Benzoyl]Amino]-1-Oxido-Pyridin-1-Ium-2-CarboxamideIC502 nMUS-12441703: Carboxamides as modulators of sodium channels
4-[[2-Fluoro-4-Methoxy-6-[2-Methoxy-4-(Trifluoromethoxy)Phenoxy]-3-Methyl-Benzoyl]Amino]Pyridine-2-CarboxamideIC502 nMUS-12441703: Carboxamides as modulators of sodium channels
4-[[6-[2-Methoxy-4-(Trifluoromethoxy)Phenoxy]-2-Methylsulfanyl-3-(Trifluoromethyl)Benzoyl]Amino]Pyridine-2-CarboxamideIC502 nMUS-12441703: Carboxamides as modulators of sodium channels
5-cyclopropyl-N-cyclopropylsulfonyl-4-[(3R)-1-(3,5-dichlorophenyl)piperidin-3-yl]oxy-2-fluorobenzamideIC502.1 nMUS-9694002: Substituted benzamides and methods of use thereof
4-[[1-[[2,5-bis(trifluoromethyl)phenyl]methyl]-4-methylpiperidin-4-yl]methoxy]-5-cyclopropyl-2-fluoro-N-methylsulfonylbenzamideIC502.1 nMUS-9694002: Substituted benzamides and methods of use thereof
4-[[1-[[3-chloro-5-(trifluoromethyl)phenyl]methyl]piperidin-4-yl]methoxy]-5-cyclopropyl-2-fluoro-N-methylsulfonylbenzamideIC502.1 nMUS-9694002: Substituted benzamides and methods of use thereof
4-[[1-[bis(4-chlorophenyl)methyl]piperidin-4-yl]methoxy]-5-cyclopropyl-N-cyclopropylsulfonyl-2-fluorobenzamideIC502.1 nMUS-9694002: Substituted benzamides and methods of use thereof

ChEMBL bioactivities

786 potent at pChembl≥5 of 832 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
9.52IC500.3nMCHEMBL4760292
9.40IC500.4nMCHEMBL4798938
9.30IC500.5nMCHEMBL4777598
9.10IC500.8nMCHEMBL4753280
9.10IC500.8nMCHEMBL5845128
9.05IC500.9nMCHEMBL4781110
9.00IC501nMCHEMBL4745699
9.00IC501nMCHEMBL3678273
9.00IC501nMCHEMBL1277958
8.89IC501.3nMCHEMBL4744908
8.89IC501.3nMCHEMBL5857630
8.85IC501.4nMCHEMBL4750365
8.85IC501.4nMCHEMBL5830546
8.85IC501.4nMCHEMBL5893052
8.80IC501.6nMCHEMBL4764433
8.80IC501.6nMCHEMBL4787299
8.80IC501.6nMCHEMBL5809224
8.77IC501.7nMCHEMBL4756380
8.74IC501.8nMCHEMBL4782190
8.72IC501.9nMCHEMBL5921039
8.70IC502nMCHEMBL4483603
8.70IC502nMCHEMBL4785523
8.70IC502nMCHEMBL4761578
8.70IC502nMCHEMBL3683097
8.70IC502nMCHEMBL5831350
8.70IC502nMCHEMBL1269882
8.70IC502nMCHEMBL1270797
8.70IC502nMCHEMBL1277877
8.70IC502nMCHEMBL1277959
8.68IC502.1nMCHEMBL5971266
8.68IC502.1nMCHEMBL5763799
8.68IC502.1nMCHEMBL5901106
8.64IC502.3nMCHEMBL4763419
8.62IC502.4nMCHEMBL5846599
8.59IC502.6nMCHEMBL4743638
8.55IC502.8nMCHEMBL4751356
8.55IC502.8nMCHEMBL6036529
8.54IC502.9nMCHEMBL6004691
8.52IC503nMCHEMBL4748189
8.52IC503nMCHEMBL4764805
8.52IC503nMCHEMBL3678270
8.52IC503nMCHEMBL1270208
8.52IC503nMCHEMBL1277514
8.51IC503.1nMCHEMBL4778738
8.49IC503.2nMCHEMBL5771593
8.48IC503.3nMCHEMBL5901106
8.42IC503.8nMCHEMBL6054432
8.41IC503.9nMCHEMBL4777784
8.41IC503.9nMCHEMBL6022104
8.40IC504nMCHEMBL4759624

