46,XY partial gonadal dysgenesis

disease
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Also known as 46,XY partial testicular dysgenesis46,XY PGD

Summary

46,XY partial gonadal dysgenesis (MONDO:0016674) is a disease (an umbrella term covering 7 Mondo subtypes) with 11 cohort genes. The dominant Reactome pathway is Transcriptional regulation of testis differentiation (5 cohort genes).

At a glance

  • Prevalence: Unknown (Worldwide)
  • Umbrella term: 7 Mondo subtypes
  • Cohort genes: 11
  • ClinVar variants: 4
  • Phenotypes (HPO): 43

Clinical features

Signs & symptoms

Clinical features (HPO)

43 HPO clinical features (Orphanet curated; top 43 by frequency):

HPO IDTermFrequency
HP:0003251Male infertilityVery frequent (80-99%)
HP:0008214Decreased serum estradiolVery frequent (80-99%)
HP:0008232Elevated circulating follicle stimulating hormone levelVery frequent (80-99%)
HP:0008665Clitoral hypertrophyVery frequent (80-99%)
HP:0008726Hypoplasia of the vaginaVery frequent (80-99%)
HP:0008730Female external genitalia in individual with 46,XY karyotypeVery frequent (80-99%)
HP:0008734Decreased testicular sizeVery frequent (80-99%)
HP:0008736Hypoplasia of penisVery frequent (80-99%)
HP:0010464Streak ovaryVery frequent (80-99%)
HP:0011969Elevated circulating luteinizing hormone levelVery frequent (80-99%)
HP:0012244Abnormal sex determinationVery frequent (80-99%)
HP:0012870Vanishing testisVery frequent (80-99%)
HP:0040171Decreased serum testosterone concentrationVery frequent (80-99%)
HP:0100779Urogenital sinus anomalyVery frequent (80-99%)
HP:0000027AzoospermiaVery frequent (80-99%)
HP:0000045Abnormality of the scrotumVery frequent (80-99%)
HP:0000047HypospadiasVery frequent (80-99%)
HP:0000054MicropenisVery frequent (80-99%)
HP:0000058Abnormality of the labiaVery frequent (80-99%)
HP:0000062Ambiguous genitaliaVery frequent (80-99%)
HP:0000133Gonadal dysgenesisVery frequent (80-99%)
HP:0000142Abnormality of the vaginaVery frequent (80-99%)
HP:0000771GynecomastiaVery frequent (80-99%)
HP:0000786Primary amenorrheaVery frequent (80-99%)
HP:0000812Abnormal internal genitaliaVery frequent (80-99%)
HP:0000815Hypergonadotropic hypogonadismVery frequent (80-99%)
HP:0000837Increased circulating gonadotropin levelVery frequent (80-99%)
HP:0000868Decreased fertility in femalesVery frequent (80-99%)
HP:0000939OsteoporosisVery frequent (80-99%)
HP:0002215Sparse axillary hairVery frequent (80-99%)
HP:0002225Sparse pubic hairVery frequent (80-99%)
HP:0000028CryptorchidismFrequent (30-79%)
HP:0000150GonadoblastomaFrequent (30-79%)
HP:0000823Delayed pubertyFrequent (30-79%)
HP:0000030Testicular gonadoblastomaOccasional (5-29%)
HP:0000149Ovarian gonadoblastomaOccasional (5-29%)
HP:0000846Adrenal insufficiencyOccasional (5-29%)
HP:0002750Delayed skeletal maturationOccasional (5-29%)
HP:0008187Absence of secondary sex characteristicsOccasional (5-29%)
HP:0008193Primary gonadal insufficiencyOccasional (5-29%)
HP:0000100Nephrotic syndromeVery rare (<1-4%)
HP:0002667NephroblastomaVery rare (<1-4%)
HP:0030680Abnormal cardiovascular system morphologyVery rare (<1-4%)

Identifiers

Disease identifiers

FieldValue
Canonical name46,XY partial gonadal dysgenesis
Mondo IDMONDO:0016674
Orphanet251510
SNOMED CT725045004
UMLSC4510744
MedGen1388250
GARD0017211
Is cancer (heuristic)no

Also known as: 46,XY partial testicular dysgenesis · 46,XY PGD

Data availability: 4 ClinVar variants · 8 GenCC gene-disease records.

Disease family

An umbrella term covering 7 Mondo subtypes.

