Early-onset nuclear cataract

disease
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Summary

Early-onset nuclear cataract (MONDO:0020376) is a disease with 19 cohort genes.

At a glance

  • Cohort genes: 19

Clinical features

No curated clinical features (Orphanet) for this disease.

Identifiers

Disease identifiers

FieldValue
Canonical nameearly-onset nuclear cataract
Mondo IDMONDO:0020376
MeSHC563333
Orphanet98991
UMLSC5681644
MedGen1842550
GARD0016887
MedDRA10007759, 10057735
Is cancer (heuristic)no

Data availability: 18 GenCC gene-disease records.

Disease family

An umbrella term covering 4 Mondo subtypes.

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

Related subtypes (2): cataract 16 multiple types, early-onset sutural cataract

Subtypes (4): cataract 41, cataract 27, cataract 35, autosomal recessive nonsyndromic congenital nuclear 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: 172 · Orphanet: 70 · 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
CRYBA1DefinitiveAutosomal dominantcataract 10 multiple types7
CRYBB1DefinitiveAutosomal dominantcataract 17 multiple types8
CRYBB2DefinitiveAutosomal dominantcataract 3 multiple types11
CRYBB3DefinitiveAutosomal recessivecataract 22 multiple types9
CRYGCDefinitiveAutosomal dominantcataract 2, multiple types7
CRYGDDefinitiveAutosomal dominantcataract 4 multiple types9
EPHA2DefinitiveAutosomal dominantcataract 6 multiple types10
FYCO1DefinitiveAutosomal recessivecataract 185
GJA3DefinitiveAutosomal dominantcataract 14 multiple types6
GJA8DefinitiveAutosomal dominantcataract 1 multiple types9
MIPDefinitiveAutosomal dominantcataract 15 multiple types10
TNPO1DefinitiveAutosomal dominantcataract 15 multiple types11
BFSP1StrongAutosomal dominantcataract 338
CRYABStrongAutosomal dominantcataract 16 multiple types16
CRYBA2StrongAutosomal dominantcataract 425
UNC45BStrongAutosomal dominantcataract 438
WFS1StrongAutosomal dominantcataract 4119
NHSSupportiveAutosomal dominantearly-onset nuclear cataract6

Orphanet rare-disease linkage (cohort genes)

GeneOrphanet IDRare disease
BFSP1Orphanet:98991Early-onset nuclear cataract
WFS1Orphanet:3463Wolfram syndrome
WFS1Orphanet:411590Wolfram-like syndrome
WFS1Orphanet:90635Rare autosomal dominant non-syndromic sensorineural deafness type DFNA
WFS1Orphanet:98991Early-onset nuclear cataract
UNC45BOrphanet:441447Early-onset posterior subcapsular cataract
UNC45BOrphanet:98991Early-onset nuclear cataract
FYCO1Orphanet:98991Early-onset nuclear cataract
FYCO1Orphanet: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
CRYABOrphanet:154Familial isolated dilated cardiomyopathy
CRYABOrphanet:280553Fatal infantile hypertonic myofibrillar myopathy
CRYABOrphanet:399058Alpha-B crystallin-related late-onset myopathy
CRYABOrphanet:441452Early-onset lamellar cataract
CRYABOrphanet:98991Early-onset nuclear cataract
CRYABOrphanet:98993Early-onset posterior polar cataract
CRYBA1Orphanet:441452Early-onset lamellar cataract
CRYBA1Orphanet:98985Early-onset sutural cataract
CRYBA1Orphanet:98991Early-onset nuclear cataract
CRYBA1Orphanet:98993Early-onset posterior polar cataract
CRYBA2Orphanet:98988Early-onset anterior polar cataract
CRYBA2Orphanet:98991Early-onset nuclear cataract
CRYBB1Orphanet:1377Cataract-microcornea syndrome
CRYBB1Orphanet:98984Pulverulent cataract
CRYBB1Orphanet:98991Early-onset nuclear 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
CRYBB3Orphanet:98988Early-onset anterior polar cataract
CRYBB3Orphanet:98991Early-onset nuclear cataract
CRYGCOrphanet:1377Cataract-microcornea syndrome
CRYGCOrphanet:441452Early-onset lamellar cataract
CRYGCOrphanet:98984Pulverulent cataract
CRYGCOrphanet:98991Early-onset nuclear cataract
CRYGDOrphanet:1377Cataract-microcornea syndrome
CRYGDOrphanet:441452Early-onset lamellar cataract
CRYGDOrphanet:98984Pulverulent cataract
CRYGDOrphanet:98989Cerulean cataract
CRYGDOrphanet:98990Coralliform cataract
CRYGDOrphanet:98991Early-onset nuclear cataract
EPHA2Orphanet:441447Early-onset posterior subcapsular cataract
EPHA2Orphanet:98991Early-onset nuclear cataract