PubChem BioAssay actives

204 with measured affinity, of 497 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

CompoundAssayTypeValueUnit
5-chloro-2-(4,4-difluoroazepan-1-yl)-6-methyl-N-(2-sulfamoyl-4-pyridinyl)pyridine-3-carboxamide1678547: Inhibition of human Nav1.8 expressed in HEK293 cells by whole cell patch clamp assayic500.0003uM
4-[[2-fluoro-6-[3-fluoro-2-methoxy-4-(trifluoromethoxy)phenoxy]-4-methoxy-3-(trifluoromethyl)benzoyl]amino]pyridine-2-carboxamide1678558: Inhibition of human Nav1.8 expressed in HEK cells applied electrical stimulus 10 Hz for 10 seconds measuring relaxation to the resting state followed by post stimulation by E-VIPR Assayic500.0004uM
2-(4,4-difluoroazepan-1-yl)-6-methyl-N-(2-sulfamoyl-4-pyridinyl)-5-(trifluoromethyl)pyridine-3-carboxamide1678547: Inhibition of human Nav1.8 expressed in HEK293 cells by whole cell patch clamp assayic500.0005uM
4-[[2-fluoro-6-[3-fluoro-2-methoxy-4-(trifluoromethoxy)phenoxy]-3-methyl-4-(trifluoromethyl)benzoyl]amino]pyridine-2-carboxamide1678558: Inhibition of human Nav1.8 expressed in HEK cells applied electrical stimulus 10 Hz for 10 seconds measuring relaxation to the resting state followed by post stimulation by E-VIPR Assayic500.0008uM
6-(cyclopropylmethyl)-2-(4,4-difluoroazepan-1-yl)-N-(2-sulfamoyl-4-pyridinyl)pyridine-3-carboxamide1678547: Inhibition of human Nav1.8 expressed in HEK293 cells by whole cell patch clamp assayic500.0009uM
5-(cyclopropylmethyl)-2-(4,4-difluoroazepan-1-yl)-N-(2-sulfamoyl-4-pyridinyl)pyridine-3-carboxamide1678547: Inhibition of human Nav1.8 expressed in HEK293 cells by whole cell patch clamp assayic500.0010uM
6-(4-ethoxyphenyl)-N-(3-methylphenyl)pyrazine-2-carboxamide536194: Inhibition of human recombinant NaV1.8 expressed in HEK293 cells by conventional voltage clamp electrophysiology assayic500.0010uM
4-[[4-chloro-2-fluoro-6-[3-fluoro-2-methoxy-4-(trifluoromethoxy)phenoxy]-3-methoxybenzoyl]amino]pyridine-2-carboxamide1678558: Inhibition of human Nav1.8 expressed in HEK cells applied electrical stimulus 10 Hz for 10 seconds measuring relaxation to the resting state followed by post stimulation by E-VIPR Assayic500.0013uM
4-[[4-chloro-2-fluoro-6-[3-fluoro-2-methoxy-4-(trifluoromethoxy)phenoxy]-3-methylbenzoyl]amino]pyridine-2-carboxamide1678558: Inhibition of human Nav1.8 expressed in HEK cells applied electrical stimulus 10 Hz for 10 seconds measuring relaxation to the resting state followed by post stimulation by E-VIPR Assayic500.0014uM
2-(4,4-difluoroazepan-1-yl)-5,6-dimethyl-N-(2-sulfamoyl-4-pyridinyl)pyridine-3-carboxamide1678547: Inhibition of human Nav1.8 expressed in HEK293 cells by whole cell patch clamp assayic500.0016uM
