Conduction system disorder

disease
On this page

Also known as conducting system of heart diseaseconducting system of heart disease or disorderdisease of conducting system of heartdisease or disorder of conducting system of heartdisorder of conducting system of heart

Summary

Conduction system disorder (MONDO:0005449) is a disease with 6 cohort genes (20 GWAS associations across 16 studies). The dominant Reactome pathway is Phase 0 - rapid depolarisation (3 cohort genes).

At a glance

  • Cohort genes: 6
  • GWAS associations: 20
  • ClinVar variants: 14

Clinical features

No curated clinical features (Orphanet) for this disease.

Identifiers

Disease identifiers

FieldValue
Canonical nameconduction system disorder
Mondo IDMONDO:0005449
EFOEFO:0005137
UMLSC2748542
MedGen412576
Anatomy (UBERON)UBERON:0002350
Is cancer (heuristic)no

Also known as: conducting system of heart disease · conducting system of heart disease or disorder · disease of conducting system of heart · disease or disorder of conducting system of heart · disorder of conducting system of heart

Data availability: 14 ClinVar variants · 20 GWAS associations (16 studies).

Disease family

An umbrella term covering 4 Mondo subtypes.

Classification path: disease › human disease › disease by body system or component › musculoskeletal system disordermuscle tissue disorderconduction system disorder

Related subtypes (12): striated muscle rhabdoid tumor, septal myocardial infarction, tonsillar pillar cancer, atrophic muscular disease, cardiomyopathy, myalgic encephalomeyelitis/chronic fatigue syndrome, myostatin-related muscle hypertrophy, caveolinopathy, distal arthrogryposis, skeletal muscle disorder, myomatous neoplasm, Kocher-debre-Semelaigne syndrome

Subtypes (4): sinoatrial node disorder, atrioventricular node disorder, progressive familial heart block, type 1A, atrial conduction disease

Genetics & variants

GWAS landscape

20 GWAS associations across 16 studies. Top hits map to 1 distinct genes (as reported by GWAS).

Top associations by p-value

rsIDp-valueGeneRisk alleleOdds ratio
chr2:1789751611e-14A0.29
chr4:238207051e-12A0.13
chr18:448480722e-11GGT0.11
rs1409176423e-11TTC34 - ACTRT2C3.01
rs5478475323e-11ANK1G1.78
chr1:852796922e-09T2.25
chr3:1712714622e-09T0.1
chr5:42458856e-09C2.91
chr7:572013239e-09A3.37
chr6:1518976272e-08C0.65
chrX:1015226822e-08C1.98
chr16:6044572e-08T2.73
chr4:1097369683e-08C3.27
chr1:1729859534e-08A2.65
chrX:1032788604e-08T1.92
chr10:732636454e-08G2.69
chr11:891109614e-08G1.99
chr12:986164924e-08T1.82
chr7:561454585e-08T3.11
chr9:777030755e-08G2.45

Top studies (by case count)

StudyLead authorYearCasesControlsTitle
GCST90297581Auwerx C202443,312179,146Rare copy-number variants as modulators of common disease susceptibility.
GCST90297635Auwerx C202443,312179,146Rare copy-number variants as modulators of common disease susceptibility.
GCST90297687Auwerx C202443,312179,146Rare copy-number variants as modulators of common disease susceptibility.
GCST90297731Auwerx C202443,312179,146Rare copy-number variants as modulators of common disease susceptibility.
GCST90473565UK Biobank Whole-Genome Sequencing Consortium20258,175450,265Whole-genome sequencing of 490,640 UK Biobank participants.
GCST90667959UK Biobank Whole-Genome Sequencing Consortium20258,175450,265Whole-genome sequencing of 490,640 UK Biobank participants.
GCST90080007Backman JD20213,184384,091Exome sequencing and analysis of 454,787 UK Biobank participants.
GCST90083993Backman JD20213,184384,091Exome sequencing and analysis of 454,787 UK Biobank participants.
GCST90477912Verma A20241,717447,263Diversity and scale: Genetic architecture of 2068 traits in the VA Million Veteran Program.
GCST90726671Kim HI202675743,269Exome sequencing and analysis of 44,028 British South Asians enriched for high autozygosity.