Classification path: disease › human disease › disease by body system or component › reproductive system disordergonadal disorderdisorder of sexual differentiation46 XY differences of sex development46,XY partial gonadal dysgenesis

Related subtypes (23): Frasier syndrome, WAGR syndrome, Denys-Drash syndrome, familial adrenal hypoplasia with absent pituitary luteinizing hormone, PAGOD syndrome, XY type gonadal dysgenesis-associated anomalies syndrome, 46,XY disorder of sex development due to 17-beta-hydroxysteroid dehydrogenase 3 deficiency, 46,XY disorder of sex development due to 5-alpha-reductase 2 deficiency, X-linked myotubular myopathy-abnormal genitalia syndrome, alpha thalassemia-X-linked intellectual disability syndrome, chondrodysplasia-pseudohermaphroditism syndrome, disorder of sex development-intellectual disability syndrome, 46,XY gonadal dysgenesis-motor and sensory neuropathy syndrome, sudden infant death-dysgenesis of the testes syndrome, Meacham syndrome, Congenital adrenal insufficiency with 46, XY sex reversal OR 46,XY disorder of sex development-adrenal insufficiency due to CYP11A1 deficiency, distal monosomy 9p, dysmorphism-short stature-deafness-disorder of sex development syndrome, testicular agenesis, 46,XY ovotesticular disorder of sex development, penile agenesis, androgen insensitivity syndrome, male pseudohermaphroditism due to defective lh molecule

Subtypes (7): 46,XY sex reversal 4, 46,XY sex reversal 2, 46,XY sex reversal 3, 46,XY sex reversal 6, testicular anomalies with or without congenital heart disease, 46,XY sex reversal 9, 46,XY sex reversal 10

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

4 retrieved; paginated sample, class counts are floors:

1 pathogenic, 1 likely pathogenic, 1 conflicting classifications of pathogenicity, 1 pathogenic/likely pathogenic

ClinVarVariant (HGVS)GeneClassificationReview
1691445NM_004959.5(NR5A1):c.991-1G>CNR5A1Pathogeniccriteria provided, single submitter
8098NM_006261.5(PROP1):c.301_302del (p.Leu102fs)PROP1Pathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
1691446NM_005633.4(SOS1):c.406T>C (p.Tyr136His)SOS1Likely pathogeniccriteria provided, single submitter
803030NM_021728.4(OTX2):c.425C>G (p.Pro142Arg)OTX2Conflicting classifications of pathogenicitycriteria provided, conflicting classifications

Genes & proteins

Mendelian disease overlap and somatic drivers

GenCC: 83 · Orphanet: 49 · 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
DHX37SupportiveAutosomal dominant46,XY complete gonadal dysgenesis9
GATA4SupportiveAutosomal dominant46,XY partial gonadal dysgenesis15
MAP3K1SupportiveAutosomal dominant46,XY complete gonadal dysgenesis7
NR5A1SupportiveAutosomal dominant46,XY complete gonadal dysgenesis12
SOX9SupportiveAutosomal dominant46,XY complete gonadal dysgenesis13
SRYSupportiveAutosomal dominant46,XY complete gonadal dysgenesis8
WWOXSupportiveAutosomal dominant46,XY partial gonadal dysgenesis11
ZFPM2SupportiveAutosomal dominant46,XY partial gonadal dysgenesis8

Orphanet rare-disease linkage (cohort genes)

