Developmental and epileptic encephalopathy, 11

disease
On this page

Also known as DEE11developmental and epileptic encephalopathy 11early infantile epileptic encephalopathy caused by mutation in SCN2AEIEE11epileptic encephalopathy, early infantile, 11epileptic encephalopathy, early infantile, type 11SCN2A early infantile epileptic encephalopathy

Summary

Developmental and epileptic encephalopathy, 11 (MONDO:0013388) is a disease caused by SCN2A (GenCC Definitive), with 5 cohort genes. The dominant Reactome pathway is Interaction between L1 and Ankyrins (3 cohort genes).

At a glance

  • Causal gene: SCN2A (GenCC Definitive)
  • Cohort genes: 5
  • ClinVar variants: 2,028

Clinical features

No curated clinical features (Orphanet) for this disease.

Identifiers

Disease identifiers

FieldValue
Canonical namedevelopmental and epileptic encephalopathy, 11
Mondo IDMONDO:0013388
OMIM613721
DOIDDOID:0080421
UMLSC3150987
MedGen462337
GARD0015699
Is cancer (heuristic)no

Also known as: DEE11 · developmental and epileptic encephalopathy 11 · early infantile epileptic encephalopathy caused by mutation in SCN2A · EIEE11 · epileptic encephalopathy, early infantile, 11 · epileptic encephalopathy, early infantile, type 11 · SCN2A early infantile epileptic encephalopathy

Data availability: 2,028 ClinVar variants · 3 GenCC gene-disease records · 3 cell lines.

Disease family

Classification path: disease › human disease › disease by etiologic mechanism › disease of genetic or genomic mechanism › hereditary diseasehereditary neurological diseaseMendelian neurodevelopmental disordergenetic developmental and epileptic encephalopathydevelopmental and epileptic encephalopathy, 11