Cohort genes → proteins

19 cohort genes, 19 distinct canonical proteins.

Evidence partition

SubsetGenes
multi_evidence19

Cohort genes (full)

SymbolHGNCEnsemblUniProtNameEvidence
BFSP1HGNC:1040ENSG00000125864Q12934Filensingencc
WFS1HGNC:12762ENSG00000109501O76024Wolframingencc
UNC45BHGNC:14304ENSG00000141161Q8IWX7Protein unc-45 homolog Bgencc
FYCO1HGNC:14673ENSG00000163820Q9BQS8FYVE and coiled-coil domain-containing protein 1gencc
CRYAAHGNC:2388ENSG00000160202P02489Alpha-crystallin A chaingencc
CRYABHGNC:2389ENSG00000109846P02511Alpha-crystallin B chaingencc
CRYBA1HGNC:2394ENSG00000108255P05813Beta-crystallin A3gencc
CRYBA2HGNC:2395ENSG00000163499P53672Beta-crystallin A2gencc
CRYBB1HGNC:2397ENSG00000100122P53674Beta-crystallin B1gencc
CRYBB2HGNC:2398ENSG00000244752P43320Beta-crystallin B2gencc
CRYBB3HGNC:2400ENSG00000100053P26998Beta-crystallin B3gencc
CRYGCHGNC:2410ENSG00000163254P07315Gamma-crystallin Cgencc
CRYGDHGNC:2411ENSG00000118231P07320Gamma-crystallin Dgencc
EPHA2HGNC:3386ENSG00000142627P29317Ephrin type-A receptor 2gencc
GJA3HGNC:4277ENSG00000121743Q9Y6H8Gap junction alpha-3 proteingencc
GJA8HGNC:4281ENSG00000121634P48165Gap junction alpha-8 proteingencc
TNPO1HGNC:6401ENSG00000083312Q92973Transportin-1gencc
MIPHGNC:7103ENSG00000135517P30301Lens fiber major intrinsic proteingencc
NHSHGNC:7820ENSG00000188158Q6T4R5Actin remodeling regulator NHSgencc

Cohort function summary

Lead sentence per gene, UniProt-curated.

