Brugada syndrome 1

disease
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Also known as BRGDA1Brugada syndrome caused by mutation in SCN5ABrugada syndrome type 1SCN5A Brugada syndrome

Summary

Brugada syndrome 1 (MONDO:0011001) is a disease caused by SCN5A (GenCC Definitive), with 18 cohort genes and 2 clinical trials. The dominant Reactome pathway is Cardiac conduction (8 cohort genes).

At a glance

  • Causal gene: SCN5A (GenCC Definitive)
  • Cohort genes: 18
  • ClinVar variants: 666
  • Clinical trials: 2

Clinical features

No curated clinical features (Orphanet) for this disease.

Identifiers

Disease identifiers

FieldValue
Canonical nameBrugada syndrome 1
Mondo IDMONDO:0011001
OMIM601144
DOIDDOID:0110218
UMLSC4551804
MedGen1646402
GARD0024766
Is cancer (heuristic)no

Also known as: BRGDA1 · Brugada syndrome 1 · Brugada syndrome caused by mutation in SCN5A · Brugada syndrome type 1 · SCN5A Brugada syndrome

Data availability: 666 ClinVar variants · 13 GenCC gene-disease records.

Disease family

Classification path: disease › human disease › disease by body system or component › cardiovascular disorderheart disorderheart conduction diseaseBrugada syndromeBrugada syndrome 1

Related subtypes (8): Brugada syndrome 2, Brugada syndrome 3, Brugada syndrome 4, Brugada syndrome 5, Brugada syndrome 6, Brugada syndrome 7, Brugada syndrome 8, Brugada syndrome 9

Genetics & variants

GWAS landscape

No GWAS associations recorded — common-variant (GWAS) studies don’t cover this disease (typical for Mendelian / rare diseases). See the curated gene cohort and Mendelian overlap below.

Variant details and genetic-evidence tiers

ClinVar germline variants

600 retrieved; paginated sample, class counts are floors:

270 uncertain significance, 198 conflicting classifications of pathogenicity, 47 benign/likely benign, 32 pathogenic/likely pathogenic, 22 likely pathogenic, 22 pathogenic, 8 likely benign, 1 benign

ClinVarVariant (HGVS)GeneClassificationReview
440848NM_198056.2(SCN5A):c.[3694C>T;4859C>T]Pathogenicno assertion criteria provided
440850NM_000335.4(SCN5A):c.[3919C>T;694G>A]Pathogenicno assertion criteria provided
264175NM_000138.5(FBN1):c.3G>T (p.Met1Ile)FBN1Pathogeniccriteria provided, multiple submitters, no conflicts
406434NM_000335.5(SCN5A):c.3282G>A (p.Trp1094Ter)LOC110121269Pathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
1327132NM_000335.5(SCN5A):c.4296+1delSCN5APathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
1527869NM_000335.5(SCN5A):c.2678G>T (p.Arg893Leu)SCN5APathogeniccriteria provided, single submitter
1691761NM_000335.5(SCN5A):c.175C>T (p.Gln59Ter)SCN5APathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
179829NM_000335.5(SCN5A):c.1936del (p.Gln646fs)SCN5APathogeniccriteria provided, multiple submitters, no conflicts
1803812NM_000335.5(SCN5A):c.104dup (p.Ser36fs)SCN5APathogenicno assertion criteria provided
180520NM_000335.5(SCN5A):c.1140+1G>ASCN5APathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
201427NM_000335.5(SCN5A):c.611+1G>ASCN5APathogeniccriteria provided, multiple submitters, no conflicts
201438NM_000335.5(SCN5A):c.664C>T (p.Arg222Ter)SCN5APathogeniccriteria provided, multiple submitters, no conflicts
201508NM_000335.5(SCN5A):c.4242+1G>CSCN5APathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
201559NM_000335.5(SCN5A):c.2533del (p.Val845fs)SCN5APathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
201560NM_000335.5(SCN5A):c.2550_2551dup (p.Phe851fs)SCN5APathogeniccriteria provided, multiple submitters, no conflicts
201566NM_000335.5(SCN5A):c.3488dup (p.Glu1164fs)SCN5APathogeniccriteria provided, multiple submitters, no conflicts
201572NM_000335.5(SCN5A):c.4844TCT[1] (p.Phe1616del)SCN5APathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
2107170NM_000335.5(SCN5A):c.1947T>A (p.Cys649Ter)SCN5APathogeniccriteria provided, multiple submitters, no conflicts
222814NM_000335.5(SCN5A):c.4471AAG[1] (p.Lys1492del)SCN5APathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
254156NM_000335.5(SCN5A):c.5353_5354del (p.Leu1785fs)SCN5APathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
254157NM_198056.2(SCN5A):c.4813+3_4813+6dupSCN5APathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
263423NM_000335.5(SCN5A):c.4716C>T (p.Gly1572=)SCN5APathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
264039NM_000335.5(SCN5A):c.4420del (p.Gln1474fs)SCN5APathogeniccriteria provided, multiple submitters, no conflicts
264276NM_000335.5(SCN5A):c.4882C>T (p.Arg1628Ter)SCN5APathogeniccriteria provided, multiple submitters, no conflicts
3238947NM_000335.5(SCN5A):c.1551del (p.Thr518fs)SCN5APathogeniccriteria provided, single submitter
3248566NM_000335.5(SCN5A):c.1978C>T (p.Gln660Ter)SCN5APathogeniccriteria provided, single submitter
3438263NM_000335.5(SCN5A):c.1576del (p.Arg526fs)SCN5APathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
3778738NM_000335.5(SCN5A):c.1036G>T (p.Glu346Ter)SCN5APathogeniccriteria provided, single submitter
39444NM_000335.5(SCN5A):c.665G>A (p.Arg222Gln)SCN5APathogeniccriteria provided, multiple submitters, no conflicts
406415NM_000335.5(SCN5A):c.5414_5417del (p.Thr1805fs)SCN5APathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts

Genes & proteins

Mendelian disease overlap and somatic drivers

GenCC: 83 · Orphanet: 68 · OMIM-shared: 0 · Dual-evidence (GWAS+Mendelian): 0

GenCC gene–disease validity (cohort genes)

the Disease column is the GenCC-asserted condition — a cohort gene’s strongest validity may be for a related predisposition syndrome.

GeneClassificationInheritanceDiseaseRecords
SCN5ADefinitiveAutosomal dominantBrugada syndrome 123
HCN4ModerateAutosomal dominantBrugada syndrome 88
SCN1BModerateAutosomal dominantBrugada syndrome 515
SCN2BSupportiveAutosomal dominantBrugada syndrome7
CACNA2D1LimitedUnknownBrugada syndrome8
GPD1LLimitedUnknownBrugada syndrome 23
KCND3LimitedAutosomal dominantBrugada syndrome 98
KCNJ8LimitedUnknownBrugada syndrome5
PKP2LimitedAutosomal dominantBrugada syndrome6

Orphanet rare-disease linkage (cohort genes)

GeneOrphanet IDRare disease
SCN1BOrphanet:130Brugada syndrome
SCN1BOrphanet:1934Early infantile developmental and epileptic encephalopathy
SCN1BOrphanet:33069Dravet syndrome
SCN1BOrphanet:334Hereditary atrial fibrillation
SCN1BOrphanet:36387Genetic epilepsy with febrile seizure plus
SCN1BOrphanet:871Hereditary progressive cardiac conduction defect
SCN5AOrphanet:101016Romano-Ward syndrome
SCN5AOrphanet:130Brugada syndrome
SCN5AOrphanet:1344Isolated atrial standstill
SCN5AOrphanet:154Familial isolated dilated cardiomyopathy
SCN5AOrphanet:166282Hereditary sick sinus syndrome
SCN5AOrphanet:228140Idiopathic ventricular fibrillation
SCN5AOrphanet:334Hereditary atrial fibrillation
SCN5AOrphanet:871Hereditary progressive cardiac conduction defect
CACNA2D1Orphanet:130Brugada syndrome
CACNA2D1Orphanet:442835Non-specific early-onset epileptic encephalopathy
CACNA2D1Orphanet:51083Congenital short QT syndrome
SCN2BOrphanet:130Brugada syndrome
SCN2BOrphanet:334Hereditary atrial fibrillation
HCN4Orphanet:130Brugada syndrome
HCN4Orphanet:166282Hereditary sick sinus syndrome
GPD1LOrphanet:130Brugada syndrome
KCND3Orphanet:130Brugada syndrome
KCND3Orphanet:98772Spinocerebellar ataxia type 19/22
KCNJ8Orphanet:130Brugada syndrome
KCNJ8Orphanet:1517Cantú syndrome
PKP2Orphanet:130Brugada syndrome
PKP2Orphanet:293888Inherited isolated arrhythmogenic cardiomyopathy, dominant-left variant
PKP2Orphanet:293899Inherited isolated arrhythmogenic ventricular dysplasia, biventricular variant
PKP2Orphanet:293910Inherited isolated arrhythmogenic cardiomyopathy, dominant-right variant
PKP2Orphanet:54260Left ventricular noncompaction
SCN10AOrphanet:101016Romano-Ward syndrome
SCN10AOrphanet:130Brugada syndrome
SCN10AOrphanet:306577Hereditary sodium channelopathy-related small fibers neuropathy
SCN10AOrphanet:46348Paroxysmal extreme pain disorder
SCN10AOrphanet:88642Congenital insensitivity to pain-anosmia-neuropathic arthropathy
SCN10AOrphanet:90026Primary erythromelalgia
SCNN1AOrphanet:130Brugada syndrome
SCNN1AOrphanet:171876Generalized pseudohypoaldosteronism type 1
SCNN1AOrphanet:526Liddle syndrome
SCNN1AOrphanet:60033Idiopathic bronchiectasis
DSPOrphanet:154Familial isolated dilated cardiomyopathy
DSPOrphanet:158687Lethal acantholytic erosive disorder
DSPOrphanet:2032Idiopathic pulmonary fibrosis
DSPOrphanet:293165Skin fragility-woolly hair-palmoplantar keratoderma syndrome
DSPOrphanet:293888Inherited isolated arrhythmogenic cardiomyopathy, dominant-left variant
DSPOrphanet:293899Inherited isolated arrhythmogenic ventricular dysplasia, biventricular variant
DSPOrphanet:293910Inherited isolated arrhythmogenic cardiomyopathy, dominant-right variant
DSPOrphanet:369992Severe dermatitis-multiple allergies-metabolic wasting syndrome
DSPOrphanet:476096Erythrokeratodermia-cardiomyopathy syndrome