4-[[2-fluoro-6-[3-fluoro-2-methoxy-4-(trifluoromethoxy)phenoxy]-3-methoxy-4-(trifluoromethyl)benzoyl]amino]pyridine-2-carboxamide1678558: Inhibition of human Nav1.8 expressed in HEK cells applied electrical stimulus 10 Hz for 10 seconds measuring relaxation to the resting state followed by post stimulation by E-VIPR Assayic500.0016uM
4-[[3-chloro-2-fluoro-6-[3-fluoro-2-methoxy-4-(trifluoromethoxy)phenoxy]-4-methoxybenzoyl]amino]pyridine-2-carboxamide1678558: Inhibition of human Nav1.8 expressed in HEK cells applied electrical stimulus 10 Hz for 10 seconds measuring relaxation to the resting state followed by post stimulation by E-VIPR Assayic500.0017uM
4-[[2-fluoro-4-methoxy-6-[2-methoxy-4-(trifluoromethoxy)phenoxy]-3-(trifluoromethyl)benzoyl]amino]pyridine-2-carboxamide1678558: Inhibition of human Nav1.8 expressed in HEK cells applied electrical stimulus 10 Hz for 10 seconds measuring relaxation to the resting state followed by post stimulation by E-VIPR Assayic500.0018uM
4-[[2-bromo-6-[2-methoxy-4-(trifluoromethoxy)phenoxy]-3-(trifluoromethyl)benzoyl]amino]pyridine-2-carboxamide1678558: Inhibition of human Nav1.8 expressed in HEK cells applied electrical stimulus 10 Hz for 10 seconds measuring relaxation to the resting state followed by post stimulation by E-VIPR Assayic500.0020uM
4-[[2-chloro-6-[2-methoxy-4-(trifluoromethoxy)phenoxy]-3-(trifluoromethyl)benzoyl]amino]pyridine-2-carboxamide1678558: Inhibition of human Nav1.8 expressed in HEK cells applied electrical stimulus 10 Hz for 10 seconds measuring relaxation to the resting state followed by post stimulation by E-VIPR Assayic500.0020uM
(1S)-1-(6-tert-butyl-1H-benzimidazol-2-yl)butan-1-amine1534919: Inhibition of human Nav1.8 expressed in HEK cells by patch-clamp electrophysiology methodic500.0020uM
N-(3,5-dimethylphenyl)-6-(4-ethoxyphenyl)pyrazine-2-carboxamide536194: Inhibition of human recombinant NaV1.8 expressed in HEK293 cells by conventional voltage clamp electrophysiology assayic500.0020uM
6-(4-ethoxyphenyl)-N-[(2-methylphenyl)methyl]pyrazine-2-carboxamide536194: Inhibition of human recombinant NaV1.8 expressed in HEK293 cells by conventional voltage clamp electrophysiology assayic500.0020uM
5-(4-chlorophenyl)-N-[(2-methylphenyl)methyl]pyridine-3-carboxamide527216: Inhibition of human NaV1.8 by electrophysiologyic500.0020uM
N-(3,5-dimethylphenyl)-5-[4-(trifluoromethoxy)phenyl]furan-2-carboxamide527216: Inhibition of human NaV1.8 by electrophysiologyic500.0020uM
4-[[3-chloro-2-fluoro-6-[3-fluoro-2-methoxy-4-(trifluoromethoxy)phenoxy]benzoyl]amino]pyridine-2-carboxamide1678558: Inhibition of human Nav1.8 expressed in HEK cells applied electrical stimulus 10 Hz for 10 seconds measuring relaxation to the resting state followed by post stimulation by E-VIPR Assayic500.0023uM
