long QT syndrome 2

disease
On this page

Also known as long QT syndrome type 2Long QT syndrome, acquired, reduced susceptibility toLQT2

Summary

long QT syndrome 2 (MONDO:0013367) is a disease caused by KCNH2 (GenCC Definitive), with 10 cohort genes and 2 clinical trials. The dominant Reactome pathway is Phase 3 - rapid repolarisation (3 cohort genes).

At a glance

  • Causal gene: KCNH2 (GenCC Definitive)
  • Cohort genes: 10
  • ClinVar variants: 464
  • Clinical trials: 2

Clinical features

No curated clinical features (Orphanet) for this disease.

Identifiers

Disease identifiers

FieldValue
Canonical namelong QT syndrome 2
Mondo IDMONDO:0013367
MeSHC563614
OMIM613688
DOIDDOID:0110645
NCITC137957
UMLSC3150943
MedGen462293
GARD0003285
Is cancer (heuristic)no

Also known as: long QT syndrome 2 · long QT syndrome type 2 · Long QT syndrome, acquired, reduced susceptibility to · LQT2

Data availability: 464 ClinVar variants · 4 GenCC gene-disease records · 42 cell lines.

Disease family

Classification path: disease › human disease › disease by body system or component › syndromic diseaselong QT syndromefamilial long QT syndromelong QT syndrome 2

Related subtypes (18): Jervell and Lange-Nielsen syndrome, Andersen-Tawil syndrome, cardiac arrhythmia, ankyrin-B-related, Timothy syndrome, long QT syndrome 3, long QT syndrome 9, long QT syndrome 10, long QT syndrome 11, long QT syndrome 12, long QT syndrome 13, long QT syndrome 6, long QT syndrome 5, long QT syndrome 14, long QT syndrome 15, long QT syndrome 8, long QT syndrome 16, long QT syndrome 1, long QT syndrome 4

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

464 retrieved; paginated sample, class counts are floors:

154 uncertain significance, 118 conflicting classifications of pathogenicity, 81 pathogenic, 38 likely pathogenic, 35 pathogenic/likely pathogenic, 19 benign/likely benign, 10 benign, 9 likely benign

ClinVarVariant (HGVS)GeneClassificationReview
2680774NM_000080.4(CHRNE):c.345-2A>GCHRNEPathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
1064605NM_000238.4(KCNH2):c.2399-28delKCNH2Pathogeniccriteria provided, single submitter
1076382NM_000238.4(KCNH2):c.817C>T (p.Arg273Ter)KCNH2Pathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
1178326NM_000238.4(KCNH2):c.1425C>A (p.Tyr475Ter)KCNH2Pathogeniccriteria provided, single submitter
1197726NM_000238.4(KCNH2):c.232G>A (p.Ala78Thr)KCNH2Pathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
1338861NM_000238.4(KCNH2):c.418del (p.Ser140fs)KCNH2Pathogeniccriteria provided, single submitter
1420193NM_000238.4(KCNH2):c.2743del (p.Ala915fs)KCNH2Pathogeniccriteria provided, multiple submitters, no conflicts
14420NM_000238.4(KCNH2):c.1682C>T (p.Ala561Val)KCNH2Pathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
14421NM_000238.4(KCNH2):c.1408A>G (p.Asn470Asp)KCNH2Pathogenicno assertion criteria provided
14423NM_000238.4(KCNH2):c.1778T>G (p.Ile593Arg)KCNH2Pathogeniccriteria provided, multiple submitters, no conflicts
14424NM_000238.4(KCNH2):c.2464G>A (p.Val822Met)KCNH2Pathogeniccriteria provided, multiple submitters, no conflicts
14426NM_000238.4(KCNH2):c.1261del (p.Thr421fs)KCNH2Pathogeniccriteria provided, single submitter
14427NM_000238.4(KCNH2):c.1882G>A (p.Gly628Ser)KCNH2Pathogeniccriteria provided, multiple submitters, no conflicts
14428NM_000238.4(KCNH2):c.1744C>T (p.Arg582Cys)KCNH2Pathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
14429NM_000238.4(KCNH2):c.1714G>C (p.Gly572Arg)KCNH2Pathogenicno assertion criteria provided
14430NM_000238.4(KCNH2):c.1468G>A (p.Ala490Thr)KCNH2Pathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
14431NM_000238.4(KCNH2):c.3003G>A (p.Trp1001Ter)KCNH2Pathogeniccriteria provided, multiple submitters, no conflicts
14432NM_000238.4(KCNH2):c.2453C>T (p.Ser818Leu)KCNH2Pathogeniccriteria provided, multiple submitters, no conflicts
14434NM_000238.4(KCNH2):c.193A>C (p.Thr65Pro)KCNH2Pathogenicno assertion criteria provided
14435NM_000238.4(KCNH2):c.2255G>A (p.Arg752Gln)KCNH2Pathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
14444NM_000238.4(KCNH2):c.1672G>C (p.Ala558Pro)KCNH2Pathogenicno assertion criteria provided
1527873NM_000238.4(KCNH2):c.1397A>C (p.Asp466Ala)KCNH2Pathogeniccriteria provided, single submitter
1527874NM_000238.4(KCNH2):c.2731_2756dup (p.Ser919fs)KCNH2Pathogeniccriteria provided, single submitter
1675096NM_000238.4(KCNH2):c.1582_1603del (p.Arg528fs)KCNH2Pathogeniccriteria provided, single submitter
180379NM_000238.4(KCNH2):c.685G>T (p.Glu229Ter)KCNH2Pathogeniccriteria provided, multiple submitters, no conflicts
180383NM_000238.4(KCNH2):c.2230C>T (p.Arg744Ter)KCNH2Pathogeniccriteria provided, multiple submitters, no conflicts
1804945NM_000238.4(KCNH2):c.3099dup (p.Pro1034fs)KCNH2Pathogeniccriteria provided, multiple submitters, no conflicts
188144NM_000238.4(KCNH2):c.2900dup (p.Pro968fs)KCNH2Pathogeniccriteria provided, multiple submitters, no conflicts
200321NM_000238.4(KCNH2):c.1096C>T (p.Arg366Ter)KCNH2Pathogeniccriteria provided, multiple submitters, no conflicts
200323NM_000238.4(KCNH2):c.1128G>A (p.Gln376=)KCNH2Pathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts

Genes & proteins

Mendelian disease overlap and somatic drivers

GenCC: 9 · 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 dominantlong QT syndrome 28
ALG10BLimitedUnknownlong QT syndrome 2

Orphanet rare-disease linkage (cohort genes)

GeneOrphanet IDRare disease
KCNH2Orphanet:101016Romano-Ward syndrome
KCNH2Orphanet:51083Congenital short QT syndrome
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
SNTA1Orphanet:101016Romano-Ward syndrome
CHRNEOrphanet:98913Postsynaptic congenital myasthenic syndrome
LRP12Orphanet:98897Oculopharyngodistal myopathy
AKAP9Orphanet:101016Romano-Ward syndrome
AKAP9Orphanet:130Brugada syndrome
KCNQ1Orphanet:101016Romano-Ward syndrome
KCNQ1Orphanet:334Hereditary atrial fibrillation
KCNQ1Orphanet:51083Congenital short QT syndrome
KCNQ1Orphanet:90647Jervell and Lange-Nielsen syndrome
MPLOrphanet:3318Essential thrombocythemia
MPLOrphanet:3319Congenital amegakaryocytic thrombocytopenia
MPLOrphanet:397692Hereditary isolated aplastic anemia
MPLOrphanet:71493Familial thrombocytosis
MPLOrphanet:824Primary myelofibrosis

Cohort genes → proteins

10 cohort genes, 10 distinct canonical proteins.

Evidence partition

SubsetGenes
multi_evidence10

Cohort genes (full)

SymbolHGNCEnsemblUniProtNameEvidence
KCNH2HGNC:6251ENSG00000055118Q12809Voltage-gated inwardly rectifying potassium channel KCNH2gencc,clinvar
ALG10BHGNC:31088ENSG00000175548Q5I7T1Dol-P-Glc:Glc(2)Man(9)GlcNAc(2)-PP-Dol alpha-1,2-glucosyltransferase Bgencc
SCN5AHGNC:10593ENSG00000183873Q14524Sodium channel protein type 5 subunit alphaclinvar
SNTA1HGNC:11167ENSG00000101400Q13424Alpha-1-syntrophinclinvar
CHRNEHGNC:1966ENSG00000108556Q04844Acetylcholine receptor subunit epsilonclinvar
ALG10HGNC:23162ENSG00000139133Q5BKT4Dol-P-Glc:Glc(2)Man(9)GlcNAc(2)-PP-Dol alpha-1,2-glucosyltransferase Aclinvar
LRP12HGNC:31708ENSG00000147650Q9Y561Low-density lipoprotein receptor-related protein 12clinvar
AKAP9HGNC:379ENSG00000127914Q99996A-kinase anchor protein 9clinvar
KCNQ1HGNC:6294ENSG00000053918P51787Potassium voltage-gated channel subfamily KQT member 1clinvar
MPLHGNC:7217ENSG00000117400P40238Thrombopoietin receptorclinvar

Cohort function summary

Lead sentence per gene, UniProt-curated.