Cohort genes → proteins

18 cohort genes, 17 distinct canonical proteins.

Evidence partition

SubsetGenes
multi_evidence18

Cohort genes (full)

SymbolHGNCEnsemblUniProtNameEvidence
SCN1BHGNC:10586ENSG00000105711Q07699Sodium channel regulatory subunit beta-1gencc,clinvar
SCN5AHGNC:10593ENSG00000183873Q14524Sodium channel protein type 5 subunit alphagencc,clinvar
CACNA2D1HGNC:1399ENSG00000153956P54289Voltage-dependent calcium channel subunit alpha-2/delta-1gencc,clinvar
SCN2BHGNC:10589ENSG00000149575O60939Sodium channel regulatory subunit beta-2gencc
HCN4HGNC:16882ENSG00000138622Q9Y3Q4Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4gencc
GPD1LHGNC:28956ENSG00000152642Q8N335Glycerol-3-phosphate dehydrogenase 1-like proteingencc
KCND3HGNC:6239ENSG00000171385Q9UK17A-type voltage-gated potassium channel KCND3gencc
KCNJ8HGNC:6269ENSG00000121361Q15842ATP-sensitive inward rectifier potassium channel 8gencc
PKP2HGNC:9024ENSG00000057294Q99959Plakophilin-2gencc
SCN10AHGNC:10582ENSG00000185313Q9Y5Y9Sodium channel protein type 10 subunit alphaclinvar
SCNN1AHGNC:10599ENSG00000111319P37088Epithelial sodium channel subunit alphaclinvar
DSPHGNC:3052ENSG00000096696P15924Desmoplakinclinvar
FBN1HGNC:3603ENSG00000166147P35555Fibrillin-1clinvar
AKAP9HGNC:379ENSG00000127914Q99996A-kinase anchor protein 9clinvar
KCNJ8-AS1HGNC:58193ENSG00000256615KCNJ8 antisense RNA 1clinvar
KCNA5HGNC:6224ENSG00000130037P22460Potassium voltage-gated channel subfamily A member 5clinvar
KCNH2HGNC:6251ENSG00000055118Q12809Voltage-gated inwardly rectifying potassium channel KCNH2clinvar
KCNJ16HGNC:6262ENSG00000153822Q9NPI9Inward rectifier potassium channel 16clinvar

Cohort function summary

Lead sentence per gene, UniProt-curated.