5-chloro-6-cyclobutyl-2-(4,4-difluoroazepan-1-yl)-N-(2-sulfamoyl-4-pyridinyl)pyridine-3-carboxamide1678547: Inhibition of human Nav1.8 expressed in HEK293 cells by whole cell patch clamp assayic500.0026uM
2-(4,4-difluoroazepan-1-yl)-N-(2-sulfamoyl-4-pyridinyl)-5-(trifluoromethoxy)pyridine-3-carboxamide1678547: Inhibition of human Nav1.8 expressed in HEK293 cells by whole cell patch clamp assayic500.0028uM
6-cyclopropyl-2-(4,4-difluoroazepan-1-yl)-N-(2-sulfamoyl-4-pyridinyl)pyridine-3-carboxamide1678547: Inhibition of human Nav1.8 expressed in HEK293 cells by whole cell patch clamp assayic500.0030uM
5-(4-chlorophenyl)-N-[[2-(2,2,2-trifluoroethoxy)-3-pyridinyl]methyl]pyridine-3-carboxamide527216: Inhibition of human NaV1.8 by electrophysiologyic500.0030uM
4-[[6-[3-fluoro-2-methoxy-4-(trifluoromethoxy)phenoxy]-2-methyl-3-(trifluoromethyl)benzoyl]amino]pyridine-2-carboxamide1678558: Inhibition of human Nav1.8 expressed in HEK cells applied electrical stimulus 10 Hz for 10 seconds measuring relaxation to the resting state followed by post stimulation by E-VIPR Assayic500.0030uM
6-(4-chlorophenyl)-N-(3,5-dimethylphenyl)pyrazine-2-carboxamide536194: Inhibition of human recombinant NaV1.8 expressed in HEK293 cells by conventional voltage clamp electrophysiology assayic500.0030uM
2-(4,4-difluoroazepan-1-yl)-6-methyl-N-(2-sulfamoyl-4-pyridinyl)pyridine-3-carboxamide1678547: Inhibition of human Nav1.8 expressed in HEK293 cells by whole cell patch clamp assayic500.0031uM
5-chloro-2-(4,4-difluoroazepan-1-yl)-N-(2-sulfamoyl-4-pyridinyl)pyridine-3-carboxamide1678547: Inhibition of human Nav1.8 expressed in HEK293 cells by whole cell patch clamp assayic500.0039uM
4-[[6-[2-methoxy-4-(trifluoromethoxy)phenoxy]-2-methyl-3-(trifluoromethyl)benzoyl]amino]pyridine-2-carboxamide1678558: Inhibition of human Nav1.8 expressed in HEK cells applied electrical stimulus 10 Hz for 10 seconds measuring relaxation to the resting state followed by post stimulation by E-VIPR Assayic500.0040uM
5-(4-chlorophenyl)-N-[(2-chlorophenyl)methyl]pyridine-3-carboxamide527216: Inhibition of human NaV1.8 by electrophysiologyic500.0040uM
2-(4,4-difluoroazepan-1-yl)-N-(2-sulfamoyl-4-pyridinyl)-5-(trifluoromethyl)pyridine-3-carboxamide1678547: Inhibition of human Nav1.8 expressed in HEK293 cells by whole cell patch clamp assayic500.0041uM
5-chloro-6-cyclopropyl-2-(4,4-difluoroazepan-1-yl)-N-(2-sulfamoyl-4-pyridinyl)pyridine-3-carboxamide1678547: Inhibition of human Nav1.8 expressed in HEK293 cells by whole cell patch clamp assayic500.0045uM
N-(3-methylphenyl)-6-[4-(trifluoromethoxy)phenyl]pyrazine-2-carboxamide536194: Inhibition of human recombinant NaV1.8 expressed in HEK293 cells by conventional voltage clamp electrophysiology assayic500.0050uM
