short QT syndrome

disease
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Also known as ventricular arrhythmia associated with short QT syndrome

Summary

short QT syndrome (MONDO:0000453) is a disease with 9 cohort genes and 1 clinical trial. The dominant Reactome pathway is Cardiac conduction (4 cohort genes).

At a glance

  • Prevalence: Unknown (Worldwide) [Orphanet-validated]
  • Cohort genes: 9
  • ClinVar variants: 14
  • Phenotypes (HPO): 9
  • Clinical trials: 1

Clinical features

Epidemiology

Prevalence records

1 prevalence record(s), Orphanet:

TypeClassValueGeographyValidation
Cases/families80WorldwideValidated

Signs & symptoms

Clinical features (HPO)

9 HPO clinical features (Orphanet curated; top 9 by frequency):

HPO IDTermFrequency
HP:0012232Shortened QT intervalObligate (100%)
HP:0001662BradycardiaVery frequent (80-99%)
HP:0001962PalpitationsFrequent (30-79%)
HP:0005110Atrial fibrillationFrequent (30-79%)
HP:0001279SyncopeOccasional (5-29%)
HP:0001645Sudden cardiac deathOccasional (5-29%)
HP:0001663Ventricular fibrillationOccasional (5-29%)
HP:0001678Atrioventricular blockOccasional (5-29%)
HP:0004308Ventricular arrhythmiaOccasional (5-29%)

Identifiers

Disease identifiers

FieldValue
Canonical nameshort QT syndrome
Mondo IDMONDO:0000453
MeSHC580439
OMIM609620
Orphanet51083
DOIDDOID:0050793
ICD-11553392015
NCITC71060
SNOMED CT698272007
UMLSC2348199
MedGen378835
GARD0016650
NORD2019
Is cancer (heuristic)no

Also known as: short QT syndrome · ventricular arrhythmia associated with short QT syndrome

Data availability: 14 ClinVar variants · 10 GenCC gene-disease records · 5 cell lines.

Disease family

An umbrella term covering 4 Mondo subtypes.

Classification path: disease › human disease › disease by body system or component › cardiovascular disorderheart disorderheart conduction diseaseshort QT syndrome

Related subtypes (9): atrioventricular block, sinoatrial node disorder, Wolff-Parkinson-White syndrome, postural orthostatic tachycardia syndrome, Brugada syndrome, catecholaminergic polymorphic ventricular tachycardia, progressive familial heart block, sinoatrial block, NKX2.5-related congenital, conduction and myopathic heart disease

Subtypes (4): short QT syndrome type 1, short QT syndrome type 2, short QT syndrome type 3, short QT syndrome 7

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

14 retrieved; paginated sample, class counts are floors:

7 uncertain significance, 2 conflicting classifications of pathogenicity, 2 pathogenic, 1 likely pathogenic, 1 pathogenic/likely pathogenic, 1 benign/likely benign

ClinVarVariant (HGVS)GeneClassificationReview
14437NM_000238.4(KCNH2):c.1764C>A (p.Asn588Lys)KCNH2Pathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
67297NM_000238.4(KCNH2):c.1853C>T (p.Thr618Ile)KCNH2Pathogeniccriteria provided, multiple submitters, no conflicts
8927NM_000891.3(KCNJ2):c.514G>A (p.Asp172Asn)KCNJ2Pathogeniccriteria provided, single submitter
14436NM_000238.4(KCNH2):c.1764C>G (p.Asn588Lys)KCNH2Likely pathogeniccriteria provided, single submitter
197406NM_000719.7(CACNA1C):c.4942G>A (p.Ala1648Thr)CACNA1CConflicting classifications of pathogenicitycriteria provided, conflicting classifications
263722NM_000722.4(CACNA2D1):c.1141A>G (p.Lys381Glu)CACNA2D1Conflicting classifications of pathogenicitycriteria provided, conflicting classifications
637981NM_000722.4(CACNA2D1):c.2721A>G (p.Ala907=)CACNA2D1Uncertain significancecriteria provided, multiple submitters, no conflicts
67211NM_000238.4(KCNH2):c.150G>T (p.Glu50Asp)KCNH2Uncertain significancecriteria provided, multiple submitters, no conflicts
67493NM_000238.4(KCNH2):c.3404G>A (p.Arg1135His)KCNH2Uncertain significancecriteria provided, multiple submitters, no conflicts
658326NM_000891.3(KCNJ2):c.1067G>T (p.Cys356Phe)KCNJ2Uncertain significancecriteria provided, multiple submitters, no conflicts
3148NM_000218.3(KCNQ1):c.919G>C (p.Val307Leu)KCNQ1Uncertain significancecriteria provided, single submitter
180561NM_017636.4(TRPM4):c.678C>G (p.Asp226Glu)TRPM4Uncertain significancecriteria provided, multiple submitters, no conflicts
2664945NM_014000.3(VCL):c.1177-3T>GVCLUncertain significancecriteria provided, single submitter
93419NM_000719.7(CACNA1C):c.5918G>A (p.Arg1973Gln)CACNA1CBenign/Likely benigncriteria provided, multiple submitters, no conflicts