SymbolProtein nameFunction (lead sentence)
SCN1BSodium channel regulatory subunit beta-1Regulatory subunit of multiple voltage-gated sodium (Nav) channels directly mediating the depolarization of excitable membranes.
SCN5ASodium channel protein type 5 subunit alphaPore-forming subunit of Nav1.5, a voltage-gated sodium (Nav) channel that directly mediates the depolarizing phase of action potentials in excitable membranes.
CACNA2D1Voltage-dependent calcium channel subunit alpha-2/delta-1The alpha-2/delta subunit of voltage-dependent calcium channels regulates calcium current density and activation/inactivation kinetics of the calcium channel.
SCN2BSodium channel regulatory subunit beta-2Regulatory subunit of multiple voltage-gated sodium (Nav) channels directly mediating the depolarization of excitable membranes.
HCN4Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4Hyperpolarization-activated ion channel that are permeable to Na(+) and K(+) ions with very slow activation and inactivation.
GPD1LGlycerol-3-phosphate dehydrogenase 1-like proteinPlays a role in regulating cardiac sodium current; decreased enzymatic activity with resulting increased levels of glycerol 3-phosphate activating the DPD1L-dependent SCN5A phosphorylation pathway, may ultimately lead to decreased sodium c…
KCND3A-type voltage-gated potassium channel KCND3Pore-forming (alpha) subunit of voltage-gated A-type potassium channels that mediates transmembrane potassium transport in excitable membranes, in brain and heart.
KCNJ8ATP-sensitive inward rectifier potassium channel 8Inward rectifier potassium channels are characterized by a greater tendency to allow potassium to flow into the cell rather than out of it.
PKP2Plakophilin-2A component of desmosome cell-cell junctions which are required for positive regulation of cellular adhesion.
SCN10ASodium channel protein type 10 subunit alphaTetrodotoxin-resistant channel that mediates the voltage-dependent sodium ion permeability of excitable membranes.
SCNN1AEpithelial sodium channel subunit alphaThis is one of the three pore-forming subunits of the heterotrimeric epithelial sodium channel (ENaC), a critical regulator of sodium balance and fluid homeostasis.
DSPDesmoplakinA component of desmosome cell-cell junctions which are required for positive regulation of cellular adhesion.
FBN1Fibrillin-1Structural component of the 10-12 nm diameter microfibrils of the extracellular matrix, which conveys both structural and regulatory properties to load-bearing connective tissues.
AKAP9A-kinase anchor protein 9Scaffolding protein that assembles several protein kinases and phosphatases on the centrosome and Golgi apparatus.
KCNA5Potassium voltage-gated channel subfamily A member 5Voltage-gated potassium channel that mediates transmembrane potassium transport in excitable membranes.
KCNH2Voltage-gated inwardly rectifying potassium channel KCNH2Pore-forming (alpha) subunit of voltage-gated inwardly rectifying potassium channel.
KCNJ16Inward rectifier potassium channel 16Inward rectifier potassium channels are characterized by a greater tendency to allow potassium to flow into the cell rather than out of it.

Protein-family classification

Druggable: 10 · Difficult: 1 · Unknown: 7 · Druggable fraction: 0.56

Family distribution

Cohort families vs a genome-wide background (hypergeometric, BH-FDR; fold = observed/expected). Counts kept; sorted by enrichment, so the catch-all Other/Unknown bucket no longer leads.

FamilyGenesFoldFDR
Ion channel849.6×6e-12
Antibody/Immunoglobulin23.2×0.250
Scaffold/PPI11.0×0.877
Other/Unknown70.7×0.954

Per-gene assignment

SymbolFamilyDruggable?ECInterPro (top 3)
SCN1BAntibody/ImmunoglobulinyesIg_V-set, Ig-like_fold, Na_channel_b1/b3
SCN5AIon channelyesNa_channel_asu, Ion_trans_dom, Na_channel_a5su
CACNA2D1Other/UnknownnoVWF_A, VWA_N, VDCC_a2/dsu
SCN2BAntibody/ImmunoglobulinyesMyelin_P0-rel, Ig_sub, Ig-like_dom
HCN4Ion channelyescNMP-bd_dom, K_chnl_volt-dep_EAG/ELK/ERG, Ion_trans_dom
GPD1LOther/UnknownnoG3P_DH_NAD-dep_C, G3P_DH_NAD-dep, 6-PGluconate_DH-like_C_sf
KCND3Ion channelyesBTB/POZ_dom, T1-type_BTB, K_chnl_volt-dep_Kv
KCNJ8Ion channelyesK_chnl_inward-rec_Kir6.1, K_chnl_inward-rec_Kir_cyto, Ig_E-set
PKP2Other/UnknownnoArmadillo, ARM-like, ARM-type_fold
SCN10AIon channelyesNa_channel_asu, Ion_trans_dom, Na_trans_assoc_dom
SCNN1AOther/UnknownnoENaC, ENaC_chordates, ENaC_CS
DSPScaffold/PPInoPlectin_repeat, SH3_domain, Spectrin/alpha-actinin
FBN1Other/UnknownnoEGF-type_Asp/Asn_hydroxyl_site, EGF, EGF-like_Ca-bd_dom
AKAP9Other/UnknownnoELK_dom, PACT_domain, AKAP9/Pericentrin
KCNJ8-AS1Other/Unknownno
KCNA5Ion channelyesBTB/POZ_dom, T1-type_BTB, K_chnl_volt-dep_Kv
KCNH2Ion channelyesPAS, cNMP-bd_dom, PAS-assoc_C
KCNJ16Ion channelyesK_chnl_inward-rec_Kir5, K_chnl_inward-rec_Kir_cyto, Ig_E-set

Expression context

Cohort genes with no expression data: 0.

14 cohort genes are a single-cell marker in ≥1 SCXA experiment.