Variant details and genetic-evidence tiers

Tier distribution (top 50 variants)

TierVariants
Tier 1: coding0
Tier 2: splice/UTR0
Tier 3: regulatory0
Tier 4: intronic/intergenic20

MAF distribution

BucketVariants
common (>=0.05)0
low_freq (0.01-0.05)0
rare (<0.01)2
unknown18

Functional consequences

ConsequenceCount
unknown18
intergenic_variant1
intron_variant1

Top variants

rsIDChrPosAllelesMAFConsequenceGenep-valueTier
chr2:1789751611e-14Tier 4: intronic/intergenic
chr4:238207051e-12Tier 4: intronic/intergenic
chr18:448480722e-11Tier 4: intronic/intergenic
rs14091764212917891C>G,T0intergenic_variantTTC34 - ACTRT23e-11Tier 4: intronic/intergenic
rs547847532841786253G>T0.001intron_variantANK13e-11Tier 4: intronic/intergenic
chr1:852796922e-09Tier 4: intronic/intergenic
chr3:1712714622e-09Tier 4: intronic/intergenic
chr5:42458856e-09Tier 4: intronic/intergenic
chr7:572013239e-09Tier 4: intronic/intergenic
chr6:1518976272e-08Tier 4: intronic/intergenic
chrX:1015226822e-08Tier 4: intronic/intergenic
chr16:6044572e-08Tier 4: intronic/intergenic
chr4:1097369683e-08Tier 4: intronic/intergenic
chr1:1729859534e-08Tier 4: intronic/intergenic
chrX:1032788604e-08Tier 4: intronic/intergenic
chr10:732636454e-08Tier 4: intronic/intergenic
chr11:891109614e-08Tier 4: intronic/intergenic
chr12:986164924e-08Tier 4: intronic/intergenic
chr7:561454585e-08Tier 4: intronic/intergenic
chr9:777030755e-08Tier 4: intronic/intergenic

ClinVar germline variants

14 retrieved; paginated sample, class counts are floors:

6 uncertain significance, 3 conflicting classifications of pathogenicity, 3 pathogenic, 1 likely pathogenic, 1 pathogenic/likely pathogenic

ClinVarVariant (HGVS)GeneClassificationReview
9256NM_001037.5(SCN1B):c.448+89G>ASCN1BPathogenicno assertion criteria provided
68032NM_000335.5(SCN5A):c.673C>T (p.Arg225Trp)SCN5APathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
9386NM_000335.5(SCN5A):c.1540G>T (p.Gly514Cys)SCN5APathogenicno assertion criteria provided
9395NM_000335.5(SCN5A):c.4219G>A (p.Gly1407Arg)SCN5APathogeniccriteria provided, multiple submitters, no conflicts
222695NM_170707.4(LMNA):c.354_355delinsAG (p.Arg119Gly)LMNALikely pathogeniccriteria provided, single submitter
67931NM_000335.5(SCN5A):c.4856C>A (p.Thr1619Lys)SCN5AConflicting classifications of pathogenicitycriteria provided, conflicting classifications
67939NM_000335.5(SCN5A):c.4892G>A (p.Arg1631His)SCN5AConflicting classifications of pathogenicitycriteria provided, conflicting classifications
68036NM_000335.5(SCN5A):c.689T>C (p.Ile230Thr)SCN5AConflicting classifications of pathogenicitycriteria provided, conflicting classifications
222519NM_201596.3(CACNB2):c.1399C>T (p.Pro467Ser)CACNB2Uncertain significancecriteria provided, single submitter
67773NM_000335.5(SCN5A):c.3022C>T (p.Pro1008Ser)LOC110121269Uncertain significancecriteria provided, multiple submitters, no conflicts
450490NM_002471.4(MYH6):c.1960C>T (p.Arg654Trp)MYH6Uncertain significancecriteria provided, multiple submitters, no conflicts
9255NM_001037.5(SCN1B):c.259G>C (p.Glu87Gln)SCN1BUncertain significancecriteria provided, multiple submitters, no conflicts
67665NM_000335.5(SCN5A):c.1535C>T (p.Thr512Ile)SCN5AUncertain significancecriteria provided, multiple submitters, no conflicts
222855NM_017636.4(TRPM4):c.3337C>G (p.Leu1113Val)TRPM4Uncertain significancecriteria provided, multiple submitters, no conflicts