Genes & proteins

Mendelian disease overlap and somatic drivers

GenCC: 71 · Orphanet: 24 · 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
KCNH2DefinitiveAutosomal dominantshort QT syndrome type 18
KCNJ2StrongAutosomal dominantshort QT syndrome type 315
KCNQ1StrongAutosomal dominantshort QT syndrome type 212
SLC4A3StrongAutosomal dominantshort QT syndrome 76
CACNA2D1SupportiveAutosomal dominantshort QT syndrome8
CACNA1CLimitedAutosomal dominantshort QT syndrome13
SLC22A5Disputed EvidenceAutosomal recessiveshort QT syndrome9

Orphanet rare-disease linkage (cohort genes)

GeneOrphanet IDRare disease
CACNA1COrphanet:101016Romano-Ward syndrome
CACNA1COrphanet:130Brugada syndrome
CACNA1COrphanet:528084Non-specific syndromic intellectual disability
CACNA1COrphanet:595098Timothy syndrome type 1
CACNA1COrphanet:595105Timothy syndrome type 2
CACNA1COrphanet:595109Atypical Timothy syndrome
CACNA2D1Orphanet:130Brugada syndrome
CACNA2D1Orphanet:442835Non-specific early-onset epileptic encephalopathy
CACNA2D1Orphanet:51083Congenital short QT syndrome
KCNH2Orphanet:101016Romano-Ward syndrome
KCNH2Orphanet:51083Congenital short QT syndrome
KCNJ2Orphanet:334Hereditary atrial fibrillation
KCNJ2Orphanet:37553Andersen-Tawil syndrome
KCNJ2Orphanet:51083Congenital short QT syndrome
KCNQ1Orphanet:101016Romano-Ward syndrome
KCNQ1Orphanet:334Hereditary atrial fibrillation
KCNQ1Orphanet:51083Congenital short QT syndrome
KCNQ1Orphanet:90647Jervell and Lange-Nielsen syndrome
SLC22A5Orphanet:158Systemic primary carnitine deficiency
SLC4A3Orphanet:51083Congenital short QT syndrome
VCLOrphanet:154Familial isolated dilated cardiomyopathy
TRPM4Orphanet:130Brugada syndrome
TRPM4Orphanet:316Progressive symmetric erythrokeratodermia
TRPM4Orphanet:871Hereditary progressive cardiac conduction defect

Cohort genes → proteins

9 cohort genes, 9 distinct canonical proteins.

Evidence partition

SubsetGenes
multi_evidence9

Cohort genes (full)

SymbolHGNCEnsemblUniProtNameEvidence
CACNA1CHGNC:1390ENSG00000151067Q13936Voltage-dependent L-type calcium channel subunit alpha-1Cgencc,clinvar
CACNA2D1HGNC:1399ENSG00000153956P54289Voltage-dependent calcium channel subunit alpha-2/delta-1gencc,clinvar
KCNH2HGNC:6251ENSG00000055118Q12809Voltage-gated inwardly rectifying potassium channel KCNH2gencc,clinvar
KCNJ2HGNC:6263ENSG00000123700P63252Inward rectifier potassium channel 2gencc,clinvar
KCNQ1HGNC:6294ENSG00000053918P51787Potassium voltage-gated channel subfamily KQT member 1gencc,clinvar
SLC22A5HGNC:10969ENSG00000197375O76082Organic cation/carnitine transporter 2gencc
SLC4A3HGNC:11029ENSG00000114923P48751Anion exchange protein 3gencc
VCLHGNC:12665ENSG00000035403P18206Vinculinclinvar
TRPM4HGNC:17993ENSG00000130529Q8TD43Transient receptor potential cation channel subfamily M member 4clinvar

Cohort function summary

Lead sentence per gene, UniProt-curated.

