Total early-onset cataract

disease
On this page

Also known as cataract, total congenitalcataract, total congenital with posterior sutural opacities in heterozygotesCCT

Summary

Total early-onset cataract (MONDO:0021548) is a disease with 16 cohort genes and 1 clinical trial.

At a glance

  • Cohort genes: 16
  • Clinical trials: 1

Clinical features

No curated clinical features (Orphanet) for this disease.

Identifiers

Disease identifiers

FieldValue
Canonical nametotal early-onset cataract
Mondo IDMONDO:0021548
Orphanet98994
UMLSC0266539
MedGen75616
GARD0001159
Is cancer (heuristic)no

Also known as: cataract, total congenital · cataract, total congenital with posterior sutural opacities in heterozygotes · CCT

Data availability: 15 GenCC gene-disease records.

Disease family

Classification path: disease › human disease › disease by body system or component › disorder of orbital regioneye disorderlens disordercataractearly-onset non-syndromic cataracttotal early-onset cataract

Related subtypes (28): cataract 32 multiple types, cataract 8 multiple types, cataract 42, cataract 20 multiple types, cataract 6 multiple types, cataract 13 with adult I phenotype, cataract 5 multiple types, cataract 46 juvenile-onset, cataract 40, cataract 10 multiple types, cataract 14 multiple types, pulverulent cataract, cataract 31 multiple types, cataract 26 multiple types, cataract 22 multiple types, cataract 21 multiple types, cataract 23, cataract 11 multiple types, cataract 33, cataract 17 multiple types, cataract 38, cataract 39 multiple types, cataract 15 multiple types, cataract 19 multiple types, cataract 43, cataract 44, cataract 45, early-onset partial cataract

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

No tiered GWAS variants or ClinVar records for this disease.

Genes & proteins

Mendelian disease overlap and somatic drivers

GenCC: 124 · Orphanet: 48 · 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
CRYAADefinitiveAutosomal recessivecataract 9 multiple types8
CRYBB2DefinitiveAutosomal dominantcataract 3 multiple types11
EPHA2DefinitiveAutosomal dominantcataract 6 multiple types10
FYCO1DefinitiveAutosomal recessivecataract 185
GCNT2DefinitiveAutosomal recessivecataract 13 with adult I phenotype6
GJA8DefinitiveAutosomal dominantcataract 1 multiple types9
HSF4DefinitiveAutosomal dominantcataract 5 multiple types7
LIM2DefinitiveAutosomal recessivecataract 19 multiple types6
MIPDefinitiveAutosomal dominantcataract 15 multiple types10
TNPO1DefinitiveAutosomal dominantcataract 15 multiple types11
DNMBPStrongAutosomal recessivecataract 483
LEMD2StrongAutosomal recessivecataract 46 juvenile-onset10
LSSStrongAutosomal recessivecataract 4411
SIPA1L3ModerateAutosomal dominantcataract 456
AGKSupportiveAutosomal dominanttotal early-onset cataract6
CRYGBSupportiveAutosomal dominantearly-onset lamellar cataract5

Orphanet rare-disease linkage (cohort genes)