Genes & proteins

Mendelian disease overlap and somatic drivers

GenCC: 0 · Orphanet: 42 · OMIM-shared: 0 · Dual-evidence (GWAS+Mendelian): 0

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
CACNB2Orphanet:130Brugada syndrome
TRPM4Orphanet:130Brugada syndrome
TRPM4Orphanet:316Progressive symmetric erythrokeratodermia
TRPM4Orphanet:871Hereditary progressive cardiac conduction defect
LMNAOrphanet:154Familial isolated dilated cardiomyopathy
LMNAOrphanet:157973Congenital muscular dystrophy due to LMNA mutation
LMNAOrphanet:1662Restrictive dermopathy
LMNAOrphanet:168796Heart-hand syndrome, Slovenian type
LMNAOrphanet:2229Dilated cardiomyopathy-hypergonadotropic hypogonadism syndrome
LMNAOrphanet:2348Familial partial lipodystrophy, Dunnigan type
LMNAOrphanet:280365Autosomal semi-dominant severe lipodystrophic laminopathy
LMNAOrphanet:293888Inherited isolated arrhythmogenic cardiomyopathy, dominant-left variant
LMNAOrphanet:293899Inherited isolated arrhythmogenic ventricular dysplasia, biventricular variant
LMNAOrphanet:293910Inherited isolated arrhythmogenic cardiomyopathy, dominant-right variant
LMNAOrphanet:300751Familial dilated cardiomyopathy with conduction defect due to LMNA mutation
LMNAOrphanet:363618LMNA-related cardiocutaneous progeria syndrome
LMNAOrphanet:54260Left ventricular noncompaction
LMNAOrphanet:675396Epithelioid hemangioma
LMNAOrphanet:740Hutchinson-Gilford progeria syndrome
LMNAOrphanet:79084Familial partial lipodystrophy, Köbberling type
LMNAOrphanet:79474Atypical Werner syndrome
LMNAOrphanet:90153Mandibuloacral dysplasia with type A lipodystrophy
LMNAOrphanet:98853Autosomal dominant Emery-Dreifuss muscular dystrophy
LMNAOrphanet:98855Autosomal recessive Emery-Dreifuss muscular dystrophy
LMNAOrphanet:98856Charcot-Marie-Tooth disease type 2B1
MYH6Orphanet:154Familial isolated dilated cardiomyopathy
MYH6Orphanet:166282Hereditary sick sinus syndrome
MYH6Orphanet:99103Atrial septal defect, ostium secundum type

Cohort genes → proteins

6 cohort genes, 6 distinct canonical proteins.

Evidence partition

SubsetGenes
multi_evidence6

Cohort genes (full)

SymbolHGNCEnsemblUniProtNameEvidence
SCN1BHGNC:10586ENSG00000105711Q07699Sodium channel regulatory subunit beta-1clinvar
SCN5AHGNC:10593ENSG00000183873Q14524Sodium channel protein type 5 subunit alphaclinvar
CACNB2HGNC:1402ENSG00000165995Q08289Voltage-dependent L-type calcium channel subunit beta-2clinvar
TRPM4HGNC:17993ENSG00000130529Q8TD43Transient receptor potential cation channel subfamily M member 4clinvar
LMNAHGNC:6636ENSG00000160789P02545Prelamin-A/Cclinvar
MYH6HGNC:7576ENSG00000197616P13533Myosin-6clinvar

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.
CACNB2Voltage-dependent L-type calcium channel subunit beta-2Beta subunit of voltage-dependent calcium channels which contributes to the function of the calcium channel by increasing peak calcium current.
TRPM4Transient receptor potential cation channel subfamily M member 4Calcium-activated selective cation channel that mediates membrane depolarization.
LMNAPrelamin-A/CLamins are intermediate filament proteins that assemble into a filamentous meshwork, and which constitute the major components of the nuclear lamina, a fibrous layer on the nucleoplasmic side of the inner nuclear membrane.
MYH6Myosin-6Muscle contraction.