GeneOrphanet IDRare disease
NR5A1Orphanet:213846,XX ovotesticular difference of sex development
NR5A1Orphanet:24246,XY complete gonadal dysgenesis
NR5A1Orphanet:24346,XX gonadal dysgenesis
NR5A1Orphanet:25151046,XY partial gonadal dysgenesis
NR5A1Orphanet:39346,XX testicular difference of sex development
NR5A1Orphanet:399805Male infertility with azoospermia or oligozoospermia due to single gene mutation
SOX9Orphanet:140Campomelic dysplasia
SOX9Orphanet:213846,XX ovotesticular difference of sex development
SOX9Orphanet:24246,XY complete gonadal dysgenesis
SOX9Orphanet:25151046,XY partial gonadal dysgenesis
SOX9Orphanet:39346,XX testicular difference of sex development
SOX9Orphanet:718Isolated Pierre Robin sequence
SRYOrphanet:177245,X/46,XY mixed gonadal dysgenesis
SRYOrphanet:213846,XX ovotesticular difference of sex development
SRYOrphanet:24246,XY complete gonadal dysgenesis
SRYOrphanet:25151046,XY partial gonadal dysgenesis
SRYOrphanet:39346,XX testicular difference of sex development
WWOXOrphanet:25151046,XY partial gonadal dysgenesis
WWOXOrphanet:284282Autosomal recessive cerebellar ataxia-epilepsy-intellectual disability syndrome due to WWOX deficiency
WWOXOrphanet:708171Facial dysmorphism-corpus callosum hypoplasia-infantile epileptic encephalopathy
WWOXOrphanet:99977Squamous cell carcinoma of the esophagus
ZFPM2Orphanet:2140Congenital diaphragmatic hernia
ZFPM2Orphanet:25151046,XY partial gonadal dysgenesis
ZFPM2Orphanet:3303Tetralogy of Fallot
DHX37Orphanet:24246,XY complete gonadal dysgenesis
DHX37Orphanet:25151046,XY partial gonadal dysgenesis
DHX37Orphanet:983Testicular regression syndrome
GATA4Orphanet:2510718p23.1 microdeletion syndrome
GATA4Orphanet:25151046,XY partial gonadal dysgenesis
GATA4Orphanet:3303Tetralogy of Fallot
GATA4Orphanet:334Hereditary atrial fibrillation
GATA4Orphanet:576232Partial atrioventricular septal defect with ventricular hypoplasia
GATA4Orphanet:99067Complete atrioventricular septal defect with ventricular hypoplasia
GATA4Orphanet:99068Complete atrioventricular septal defect-tetralogy of Fallot
GATA4Orphanet:99103Atrial septal defect, ostium secundum type
MAP3K1Orphanet:24246,XY complete gonadal dysgenesis
MAP3K1Orphanet:25151046,XY partial gonadal dysgenesis
SOS1Orphanet:2024Hereditary gingival fibromatosis
SOS1Orphanet:648Noonan syndrome
OTX2Orphanet:178364Syndromic microphthalmia type 5
OTX2Orphanet:3157Septo-optic dysplasia spectrum
OTX2Orphanet:35612Nanophthalmos
OTX2Orphanet:95494Combined pituitary hormone deficiencies, genetic forms
OTX2Orphanet:98938Colobomatous microphthalmia
OTX2Orphanet:990Agnathia-holoprosencephaly-situs inversus syndrome
OTX2Orphanet:99001Butterfly-shaped pigment dystrophy
PROP1Orphanet:226307Hypothyroidism due to deficient transcription factors involved in pituitary development or function
PROP1Orphanet:90695Non-acquired panhypopituitarism
PROP1Orphanet:95494Combined pituitary hormone deficiencies, genetic forms

Cohort genes → proteins

11 cohort genes, 11 distinct canonical proteins.

Evidence partition

SubsetGenes
multi_evidence11

Cohort genes (full)

SymbolHGNCEnsemblUniProtNameEvidence
NR5A1HGNC:7983ENSG00000136931Q13285Steroidogenic factor 1gencc,clinvar
SOX9HGNC:11204ENSG00000125398P48436Transcription factor SOX-9gencc
SRYHGNC:11311ENSG00000184895Q05066Sex-determining region Y proteingencc
WWOXHGNC:12799ENSG00000186153Q9NZC7WW domain-containing oxidoreductasegencc
ZFPM2HGNC:16700ENSG00000169946Q8WW38Zinc finger protein ZFPM2gencc
DHX37HGNC:17210ENSG00000150990Q8IY37Probable ATP-dependent RNA helicase DHX37gencc
GATA4HGNC:4173ENSG00000136574P43694Transcription factor GATA-4gencc
MAP3K1HGNC:6848ENSG00000095015Q13233Mitogen-activated protein kinase kinase kinase 1gencc
SOS1HGNC:11187ENSG00000115904Q07889Son of sevenless homolog 1clinvar
OTX2HGNC:8522ENSG00000165588P32243Homeobox protein OTX2clinvar
PROP1HGNC:9455ENSG00000175325O75360Homeobox protein prophet of Pit-1clinvar

Cohort function summary

Lead sentence per gene, UniProt-curated.