GeneOrphanet IDRare disease
FYCO1Orphanet:98991Early-onset nuclear cataract
FYCO1Orphanet:98994Total early-onset cataract
LEMD2Orphanet:441447Early-onset posterior subcapsular cataract
LEMD2Orphanet:659873Wormian bones-micrognathia-abnormal dentition-progeroid syndrome
LEMD2Orphanet:98994Total early-onset cataract
AGKOrphanet:1369Congenital cataract-hypertrophic cardiomyopathy-mitochondrial myopathy syndrome
AGKOrphanet:98994Total early-onset cataract
SIPA1L3Orphanet:98994Total early-onset cataract
CRYAAOrphanet:1377Cataract-microcornea syndrome
CRYAAOrphanet:441452Early-onset lamellar cataract
CRYAAOrphanet:98988Early-onset anterior polar cataract
CRYAAOrphanet:98991Early-onset nuclear cataract
CRYAAOrphanet:98994Total early-onset cataract
CRYBB2Orphanet:1377Cataract-microcornea syndrome
CRYBB2Orphanet:441447Early-onset posterior subcapsular cataract
CRYBB2Orphanet:98984Pulverulent cataract
CRYBB2Orphanet:98985Early-onset sutural cataract
CRYBB2Orphanet:98989Cerulean cataract
CRYBB2Orphanet:98991Early-onset nuclear cataract
CRYBB2Orphanet:98994Total early-onset cataract
CRYGBOrphanet:441452Early-onset lamellar cataract
CRYGBOrphanet:98988Early-onset anterior polar cataract
CRYGBOrphanet:98994Total early-onset cataract
DNMBPOrphanet:98994Total early-onset cataract
EPHA2Orphanet:441447Early-onset posterior subcapsular cataract
EPHA2Orphanet:98991Early-onset nuclear cataract
EPHA2Orphanet:98993Early-onset posterior polar cataract
EPHA2Orphanet:98994Total early-onset cataract
GCNT2Orphanet:98994Total early-onset cataract
GJA8Orphanet:1377Cataract-microcornea syndrome
GJA8Orphanet:91490Isolated congenital sclerocornea
GJA8Orphanet:98984Pulverulent cataract
GJA8Orphanet:98985Early-onset sutural cataract
GJA8Orphanet:98991Early-onset nuclear cataract
GJA8Orphanet:98994Total early-onset cataract
HSF4Orphanet:441452Early-onset lamellar cataract
HSF4Orphanet:98994Total early-onset cataract
LIM2Orphanet:98994Total early-onset cataract
LSSOrphanet:1366Autosomal recessive palmoplantar keratoderma and congenital alopecia
LSSOrphanet:2850Alopecia-intellectual disability syndrome
LSSOrphanet:55654Hypotrichosis simplex
LSSOrphanet:98994Total early-onset cataract
MIPOrphanet:441452Early-onset lamellar cataract
MIPOrphanet:98985Early-onset sutural cataract
MIPOrphanet:98989Cerulean cataract
MIPOrphanet:98991Early-onset nuclear cataract
MIPOrphanet:98993Early-onset posterior polar cataract
MIPOrphanet:98994Total early-onset cataract

Cohort genes → proteins

16 cohort genes, 16 distinct canonical proteins.

Evidence partition

SubsetGenes
multi_evidence16

Cohort genes (full)

SymbolHGNCEnsemblUniProtNameEvidence
FYCO1HGNC:14673ENSG00000163820Q9BQS8FYVE and coiled-coil domain-containing protein 1gencc
LEMD2HGNC:21244ENSG00000161904Q8NC56LEM domain-containing protein 2gencc
AGKHGNC:21869ENSG00000006530Q53H12Acylglycerol kinase, mitochondrialgencc
SIPA1L3HGNC:23801ENSG00000105738O60292Signal-induced proliferation-associated 1-like protein 3gencc
CRYAAHGNC:2388ENSG00000160202P02489Alpha-crystallin A chaingencc
CRYBB2HGNC:2398ENSG00000244752P43320Beta-crystallin B2gencc
CRYGBHGNC:2409ENSG00000182187P07316Gamma-crystallin Bgencc
DNMBPHGNC:30373ENSG00000107554Q6XZF7Dynamin-binding proteingencc
EPHA2HGNC:3386ENSG00000142627P29317Ephrin type-A receptor 2gencc
GCNT2HGNC:4204ENSG00000111846Q8N0V5N-acetyllactosaminide beta-1,6-N-acetylglucosaminyl-transferasegencc
GJA8HGNC:4281ENSG00000121634P48165Gap junction alpha-8 proteingencc
HSF4HGNC:5227ENSG00000102878Q9ULV5Heat shock factor protein 4gencc
TNPO1HGNC:6401ENSG00000083312Q92973Transportin-1gencc
LIM2HGNC:6610ENSG00000105370P55344Lens fiber membrane intrinsic proteingencc
LSSHGNC:6708ENSG00000160285P48449Lanosterol synthasegencc
MIPHGNC:7103ENSG00000135517P30301Lens fiber major intrinsic proteingencc

Cohort function summary

Lead sentence per gene, UniProt-curated.