2-(4,4-difluoroazepan-1-yl)-N-(2-sulfamoyl-4-pyridinyl)-6-(trifluoromethyl)pyridine-3-carboxamide1678547: Inhibition of human Nav1.8 expressed in HEK293 cells by whole cell patch clamp assayic500.0053uM
6-chloro-2-(4,4-difluoroazepan-1-yl)-N-(2-sulfamoyl-4-pyridinyl)pyridine-3-carboxamide1678547: Inhibition of human Nav1.8 expressed in HEK293 cells by whole cell patch clamp assayic500.0058uM
2-(4,4-difluoroazepan-1-yl)-N-(3-sulfamoylphenyl)-5-(trifluoromethyl)pyridine-3-carboxamide2094925: Inhibition of recombinant human Nav1.8 expressed in HEK293 cells by whole cell patch clamp methodec500.0060uM
6-(4-chlorophenyl)-N-(3-methylphenyl)pyrazine-2-carboxamide536194: Inhibition of human recombinant NaV1.8 expressed in HEK293 cells by conventional voltage clamp electrophysiology assayic500.0060uM
6-(4-chlorophenyl)-N-(3,5-dimethoxyphenyl)pyrazine-2-carboxamide536194: Inhibition of human recombinant NaV1.8 expressed in HEK293 cells by conventional voltage clamp electrophysiology assayic500.0060uM
5-cyclobutyl-2-(4,4-difluoropiperidin-1-yl)-6-methyl-N-(2-sulfamoyl-4-pyridinyl)pyridine-3-carboxamide1678547: Inhibition of human Nav1.8 expressed in HEK293 cells by whole cell patch clamp assayic500.0065uM
5-(4-chlorophenyl)-N-[(2-ethoxy-3-pyridinyl)methyl]pyridine-3-carboxamide527216: Inhibition of human NaV1.8 by electrophysiologyic500.0070uM
5-(4-chlorophenyl)-N-(3,5-dimethoxyphenyl)furan-2-carboxamide1974346: Inhibition of Nav1.8 (unknown origin)ic500.0080uM
6-(4-cyanophenyl)-N-(3,5-dimethylphenyl)pyrazine-2-carboxamide536194: Inhibition of human recombinant NaV1.8 expressed in HEK293 cells by conventional voltage clamp electrophysiology assayic500.0080uM
N-(3,5-dimethylphenyl)-5-[4-(trifluoromethoxy)phenyl]-1,2,4-thiadiazole-3-carboxamide527216: Inhibition of human NaV1.8 by electrophysiologyic500.0080uM
5-(4-chlorophenyl)-N-[(2-piperidin-1-ylphenyl)methyl]pyridine-3-carboxamide527216: Inhibition of human NaV1.8 by electrophysiologyic500.0080uM
5-(4-chlorophenyl)-N-(3,5-dimethylphenyl)pyridine-3-carboxamide527216: Inhibition of human NaV1.8 by electrophysiologyic500.0090uM
5-(4-chlorophenyl)-N-[(2-morpholin-4-ylphenyl)methyl]pyridine-3-carboxamide527216: Inhibition of human NaV1.8 by electrophysiologyic500.0100uM
4-[2-[(1R,2R)-1-amino-2-methoxypropyl]-3H-benzimidazol-5-yl]-2-fluorobenzonitrile1246068: Inhibition of human NaV1.8 channel in HEK cells by patch clamp electrophysiology assayic500.0105uM
5-(2-cyclopropylethynyl)-2-(4,4-difluoropiperidin-1-yl)-6-methyl-N-(2-sulfamoyl-4-pyridinyl)pyridine-3-carboxamide1678547: Inhibition of human Nav1.8 expressed in HEK293 cells by whole cell patch clamp assayic500.0120uM
2-(azepan-1-yl)-N-(3-sulfamoylphenyl)-5-(trifluoromethyl)pyridine-3-carboxamide2094925: Inhibition of recombinant human Nav1.8 expressed in HEK293 cells by whole cell patch clamp methodec500.0120uM