Breadth distribution (Bgee present_calls)

BucketGenes
narrow (1-5 tissues)0
moderate (6-20)0
broad (>20)18
unknown0

Top tissues across cohort

TissueCohort genes
apex of heart3
cardiac atrium3
heart right ventricle3
cardiac ventricle2
biceps brachii2
skeletal muscle tissue of biceps brachii2
lateral nuclear group of thalamus2
right atrium auricular region2
left ventricle myocardium2
skin of hip2
cerebellum1
primary visual cortex1
right hemisphere of cerebellum1
heart left ventricle1
skeletal muscle tissue of rectus abdominis1
cerebellar cortex1
middle temporal gyrus1
tibialis anterior1
cerebellar vermis1
substantia nigra pars reticulata1

Per-gene tissue summary (top 30)

SymbolBgee breadthFANTOM5 breadthSCXATop tissues
SCN1B133ubiquitousmarkerprimary visual cortex, right hemisphere of cerebellum, cerebellum
SCN5A161broadyesapex of heart, heart left ventricle, cardiac ventricle
CACNA2D1261ubiquitousmarkerbiceps brachii, skeletal muscle tissue of biceps brachii, skeletal muscle tissue of rectus abdominis
SCN2B182broadyesmiddle temporal gyrus, lateral nuclear group of thalamus, cerebellar cortex
HCN486tissue_specificyestibialis anterior, right atrium auricular region, cardiac atrium
GPD1L297ubiquitousmarkerbiceps brachii, heart right ventricle, skeletal muscle tissue of biceps brachii
KCND3262broadmarkercerebellar vermis, substantia nigra pars reticulata, lateral nuclear group of thalamus
KCNJ8233broadmarkerheart right ventricle, left ventricle myocardium, cardiac ventricle
PKP2237ubiquitousmarkerheart right ventricle, apex of heart, left ventricle myocardium
SCN10A21markertype B pancreatic cell, olfactory bulb, diaphragm
SCNN1A283broadmarkernasal cavity epithelium, metanephros cortex, right uterine tube
DSP253ubiquitousmarkerskin of hip, upper leg skin, hair follicle
FBN1275ubiquitousmarkersynovial joint, skin of hip, decidua
AKAP9292ubiquitousmarkerjejunal mucosa, bronchial epithelial cell, cortical plate
KCNJ8-AS183yesprimordial germ cell in gonad, male germ line stem cell (sensu Vertebrata) in testis, small intestine
KCNA5179broadmarkercardiac muscle of right atrium, blood vessel layer, cardiac atrium
KCNH2211broadmarkerapex of heart, right atrium auricular region, cardiac atrium
KCNJ16212broadmarkerrenal medulla, nephron tubule, caput epididymis

Protein interactions among cohort

Intra-cohort edges: 30.

Hub genes (top 10 by interactor count)

SymbolInteractor count
FBN13,640
AKAP93,537
DSP2,897
GPD1L2,618
KCNA52,288
KCND32,215
SCN5A2,090
CACNA2D12,002
KCNH21,932
PKP21,861

Intra-cohort edges

ABSources
AKAP9KCNH2string_interaction
CACNA2D1KCNJ8string_interaction
CACNA2D1SCN5Astring_interaction
DSPPKP2string_interaction
GPD1LHCN4string_interaction
GPD1LKCNJ8string_interaction
GPD1LSCN10Astring_interaction
GPD1LSCN1Bstring_interaction
GPD1LSCN2Bstring_interaction
GPD1LSCN5Aintact, string_interaction
HCN4SCN1Bstring_interaction
HCN4SCN5Astring_interaction
KCNA5KCND3biogrid_interaction
KCNA5KCNH2string_interaction
KCNA5KCNJ8string_interaction
KCNA5SCN5Astring_interaction
KCND3KCNH2biogrid_interaction, string_interaction
KCND3KCNJ8string_interaction
KCND3SCN1Bbiogrid_interaction, string_interaction
KCND3SCN2Bstring_interaction
KCND3SCN5Astring_interaction
KCNH2SCN5Astring_interaction
KCNJ8SCN1Bstring_interaction
KCNJ8SCN2Bstring_interaction
KCNJ8SCN5Astring_interaction
PKP2SCN5Astring_interaction
SCN10ASCN1Bstring_interaction
SCN1BSCN2Bintact, string_interaction
SCN1BSCN5Astring_interaction
SCN2BSCN5Astring_interaction

Structural data

PDB: 14 · AlphaFold-only: 3 · No structure: 1

Cohort genes with PDB structures (top 30)

SymbolUniProtPDB entries
SCN1BQ0769939
SCN2BO6093935
CACNA2D1P5428930
KCNH2Q1280924
SCN5AQ1452416
FBN1P3555511
HCN4Q9Y3Q48
SCN10AQ9Y5Y98
KCND3Q9UK176
DSPP159244
KCNJ16Q9NPI94
SCNN1AP370883
GPD1LQ8N3351
PKP2Q999591

AlphaFold-only cohort genes (top 30 by pLDDT)

SymbolUniProtpLDDT
KCNJ8Q1584284.00
KCNA5P2246072.64
AKAP9Q99996

Function

Pathway analysis

Distinct Reactome pathways touched by cohort: 70. Enrichment computed across 18 evidence-associated genes (17 with Reactome annotation).