SymbolProtein nameFunction (lead sentence)
FYCO1FYVE and coiled-coil domain-containing protein 1May mediate microtubule plus end-directed vesicle transport.
LEMD2LEM domain-containing protein 2Nuclear lamina-associated inner nuclear membrane protein that is involved in nuclear structure organization, maintenance of nuclear envelope (NE) integrity and NE reformation after mitosis.
AGKAcylglycerol kinase, mitochondrialLipid kinase that can phosphorylate both monoacylglycerol and diacylglycerol to form lysophosphatidic acid (LPA) and phosphatidic acid (PA), respectively.
SIPA1L3Signal-induced proliferation-associated 1-like protein 3Plays a critical role in epithelial cell morphogenesis, polarity, adhesion and cytoskeletal organization in the lens.
CRYAAAlpha-crystallin A chainContributes to the transparency and refractive index of the lens.
CRYBB2Beta-crystallin B2Crystallins are the dominant structural components of the vertebrate eye lens.
CRYGBGamma-crystallin BCrystallins are the dominant structural components of the vertebrate eye lens.
DNMBPDynamin-binding proteinPlays a critical role as a guanine nucleotide exchange factor (GEF) for CDC42 in several intracellular processes associated with the actin and microtubule cytoskeleton.
EPHA2Ephrin type-A receptor 2Receptor tyrosine kinase which binds promiscuously membrane-bound ephrin-A family ligands residing on adjacent cells, leading to contact-dependent bidirectional signaling into neighboring cells.
GCNT2N-acetyllactosaminide beta-1,6-N-acetylglucosaminyl-transferaseBranching enzyme that converts linear into branched poly-N-acetyllactosaminoglycans.
GJA8Gap junction alpha-8 proteinStructural component of eye lens gap junctions.
HSF4Heat shock factor protein 4Heat-shock transcription factor that specifically binds heat shock promoter elements (HSE).
TNPO1Transportin-1Functions in nuclear protein import as nuclear transport receptor.
LIM2Lens fiber membrane intrinsic proteinPresent in the thicker 16-17 nm junctions of mammalian lens fiber cells, where it may contribute to cell junctional organization.
LSSLanosterol synthaseKey enzyme in the cholesterol biosynthesis pathway.
MIPLens fiber major intrinsic proteinAquaporins form homotetrameric transmembrane channels, with each monomer independently mediating water transport across the plasma membrane along its osmotic gradient.

Protein-family classification

Druggable: 4 · Difficult: 3 · Unknown: 9 · Druggable fraction: 0.25

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
Kinase23.5×0.559
Scaffold/PPI22.2×0.590
Enzyme (other)21.5×0.651
Other/Unknown91.0×0.736
Transcription factor10.5×0.873