CTD chemical–gene interactions

15 total (human), top 15 by PubMed support.

ChemicalActions (top 5)PubMed papers
Benzo(a)pyrenedecreases expression, increases methylation2
kojic aciddecreases expression1
decamethrindecreases reaction, increases activity1
cupric oxidedecreases phosphorylation1
CGP 52608affects binding, increases reaction1
BIII 890 CLdecreases reaction, increases activity1
NW 1029decreases reaction, increases activity1
Diethylhexyl Phthalatedecreases expression1
Mexiletinedecreases reaction, increases activity1
Sarinincreases expression1
Smokeincreases expression1
Tetracainedecreases reaction, increases activity1
Valproic Aciddecreases methylation1
Vanadiumincreases expression1
Aflatoxin B1decreases methylation1

ChEMBL screening assays

144 unique, capped per target: 124 binding, 16 functional, 4 admet

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL3430568FunctionalInhibition of Na channel (species unknown)Simulation of multiple ion channel block provides improved early prediction of compounds’ clinical torsadogenic risk. — Cardiovasc Res
CHEMBL4880115BindingNa+ channel CEREP ligand profilingData for DCP probe A-079
CHEMBL4623838ADMETInhibition of human Nav1.8 expressed in ND7/23 cells at 100 uM with -120 mV holding potential by whole cell manual patch clamp method relative to controlDiscovery of DS-1971a, a Potent, Selective NaV1.7 Inhibitor. — J Med Chem

Cellosaurus cell lines

11 cell lines: 9 induced pluripotent stem cell, 1 spontaneously immortalized cell line, 1 transformed cell line

First 10 cell lines (id-ordered, not curated):

CellosaurusNameCategorySex
CVCL_A4UDUMGi126-A.9Induced pluripotent stem cellMale
CVCL_A4UEUMGi126-A.12Induced pluripotent stem cellMale
CVCL_A4UFUMGi126-A.13Induced pluripotent stem cellMale
CVCL_C0GNUMGi158-A-1.1Induced pluripotent stem cellFemale
CVCL_C0GPUMGi158-A-1.2Induced pluripotent stem cellFemale
CVCL_C0YDB’SYS CHO Nav1.8/beta3Spontaneously immortalized cell lineFemale
CVCL_D1KKPrecisION hNav1.8/beta1-HEKTransformed cell lineFemale
CVCL_VR98UKWNLi003-AInduced pluripotent stem cellFemale
CVCL_VR99UKWNLi004-AInduced pluripotent stem cellFemale
CVCL_WZ29XACHi001-AInduced pluripotent stem cellMale

Clinical trials (associated diseases)

300 trials via MONDO — disease-level, not drug-specific.