SymbolProtein nameFunction (lead sentence)
BFSP1FilensinRequired for the correct formation of lens intermediate filaments as part of a complex composed of BFSP1, BFSP2 and CRYAA.
WFS1WolframinParticipates in the regulation of cellular Ca(2+) homeostasis, at least partly, by modulating the filling state of the endoplasmic reticulum Ca(2+) store.
UNC45BProtein unc-45 homolog BActs as a co-chaperone for HSP90 and is required for proper folding of the myosin motor domain.
FYCO1FYVE and coiled-coil domain-containing protein 1May mediate microtubule plus end-directed vesicle transport.
CRYAAAlpha-crystallin A chainContributes to the transparency and refractive index of the lens.
CRYABAlpha-crystallin B chainMay contribute to the transparency and refractive index of the lens.
CRYBA1Beta-crystallin A3Crystallins are the dominant structural components of the vertebrate eye lens.
CRYBA2Beta-crystallin A2Crystallins are the dominant structural components of the vertebrate eye lens.
CRYBB1Beta-crystallin B1Crystallins are the dominant structural components of the vertebrate eye lens.
CRYBB2Beta-crystallin B2Crystallins are the dominant structural components of the vertebrate eye lens.
CRYBB3Beta-crystallin B3Crystallins are the dominant structural components of the vertebrate eye lens.
CRYGCGamma-crystallin CCrystallins are the dominant structural components of the vertebrate eye lens.
CRYGDGamma-crystallin DCrystallins are the dominant structural components of the vertebrate eye lens.
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.
GJA3Gap junction alpha-3 proteinStructural component of lens fiber gap junctions.
GJA8Gap junction alpha-8 proteinStructural component of eye lens gap junctions.
TNPO1Transportin-1Functions in nuclear protein import as nuclear transport receptor.
MIPLens fiber major intrinsic proteinAquaporins form homotetrameric transmembrane channels, with each monomer independently mediating water transport across the plasma membrane along its osmotic gradient.
NHSActin remodeling regulator NHSMay function in cell morphology by maintaining the integrity of the circumferential actin ring and controlling lamellipod formation.

Protein-family classification

Druggable: 1 · Difficult: 1 · Unknown: 17 · Druggable fraction: 0.05

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
Other/Unknown171.6×0.006
Kinase11.5×0.754
Transcription factor10.4×0.914

Per-gene assignment

SymbolFamilyDruggable?ECInterPro (top 3)
BFSP1Other/UnknownnoIF_rod_dom, BFSP1
WFS1Other/UnknownnoTPR-like_helical_dom_sf, Wolframin, Wolframin_fam
UNC45BOther/UnknownnoArmadillo, ARM-like, TPR-like_helical_dom_sf
FYCO1Transcription factornoZnf_FYVE, Run_dom, GOLD_dom
CRYAAOther/UnknownnoAlpha-crystallin/sHSP_animal, A-crystallin/Hsp20_dom, Alpha-crystallin_N
CRYABOther/UnknownnoAlpha-crystallin/sHSP_animal, A-crystallin/Hsp20_dom, Alpha-crystallin_N
CRYBA1Other/UnknownnoBeta/gamma_crystallin, G_crystallin-like, Beta/Gamma-Crystallin
CRYBA2Other/UnknownnoBeta/gamma_crystallin, G_crystallin-like, Beta/Gamma-Crystallin
CRYBB1Other/UnknownnoBeta/gamma_crystallin, G_crystallin-like, Beta/Gamma-Crystallin
CRYBB2Other/UnknownnoBeta/gamma_crystallin, G_crystallin-like, Beta/Gamma-Crystallin
CRYBB3Other/UnknownnoBeta/gamma_crystallin, G_crystallin-like, Beta/Gamma-Crystallin
CRYGCOther/UnknownnoBeta/gamma_crystallin, G_crystallin-like, Beta/Gamma-Crystallin
CRYGDOther/UnknownnoBeta/gamma_crystallin, G_crystallin-like, Beta/Gamma-Crystallin
EPHA2Kinaseyes2.7.10.1Prot_kinase_dom, EPH_LBD, Ser-Thr/Tyr_kinase_cat_dom
GJA3Other/UnknownnoConnexin, Connexin46, Connexin_N
GJA8Other/UnknownnoConnexin, Connexin50_C, Connexin_N
TNPO1Other/UnknownnoImportin-beta_N, ARM-like, ARM-type_fold
MIPOther/UnknownnoMIP, MIP_CS, Aquaporin-like
NHSOther/UnknownnoNHS-like

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)2
broad (>20)17
unknown0

Top tissues across cohort

TissueCohort genes
male germ line stem cell (sensu Vertebrata) in testis7
primordial germ cell in gonad7
left ventricle myocardium3
buccal mucosa cell3
right lobe of liver2
tendon of biceps brachii1
body of uterus1
left ovary1
right ovary1
cardiac muscle of right atrium1
tibialis anterior1
biceps brachii1
skeletal muscle tissue of biceps brachii1
skeletal muscle tissue of rectus abdominis1
adult mammalian kidney1
liver1
cardiac ventricle1
middle frontal gyrus1
lens of camera-type eye1
islet of Langerhans1