SymbolProtein nameFunction (lead sentence)
KCNH2Voltage-gated inwardly rectifying potassium channel KCNH2Pore-forming (alpha) subunit of voltage-gated inwardly rectifying potassium channel.
ALG10BDol-P-Glc:Glc(2)Man(9)GlcNAc(2)-PP-Dol alpha-1,2-glucosyltransferase BDol-P-Glc:Glc(2)Man(9)GlcNAc(2)-PP-Dol alpha-1,2-glucosyltransferase that operates in the biosynthetic pathway of dolichol-linked oligosaccharides, the glycan precursors employed in protein asparagine (N)-glycosylation.
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.
SNTA1Alpha-1-syntrophinAdapter protein that binds to and probably organizes the subcellular localization of a variety of membrane proteins.
CHRNEAcetylcholine receptor subunit epsilonAfter binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane.
ALG10Dol-P-Glc:Glc(2)Man(9)GlcNAc(2)-PP-Dol alpha-1,2-glucosyltransferase ADol-P-Glc:Glc(2)Man(9)GlcNAc(2)-PP-Dol alpha-1,2-glucosyltransferase that operates in the biosynthetic pathway of dolichol-linked oligosaccharides, the glycan precursors employed in protein asparagine (N)-glycosylation.
LRP12Low-density lipoprotein receptor-related protein 12Probable receptor, which may be involved in the internalization of lipophilic molecules and/or signal transduction.
AKAP9A-kinase anchor protein 9Scaffolding protein that assembles several protein kinases and phosphatases on the centrosome and Golgi apparatus.
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.
MPLThrombopoietin receptorReceptor for thrombopoietin that regulates hematopoietic stem cell renewal, megakaryocyte differentiation, and platelet formation.

Protein-family classification

Druggable: 5 · Difficult: 1 · Unknown: 4 · 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 channel333.5×4e-04
Antibody/Immunoglobulin12.9×0.727
Scaffold/PPI11.7×0.727
Enzyme (other)11.2×0.727
Other/Unknown40.7×0.907

Per-gene assignment

SymbolFamilyDruggable?ECInterPro (top 3)
KCNH2Ion channelyesPAS, cNMP-bd_dom, PAS-assoc_C
ALG10BOther/UnknownnoAlg10
SCN5AIon channelyesNa_channel_asu, Ion_trans_dom, Na_channel_a5su
SNTA1Scaffold/PPInoPDZ, PH_domain, PH-like_dom_sf
CHRNEOther/UnknownnoNicotinic_acetylcholine_rcpt, Neurotrans-gated_channel_TM, Neur_channel
ALG10Enzyme (other)yes2.4.1.256Alg10
LRP12Other/UnknownnoCUB_dom, LDrepeatLR_classA_rpt, LDLR_class-A_CS
AKAP9Other/UnknownnoELK_dom, PACT_domain, AKAP9/Pericentrin
KCNQ1Ion channelyesK_chnl_volt-dep_KCNQ, Ion_trans_dom, K_chnl_volt-dep_KCQN1
MPLAntibody/ImmunoglobulinyesLong_hematopoietin_rcpt_CS, FN3_dom, Ig-like_fold

Expression context

Cohort genes with no expression data: 0.