Protein-family classification

Druggable: 3 · Difficult: 2 · Unknown: 1 · Druggable fraction: 0.5

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 channel237.2×0.005
Scaffold/PPI25.8×0.086
Antibody/Immunoglobulin14.9×0.252
Other/Unknown10.3×0.993

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
CACNB2Scaffold/PPInoVDCC_L_bsu, SH3_domain, VDCC_L_b2su
TRPM4Ion channelyesIon_trans_dom, TRPM_SLOG, TRPM
LMNAOther/UnknownnoLamin_tail_dom, IF_conserved, Lamin_tail_dom_sf
MYH6Scaffold/PPInoMyosin_head_motor_dom-like, Myosin_tail, SH3_Myosin

Expression context

Cohort genes with no expression data: 0.

4 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)6
unknown0

Top tissues across cohort

TissueCohort genes
apex of heart2
mucosa of stomach2
cerebellum1
primary visual cortex1
right hemisphere of cerebellum1
cardiac ventricle1
heart left ventricle1
adrenal tissue1
buccal mucosa cell1
mucosa of transverse colon1
rectum1
nipple1
skin of abdomen1
cardiac atrium1
cardiac muscle of right atrium1
vena cava1

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
CACNB2237broadmarkeradrenal tissue, mucosa of stomach, buccal mucosa cell
TRPM4201ubiquitousmarkermucosa of transverse colon, rectum, apex of heart
LMNA295ubiquitousmarkernipple, mucosa of stomach, skin of abdomen
MYH6154tissue_specificyescardiac muscle of right atrium, cardiac atrium, vena cava

Protein interactions among cohort

Intra-cohort edges: 4.

Hub genes (top 10 by interactor count)

SymbolInteractor count
LMNA7,173
MYH63,119
SCN5A2,090
CACNB21,425
SCN1B1,328
TRPM41,217

Intra-cohort edges

ABSources
CACNB2SCN1Bstring_interaction
CACNB2SCN5Astring_interaction
SCN1BSCN5Astring_interaction
SCN5ATRPM4string_interaction

Structural data

PDB: 5 · AlphaFold-only: 1 · No structure: 0

Cohort genes with PDB structures (top 30)

SymbolUniProtPDB entries
SCN1BQ0769939
TRPM4Q8TD4329
LMNAP0254528
SCN5AQ1452416
CACNB2Q082893

AlphaFold-only cohort genes (top 30 by pLDDT)

SymbolUniProtpLDDT
MYH6P1353374.91

Function

Pathway analysis

Distinct Reactome pathways touched by cohort: 42. Enrichment computed across 6 evidence-associated genes (6 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 6 annotated cohort genes). Counts and members are kept as ground-truth; sorted by enrichment.

PathwayCohort genesFoldFDRSample cohort genes
Phase 0 - rapid depolarisation3173.0×9e-06SCN1B, SCN5A, CACNB2
Muscle contraction451.4×9e-06SCN1B, SCN5A, CACNB2, MYH6
Cardiac conduction354.4×2e-04SCN1B, SCN5A, CACNB2
Interaction between L1 and Ankyrins2122.8×0.001SCN1B, SCN5A
Sensory perception of sweet, bitter, and umami (glutamate) taste292.8×0.001SCN1B, TRPM4
Axon guidance322.6×0.001SCN1B, SCN5A, CACNB2
Nervous system development321.5×0.001SCN1B, SCN5A, CACNB2
L1CAM interactions240.1×0.005SCN1B, SCN5A
Breakdown of the nuclear lamina1634.4×0.007LMNA
Sensory Perception231.7×0.007SCN1B, CACNB2
Developmental Biology37.2×0.021SCN1B, SCN5A, CACNB2
Presynaptic depolarization and calcium channel opening1158.6×0.022CACNB2
Depolymerization of the Nuclear Lamina1126.9×0.024LMNA
Phase 2 - plateau phase1126.9×0.024CACNB2
Mechanical load activates signaling by PIEZO1 and integrins in osteocytes1112.0×0.025CACNB2
Initiation of Nuclear Envelope (NE) Reformation1100.2×0.026LMNA
IRE1alpha activates chaperones186.5×0.027LMNA
Deregulated CDK5 triggers multiple neurodegenerative pathways in Alzheimer’s disease models186.5×0.027LMNA
Nuclear Envelope Breakdown176.1×0.029LMNA
TRP channels168.0×0.029TRPM4
Adrenaline,noradrenaline inhibits insulin secretion165.6×0.029CACNB2
Cellular responses to stimuli210.5×0.029CACNB2, LMNA
Unfolded Protein Response (UPR)159.5×0.030LMNA
Sensory perception of taste156.0×0.031SCN1B
Striated Muscle Contraction151.4×0.031MYH6
Sensory processing of sound151.4×0.031CACNB2
NCAM signaling for neurite out-growth145.3×0.034CACNB2
Cellular responses to mechanical stimuli143.3×0.034CACNB2
NCAM1 interactions141.4×0.034CACNB2
Oncogenic MAPK signaling141.4×0.034LMNA