Per-gene tissue summary (top 30)

SymbolBgee breadthFANTOM5 breadthSCXATop tissues
BFSP1176broadyestendon of biceps brachii, primordial germ cell in gonad, male germ line stem cell (sensu Vertebrata) in testis
WFS1280ubiquitousmarkerright ovary, left ovary, body of uterus
UNC45B111tissue_specificyesleft ventricle myocardium, cardiac muscle of right atrium, tibialis anterior
FYCO1284ubiquitousmarkerskeletal muscle tissue of rectus abdominis, biceps brachii, skeletal muscle tissue of biceps brachii
CRYAA42markeradult mammalian kidney, right lobe of liver, liver
CRYAB289ubiquitousmarkermiddle frontal gyrus, left ventricle myocardium, cardiac ventricle
CRYBA1138tissue_specificyeslens of camera-type eye, primordial germ cell in gonad, male germ line stem cell (sensu Vertebrata) in testis
CRYBA2128tissue_specificmarkerislet of Langerhans, primordial germ cell in gonad, male germ line stem cell (sensu Vertebrata) in testis
CRYBB1154broadyesprimordial germ cell in gonad, prefrontal cortex, Brodmann (1909) area 10
CRYBB2144tissue_specificyestriceps brachii, gluteal muscle, trabecular bone tissue
CRYBB3145tissue_specificyesmale germ line stem cell (sensu Vertebrata) in testis, buccal mucosa cell, mucosa of transverse colon
CRYGC15tissue_specificyesmale germ line stem cell (sensu Vertebrata) in testis, primordial germ cell in gonad, testis
CRYGD60tissue_specificmarkermale germ line stem cell (sensu Vertebrata) in testis, primordial germ cell in gonad, ventricular zone
EPHA2224ubiquitousmarkerlower esophagus mucosa, esophagus mucosa, pharyngeal mucosa
GJA375broadyesleft ventricle myocardium, heart right ventricle, myocardium
GJA817tissue_specificyesbuccal mucosa cell, frontal pole, paraflocculus
TNPO1295ubiquitousmarkercorpus epididymis, caput epididymis, cauda epididymis
MIP91tissue_specificyesmale germ line stem cell (sensu Vertebrata) in testis, primordial germ cell in gonad, right lobe of liver
NHS214ubiquitousmarkeroviduct epithelium, buccal mucosa cell, endothelial cell

Protein interactions among cohort

Intra-cohort edges: 57.

Hub genes (top 10 by interactor count)

SymbolInteractor count
EPHA24,794
WFS13,409
CRYAB3,368
TNPO13,147
MIP2,496
CRYGC2,111
CRYBB31,718
FYCO11,637
CRYBB11,508
CRYAA1,464