6 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)10
unknown0

Top tissues across cohort

TissueCohort genes
apex of heart3
cardiac atrium2
right atrium auricular region2
male germ line stem cell (sensu Vertebrata) in testis2
cortical plate2
calcaneal tendon1
pigmented layer of retina1
tibia1
cardiac ventricle1
heart left ventricle1
gastrocnemius1
hindlimb stylopod muscle1
adenohypophysis1
bone marrow cell1
primordial germ cell in gonad1
ganglionic eminence1
stromal cell of endometrium1
bronchial epithelial cell1
jejunal mucosa1
left adrenal gland1

Per-gene tissue summary (top 30)

SymbolBgee breadthFANTOM5 breadthSCXATop tissues
KCNH2211broadmarkerapex of heart, right atrium auricular region, cardiac atrium
ALG10B223ubiquitousyescalcaneal tendon, pigmented layer of retina, tibia
SCN5A161broadyesapex of heart, heart left ventricle, cardiac ventricle
SNTA1266ubiquitousmarkerapex of heart, hindlimb stylopod muscle, gastrocnemius
CHRNE162broadyesright atrium auricular region, cardiac atrium, adenohypophysis
ALG10172ubiquitousyesprimordial germ cell in gonad, male germ line stem cell (sensu Vertebrata) in testis, bone marrow cell
LRP12255ubiquitousmarkerstromal cell of endometrium, cortical plate, ganglionic eminence
AKAP9292ubiquitousmarkerjejunal mucosa, bronchial epithelial cell, cortical plate
KCNQ1132broadmarkerleft adrenal gland cortex, left adrenal gland, right adrenal gland cortex
MPL166tissue_specificmarkermale germ line stem cell (sensu Vertebrata) in testis, mononuclear cell, monocyte

Protein interactions among cohort

Intra-cohort edges: 10.

Hub genes (top 10 by interactor count)

SymbolInteractor count
AKAP93,537
KCNQ13,235
SCN5A2,090
KCNH21,932
SNTA11,499
MPL1,039
LRP12920
CHRNE896
ALG10638
ALG10B509

Intra-cohort edges

ABSources
AKAP9KCNH2string_interaction
AKAP9KCNQ1biogrid_interaction, intact, string_interaction
AKAP9SNTA1string_interaction
ALG10BKCNH2biogrid_interaction, string_interaction
CHRNELRP12biogrid_interaction
KCNH2KCNQ1string_interaction
KCNH2SCN5Astring_interaction
KCNQ1SCN5Astring_interaction
LRP12MPLbiogrid_interaction
SCN5ASNTA1biogrid_interaction, string_interaction

Structural data

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

Cohort genes with PDB structures (top 30)

SymbolUniProtPDB entries
KCNQ1P5178728
KCNH2Q1280924
SCN5AQ1452416
CHRNEQ0484413
MPLP402381

AlphaFold-only cohort genes (top 30 by pLDDT)

SymbolUniProtpLDDT
ALG10Q5BKT493.51
ALG10BQ5I7T193.14
SNTA1Q1342480.00
LRP12Q9Y56163.10
AKAP9Q99996

Function

Pathway analysis

Distinct Reactome pathways touched by cohort: 53. Enrichment computed across 10 evidence-associated genes (10 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 10 annotated cohort genes). Counts and members are kept as ground-truth; sorted by enrichment.

PathwayCohort genesFoldFDRSample cohort genes
Phase 3 - rapid repolarisation3342.6×3e-06KCNH2, AKAP9, KCNQ1
Cardiac conduction443.5×4e-05KCNH2, SCN5A, AKAP9, KCNQ1
Muscle contraction430.9×9e-05KCNH2, SCN5A, AKAP9, KCNQ1
Phase 2 - plateau phase2152.3×1e-03AKAP9, KCNQ1
Voltage gated Potassium channels248.6×0.008KCNH2, KCNQ1
Biosynthesis of the N-glycan precursor (dolichol lipid-linked oligosaccharide, LLO) and transfer to a nascent protein241.5×0.009ALG10, ALG10B
Neuronal System313.3×0.009KCNH2, CHRNE, KCNQ1
Potassium Channels226.9×0.016KCNH2, KCNQ1
Highly sodium permeable postsynaptic acetylcholine nicotinic receptors1163.1×0.036CHRNE
Presynaptic nicotinic acetylcholine receptors195.2×0.050CHRNE
Acetylcholine binding and downstream events181.6×0.050CHRNE
Postsynaptic nicotinic acetylcholine receptors181.6×0.050CHRNE
Asparagine N-linked glycosylation212.0×0.050ALG10, ALG10B
Platelet Aggregation (Plug Formation)143.9×0.085MPL
Metabolism of fat-soluble vitamins138.1×0.089LRP12
Interaction between L1 and Ankyrins136.8×0.089SCN5A
Phase 0 - rapid depolarisation134.6×0.089SCN5A
Formation of the dystrophin-glycoprotein complex (DGC)130.9×0.094SNTA1
Visual phototransduction125.9×0.095LRP12
Centrosome maturation125.4×0.095AKAP9
Oncogenic MAPK signaling124.8×0.095AKAP9
Retinoid metabolism and transport124.8×0.095LRP12
Signaling by BRAF and RAF1 fusions117.0×0.125AKAP9
Loss of Nlp from mitotic centrosomes115.9×0.125AKAP9
Loss of proteins required for interphase microtubule organization from the centrosome115.9×0.125AKAP9
Non-integrin membrane-ECM interactions115.4×0.125SNTA1
AURKA Activation by TPX2115.2×0.125AKAP9
Recruitment of mitotic centrosome proteins and complexes113.6×0.129AKAP9
Regulation of PLK1 Activity at G2/M Transition112.7×0.129AKAP9
Mitotic G2-G2/M phases112.7×0.129AKAP9