Pathways by enrichment

Over-representation of cohort genes vs the genome-wide background (hypergeometric test, Benjamini-Hochberg FDR; fold = observed/expected over 17 annotated cohort genes). Counts and members are kept as ground-truth; sorted by enrichment.

PathwayCohort genesFoldFDRSample cohort genes
Cardiac conduction851.2×6e-11SCN1B, SCN5A, SCN10A, SCN2B, AKAP9, KCNA5, KCND3, KCNH2
Muscle contraction836.3×5e-10SCN1B, SCN5A, SCN10A, SCN2B, AKAP9, KCNA5, KCND3, KCNH2
Interaction between L1 and Ankyrins486.7×2e-06SCN1B, SCN5A, SCN10A, SCN2B
Phase 0 - rapid depolarisation481.4×2e-06SCN1B, SCN5A, SCN10A, SCN2B
Potassium Channels539.5×2e-06KCNA5, KCND3, KCNH2, KCNJ16, KCNJ8
Phase 3 - rapid repolarisation3201.5×4e-06AKAP9, KCNA5, KCNH2
L1CAM interactions428.3×1e-04SCN1B, SCN5A, SCN10A, SCN2B
Sensory perception of taste359.3×1e-04SCN1B, SCN2B, SCNN1A
Neuronal System513.0×2e-04KCNA5, KCND3, KCNH2, KCNJ16, KCNJ8
Voltage gated Potassium channels342.9×3e-04KCNA5, KCND3, KCNH2
Inwardly rectifying K+ channels284.0×0.002KCNJ16, KCNJ8
Axon guidance410.6×0.003SCN1B, SCN5A, SCN10A, SCN2B
Nervous system development410.1×0.003SCN1B, SCN5A, SCN10A, SCN2B
Sensory Perception316.8×0.003SCN1B, SCN2B, SCNN1A
Sensory perception of sweet, bitter, and umami (glutamate) taste232.8×0.008SCN1B, SCN2B
Potassium transport channels1223.9×0.020KCNJ16
ATP sensitive Potassium channels1167.9×0.023KCNJ8
HCN channels1167.9×0.023HCN4
Sensory perception of salty taste1112.0×0.033SCNN1A
Phase 1 - inactivation of fast Na+ channels196.0×0.036KCND3
G protein gated Potassium channels167.2×0.049KCNJ16
Apoptotic cleavage of cell adhesion proteins161.1×0.049DSP
Formation of the cornified envelope210.3×0.049DSP, PKP2
Phase 2 - plateau phase144.8×0.064AKAP9
Mechanical load activates signaling by PIEZO1 and integrins in osteocytes139.5×0.070CACNA2D1
Developmental Biology43.4×0.071SCN1B, SCN5A, SCN10A, SCN2B
Activation of GABAB receptors135.4×0.072KCNJ16
GABA B receptor activation132.0×0.077KCNJ16
Keratinization26.5×0.088DSP, PKP2
Activation of G protein gated Potassium channels123.2×0.096KCNJ16

GO biological processes by enrichment

Over-representation of cohort genes vs the genome-wide background (hypergeometric test, Benjamini-Hochberg FDR; fold = observed/expected over 17 annotated cohort genes). Counts and members are kept as ground-truth; sorted by enrichment.