Per-gene assignment

SymbolFamilyDruggable?ECInterPro (top 3)
FYCO1Transcription factornoZnf_FYVE, Run_dom, GOLD_dom
LEMD2Other/UnknownnoLEM_dom, LEM/LEM-like_dom_sf, Man1/Src1-like_C
AGKKinaseyes2.7.1.94Diacylglycerol_kinase_cat_dom, NAD/diacylglycerol_kinase_sf, ATP-NAD_kinase_N
SIPA1L3Scaffold/PPInoRap/Ran_GAP_dom, PDZ, SIPA1L_C
CRYAAOther/UnknownnoAlpha-crystallin/sHSP_animal, A-crystallin/Hsp20_dom, Alpha-crystallin_N
CRYBB2Other/UnknownnoBeta/gamma_crystallin, G_crystallin-like, Beta/Gamma-Crystallin
CRYGBOther/UnknownnoBeta/gamma_crystallin, G_crystallin-like, Beta/Gamma-Crystallin
DNMBPScaffold/PPInoDH_dom, GDS_CDC24_CS, SH3_domain
EPHA2Kinaseyes2.7.10.1Prot_kinase_dom, EPH_LBD, Ser-Thr/Tyr_kinase_cat_dom
GCNT2Enzyme (other)yes2.4.1.150Glyco_trans_14
GJA8Other/UnknownnoConnexin, Connexin50_C, Connexin_N
HSF4Other/UnknownnoHSF_DNA-bd, WH-like_DNA-bd_sf, WH_DNA-bd_sf
TNPO1Other/UnknownnoImportin-beta_N, ARM-like, ARM-type_fold
LIM2Other/UnknownnoLMIP, PMP22/EMP/MP20/Claudin, PMP22_EMP_MP20
LSSEnzyme (other)yes5.4.99.7Terpene_synthase_CS, Terpenoid_cyclase/PrenylTrfase, Squalene_cyclase
MIPOther/UnknownnoMIP, MIP_CS, Aquaporin-like

Expression context

Cohort genes with no expression data: 0.

12 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)1
broad (>20)15
unknown0

Top tissues across cohort

TissueCohort genes
cerebellar cortex3
cerebellar hemisphere3
male germ line stem cell (sensu Vertebrata) in testis3
primordial germ cell in gonad3
skeletal muscle tissue of rectus abdominis2
right hemisphere of cerebellum2
buccal mucosa cell2
right lobe of liver2
biceps brachii1
skeletal muscle tissue of biceps brachii1
adrenal tissue1
endometrium epithelium1
islet of Langerhans1
adult mammalian kidney1
liver1
gluteal muscle1
trabecular bone tissue1
triceps brachii1
sperm1
colonic mucosa1

Per-gene tissue summary (top 30)

SymbolBgee breadthFANTOM5 breadthSCXATop tissues
FYCO1284ubiquitousmarkerskeletal muscle tissue of rectus abdominis, biceps brachii, skeletal muscle tissue of biceps brachii
LEMD2186ubiquitousmarkerright hemisphere of cerebellum, cerebellar hemisphere, cerebellar cortex
AGK161ubiquitousmarkeradrenal tissue, cerebellar hemisphere, cerebellar cortex
SIPA1L3257ubiquitousmarkerbuccal mucosa cell, endometrium epithelium, islet of Langerhans
CRYAA42markeradult mammalian kidney, right lobe of liver, liver
CRYBB2144tissue_specificyestriceps brachii, gluteal muscle, trabecular bone tissue
CRYGB35tissue_specificyesmale germ line stem cell (sensu Vertebrata) in testis, sperm, skeletal muscle tissue of rectus abdominis
DNMBP279ubiquitousmarkerjejunal mucosa, ileal mucosa, colonic mucosa
EPHA2224ubiquitousmarkerlower esophagus mucosa, esophagus mucosa, pharyngeal mucosa
GCNT2136ubiquitousmarkerprimordial germ cell in gonad, heart left ventricle, male germ line stem cell (sensu Vertebrata) in testis
GJA817tissue_specificyesbuccal mucosa cell, frontal pole, paraflocculus
HSF4186tissue_specificmarkerright hemisphere of cerebellum, cerebellar hemisphere, cerebellar cortex
TNPO1295ubiquitousmarkercorpus epididymis, caput epididymis, cauda epididymis
LIM226tissue_specificmarkerprimordial germ cell in gonad, lens of camera-type eye, granulocyte
LSS134ubiquitousmarkermucosa of stomach, C1 segment of cervical spinal cord, skin of leg
MIP91tissue_specificyesmale germ line stem cell (sensu Vertebrata) in testis, primordial germ cell in gonad, right lobe of liver

Protein interactions among cohort

Intra-cohort edges: 22.