GO biological processes by enrichment

Over-representation of cohort genes vs the genome-wide background (hypergeometric test, Benjamini-Hochberg FDR; fold = observed/expected over 10 annotated cohort genes). Counts and members are kept as ground-truth; sorted by enrichment.

GO termCohort genesFoldFDRSample cohort genes
regulation of ventricular cardiac muscle cell membrane repolarization5421.3×4e-11KCNH2, SCN5A, SNTA1, AKAP9, KCNQ1
ventricular cardiac muscle cell action potential4396.5×9e-09KCNH2, SCN5A, SNTA1, KCNQ1
regulation of heart rate by cardiac conduction4149.8×4e-07KCNH2, SCN5A, AKAP9, KCNQ1
regulation of membrane repolarization3388.9×1e-06KCNH2, AKAP9, KCNQ1
cardiac muscle contraction3120.4×4e-05KCNH2, SCN5A, KCNQ1
regulation of atrial cardiac muscle cell membrane repolarization2481.5×1e-04SCN5A, KCNQ1
membrane depolarization during action potential2337.0×2e-04KCNH2, SCN5A
membrane repolarization during action potential2337.0×2e-04KCNH2, KCNQ1
membrane repolarization during cardiac muscle cell action potential2337.0×2e-04KCNH2, KCNQ1
atrial cardiac muscle cell action potential2337.0×2e-04SCN5A, KCNQ1
membrane repolarization during ventricular cardiac muscle cell action potential2337.0×2e-04KCNH2, KCNQ1
potassium ion export across plasma membrane2210.7×4e-04KCNH2, KCNQ1
regulation of sodium ion transmembrane transport2210.7×4e-04SCN5A, SNTA1
positive regulation of potassium ion transmembrane transport2198.3×4e-04KCNH2, KCNQ1
dolichol-linked oligosaccharide biosynthetic process2168.5×5e-04ALG10, ALG10B
potassium ion homeostasis2153.2×6e-04KCNH2, KCNQ1
membrane depolarization2102.1×0.001SCN5A, CHRNE
regulation of heart rate293.6×0.001SCN5A, SNTA1
potassium ion import across plasma membrane273.3×0.002KCNH2, KCNQ1
cellular response to cAMP258.1×0.003AKAP9, KCNQ1
gastrin-induced gastric acid secretion11685.2×0.003KCNQ1
negative regulation of voltage-gated potassium channel activity11685.2×0.003KCNQ1
basophil homeostasis11685.2×0.003MPL
protein N-linked glycosylation252.7×0.003ALG10, ALG10B
cellular response to xenobiotic stimulus248.1×0.004KCNH2, KCNQ1
regulation of membrane potential246.2×0.004KCNH2, KCNQ1
regulation of heart rate by hormone1842.6×0.004KCNH2
rhythmic behavior1842.6×0.004KCNQ1
corticosterone secretion1842.6×0.004KCNQ1
stomach development1842.6×0.004KCNQ1

Therapeutics

Drug target analysis

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

Druggability breadth: 5 of 10 evidence-associated genes (50%) 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
KCNH2CETIRIZINE
SCN5ABEPRIDIL
CHRNEMECAMYLAMINE
KCNQ1AMBRISENTAN
MPLLUSUTROMBOPAG

Top cohort targets by molecule count

SymbolMoleculesMax phase
KCNH27064
SCN5A1084
KCNQ1154
CHRNE44
MPL24
ALG10B00
SNTA100
ALG1000
LRP1200
AKAP900

Drugs targeting cohort genes (top 30)