GO termCohort genesFoldFDRSample cohort genes
regulation of heart rate by cardiac conduction11242.3×3e-23SCN1B, SCN5A, CACNA2D1, SCN2B, HCN4, DSP, AKAP9, KCNA5 (+3 more)
cardiac muscle cell action potential involved in contraction6247.8×5e-12SCN1B, SCN5A, CACNA2D1, SCN10A, SCN2B, PKP2
membrane depolarization during action potential5495.6×9e-12SCN1B, SCN5A, SCN10A, SCN2B, KCNH2
positive regulation of sodium ion transport5247.8×3e-10SCN1B, SCN5A, SCN2B, GPD1L, PKP2
regulation of ventricular cardiac muscle cell membrane repolarization5247.8×3e-10SCN1B, SCN5A, CACNA2D1, AKAP9, KCNH2
regulation of atrial cardiac muscle cell membrane depolarization4440.6×3e-09SCN1B, SCN5A, SCN10A, SCN2B
regulation of heart rate5137.7×6e-09SCN5A, SCN10A, HCN4, GPD1L, KCNJ8
membrane depolarization during cardiac muscle cell action potential4330.4×9e-09SCN1B, SCN5A, SCN2B, HCN4
ventricular cardiac muscle cell action potential4233.2×3e-08SCN5A, GPD1L, KCNH2, PKP2
potassium ion transmembrane transport648.0×3e-08HCN4, KCNA5, KCND3, KCNH2, KCNJ16, KCNJ8
sodium ion transmembrane transport559.7×3e-07SCN1B, SCN5A, SCN10A, SCNN1A, HCN4
potassium ion transport556.3×3e-07KCNA5, KCND3, KCNH2, KCNJ16, KCNJ8
cardiac muscle contraction494.4×1e-06SCN1B, SCN5A, SCN2B, KCNH2
membrane repolarization during ventricular cardiac muscle cell action potential3297.4×1e-06KCND3, KCNH2, KCNJ8
potassium ion import across plasma membrane486.2×2e-06HCN4, KCNH2, KCNJ16, KCNJ8
potassium ion export across plasma membrane3185.9×6e-06KCNA5, KCND3, KCNH2
bundle of His cell action potential2991.3×1e-05SCN5A, SCN10A
regulation of monoatomic ion transmembrane transport3129.3×2e-05SCN10A, KCNJ16, KCNJ8
membrane depolarization during Purkinje myocyte cell action potential2660.9×3e-05SCN1B, SCN5A
membrane depolarization during bundle of His cell action potential2660.9×3e-05SCN5A, CACNA2D1
AV node cell action potential2495.6×6e-05SCN5A, SCN10A
membrane depolarization during SA node cell action potential2396.5×9e-05SCN5A, HCN4
regulation of ventricular cardiac muscle cell membrane depolarization2330.4×1e-04SCN5A, GPD1L
SA node cell action potential2330.4×1e-04SCN5A, HCN4
regulation of atrial cardiac muscle cell membrane repolarization2283.2×2e-04SCN5A, KCNA5
bundle of His cell-Purkinje myocyte adhesion involved in cell communication2283.2×2e-04DSP, PKP2
desmosome organization2247.8×2e-04DSP, PKP2
regulation of cardiac muscle cell action potential involved in regulation of contraction2220.3×3e-04HCN4, AKAP9
cardiac conduction2198.3×3e-04SCN1B, SCN2B
membrane repolarization during cardiac muscle cell action potential2198.3×3e-04KCND3, KCNH2

Therapeutics

Drug target analysis

Approved (phase 4): 8 · Phase ≥3: 8 · Phased (≥1): 11 · Undrugged: 7

Druggability breadth: 12 of 18 evidence-associated genes (67%) have a ChEMBL target (buckets above are over the deeply-mined display cohort).

Genes with an approved drug

The molecule shown is one approved compound that hits the gene — not necessarily a drug of choice or one indicated for this disease.

SymbolExample approved molecule
SCN5ABEPRIDIL
CACNA2D1PREGABALIN
HCN4IVABRADINE
KCND3DULOXETINE
SCN10AIMIPRAMINE
SCNN1AAMILORIDE
KCNA5DRONEDARONE HYDROCHLORIDE
KCNH2CETIRIZINE

Top cohort targets by molecule count

SymbolMoleculesMax phase
KCNH27064
SCN5A1084
SCN10A214
KCND3104
KCNA584
CACNA2D154
SCN1B22
SCN2B22
HCN424
SCNN1A24

Drugs targeting cohort genes (top 30)

MoleculeMax phaseTargets in cohort
BEPRIDIL4KCNH2, SCN5A
CANDESARTAN CILEXETIL4SCN5A
TELMISARTAN4SCN5A
CARBAMAZEPINE4SCN5A
DIBUCAINE4KCNH2, SCN5A
IMIPRAMINE4KCNH2, SCN10A, SCN5A
DROPERIDOL4KCNH2, SCN5A
PONATINIB4KCNH2, SCN5A
DULOXETINE4KCND3, KCNH2, SCN5A
PALONOSETRON4KCNH2, SCN5A
VILANTEROL4SCN5A
MEXILETINE HYDROCHLORIDE4SCN5A
UNOPROSTONE ISOPROPYL4SCN5A
LURASIDONE4KCNH2, SCN5A
LETERMOVIR4SCN5A
SERTINDOLE4KCNA5, KCNH2, SCN10A, SCN5A
FEDRATINIB4KCNH2, SCN5A
QUINIDINE4KCNA5, KCNH2, SCN5A
DARUNAVIR4KCND3, KCNH2, SCN5A
DARIFENACIN4KCND3, KCNH2, SCN5A
BENZONATATE4SCN5A
TOLTERODINE4KCND3, KCNH2, SCN5A
RANOLAZINE4KCNH2, SCN5A
PIMOZIDE4KCNH2, SCN10A, SCN5A
NIMODIPINE4CACNA2D1, SCN5A
FELODIPINE4SCN5A
NICARDIPINE4KCNH2, SCN5A
AMLODIPINE4KCNH2, SCN5A
PHENYTOIN4KCNH2, SCN5A
PALIPERIDONE4KCND3, KCNH2, SCN5A

Bioactivity and enzyme data

Enzyme cohort genes (≥1 EC): 0.