Related subtypes (104): developmental and epileptic encephalopathy, 9, developmental and epileptic encephalopathy, 8, developmental and epileptic encephalopathy, 2, multiple congenital anomalies-hypotonia-seizures syndrome 2, developmental and epileptic encephalopathy, 36, developmental and epileptic encephalopathy, 1, developmental and epileptic encephalopathy, 3, developmental and epileptic encephalopathy, 4, microcephaly, seizures, and developmental delay, developmental and epileptic encephalopathy, 5, developmental and epileptic encephalopathy, 7, neonatal-onset encephalopathy with rigidity and seizures, developmental and epileptic encephalopathy, 14, developmental and epileptic encephalopathy, 15, developmental and epileptic encephalopathy, 17, developmental and epileptic encephalopathy, 18, developmental and epileptic encephalopathy, 19, developmental and epileptic encephalopathy, 23, developmental and epileptic encephalopathy, 27, developmental and epileptic encephalopathy, 30, developmental and epileptic encephalopathy, 50, developmental and epileptic encephalopathy, 35, developmental and epileptic encephalopathy, 37, developmental and epileptic encephalopathy, 38, developmental and epileptic encephalopathy, 40, developmental and epileptic encephalopathy, 48, developmental and epileptic encephalopathy, 49, developmental and epileptic encephalopathy, 51, Lennox-Gastaut syndrome, developmental and epileptic encephalopathy 91, developmental and epileptic encephalopathy 92, developmental and epileptic encephalopathy 93, developmental and epileptic encephalopathy 96, developmental and epileptic encephalopathy, 90, developmental and epileptic encephalopathy, 85, with or without midline brain defects, developmental and epileptic encephalopathy, 67, developmental and epileptic encephalopathy, 86, developmental and epileptic encephalopathy, 87, developmental and epileptic encephalopathy, 88, developmental and epileptic encephalopathy 6B, developmental and epileptic encephalopathy 97, developmental and epileptic encephalopathy 98, developmental and epileptic encephalopathy 99, developmental and epileptic encephalopathy 100, developmental and epileptic encephalopathy 101, developmental and epileptic encephalopathy 89, developmental and epileptic encephalopathy 102, developmental and epileptic encephalopathy 103, developmental and epileptic encephalopathy 104, developmental and epileptic encephalopathy 105 with hypopituitarism, developmental and epileptic encephalopathy 106, developmental and epileptic encephalopathy 107, developmental and epileptic encephalopathy, 68, developmental and epileptic encephalopathy, 69, developmental and epileptic encephalopathy, 70, developmental and epileptic encephalopathy, 71, developmental and epileptic encephalopathy, 72, developmental and epileptic encephalopathy, 74, developmental and epileptic encephalopathy, 75, developmental and epileptic encephalopathy, 76, developmental and epileptic encephalopathy, 77, developmental and epileptic encephalopathy, 78, developmental and epileptic encephalopathy, 79, developmental and epileptic encephalopathy, 80, developmental and epileptic encephalopathy, 81, developmental and epileptic encephalopathy, 82, developmental and epileptic encephalopathy, 83, developmental and epileptic encephalopathy, 84, developmental and epileptic encephalopathy, 52, developmental and epileptic encephalopathy, 53, developmental and epileptic encephalopathy, 54, developmental and epileptic encephalopathy, 55, developmental and epileptic encephalopathy, 56, developmental and epileptic encephalopathy, 57, developmental and epileptic encephalopathy, 58, developmental and epileptic encephalopathy, 59, developmental and epileptic encephalopathy, 60, developmental and epileptic encephalopathy, 61, developmental and epileptic encephalopathy, 62, developmental and epileptic encephalopathy, 63, developmental and epileptic encephalopathy, 64, developmental and epileptic encephalopathy, 65, developmental and epileptic encephalopathy, 73, developmental and epileptic encephalopathy, 66, developmental and epileptic encephalopathy, 6A, non-neonatal early infantile epileptic encephalopathy, Dravet syndrome, neonatal-onset developmental and epileptic encephalopathy, hemiplegic migraine-developmental and epileptic encephalopathy spectrum, DNM1-encephalopathy and neurodevelopmental disorder, TMEM63B-related developmental and epileptic encephalopathy with anemia, developmental and epileptic encephalopathy 108, developmental and epileptic encephalopathy 109, developmental and epileptic encephalopathy 110, developmental and epileptic encephalopathy 111, developmental and epileptic encephalopathy 112, developmental and epileptic encephalopathy 113, developmental and epileptic encephalopathy 114, developmental and epileptic encephalopathy 115, developmental and epileptic encephalopathy 116, developmental and epileptic encephalopathy 118, developmental and epileptic encephalopathy 120, developmental and epileptic encephalopathy 121, developmental and epileptic encephalopathy 119

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:

237 uncertain significance, 200 likely benign, 52 pathogenic, 36 likely pathogenic, 36 conflicting classifications of pathogenicity, 18 benign/likely benign, 16 benign, 5 pathogenic/likely pathogenic