Hub genes (top 10 by interactor count)

SymbolInteractor count
EPHA24,794
TNPO13,147
MIP2,496
AGK2,341
LEMD22,340
FYCO11,637
LIM21,593
LSS1,562
CRYAA1,464
DNMBP1,328

Intra-cohort edges

ABSources
CRYAACRYBB2biogrid_interaction, intact, string_interaction
CRYAACRYGBstring_interaction
CRYAAFYCO1string_interaction
CRYAAGJA8string_interaction
CRYAAHSF4string_interaction
CRYAALIM2string_interaction
CRYAASIPA1L3string_interaction
CRYBB2GCNT2string_interaction
CRYBB2GJA8string_interaction
CRYBB2HSF4string_interaction
CRYBB2LIM2string_interaction
CRYGBGJA8string_interaction
CRYGBLIM2string_interaction
DNMBPSIPA1L3string_interaction
GCNT2HSF4string_interaction
GJA8HSF4string_interaction
GJA8LIM2string_interaction
GJA8MIPstring_interaction
GJA8SIPA1L3string_interaction
HSF4LIM2string_interaction
HSF4MIPstring_interaction
LIM2MIPstring_interaction

Structural data

PDB: 11 · AlphaFold-only: 5 · No structure: 0

Cohort genes with PDB structures (top 30)

SymbolUniProtPDB entries
EPHA2P29317103
TNPO1Q9297321
DNMBPQ6XZF77
CRYAAP024895
FYCO1Q9BQS83
CRYBB2P433203
CRYGBP073162
HSF4Q9ULV52
LSSP484492
AGKQ53H121
LIM2P553441

AlphaFold-only cohort genes (top 30 by pLDDT)

SymbolUniProtpLDDT
GCNT2Q8N0V591.66
MIPP3030191.08
LEMD2Q8NC5671.49
GJA8P4816565.85
SIPA1L3O6029256.37

Function

Pathway analysis

Distinct Reactome pathways touched by cohort: 44. Enrichment computed across 16 evidence-associated genes (8 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 8 annotated cohort genes). Counts and members are kept as ground-truth; sorted by enrichment.

PathwayCohort genesFoldFDRSample cohort genes
Cholesterol biosynthesis1142.8×0.058LSS
Passive transport by Aquaporins1109.8×0.058MIP
Depolymerization of the Nuclear Lamina195.2×0.058LEMD2
Lanosterol biosynthesis195.2×0.058LSS
Tristetraprolin (TTP, ZFP36) binds and destabilizes mRNA179.3×0.058TNPO1
Initiation of Nuclear Envelope (NE) Reformation175.1×0.058LEMD2
Nuclear Envelope Breakdown157.1×0.058LEMD2
Postmitotic nuclear pore complex (NPC) reformation151.0×0.058TNPO1
EPHA-mediated growth cone collapse147.6×0.058EPHA2
Aquaporin-mediated transport146.0×0.058MIP
Mitotic Prophase146.0×0.058LEMD2
Sealing of the nuclear envelope (NE) by ESCRT-III143.3×0.058LEMD2
Glycerophospholipid biosynthesis142.0×0.058AGK
Regulation of cholesterol biosynthesis by SREBP (SREBF)139.6×0.058LSS
Gap junction assembly136.6×0.058GJA8
Nuclear Envelope (NE) Reassembly136.6×0.058LEMD2
RHOV GTPase cycle135.7×0.058EPHA2
RHOU GTPase cycle134.8×0.058EPHA2
RND1 GTPase cycle133.2×0.058EPHA2
Activation of gene expression by SREBF (SREBP)132.4×0.058LSS
RND3 GTPase cycle132.4×0.058EPHA2
RND2 GTPase cycle132.4×0.058EPHA2
Metabolism of lipids27.9×0.058AGK, LSS
Oncogenic MAPK signaling131.0×0.058AGK
EPH-ephrin mediated repulsion of cells127.4×0.063EPHA2
Phospholipid metabolism125.0×0.064AGK
Intraflagellar transport125.0×0.064TNPO1
Signaling by BRAF and RAF1 fusions121.3×0.072AGK
EPH-Ephrin signaling120.7×0.072EPHA2
RHOG GTPase cycle118.5×0.077EPHA2