Cohort genes with ChEMBL bioactivity (full, sorted by assay count)

SymbolAssaysType breakdown
KCNH24,851Binding:3558, Toxicity:1071, Functional:169, ADMET:53
SCN5A594Binding:380, Functional:98, ADMET:72, Toxicity:43, Unclassified:1
KCNA5152Binding:130, Functional:14, ADMET:5, Toxicity:3
SCN10A144Binding:124, Functional:16, ADMET:4
KCND3118Binding:55, Functional:44, ADMET:12, Toxicity:7
CACNA2D147Binding:45, ADMET:1, Toxicity:1
KCNJ843Functional:38, Binding:5
HCN430Binding:20, ADMET:5, Functional:4, Toxicity:1
SCN1B15Binding:7, ADMET:6, Toxicity:2
SCN2B9ADMET:4, Binding:3, Toxicity:2
SCNN1A6Binding:4, ADMET:1, Functional:1
DSP2Binding:2

Cohort genes with high screening signal

≥100 ChEMBL assays — a studied-ness signal; see Therapeutics for approved-drug status.

SymbolChEMBL assays
SCN5A594
KCND3118
SCN10A144
KCNA5152
KCNH24,851

Pharmacogenomics

Cohort genes with a PharmGKB record: 17; with CPIC/DPWG dosing guidelines: 0.

No cohort gene has a CPIC/DPWG genotype-guided dosing guideline (PharmGKB).

Chemical tractability of cohort targets

30 approved/phased compounds have measured bioactivity against a cohort gene (and aren’t yet in disease-level trials). This is a research / tractability signal, NOT a therapeutic recommendation — a bioactivity row often reflects off-target or screening binding (e.g. promiscuous kinase inhibitors against a cohort kinase), implying no disease mechanism.

CompoundMax phaseCohort target (bioactivity)
BEPRIDIL4KCNH2, SCN5A
CANDESARTAN CILEXETIL4SCN5A
TELMISARTAN4SCN5A
CARBAMAZEPINE4SCN5A
DIBUCAINE4KCNH2, SCN5A
IMIPRAMINE4KCNH2, SCN10A, SCN5A
DROPERIDOL4KCNH2, SCN5A
PONATINIB4KCNH2, SCN5A
DULOXETINE4KCND3, KCNH2, SCN5A
PALONOSETRON4KCNH2, SCN5A
VILANTEROL4SCN5A
MEXILETINE HYDROCHLORIDE4SCN5A
UNOPROSTONE ISOPROPYL4SCN5A
LURASIDONE4KCNH2, SCN5A
LETERMOVIR4SCN5A
SERTINDOLE4KCNA5, KCNH2, SCN10A, SCN5A
FEDRATINIB4KCNH2, SCN5A
QUINIDINE4KCNA5, KCNH2, SCN5A
DARUNAVIR4KCND3, KCNH2, SCN5A
DARIFENACIN4KCND3, KCNH2, SCN5A
BENZONATATE4SCN5A
TOLTERODINE4KCND3, KCNH2, SCN5A
RANOLAZINE4KCNH2, SCN5A
PIMOZIDE4KCNH2, SCN10A, SCN5A
NIMODIPINE4CACNA2D1, SCN5A
FELODIPINE4SCN5A
NICARDIPINE4KCNH2, SCN5A
AMLODIPINE4KCNH2, SCN5A
PHENYTOIN4KCNH2, SCN5A
PALIPERIDONE4KCND3, KCNH2, SCN5A

Druggability pyramid

Cohort genes binned by druggability tier (high → low):

TierDefinitionGenesSymbols
AApproved (phase 4 drug)8SCN5A, CACNA2D1, HCN4, KCND3, SCN10A, SCNN1A, KCNA5, KCNH2
BPhased (≥1) drug, not yet approved3SCN1B, SCN2B, KCNJ8
CDruggable family + PDB, no drug1KCNJ16
DDruggable family + AlphaFold only, no drug0
EDifficult family or no structure, no drug6GPD1L, PKP2, DSP, FBN1, AKAP9, KCNJ8-AS1

Undrugged target profiles

7 cohort genes are undrugged. Ranked by ‘starting-point quality’ (assay depth + drugged-partner adjacency).

SymbolChEMBL assaysDrugged partners (top 3)
GPD1L0SCN5A, SCN1B
PKP20SCN5A
DSP2
FBN10
AKAP90
KCNJ8-AS10
KCNJ160

Clinical trials & evidence

Clinical trials

Clinical trials: 2.

Phase distribution (across all retrieved trials)

PhaseTrials
Not specified2

Top trials by phase / activity

NCTPhaseStatusTitle
NCT03572881Not specifiedUNKNOWNRhythmic Risk of Type 1 Brugada Syndrome and Pulmonary Infundibulum Mapping
NCT04641585Not specifiedUNKNOWNBrugada Syndrome and Artificial Intelligence Applications to Diagnosis