GO biological processes by enrichment

Over-representation of cohort genes vs the genome-wide background (hypergeometric test, Benjamini-Hochberg FDR; fold = observed/expected over 6 annotated cohort genes). Counts and members are kept as ground-truth; sorted by enrichment.

GO termCohort genesFoldFDRSample cohort genes
membrane depolarization during Purkinje myocyte cell action potential32808.7×3e-09SCN1B, SCN5A, TRPM4
membrane depolarization during AV node cell action potential31685.2×2e-08SCN5A, CACNB2, TRPM4
regulation of heart rate by cardiac conduction4249.7×3e-08SCN1B, SCN5A, CACNB2, TRPM4
membrane depolarization during bundle of His cell action potential21872.4×6e-06SCN5A, TRPM4
membrane depolarization during atrial cardiac muscle cell action potential21872.4×6e-06SCN5A, CACNB2
cardiac muscle contraction3200.6×6e-06SCN1B, SCN5A, MYH6
regulation of atrial cardiac muscle cell membrane depolarization2624.1×7e-05SCN1B, SCN5A
membrane depolarization during action potential2561.7×7e-05SCN1B, SCN5A
membrane depolarization during cardiac muscle cell action potential2468.1×9e-05SCN1B, SCN5A
regulation of sodium ion transmembrane transport2351.1×2e-04SCN1B, SCN5A
positive regulation of sodium ion transport2280.9×2e-04SCN1B, SCN5A
regulation of ventricular cardiac muscle cell membrane repolarization2280.9×2e-04SCN1B, SCN5A
cardiac muscle cell action potential involved in contraction2234.1×3e-04SCN1B, SCN5A
membrane depolarization2170.2×5e-04SCN1B, SCN5A
regulation of heart rate2156.0×5e-04SCN5A, MYH6
visceral muscle development12808.7×0.002MYH6
corticospinal neuron axon guidance12808.7×0.002SCN1B
positive regulation of atrial cardiac muscle cell action potential12808.7×0.002TRPM4
positive regulation of regulation of vascular associated smooth muscle cell membrane depolarization12808.7×0.002TRPM4
calcium ion transmembrane transport270.2×0.002CACNB2, TRPM4
sodium ion transmembrane transport267.7×0.002SCN1B, SCN5A
regulation of heart growth11404.3×0.003MYH6
bundle of His cell action potential11404.3×0.003SCN5A
AV node cell to bundle of His cell communication11404.3×0.003SCN5A
positive regulation of calcium ion transmembrane transport via high voltage-gated calcium channel11404.3×0.003CACNB2
positive regulation of voltage-gated sodium channel activity1936.2×0.005SCN1B
DNA double-strand break attachment to nuclear envelope1936.2×0.005LMNA
regulation of T cell cytokine production1702.2×0.006TRPM4
establishment or maintenance of microtubule cytoskeleton polarity1702.2×0.006LMNA
AV node cell action potential1702.2×0.006SCN5A

Therapeutics

Drug target analysis

Approved (phase 4): 3 · Phase ≥3: 3 · Phased (≥1): 4 · Undrugged: 2

Druggability breadth: 6 of 6 evidence-associated genes (100%) 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
CACNB2NIMODIPINE
LMNABEPRIDIL