Intra-cohort edges

ABSources
BFSP1CRYAAstring_interaction
BFSP1CRYBA1string_interaction
BFSP1CRYBA2string_interaction
BFSP1CRYBB1string_interaction
BFSP1CRYBB2string_interaction
BFSP1CRYBB3string_interaction
BFSP1CRYGDstring_interaction
BFSP1GJA3string_interaction
BFSP1GJA8string_interaction
BFSP1MIPstring_interaction
CRYAACRYABbiogrid_interaction, intact
CRYAACRYBA1biogrid_interaction, string_interaction
CRYAACRYBA2string_interaction
CRYAACRYBB1string_interaction
CRYAACRYBB2biogrid_interaction, intact, string_interaction
CRYAACRYBB3intact, string_interaction
CRYAACRYGCbiogrid_interaction, intact, string_interaction
CRYAACRYGDbiogrid_interaction, string_interaction
CRYAAFYCO1string_interaction
CRYAAGJA3string_interaction
CRYAAGJA8string_interaction
CRYABCRYBA1string_interaction
CRYABCRYBA2string_interaction
CRYABCRYBB1string_interaction
CRYABCRYBB2biogrid_interaction, intact, string_interaction
CRYABCRYBB3string_interaction
CRYABCRYGCbiogrid_interaction, intact
CRYABCRYGDbiogrid_interaction, string_interaction
CRYABGJA8string_interaction
CRYBA1CRYBB1biogrid_interaction, intact
CRYBA1CRYBB2biogrid_interaction, intact
CRYBA1CRYBB3biogrid_interaction, intact
CRYBA1GJA3string_interaction
CRYBA1GJA8string_interaction
CRYBA2CRYBB1intact
CRYBA2CRYBB2intact
CRYBA2GJA3string_interaction
CRYBA2GJA8string_interaction
CRYBB1CRYBB3intact
CRYBB1FYCO1string_interaction
CRYBB1GJA3string_interaction
CRYBB1GJA8string_interaction
CRYBB1MIPstring_interaction
CRYBB2CRYGCbiogrid_interaction, intact
CRYBB2GJA3string_interaction
CRYBB2GJA8string_interaction
CRYBB3GJA3string_interaction
CRYBB3GJA8string_interaction
CRYGCCRYGDbiogrid_interaction
CRYGCGJA3string_interaction

Structural data

PDB: 10 · AlphaFold-only: 9 · No structure: 0

Cohort genes with PDB structures (top 30)

SymbolUniProtPDB entries
EPHA2P29317103
CRYABP0251121
TNPO1Q9297321
CRYGDP0732016
CRYAAP024895
FYCO1Q9BQS83
CRYBB2P433203
CRYBB1P536741
CRYBB3P269981
CRYGCP073151

AlphaFold-only cohort genes (top 30 by pLDDT)

SymbolUniProtpLDDT
CRYBA2P5367293.12
MIPP3030191.08
UNC45BQ8IWX788.38
CRYBA1P0581388.27
WFS1O7602473.85
GJA3Q9Y6H869.53
GJA8P4816565.85
BFSP1Q1293464.66
NHSQ6T4R543.65

Function

Pathway analysis

Distinct Reactome pathways touched by cohort: 23. Enrichment computed across 19 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
Gap junction assembly273.2×0.007GJA3, GJA8
RAC2 GTPase cycle231.7×0.015EPHA2, NHS
RAC3 GTPase cycle229.7×0.015EPHA2, NHS
RAC1 GTPase cycle215.3×0.040EPHA2, NHS
Passive transport by Aquaporins1109.8×0.042MIP
Tristetraprolin (TTP, ZFP36) binds and destabilizes mRNA179.3×0.047TNPO1
Postmitotic nuclear pore complex (NPC) reformation151.0×0.047TNPO1
EPHA-mediated growth cone collapse147.6×0.047EPHA2
Aquaporin-mediated transport146.0×0.047MIP
HSF1-dependent transactivation139.6×0.047CRYAB
RHOV GTPase cycle135.7×0.047EPHA2
RHOU GTPase cycle134.8×0.047EPHA2
RND1 GTPase cycle133.2×0.047EPHA2
RND3 GTPase cycle132.4×0.047EPHA2
RND2 GTPase cycle132.4×0.047EPHA2
EPH-ephrin mediated repulsion of cells127.4×0.049EPHA2
XBP1(S) activates chaperone genes126.9×0.049WFS1
Intraflagellar transport125.0×0.050TNPO1
EPH-Ephrin signaling120.7×0.057EPHA2
RHOG GTPase cycle118.5×0.061EPHA2
Post-translational protein phosphorylation112.5×0.084WFS1
Regulation of Insulin-like Growth Factor (IGF) transport and uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs)110.8×0.093WFS1
Transport of small molecules13.1×0.277MIP

GO biological processes by enrichment

Over-representation of cohort genes vs the genome-wide background (hypergeometric test, Benjamini-Hochberg FDR; fold = observed/expected over 19 annotated cohort genes). Counts and members are kept as ground-truth; sorted by enrichment.