ClinVarVariant (HGVS)GeneClassificationReview
1054402NC_000002.11:g.(?165946660)(167168266_?)delSCN1APathogeniccriteria provided, single submitter
1459193NC_000002.11:g.(?166210682)(167168266_?)delSCN1APathogeniccriteria provided, single submitter
1000049NM_001040142.2(SCN2A):c.4901G>T (p.Gly1634Val)SCN2APathogeniccriteria provided, single submitter
1066198NM_001040142.2(SCN2A):c.4551+1G>ASCN2APathogeniccriteria provided, single submitter
1068258NM_001040142.2(SCN2A):c.4501A>G (p.Met1501Val)SCN2APathogeniccriteria provided, single submitter
1070304NM_001040142.2(SCN2A):c.787G>A (p.Ala263Thr)SCN2APathogeniccriteria provided, single submitter
1071664NM_001040142.2(SCN2A):c.718del (p.Ala240fs)SCN2APathogeniccriteria provided, single submitter
1071677NM_001040142.2(SCN2A):c.1497del (p.Glu500fs)SCN2APathogeniccriteria provided, single submitter
1072191NM_001040142.2(SCN2A):c.1267G>T (p.Val423Leu)SCN2APathogeniccriteria provided, single submitter
1073234NM_001040142.2(SCN2A):c.4533dup (p.Pro1512fs)SCN2APathogeniccriteria provided, single submitter
1074161NM_001040142.2(SCN2A):c.3782G>A (p.Trp1261Ter)SCN2APathogeniccriteria provided, single submitter
1074300NM_001040142.2(SCN2A):c.4543C>T (p.Arg1515Ter)SCN2APathogeniccriteria provided, multiple submitters, no conflicts
1074301NM_001040142.2(SCN2A):c.4787T>G (p.Ile1596Ser)SCN2APathogeniccriteria provided, single submitter
1173107NM_001040142.2(SCN2A):c.330C>A (p.Tyr110Ter)SCN2APathogeniccriteria provided, single submitter
1180439NM_001040142.2(SCN2A):c.986dup (p.Leu329fs)SCN2APathogeniccriteria provided, single submitter
1219256NM_001040142.2(SCN2A):c.1729del (p.Leu577fs)SCN2APathogeniccriteria provided, multiple submitters, no conflicts
1256055NM_001040142.2(SCN2A):c.2588C>A (p.Ser863Tyr)SCN2APathogeniccriteria provided, single submitter
12876NM_001040142.2(SCN2A):c.3988C>T (p.Leu1330Phe)SCN2APathogeniccriteria provided, single submitter
12877NM_001040142.2(SCN2A):c.4687C>G (p.Leu1563Val)SCN2APathogeniccriteria provided, multiple submitters, no conflicts
12878NM_001040142.2(SCN2A):c.2674G>A (p.Val892Ile)SCN2APathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
12879NM_001040142.2(SCN2A):c.668G>A (p.Arg223Gln)SCN2APathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
12880NM_001040142.2(SCN2A):c.3956G>A (p.Arg1319Gln)SCN2APathogeniccriteria provided, multiple submitters, no conflicts
1318908NM_001040142.2(SCN2A):c.718G>T (p.Ala240Ser)SCN2APathogeniccriteria provided, multiple submitters, no conflicts
1333343NM_001040142.2(SCN2A):c.1570C>T (p.Arg524Ter)SCN2APathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
1342674NM_001040142.2(SCN2A):c.4498G>A (p.Ala1500Thr)SCN2APathogeniccriteria provided, single submitter
1342682NM_001040142.2(SCN2A):c.4712T>C (p.Ile1571Thr)SCN2APathogeniccriteria provided, single submitter
1343156NM_001040142.2(SCN2A):c.1136G>A (p.Arg379His)SCN2APathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
1365870NM_001040142.2(SCN2A):c.1819_1831del (p.Arg607fs)SCN2APathogeniccriteria provided, single submitter
1381138NM_001040142.2(SCN2A):c.3802dup (p.Val1268fs)SCN2APathogeniccriteria provided, single submitter
1403875NM_001040142.2(SCN2A):c.1147C>T (p.Gln383Ter)SCN2APathogeniccriteria provided, single submitter

Genes & proteins

Mendelian disease overlap and somatic drivers

GenCC: 16 · Orphanet: 32 · 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
SCN2ADefinitiveAutosomal dominantdevelopmental and epileptic encephalopathy, 1116

Orphanet rare-disease linkage (cohort genes)