MoleculeMax phaseTargets in cohort
CETIRIZINE4KCNH2
BEPRIDIL4KCNH2, SCN5A
BEXAROTENE4KCNH2
CLOTRIMAZOLE4KCNH2
MORICIZINE4KCNH2
PROPIVERINE4KCNH2
SUVOREXANT4KCNH2
ACETOPHENAZINE4KCNH2
DIBUCAINE4KCNH2, SCN5A
MESORIDAZINE4KCNH2
NIRAPARIB4KCNH2
BUPIVACAINE4KCNH2
IMIPRAMINE4KCNH2, SCN5A
BIPERIDEN4KCNH2
EPINASTINE4KCNH2
HALOFANTRINE4KCNH2
DROPERIDOL4KCNH2, SCN5A
RIMONABANT4KCNH2
ALOSETRON4KCNH2
ARIPIPRAZOLE4KCNH2
AMOXAPINE4KCNH2
IDARUBICIN4KCNH2
DICYCLOMINE4KCNH2
TELITHROMYCIN4KCNH2
EZETIMIBE4KCNH2
SAQUINAVIR4KCNH2
VINCAMINE4KCNH2
PONATINIB4KCNH2, SCN5A
DESLORATADINE4KCNH2
PRUCALOPRIDE4KCNH2

Bioactivity and enzyme data

Enzyme cohort genes (≥1 EC): 1.

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
KCNQ1179Binding:96, Functional:64, ADMET:14, Toxicity:5
CHRNE28Binding:26, Functional:2
MPL23Functional:15, Binding:7, ADMET:1

Cohort enzymes (BRENDA EC)

SymbolEC numbersNames
ALG102.4.1.256dolichyl-P-Glc:Glc2Man9GlcNAc2-PP-dolichol alpha-1,2-glucosyltransferase

Cohort genes with high screening signal

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

SymbolChEMBL assays
KCNH24,851
SCN5A594
KCNQ1179

Pharmacogenomics

Cohort genes with a PharmGKB record: 10; 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)
CETIRIZINE4KCNH2
BEPRIDIL4KCNH2, SCN5A
BEXAROTENE4KCNH2
CLOTRIMAZOLE4KCNH2
MORICIZINE4KCNH2
PROPIVERINE4KCNH2
SUVOREXANT4KCNH2
ACETOPHENAZINE4KCNH2
DIBUCAINE4KCNH2, SCN5A
MESORIDAZINE4KCNH2
NIRAPARIB4KCNH2
BUPIVACAINE4KCNH2
IMIPRAMINE4KCNH2, SCN5A
BIPERIDEN4KCNH2
EPINASTINE4KCNH2
HALOFANTRINE4KCNH2
DROPERIDOL4KCNH2, SCN5A
RIMONABANT4KCNH2
ALOSETRON4KCNH2
ARIPIPRAZOLE4KCNH2
AMOXAPINE4KCNH2
IDARUBICIN4KCNH2
DICYCLOMINE4KCNH2
TELITHROMYCIN4KCNH2
EZETIMIBE4KCNH2
SAQUINAVIR4KCNH2
VINCAMINE4KCNH2
PONATINIB4KCNH2, SCN5A
DESLORATADINE4KCNH2
PRUCALOPRIDE4KCNH2

Druggability pyramid

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

TierDefinitionGenesSymbols
AApproved (phase 4 drug)5KCNH2, SCN5A, CHRNE, KCNQ1, MPL
BPhased (≥1) drug, not yet approved0
CDruggable family + PDB, no drug0
DDruggable family + AlphaFold only, no drug1ALG10
EDifficult family or no structure, no drug4ALG10B, SNTA1, LRP12, AKAP9

Undrugged target profiles

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

SymbolChEMBL assaysDrugged partners (top 3)
ALG10B0KCNH2
SNTA10SCN5A
AKAP90KCNQ1
ALG100
LRP120

Clinical trials & evidence

Clinical trials

Clinical trials: 2.

Phase distribution (across all retrieved trials)

PhaseTrials
PHASE2/PHASE31
Not specified1

Top trials by phase / activity

NCTPhaseStatusTitle
NCT07277582PHASE2/PHASE3RECRUITINGEvaluation of Efficacy and Safety of THRV-1268 in Long QT Syndrome Type 2 (LQTS 2)
NCT07075445Not specifiedRECRUITINGObservational Study to Describe Health-Related Quality of Life and Measure Disease Burden Among Patients With Long QT Syndrome Types (LQTS) 2 and 3