GO biological processes by enrichment

Over-representation of cohort genes vs the genome-wide background (hypergeometric test, Benjamini-Hochberg FDR; fold = observed/expected over 16 annotated cohort genes). Counts and members are kept as ground-truth; sorted by enrichment.

GO termCohort genesFoldFDRSample cohort genes
lens development in camera-type eye6140.4×2e-10CRYAA, CRYBB2, CRYGB, GJA8, LIM2, MIP
lens fiber cell morphogenesis3395.0×2e-06CRYAA, CRYGB, EPHA2
gap junction-mediated intercellular transport2351.1×5e-04GJA8, MIP
maintenance of lens transparency2263.3×6e-04GCNT2, MIP
visual perception419.9×9e-04CRYAA, CRYBB2, CRYGB, MIP
triterpenoid biosynthetic process11053.2×0.015LSS
notochord cell development11053.2×0.015EPHA2
multicellular organism development1526.6×0.023GCNT2
axial mesoderm formation1526.6×0.023EPHA2
notochord formation1351.1×0.026EPHA2
negative regulation of intracellular transport1351.1×0.026CRYAA
negative regulation of lymphangiogenesis1351.1×0.026EPHA2
cAMP metabolic process1263.3×0.030EPHA2
response to UV-A1263.3×0.030CRYAA
heart formation1210.7×0.031LEMD2
pericyte cell differentiation1210.7×0.031EPHA2
regulation of blood vessel endothelial cell migration1175.5×0.031EPHA2
apoptotic process involved in morphogenesis1175.5×0.031CRYAA
plus-end-directed vesicle transport along microtubule1175.5×0.031FYCO1
regulation of small GTPase mediated signal transduction218.0×0.031SIPA1L3, DNMBP
blood vessel endothelial cell proliferation involved in sprouting angiogenesis1150.5×0.031EPHA2
nuclear membrane organization1150.5×0.031LEMD2
positive regulation of autophagosome maturation1150.5×0.031FYCO1
negative regulation of chemokine production1131.7×0.033EPHA2
glycerolipid metabolic process1131.7×0.033AGK
regulation of lamellipodium assembly1117.0×0.034EPHA2
tubulin complex assembly1105.3×0.034CRYAA
homotypic cell-cell adhesion1105.3×0.034MIP
lipid phosphorylation1105.3×0.034AGK
positive regulation of bicellular tight junction assembly1105.3×0.034EPHA2

Therapeutics

Drug target analysis

Approved (phase 4): 1 · Phase ≥3: 1 · Phased (≥1): 1 · Undrugged: 15

Druggability breadth: 8 of 16 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
EPHA2PONATINIB

Top cohort targets by molecule count

SymbolMoleculesMax phase
EPHA2504
FYCO100
LEMD200
AGK00
SIPA1L300
CRYAA00
CRYBB200
CRYGB00
DNMBP00
GCNT200

Drugs targeting cohort genes (top 30)