GeneOrphanet IDRare disease
SCN2AOrphanet:140927Self-limited neonatal-infantile epilepsy
SCN2AOrphanet:1934Early infantile developmental and epileptic encephalopathy
SCN2AOrphanet:2131Alternating hemiplegia of childhood
SCN2AOrphanet:293181Epilepsy of infancy with migrating focal seizures
SCN2AOrphanet:306Self-limited infantile epilepsy
SCN2AOrphanet:33069Dravet syndrome
SCN2AOrphanet:36387Genetic epilepsy with febrile seizure plus
SCN2AOrphanet:697160Infantile epileptic spasms syndrome
SCN1AOrphanet:1942Epilepsy with myoclonic-atonic seizures
SCN1AOrphanet:2382Lennox-Gastaut syndrome
SCN1AOrphanet:293181Epilepsy of infancy with migrating focal seizures
SCN1AOrphanet:33069Dravet syndrome
SCN1AOrphanet:36387Genetic epilepsy with febrile seizure plus
SCN1AOrphanet:442835Non-specific early-onset epileptic encephalopathy
SCN1AOrphanet:569Familial or sporadic hemiplegic migraine
SCN3AOrphanet:442835Non-specific early-onset epileptic encephalopathy
SCN3AOrphanet:98820Familial focal epilepsy with variable foci
SHHOrphanet:220386Semilobar holoprosencephaly
SHHOrphanet:280195Septopreoptic holoprosencephaly
SHHOrphanet:280200Microform holoprosencephaly
SHHOrphanet:476119Autosomal dominant preaxial polydactyly-upperback hypertrichosis syndrome
SHHOrphanet:485275Acquired schizencephaly
SHHOrphanet:93321Isolated radial hemimelia
SHHOrphanet:93336Polydactyly of a triphalangeal thumb
SHHOrphanet:93405Syndactyly type 4
SHHOrphanet:93924Lobar holoprosencephaly
SHHOrphanet:93925Alobar holoprosencephaly
SHHOrphanet:93926Midline interhemispheric variant of holoprosencephaly
SHHOrphanet:988Tibial hemimelia-polysyndactyly-triphalangeal thumb syndrome
SHHOrphanet:98938Colobomatous microphthalmia
TTC21BOrphanet:474Jeune syndrome
TTC21BOrphanet:93591Infantile nephronophthisis

Cohort genes → proteins

5 cohort genes, 5 distinct canonical proteins.

Evidence partition

SubsetGenes
multi_evidence5

Cohort genes (full)

SymbolHGNCEnsemblUniProtNameEvidence
SCN2AHGNC:10588ENSG00000136531Q99250Sodium channel protein type 2 subunit alphagencc,clinvar
SCN1AHGNC:10585ENSG00000144285P35498Sodium channel protein type 1 subunit alphaclinvar
SCN3AHGNC:10590ENSG00000153253Q9NY46Sodium channel protein type 3 subunit alphaclinvar
SHHHGNC:10848ENSG00000164690Q15465Sonic hedgehog proteinclinvar
TTC21BHGNC:25660ENSG00000123607Q7Z4L5Tetratricopeptide repeat protein 21Bclinvar

Cohort function summary

Lead sentence per gene, UniProt-curated.

SymbolProtein nameFunction (lead sentence)
SCN2ASodium channel protein type 2 subunit alphaMediates the voltage-dependent sodium ion permeability of excitable membranes.
SCN1ASodium channel protein type 1 subunit alphaPore-forming subunit of Nav1.1, a voltage-gated sodium (Nav) channel that directly mediates the depolarizing phase of action potentials in excitable membranes.
SCN3ASodium channel protein type 3 subunit alphaPore-forming subunit of Nav1.3, a voltage-gated sodium (Nav) channel that directly mediates the depolarizing phase of action potentials in excitable membranes.
SHHSonic hedgehog proteinThe C-terminal part of the sonic hedgehog protein precursor displays an autoproteolysis and a cholesterol transferase activity.
TTC21BTetratricopeptide repeat protein 21BComponent of the IFT complex A (IFT-A), a complex required for retrograde ciliary transport and entry into cilia of G protein-coupled receptors (GPCRs).

Protein-family classification

Druggable: 3 · Difficult: 0 · Unknown: 2 · Druggable fraction: 0.6

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 channel366.9×1e-05
Other/Unknown20.7×0.877

Per-gene assignment

SymbolFamilyDruggable?ECInterPro (top 3)
SCN2AIon channelyesIQ_motif_EF-hand-BS, Na_channel_asu, Ion_trans_dom
SCN1AIon channelyesNa_channel_asu, Ion_trans_dom, Na_channel_a1su
SCN3AIon channelyesNa_channel_asu, Ion_trans_dom, Na_trans_assoc_dom
SHHOther/UnknownnoHedgehog_signalling_dom, Hedgehog, Hedgehog_Hint
TTC21BOther/UnknownnoTPR-like_helical_dom_sf, TPR_rpt, TTC21A/TTC21B

Expression context

Cohort genes with no expression data: 0.