TrialPhaseStatusTitle
NCT00702117PHASE4COMPLETEDAjmaline Utilization in the Diagnosis and Treatment of Cardiac Arrhythmias
NCT00211796PHASE4COMPLETEDDivalproex Sodium ER in Adult Autism
NCT00391261PHASE4COMPLETEDAn Open-label Trial of Metformin for Weight Control of Pediatric Patients on Antipsychotic Medications.
NCT00409747PHASE4COMPLETEDMinocycline to Treat Childhood Regressive Autism
NCT00576732PHASE4COMPLETEDA Study of the Effectiveness and Safety of Two Doses of Risperidone in the Treatment of Children and Adolescents With Autistic Disorder
NCT00844753PHASE4COMPLETEDAtomoxetine, Placebo and Parent Management Training in Autism
NCT01028820PHASE4COMPLETEDFMRI Brain Activation of Aripiprazole Treatment in Autism Spectrum Disorders
NCT01098383PHASE4UNKNOWNTreatment With Acetyl-Choline Esterase Inhibitors in Children With Autism Spectrum Disorders
NCT01333865PHASE4COMPLETEDA Study of Memantine Hydrochloride (Namenda®) for Cognitive and Behavioral Impairment in Adults With Autism Spectrum Disorders
NCT01337700PHASE4COMPLETEDMilnacipran in Autism and the Functional Locus Coeruleus and Noradrenergic Model of Autism
NCT01695200PHASE4COMPLETEDOmega-3 Fatty Acids in Autism Spectrum Disorders
NCT02069977PHASE4UNKNOWNStudy to Evaluate the Efficacy and Safety of Aripiprazole
NCT02096952PHASE4COMPLETEDMethylphenidate ER Liquid Formulation in Adults With ASD and ADHD
NCT02199925PHASE4UNKNOWNAn Open-Label Study to Evaluate the Efficacy of High-Dose Gammaplex in Children on the Autism Spectrum
NCT02235467PHASE4COMPLETEDMultisite Study: Parental Training Using Video Modelling to Develop Social Skills in Children With Autism
NCT02255565PHASE4COMPLETEDDose Response Effects of Quillivant XR in Children With ADHD and Autism: A Pilot Study
NCT02940574PHASE4COMPLETEDNeural and Behavioral Effects of Oxytocin in Autism Spectrum Disorders
NCT03333629PHASE4COMPLETEDPromoting Positive Outcomes for Individuals With ASD: Linking Early Detection, Treatment, and Long-term Outcomes
NCT03337646PHASE4COMPLETEDEvaluation of the Effect and Safety of Lisdexamfetamine in Children Aged 6-12 With ADHD and Autism
NCT03538431PHASE4COMPLETEDImproving Driving in Young People With Autism Spectrum Disorders
NCT03757585PHASE4COMPLETEDNatural Treatments for the Management of Emotional Dysregulation in Youth With Non-verbal Learning Disability (NVLD) and/or Autism Spectrum Disorders (ASD)
NCT04903353PHASE4COMPLETEDPragmatic Trial Comparing Weight Gain in Children With Autism Taking Risperidone Versus Aripiprazole
NCT05063656PHASE4COMPLETEDBiomarker-Driven Pharmacological Treatment of Adolescents With Autism Spectrum Disorder With Gabapentin
NCT05146245PHASE4UNKNOWNSafety and Pharmacokinetics of Antipsychotics in Children 2: Studying TDM in an RCT
NCT05916339PHASE4RECRUITINGAWARE: Management of ADHD in Autism Spectrum Disorder
NCT05954052PHASE4TERMINATEDA Study of Glutathione in Children With Autism Spectrum Disorder
NCT06853665PHASE4RECRUITINGThe TEAM Study - Treatment Efficacy for Autism/Attention Using Mixed Amphetamine
NCT07054697PHASE4COMPLETEDPilot-RCT With Individualized Homeopathic Treatment in the Children With Autism Spectrum Disorder
NCT07161804PHASE4COMPLETEDPilot RCT Using Homeopathic Medicines in ASD
NCT07439042PHASE4NOT_YET_RECRUITINGBuspirone for Anxiety in Autistic Youth
NCT00701077PHASE3TERMINATEDDAPERB 3,4-DiAminoPyridine and Electrophysiological Response in Brugada Syndrome
NCT00927732PHASE3TERMINATEDHydroquinidine Versus Placebo in Patients With Brugada Syndrome
NCT00036231PHASE3TERMINATEDSynthetic Human Secretin in Children With Autism and Gastrointestinal Dysfunction
NCT00036244PHASE3COMPLETEDSynthetic Human Secretin in Children With Autism
NCT00065884PHASE3UNKNOWNValproate Response in Aggressive Autistic Adolescents
NCT00065962PHASE3COMPLETEDSecretin for the Treatment of Autism
NCT00252603PHASE3COMPLETEDGalantamine Versus Placebo in Childhood Autism
NCT00346736PHASE3COMPLETEDUse of Acupuncture In Children With Autistic Spectrum Disorder
NCT00352248PHASE3COMPLETEDRandomized Controlled Trial of Acupuncture Versus Sham Acupuncture in Autistic Spectrum Disorder
NCT00352352PHASE3COMPLETEDUse of Acupuncture In Children With Autistic Spectrum Disorder