SymbolProtein nameFunction (lead sentence)
CACNA1CVoltage-dependent L-type calcium channel subunit alpha-1CPore-forming, alpha-1C subunit of the voltage-gated calcium channel that gives rise to L-type calcium currents.
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.
KCNH2Voltage-gated inwardly rectifying potassium channel KCNH2Pore-forming (alpha) subunit of voltage-gated inwardly rectifying potassium channel.
KCNJ2Inward rectifier potassium channel 2Inward rectifier potassium channels are characterized by a greater tendency to allow potassium to flow into the cell rather than out of it.
KCNQ1Potassium voltage-gated channel subfamily KQT member 1Pore-forming subunit of the voltage-gated potassium (Kv) channel involved in the regulation of cardiomyocyte excitability and important in normal development and functions of myocardium, inner ear, stomach and colon.
SLC22A5Organic cation/carnitine transporter 2Sodium-ion dependent, high affinity carnitine transporter.
SLC4A3Anion exchange protein 3Sodium-independent anion exchanger which mediates the electroneutral exchange of chloride for bicarbonate ions across the cell membrane.
VCLVinculinActin filament (F-actin)-binding protein involved in cell-matrix adhesion and cell-cell adhesion.
TRPM4Transient receptor potential cation channel subfamily M member 4Calcium-activated selective cation channel that mediates membrane depolarization.

Protein-family classification

Druggable: 6 · Difficult: 0 · Unknown: 3 · Druggable fraction: 0.67

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 channel562.0×2e-08
Transporter18.6×0.165
Other/Unknown30.6×0.955

Per-gene assignment

SymbolFamilyDruggable?ECInterPro (top 3)
CACNA1CIon channelyesVDCCAlpha1, VDCC_L_a1su, VDCC_L_a1csu
CACNA2D1Other/UnknownnoVWF_A, VWA_N, VDCC_a2/dsu
KCNH2Ion channelyesPAS, cNMP-bd_dom, PAS-assoc_C
KCNJ2Ion channelyesK_chnl_inward-rec_Kir2.1, K_chnl_inward-rec_Kir_cyto, K_chnl_inward-rec_Kir_N
KCNQ1Ion channelyesK_chnl_volt-dep_KCNQ, Ion_trans_dom, K_chnl_volt-dep_KCQN1
SLC22A5TransporteryesOrgcat_transp/SVOP, MFS_sugar_transport-like, Sugar_transporter_CS
SLC4A3Other/UnknownnoAnion_exchange, Anion_exchange_3, HCO3_transpt_euk
VCLOther/UnknownnoVinculin_CS, Vinculin/catenin, Vinculin
TRPM4Ion channelyesIon_trans_dom, TRPM_SLOG, TRPM

Expression context

Cohort genes with no expression data: 0.

9 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)9
unknown0

Top tissues across cohort

TissueCohort genes
apex of heart4
skeletal muscle tissue of rectus abdominis2
cardiac atrium2
right atrium auricular region2
mucosa of transverse colon2
muscle layer of sigmoid colon1
right coronary artery1
biceps brachii1
skeletal muscle tissue of biceps brachii1
dorsal motor nucleus of vagus nerve1
inferior vagus X ganglion1
left adrenal gland1
left adrenal gland cortex1
right adrenal gland cortex1
gastrocnemius1
muscle of leg1
blood vessel layer1
saphenous vein1
urethra1
rectum1

Per-gene tissue summary (top 30)

SymbolBgee breadthFANTOM5 breadthSCXATop tissues
CACNA1C134broadmarkerapex of heart, right coronary artery, muscle layer of sigmoid colon
CACNA2D1261ubiquitousmarkerbiceps brachii, skeletal muscle tissue of biceps brachii, skeletal muscle tissue of rectus abdominis
KCNH2211broadmarkerapex of heart, right atrium auricular region, cardiac atrium
KCNJ2256ubiquitousmarkerinferior vagus X ganglion, skeletal muscle tissue of rectus abdominis, dorsal motor nucleus of vagus nerve
KCNQ1132broadmarkerleft adrenal gland cortex, left adrenal gland, right adrenal gland cortex
SLC22A5235ubiquitousmarkergastrocnemius, mucosa of transverse colon, muscle of leg
SLC4A3203ubiquitousmarkerapex of heart, right atrium auricular region, cardiac atrium
VCL300ubiquitousmarkersaphenous vein, blood vessel layer, urethra
TRPM4201ubiquitousmarkermucosa of transverse colon, rectum, apex of heart

Protein interactions among cohort

Intra-cohort edges: 3.