5 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)5
unknown0

Top tissues across cohort

TissueCohort genes
Brodmann (1909) area 232
middle temporal gyrus2
cerebellar vermis1
lateral nuclear group of thalamus1
primary visual cortex1
cortical plate1
endothelial cell1
buccal mucosa cell1
epithelial cell of pancreas1
right lobe of liver1
calcaneal tendon1
cerebellar hemisphere1
right uterine tube1

Per-gene tissue summary (top 30)

SymbolBgee breadthFANTOM5 breadthSCXATop tissues
SCN2A187broadmarkermiddle temporal gyrus, Brodmann (1909) area 23, cerebellar vermis
SCN1A154tissue_specificmarkerBrodmann (1909) area 23, lateral nuclear group of thalamus, primary visual cortex
SCN3A221broadmarkerendothelial cell, cortical plate, middle temporal gyrus
SHH131broadmarkerbuccal mucosa cell, right lobe of liver, epithelial cell of pancreas
TTC21B179ubiquitousmarkerright uterine tube, calcaneal tendon, cerebellar hemisphere

Protein interactions among cohort

Intra-cohort edges: 2.

Hub genes (top 10 by interactor count)

SymbolInteractor count
SHH4,953
SCN2A2,810
SCN1A2,287
TTC21B1,588
SCN3A1,454

Intra-cohort edges

ABSources
SCN1ASCN2Abiogrid_interaction, string_interaction
SCN2ASCN3Aintact

Structural data

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

Cohort genes with PDB structures (top 30)

SymbolUniProtPDB entries
SHHQ1546520
SCN2AQ992505
TTC21BQ7Z4L53
SCN3AQ9NY462
SCN1AP354981

Function

Pathway analysis

Distinct Reactome pathways touched by cohort: 34. Enrichment computed across 5 evidence-associated genes (5 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 5 annotated cohort genes). Counts and members are kept as ground-truth; sorted by enrichment.

PathwayCohort genesFoldFDRSample cohort genes
Interaction between L1 and Ankyrins3221.0×4e-06SCN2A, SCN1A, SCN3A
Phase 0 - rapid depolarisation3207.6×4e-06SCN2A, SCN1A, SCN3A
L1CAM interactions372.1×6e-05SCN2A, SCN1A, SCN3A
Cardiac conduction365.3×6e-05SCN2A, SCN1A, SCN3A
Muscle contraction346.3×1e-04SCN2A, SCN1A, SCN3A
Sensory perception of taste2134.3×4e-04SCN2A, SCN3A
Sensory perception of sweet, bitter, and umami (glutamate) taste2111.4×4e-04SCN2A, SCN3A
Axon guidance327.1×4e-04SCN2A, SCN1A, SCN3A
Nervous system development325.8×4e-04SCN2A, SCN1A, SCN3A
Developmental Biology411.6×4e-04SCN2A, SCN1A, SCN3A, SHH
Sensory Perception238.1×0.003SCN2A, SCN3A
HHAT G278V doesn’t palmitoylate Hh-Np1456.8×0.006SHH
Formation of lateral plate mesoderm1456.8×0.006SHH
Release of Hh-Np from the secreting cell1285.5×0.007SHH
Hh mutants abrogate ligand secretion1285.5×0.007SHH
Ligand-receptor interactions1285.5×0.007SHH
Formation of axial mesoderm1163.1×0.012SHH
Activation of SMO1126.9×0.015SHH
Developmental Lineage of Multipotent Pancreatic Progenitor Cells1120.2×0.015SHH
Developmental Lineage of Pancreatic Acinar Cells160.1×0.028SHH
Gastrulation151.9×0.031SHH
Hh mutants are degraded by ERAD148.6×0.032SHH
Developmental Cell Lineages144.8×0.033SHH
Hedgehog ligand biogenesis142.3×0.033SHH
Intraflagellar transport140.1×0.034TTC21B
Class B/2 (Secretin family receptors)138.1×0.034SHH
Signaling by Hedgehog136.8×0.034SHH
Hedgehog ‘off’ state135.7×0.034TTC21B
Hedgehog ‘on’ state131.7×0.037SHH
GPCR ligand binding112.8×0.086SHH

GO biological processes by enrichment

Over-representation of cohort genes vs the genome-wide background (hypergeometric test, Benjamini-Hochberg FDR; fold = observed/expected over 5 annotated cohort genes). Counts and members are kept as ground-truth; sorted by enrichment.