MoleculeMax phaseTargets in cohort
PONATINIB4EPHA2
FEDRATINIB4EPHA2
TIVOZANIB4EPHA2
SORAFENIB4EPHA2
DASATINIB ANHYDROUS4EPHA2
REGORAFENIB4EPHA2
CABOZANTINIB4EPHA2
VANDETANIB4EPHA2
NILOTINIB4EPHA2
BOSUTINIB4EPHA2
TOVORAFENIB4EPHA2
NINTEDANIB4EPHA2
DASATINIB4EPHA2
CRIZOTINIB4EPHA2
SARACATINIB3EPHA2
LINIFANIB3EPHA2
TESEVATINIB3EPHA2
ALVOCIDIB3EPHA2
ALISERTIB3EPHA2
LESTAURTINIB3EPHA2
DORAMAPIMOD2EPHA2
NEFLAMAPIMOD2EPHA2
FORETINIB2EPHA2
ILORASERTIB2EPHA2
CEP-324962EPHA2
BAFETINIB2EPHA2
SAPITINIB2EPHA2
OSI-6322EPHA2
GOLVATINIB2EPHA2
PEXMETINIB2EPHA2

Bioactivity and enzyme data

Enzyme cohort genes (≥1 EC): 4.

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

SymbolAssaysType breakdown
EPHA2567Binding:565, Functional:1, ADMET:1
LSS46Binding:45, Functional:1
CRYAA25Binding:25
AGK19Binding:19
CRYBB29Binding:9
TNPO17Binding:7
DNMBP1Binding:1
HSF41Binding:1

Cohort enzymes (BRENDA EC)

SymbolEC numbersNames
AGK2.7.1.94acylglycerol kinase
EPHA22.7.10.1receptor protein-tyrosine kinase
GCNT22.4.1.150N-acetyllactosaminide beta-1,6-N-acetylglucosaminyltransferase
LSS5.4.99.7Lanosterol synthase

Cohort genes with high screening signal

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

SymbolChEMBL assays
EPHA2567

Pharmacogenomics

Cohort genes with a PharmGKB record: 16; 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)
PONATINIB4EPHA2
FEDRATINIB4EPHA2
TIVOZANIB4EPHA2
SORAFENIB4EPHA2
DASATINIB ANHYDROUS4EPHA2
REGORAFENIB4EPHA2
CABOZANTINIB4EPHA2
VANDETANIB4EPHA2
NILOTINIB4EPHA2
BOSUTINIB4EPHA2
TOVORAFENIB4EPHA2
NINTEDANIB4EPHA2
DASATINIB4EPHA2
CRIZOTINIB4EPHA2
SARACATINIB3EPHA2
LINIFANIB3EPHA2
TESEVATINIB3EPHA2
ALVOCIDIB3EPHA2
ALISERTIB3EPHA2
LESTAURTINIB3EPHA2
DORAMAPIMOD2EPHA2
NEFLAMAPIMOD2EPHA2
FORETINIB2EPHA2
ILORASERTIB2EPHA2
CEP-324962EPHA2
BAFETINIB2EPHA2
SAPITINIB2EPHA2
OSI-6322EPHA2
GOLVATINIB2EPHA2
PEXMETINIB2EPHA2

Druggability pyramid

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

TierDefinitionGenesSymbols
AApproved (phase 4 drug)1EPHA2
BPhased (≥1) drug, not yet approved0
CDruggable family + PDB, no drug2AGK, LSS
DDruggable family + AlphaFold only, no drug1GCNT2
EDifficult family or no structure, no drug12FYCO1, LEMD2, SIPA1L3, CRYAA, CRYBB2, CRYGB, DNMBP, GJA8, HSF4, TNPO1 (+2 more)

Undrugged target profiles

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

SymbolChEMBL assaysDrugged partners (top 3)
FYCO10
LEMD20
AGK19
SIPA1L30
CRYAA25
CRYBB29
CRYGB0
DNMBP1
GCNT20
GJA80
HSF41
TNPO17
LIM20
LSS46
MIP0

Clinical trials & evidence

Clinical trials

Clinical trials: 1.

Phase distribution (across all retrieved trials)

PhaseTrials
Not specified1

Top trials by phase / activity

NCTPhaseStatusTitle
NCT06068348Not specifiedACTIVE_NOT_RECRUITINGLiquid Biopsy Collection Study