Hub genes (top 10 by interactor count)

SymbolInteractor count
VCL4,495
KCNQ13,235
CACNA1C3,145
CACNA2D12,002
KCNH21,932
SLC22A51,492
TRPM41,217
SLC4A3859
KCNJ265

Intra-cohort edges

ABSources
CACNA1CCACNA2D1intact, string_interaction
CACNA1CKCNH2string_interaction
KCNH2KCNQ1string_interaction

Structural data

PDB: 9 · AlphaFold-only: 0 · No structure: 0

Cohort genes with PDB structures (top 30)

SymbolUniProtPDB entries
VCLP1820637
CACNA1CQ1393633
CACNA2D1P5428930
TRPM4Q8TD4329
KCNQ1P5178728
KCNH2Q1280924
SLC4A3P487514
KCNJ2P632523
SLC22A5O760823

Function

Pathway analysis

Distinct Reactome pathways touched by cohort: 65. Enrichment computed across 9 evidence-associated genes (9 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 9 annotated cohort genes). Counts and members are kept as ground-truth; sorted by enrichment.

PathwayCohort genesFoldFDRSample cohort genes
Cardiac conduction448.3×5e-05CACNA1C, KCNH2, KCNJ2, KCNQ1
Muscle contraction434.3×1e-04CACNA1C, KCNH2, KCNJ2, KCNQ1
Phase 3 - rapid repolarisation2253.8×5e-04KCNH2, KCNQ1
Potassium Channels344.8×5e-04KCNH2, KCNJ2, KCNQ1
Phase 2 - plateau phase2169.2×7e-04CACNA1C, KCNQ1
Voltage gated Potassium channels254.0×0.006KCNH2, KCNQ1
Neuronal System314.8×0.008KCNH2, KCNJ2, KCNQ1
Defective SLC22A5 causes systemic primary carnitine deficiency (CDSP)1634.4×0.011SLC22A5
Sensory perception of sour taste1634.4×0.011KCNJ2
Classical Kir channels1317.2×0.020KCNJ2
G protein gated Potassium channels1126.9×0.043KCNJ2
Bicarbonate transporters1126.9×0.043SLC4A3
Regulation of CDH1 Function1105.7×0.044VCL
SLC-mediated transmembrane transport213.2×0.044SLC22A5, SLC4A3
Carnitine shuttle184.6×0.045SLC22A5
SLC-mediated transport of organic cations184.6×0.045SLC22A5
R-HSA-549132184.6×0.045SLC22A5
Inwardly rectifying K+ channels179.3×0.045KCNJ2
Mechanical load activates signaling by PIEZO1 and integrins in osteocytes174.6×0.046CACNA2D1
Phase 4 - resting membrane potential166.8×0.046KCNJ2
Activation of GABAB receptors166.8×0.046KCNJ2
GABA B receptor activation160.4×0.049KCNJ2
TRP channels145.3×0.057TRPM4
Activation of G protein gated Potassium channels143.8×0.057KCNJ2
Adrenaline,noradrenaline inhibits insulin secretion143.8×0.057CACNA1C
Inhibition of voltage gated Ca2+ channels via Gbeta/gamma subunits143.8×0.057KCNJ2
Turbulent (oscillatory, disturbed) flow shear stress activates signaling by PIEZO1 and integrins in endothelial cells139.6×0.057VCL
Phase 0 - rapid depolarisation138.5×0.057CACNA1C
Sensory perception of taste137.3×0.057KCNJ2
Signaling by high-kinase activity BRAF mutants135.2×0.057VCL