GO termCohort genesFoldFDRSample cohort genes
cardiac muscle cell action potential involved in contraction3421.3×5e-06SCN2A, SCN1A, SCN3A
sodium ion transport3163.1×4e-05SCN2A, SCN1A, SCN3A
sodium ion transmembrane transport3121.8×7e-05SCN2A, SCN1A, SCN3A
membrane depolarization during action potential2674.1×1e-04SCN1A, SCN3A
Bergmann glial cell differentiation2612.8×1e-04SHH, TTC21B
neuronal action potential2192.6×0.001SCN2A, SCN1A
polarity specification of anterior/posterior axis13370.4×0.003SHH
trachea morphogenesis13370.4×0.003SHH
right lung development13370.4×0.003SHH
left lung development13370.4×0.003SHH
primary prostatic bud elongation13370.4×0.003SHH
regulation of prostatic bud formation13370.4×0.003SHH
obsolete regulation of mesenchymal cell proliferation involved in prostate gland development13370.4×0.003SHH
mesenchymal smoothened signaling pathway involved in prostate gland development13370.4×0.003SHH
positive regulation of sclerotome development13370.4×0.003SHH
tracheoesophageal septum formation13370.4×0.003SHH
negative regulation of ureter smooth muscle cell differentiation13370.4×0.003SHH
positive regulation of ureter smooth muscle cell differentiation13370.4×0.003SHH
negative regulation of kidney smooth muscle cell differentiation13370.4×0.003SHH
positive regulation of kidney smooth muscle cell differentiation13370.4×0.003SHH
smoothened signaling pathway272.5×0.003SHH, TTC21B
intrinsic apoptotic signaling pathway in response to osmotic stress11685.2×0.004SCN2A
positive regulation of skeletal muscle cell proliferation11685.2×0.004SHH
intein-mediated protein splicing11685.2×0.004SHH
trunk neural crest cell migration11685.2×0.004SHH
regulation of nodal signaling pathway11685.2×0.004SHH
regulation of intraciliary retrograde transport11685.2×0.004TTC21B
positive regulation of mesenchymal cell proliferation involved in ureter development11685.2×0.004SHH
ventral midline development11123.5×0.005SHH
CD4-positive or CD8-positive, alpha-beta T cell lineage commitment11123.5×0.005SHH

Therapeutics

Drug target analysis

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

Druggability breadth: 4 of 5 evidence-associated genes (80%) 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
SCN2ABEPRIDIL
SCN1AMEXILETINE HYDROCHLORIDE
SCN3ABEPRIDIL
SHHVISMODEGIB

Top cohort targets by molecule count

SymbolMoleculesMax phase
SCN2A994
SCN1A944
SCN3A934
SHH14
TTC21B00

Drugs targeting cohort genes (top 30)

MoleculeMax phaseTargets in cohort
BEPRIDIL4SCN1A, SCN2A, SCN3A
DIBUCAINE4SCN1A, SCN2A, SCN3A
ARTICAINE4SCN1A, SCN2A, SCN3A
BUPIVACAINE4SCN1A, SCN2A, SCN3A
IMIPRAMINE4SCN1A, SCN2A, SCN3A
DROPERIDOL4SCN1A, SCN2A, SCN3A
DICYCLOMINE4SCN1A, SCN2A, SCN3A
TETRABENAZINE4SCN1A, SCN2A, SCN3A
PHENIRAMINE4SCN1A, SCN2A, SCN3A
PRILOCAINE4SCN1A, SCN2A, SCN3A
PROPOXYCAINE4SCN1A, SCN2A, SCN3A
PROPARACAINE4SCN1A, SCN2A, SCN3A
HEXYLCAINE4SCN1A, SCN2A, SCN3A
PRAMOXINE4SCN1A, SCN2A, SCN3A
BENOXINATE4SCN1A, SCN2A, SCN3A
QUINIDINE4SCN1A, SCN2A, SCN3A
FELODIPINE4SCN1A, SCN2A, SCN3A
PHENYTOIN4SCN1A, SCN2A, SCN3A
QUININE4SCN1A, SCN2A, SCN3A
NISOLDIPINE4SCN1A, SCN2A, SCN3A
NIFEDIPINE4SCN1A, SCN2A, SCN3A
PRAZOSIN4SCN1A, SCN2A, SCN3A
DILTIAZEM4SCN1A, SCN2A, SCN3A
PRENYLAMINE4SCN1A, SCN2A, SCN3A
COCAINE4SCN1A, SCN2A, SCN3A
TRIFLUOPERAZINE4SCN1A, SCN2A, SCN3A
CINNARIZINE4SCN1A, SCN2A, SCN3A
THIORIDAZINE4SCN1A, SCN2A, SCN3A
ETIDOCAINE4SCN1A, SCN2A, SCN3A
CHLORPHENIRAMINE4SCN1A, SCN2A, SCN3A