Top cohort targets by molecule count

SymbolMoleculesMax phase
LMNA8234
SCN5A1084
SCN1B22
CACNB224
TRPM400
MYH600

Drugs targeting cohort genes (top 30)

MoleculeMax phaseTargets in cohort
BEPRIDIL4LMNA, SCN5A
CANDESARTAN CILEXETIL4SCN5A
TELMISARTAN4SCN5A
CARBAMAZEPINE4LMNA, SCN5A
DIBUCAINE4LMNA, SCN5A
IMIPRAMINE4LMNA, SCN5A
DROPERIDOL4LMNA, SCN5A
PONATINIB4SCN5A
DULOXETINE4SCN5A
PALONOSETRON4SCN5A
VILANTEROL4SCN5A
MEXILETINE HYDROCHLORIDE4LMNA, SCN5A
UNOPROSTONE ISOPROPYL4SCN5A
LURASIDONE4SCN5A
LETERMOVIR4SCN5A
SERTINDOLE4SCN5A
FEDRATINIB4SCN5A
QUINIDINE4SCN5A
DARUNAVIR4SCN5A
DARIFENACIN4SCN5A
BENZONATATE4SCN5A
TOLTERODINE4LMNA, SCN5A
RANOLAZINE4SCN5A
PIMOZIDE4LMNA, SCN5A
NIMODIPINE4CACNB2, LMNA, SCN5A
FELODIPINE4LMNA, SCN5A
NICARDIPINE4LMNA, SCN5A
AMLODIPINE4SCN5A
PHENYTOIN4SCN5A
PALIPERIDONE4SCN5A

Bioactivity and enzyme data

Enzyme cohort genes (≥1 EC): 0.

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

SymbolAssaysType breakdown
SCN5A594Binding:380, Functional:98, ADMET:72, Toxicity:43, Unclassified:1
CACNB222Binding:20, ADMET:1, Toxicity:1
SCN1B15Binding:7, ADMET:6, Toxicity:2
TRPM414Binding:13, Functional:1
LMNA12Binding:9, Functional:3

Cohort genes with high screening signal

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

SymbolChEMBL assays
SCN5A594

Pharmacogenomics

Cohort genes with a PharmGKB record: 6; 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)
BEPRIDIL4LMNA, SCN5A
CANDESARTAN CILEXETIL4SCN5A
TELMISARTAN4SCN5A
CARBAMAZEPINE4LMNA, SCN5A
DIBUCAINE4LMNA, SCN5A
IMIPRAMINE4LMNA, SCN5A
DROPERIDOL4LMNA, SCN5A
PONATINIB4SCN5A
DULOXETINE4SCN5A
PALONOSETRON4SCN5A
VILANTEROL4SCN5A
MEXILETINE HYDROCHLORIDE4LMNA, SCN5A
UNOPROSTONE ISOPROPYL4SCN5A
LURASIDONE4SCN5A
LETERMOVIR4SCN5A
SERTINDOLE4SCN5A
FEDRATINIB4SCN5A
QUINIDINE4SCN5A
DARUNAVIR4SCN5A
DARIFENACIN4SCN5A
BENZONATATE4SCN5A
TOLTERODINE4LMNA, SCN5A
RANOLAZINE4SCN5A
PIMOZIDE4LMNA, SCN5A
NIMODIPINE4CACNB2, LMNA, SCN5A
FELODIPINE4LMNA, SCN5A
NICARDIPINE4LMNA, SCN5A
AMLODIPINE4SCN5A
PHENYTOIN4SCN5A
PALIPERIDONE4SCN5A

Druggability pyramid

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

TierDefinitionGenesSymbols
AApproved (phase 4 drug)3SCN5A, CACNB2, LMNA
BPhased (≥1) drug, not yet approved1SCN1B
CDruggable family + PDB, no drug1TRPM4
DDruggable family + AlphaFold only, no drug0
EDifficult family or no structure, no drug1MYH6

Undrugged target profiles

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

SymbolChEMBL assaysDrugged partners (top 3)
TRPM414
MYH60

Clinical trials & evidence

Clinical trials

Clinical trials: 0.