GO biological processes by enrichment

Over-representation of cohort genes vs the genome-wide background (hypergeometric test, Benjamini-Hochberg FDR; fold = observed/expected over 9 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 conduction6249.7×3e-12CACNA1C, CACNA2D1, KCNH2, KCNJ2, KCNQ1, TRPM4
membrane repolarization during action potential3561.7×6e-07KCNH2, KCNJ2, KCNQ1
membrane repolarization during cardiac muscle cell action potential3561.7×6e-07KCNH2, KCNJ2, KCNQ1
regulation of membrane repolarization3432.1×1e-06KCNH2, KCNJ2, KCNQ1
positive regulation of potassium ion transmembrane transport3330.4×2e-06KCNH2, KCNJ2, KCNQ1
regulation of ventricular cardiac muscle cell membrane repolarization3280.9×3e-06CACNA2D1, KCNH2, KCNQ1
cardiac muscle cell action potential involved in contraction3234.1×4e-06CACNA1C, CACNA2D1, KCNJ2
calcium ion transmembrane transport via high voltage-gated calcium channel21248.3×1e-05CACNA1C, CACNA2D1
membrane depolarization during bundle of His cell action potential21248.3×1e-05CACNA2D1, TRPM4
potassium ion import across plasma membrane3122.1×2e-05KCNH2, KCNJ2, KCNQ1
membrane depolarization during AV node cell action potential2749.0×3e-05CACNA1C, TRPM4
cardiac conduction2374.5×1e-04CACNA1C, SLC4A3
membrane repolarization during ventricular cardiac muscle cell action potential2374.5×1e-04KCNH2, KCNQ1
membrane depolarization during cardiac muscle cell action potential2312.1×2e-04CACNA1C, KCNJ2
regulation of ventricular cardiac muscle cell action potential2312.1×2e-04CACNA1C, TRPM4
calcium ion transport into cytosol2267.5×2e-04CACNA1C, CACNA2D1
potassium ion export across plasma membrane2234.1×3e-04KCNH2, KCNQ1
potassium ion transmembrane transport345.3×3e-04KCNH2, KCNJ2, KCNQ1
ventricular cardiac muscle cell action potential2220.3×3e-04KCNH2, KCNQ1
potassium ion homeostasis2170.2×4e-04KCNH2, KCNQ1
positive regulation of heart rate2156.0×5e-04KCNQ1, TRPM4
calcium ion import across plasma membrane2120.8×8e-04CACNA1C, CACNA2D1
cardiac muscle contraction289.2×0.001KCNH2, KCNQ1
gastrin-induced gastric acid secretion11872.4×0.003KCNQ1
regulation of skeletal muscle contraction via regulation of action potential11872.4×0.003KCNJ2
negative regulation of voltage-gated potassium channel activity11872.4×0.003KCNQ1
positive regulation of atrial cardiac muscle cell action potential11872.4×0.003TRPM4
positive regulation of regulation of vascular associated smooth muscle cell membrane depolarization11872.4×0.003TRPM4
regulation of protein localization to adherens junction11872.4×0.003VCL
cellular response to xenobiotic stimulus253.5×0.003KCNH2, KCNQ1

Therapeutics

Drug target analysis

Approved (phase 4): 4 · Phase ≥3: 4 · Phased (≥1): 4 · Undrugged: 5

Druggability breadth: 8 of 9 evidence-associated genes (89%) 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
CACNA1CREMIFENTANIL
CACNA2D1PREGABALIN
KCNH2CETIRIZINE
KCNQ1AMBRISENTAN

Top cohort targets by molecule count

SymbolMoleculesMax phase
KCNH27064
CACNA1C854
KCNQ1154
CACNA2D154
KCNJ200
SLC22A500
SLC4A300
VCL00
TRPM400

Drugs targeting cohort genes (top 30)