Bioactivity and enzyme data

Enzyme cohort genes (≥1 EC): 0.

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

SymbolAssaysType breakdown
SCN2A203Binding:172, Functional:20, ADMET:10, Toxicity:1
SCN1A149Binding:115, Functional:18, ADMET:14, Toxicity:2
SCN3A102Binding:79, Functional:18, ADMET:4, Toxicity:1
SHH27Binding:23, Functional:4

Cohort genes with high screening signal

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

SymbolChEMBL assays
SCN2A203
SCN1A149
SCN3A102

Pharmacogenomics

Cohort genes with a PharmGKB record: 5; 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)
BEPRIDIL4SCN1A, SCN2A, SCN3A
DIBUCAINE4SCN1A, SCN2A, SCN3A
ARTICAINE4SCN1A, SCN2A, SCN3A
BUPIVACAINE4SCN1A, SCN2A, SCN3A
IMIPRAMINE4SCN1A, SCN2A, SCN3A
DROPERIDOL4SCN1A, SCN2A, SCN3A
DICYCLOMINE4SCN1A, SCN2A, SCN3A
TETRABENAZINE4SCN1A, SCN2A, SCN3A
PHENIRAMINE4SCN1A, SCN2A, SCN3A
PRILOCAINE4SCN1A, SCN2A, SCN3A
PROPOXYCAINE4SCN1A, SCN2A, SCN3A
PROPARACAINE4SCN1A, SCN2A, SCN3A
HEXYLCAINE4SCN1A, SCN2A, SCN3A
PRAMOXINE4SCN1A, SCN2A, SCN3A
BENOXINATE4SCN1A, SCN2A, SCN3A
QUINIDINE4SCN1A, SCN2A, SCN3A
FELODIPINE4SCN1A, SCN2A, SCN3A
PHENYTOIN4SCN1A, SCN2A, SCN3A
QUININE4SCN1A, SCN2A, SCN3A
NISOLDIPINE4SCN1A, SCN2A, SCN3A
NIFEDIPINE4SCN1A, SCN2A, SCN3A
PRAZOSIN4SCN1A, SCN2A, SCN3A
DILTIAZEM4SCN1A, SCN2A, SCN3A
PRENYLAMINE4SCN1A, SCN2A, SCN3A
COCAINE4SCN1A, SCN2A, SCN3A
TRIFLUOPERAZINE4SCN1A, SCN2A, SCN3A
CINNARIZINE4SCN1A, SCN2A, SCN3A
THIORIDAZINE4SCN1A, SCN2A, SCN3A
ETIDOCAINE4SCN1A, SCN2A, SCN3A
CHLORPHENIRAMINE4SCN1A, SCN2A, SCN3A

Druggability pyramid

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

TierDefinitionGenesSymbols
AApproved (phase 4 drug)4SCN2A, SCN1A, SCN3A, SHH
BPhased (≥1) drug, not yet approved0
CDruggable family + PDB, no drug0
DDruggable family + AlphaFold only, no drug0
EDifficult family or no structure, no drug1TTC21B

Undrugged target profiles

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

SymbolChEMBL assaysDrugged partners (top 3)
TTC21B0

Clinical trials & evidence

Clinical trials

Clinical trials: 0.