GO termCohort genesFoldFDRSample cohort genes
lens development in camera-type eye13256.2×2e-28UNC45B, CRYAA, CRYAB, CRYBA1, CRYBA2, CRYBB1, CRYBB2, CRYBB3 (+5 more)
visual perception1146.0×4e-15WFS1, CRYAA, CRYBA1, CRYBA2, CRYBB1, CRYBB2, CRYBB3, CRYGC (+3 more)
gap junction-mediated intercellular transport3443.5×1e-06GJA3, GJA8, MIP
negative regulation of intracellular transport2591.3×1e-04CRYAA, CRYAB
apoptotic process involved in morphogenesis2295.6×4e-04CRYAA, CRYAB
lens fiber cell morphogenesis2221.7×7e-04CRYAA, EPHA2
tubulin complex assembly2177.4×9e-04CRYAA, CRYAB
protein refolding265.7×0.006CRYAA, CRYAB
response to hydrogen peroxide249.3×0.010CRYAA, CRYAB
response to heat244.4×0.011CRYAA, CRYAB
microtubule polymerization or depolymerization1887.0×0.012CRYAB
notochord cell development1887.0×0.012EPHA2
axial mesoderm formation1443.5×0.020EPHA2
negative regulation of ATF6-mediated unfolded protein response1443.5×0.020WFS1
protein stabilization310.6×0.022WFS1, CRYAA, CRYAB
notochord formation1295.6×0.024EPHA2
negative regulation of lymphangiogenesis1295.6×0.024EPHA2
positive regulation of growth1221.7×0.028WFS1
cAMP metabolic process1221.7×0.028EPHA2
response to UV-A1221.7×0.028CRYAA
pericyte cell differentiation1177.4×0.032EPHA2
muscle organ development217.6×0.032UNC45B, CRYAB
regulation of programmed cell death1147.8×0.033CRYAB
regulation of blood vessel endothelial cell migration1147.8×0.033EPHA2
plus-end-directed vesicle transport along microtubule1147.8×0.033FYCO1
blood vessel endothelial cell proliferation involved in sprouting angiogenesis1126.7×0.035EPHA2
positive regulation of autophagosome maturation1126.7×0.035FYCO1
negative regulation of response to endoplasmic reticulum stress1126.7×0.035WFS1
negative regulation of chemokine production1110.9×0.035EPHA2
maintenance of lens transparency1110.9×0.035MIP

Therapeutics

Drug target analysis

Approved (phase 4): 1 · Phase ≥3: 1 · Phased (≥1): 1 · Undrugged: 18

Druggability breadth: 8 of 19 evidence-associated genes (42%) 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
BFSP100
WFS100
UNC45B00
FYCO100
CRYAA00
CRYAB00
CRYBA100
CRYBA200
CRYBB100

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): 1.

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

SymbolAssaysType breakdown
EPHA2567Binding:565, Functional:1, ADMET:1
CRYAA25Binding:25
CRYAB13Binding:13
CRYBB29Binding:9
CRYGC9Binding:9
CRYGD9Binding:9
TNPO17Binding:7
WFS11Binding:1

Cohort enzymes (BRENDA EC)

SymbolEC numbersNames
EPHA22.7.10.1receptor protein-tyrosine kinase

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: 19; 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 drug0
DDruggable family + AlphaFold only, no drug0
EDifficult family or no structure, no drug18BFSP1, WFS1, UNC45B, FYCO1, CRYAA, CRYAB, CRYBA1, CRYBA2, CRYBB1, CRYBB2 (+8 more)

Undrugged target profiles

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

SymbolChEMBL assaysDrugged partners (top 3)
BFSP10
WFS11
UNC45B0
FYCO10
CRYAA25
CRYAB13
CRYBA10
CRYBA20
CRYBB10
CRYBB29
CRYBB30
CRYGC9
CRYGD9
GJA30
GJA80
TNPO17
MIP0
NHS0

Clinical trials & evidence

Clinical trials

Clinical trials: 0.