MoleculeMax phaseTargets in cohort
REMIFENTANIL4CACNA1C
BEPRIDIL4CACNA1C, KCNH2
CLOTRIMAZOLE4CACNA1C, KCNH2
PROPIVERINE4CACNA1C, KCNH2
DIBUCAINE4CACNA1C, KCNH2
IMIPRAMINE4CACNA1C, KCNH2
DULOXETINE4CACNA1C, KCNH2, KCNQ1
QUINIDINE4CACNA1C, KCNH2
ESTRADIOL4CACNA1C
TOLTERODINE4CACNA1C, KCNH2, KCNQ1
PIMOZIDE4CACNA1C, KCNH2
NIMODIPINE4CACNA1C, CACNA2D1
NICARDIPINE4CACNA1C, KCNH2
AMLODIPINE4CACNA1C, KCNH2
VARDENAFIL4CACNA1C, KCNH2
CLEMASTINE4CACNA1C, KCNH2
ISRADIPINE4CACNA1C, KCNH2
TERFENADINE4CACNA1C, KCNH2
NISOLDIPINE4CACNA1C, KCNH2
SOLIFENACIN4CACNA1C, KCNH2, KCNQ1
PINAVERIUM4CACNA1C
SILDENAFIL4CACNA1C, KCNH2
NIFEDIPINE4CACNA1C, KCNH2
XANOMELINE4CACNA1C, KCNH2
DILTIAZEM4CACNA1C, KCNH2
PRENYLAMINE4CACNA1C, KCNH2
OLICERIDINE4CACNA1C, KCNH2
PROPRANOLOL4CACNA1C, KCNH2
ALVIMOPAN4CACNA1C, KCNQ1
ASTEMIZOLE4CACNA1C, KCNH2

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
CACNA1C575Binding:319, Functional:211, Toxicity:26, ADMET:19
KCNQ1179Binding:96, Functional:64, ADMET:14, Toxicity:5
SLC22A597Functional:79, ADMET:18
CACNA2D147Binding:45, ADMET:1, Toxicity:1
KCNJ231Binding:23, ADMET:8
TRPM414Binding:13, Functional:1
VCL2Binding:2

Cohort genes with high screening signal

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

SymbolChEMBL assays
CACNA1C575
KCNH24,851
KCNQ1179

Pharmacogenomics

Cohort genes with a PharmGKB record: 9; 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)
REMIFENTANIL4CACNA1C
BEPRIDIL4CACNA1C, KCNH2
CLOTRIMAZOLE4CACNA1C, KCNH2
PROPIVERINE4CACNA1C, KCNH2
DIBUCAINE4CACNA1C, KCNH2
IMIPRAMINE4CACNA1C, KCNH2
DULOXETINE4CACNA1C, KCNH2, KCNQ1
QUINIDINE4CACNA1C, KCNH2
ESTRADIOL4CACNA1C
TOLTERODINE4CACNA1C, KCNH2, KCNQ1
PIMOZIDE4CACNA1C, KCNH2
NIMODIPINE4CACNA1C, CACNA2D1
NICARDIPINE4CACNA1C, KCNH2
AMLODIPINE4CACNA1C, KCNH2
VARDENAFIL4CACNA1C, KCNH2
CLEMASTINE4CACNA1C, KCNH2
ISRADIPINE4CACNA1C, KCNH2
TERFENADINE4CACNA1C, KCNH2
NISOLDIPINE4CACNA1C, KCNH2
SOLIFENACIN4CACNA1C, KCNH2, KCNQ1
PINAVERIUM4CACNA1C
SILDENAFIL4CACNA1C, KCNH2
NIFEDIPINE4CACNA1C, KCNH2
XANOMELINE4CACNA1C, KCNH2
DILTIAZEM4CACNA1C, KCNH2
PRENYLAMINE4CACNA1C, KCNH2
OLICERIDINE4CACNA1C, KCNH2
PROPRANOLOL4CACNA1C, KCNH2
ALVIMOPAN4CACNA1C, KCNQ1
ASTEMIZOLE4CACNA1C, KCNH2

Druggability pyramid

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

TierDefinitionGenesSymbols
AApproved (phase 4 drug)4CACNA1C, CACNA2D1, KCNH2, KCNQ1
BPhased (≥1) drug, not yet approved0
CDruggable family + PDB, no drug3KCNJ2, SLC22A5, TRPM4
DDruggable family + AlphaFold only, no drug0
EDifficult family or no structure, no drug2SLC4A3, VCL

Undrugged target profiles

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

SymbolChEMBL assaysDrugged partners (top 3)
KCNJ231
SLC22A597
SLC4A30
VCL2
TRPM414

Clinical trials & evidence

Clinical trials

Clinical trials: 1.

Phase distribution (across all retrieved trials)

PhaseTrials
Not specified1

Top trials by phase / activity

NCTPhaseStatusTitle
NCT06546137Not specifiedRECRUITINGNational Network for Cardiovascular Genomics: Advancing Cardiovascular Healthcare for Hereditary Diseases in Brazil’s Unified Health System Through a Multicenter Registry