SymbolProtein nameFunction (lead sentence)
NR5A1Steroidogenic factor 1Transcriptional activator.
SOX9Transcription factor SOX-9Transcription factor that plays a key role in chondrocytes differentiation and skeletal development.
SRYSex-determining region Y proteinTranscriptional regulator that controls a genetic switch in male development.
WWOXWW domain-containing oxidoreductasePutative oxidoreductase.
ZFPM2Zinc finger protein ZFPM2Transcription regulator that plays a central role in heart morphogenesis and development of coronary vessels from epicardium, by regulating genes that are essential during cardiogenesis.
DHX37Probable ATP-dependent RNA helicase DHX37ATP-binding RNA helicase that plays a role in maturation of the small ribosomal subunit in ribosome biogenesis.
GATA4Transcription factor GATA-4Transcriptional activator that binds to the consensus sequence 5’-AGATAG-3’ and plays a key role in cardiac development and function.
MAP3K1Mitogen-activated protein kinase kinase kinase 1Component of a protein kinase signal transduction cascade.
SOS1Son of sevenless homolog 1Promotes the exchange of Ras-bound GDP by GTP.
OTX2Homeobox protein OTX2Transcription factor probably involved in the development of the brain and the sense organs.
PROP1Homeobox protein prophet of Pit-1Possibly involved in the ontogenesis of pituitary gonadotropes, as well as somatotropes, lactotropes and caudomedial thyrotropes.

Protein-family classification

Druggable: 2 · Difficult: 8 · Unknown: 1 · Druggable fraction: 0.18

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
Transcription factor64.5×0.004
Nuclear receptor135.1×0.070
Scaffold/PPI23.1×0.217
Kinase12.5×0.416
Other/Unknown10.2×1.000

Per-gene assignment

SymbolFamilyDruggable?ECInterPro (top 3)
NR5A1Nuclear receptoryesNucl_hrmn_rcpt_lig-bd, Znf_hrmn_rcpt, Nuclear_hrmn_rcpt
SOX9Transcription factornoHMG_box_dom, Sox_N, HMG_box_dom_sf
SRYTranscription factornoHMG_box_dom, SRY, HMG_box_dom_sf
WWOXScaffold/PPInoWW_dom, SDR_fam, WW_dom_sf
ZFPM2Transcription factornoZnf_C2H2_type, Znf_CCHC_FOG, Znf_C2H2_sf
DHX37Other/UnknownnoHelicase_C-like, Helicase-assoc_dom, DEAD/DEAH_box_helicase_dom
GATA4Transcription factornoZnf_GATA, GATA_N, Znf_NHR/GATA
MAP3K1Kinaseyes2.7.11.25Prot_kinase_dom, Znf_RING, Znf_SWIM
SOS1Scaffold/PPInoDH_dom, Ras-like_Gua-exchang_fac_N, PH_domain
OTX2Transcription factornoHD, Otx2_TF, Otx_TF
PROP1Transcription factornoHTH_motif, HD, Homeodomain-like_sf

Expression context

Cohort genes with no expression data: 0.

7 cohort genes are a single-cell marker in ≥1 SCXA experiment.

Breadth distribution (Bgee present_calls)

BucketGenes
narrow (1-5 tissues)1
moderate (6-20)0
broad (>20)10
unknown0

Top tissues across cohort

TissueCohort genes
tendon of biceps brachii3
cranial nerve II2
left adrenal gland1
right adrenal gland1
right adrenal gland cortex1
hair follicle1
ventricular zone1
primordial germ cell in gonad1
right testis1
cervix squamous epithelium1
parotid gland1
biceps brachii1
germinal epithelium of ovary1
skeletal muscle tissue of biceps brachii1
medial globus pallidus1
pancreatic ductal cell1
duodenum1
heart left ventricle1
right atrium auricular region1
buccal mucosa cell1

Per-gene tissue summary (top 30)

SymbolBgee breadthFANTOM5 breadthSCXATop tissues
NR5A177tissue_specificyesright adrenal gland cortex, right adrenal gland, left adrenal gland
SOX9274ubiquitousmarkerventricular zone, cranial nerve II, hair follicle
SRY66tissue_specificyesprimordial germ cell in gonad, tendon of biceps brachii, right testis
WWOX286ubiquitousmarkerparotid gland, cervix squamous epithelium, cranial nerve II
ZFPM2239ubiquitousmarkerskeletal muscle tissue of biceps brachii, germinal epithelium of ovary, biceps brachii
DHX37236ubiquitousyespancreatic ductal cell, tendon of biceps brachii, medial globus pallidus
GATA485broadmarkerright atrium auricular region, heart left ventricle, duodenum
MAP3K1264ubiquitousmarkerbuccal mucosa cell, upper leg skin, skin of hip
SOS1289ubiquitousmarkercolonic epithelium, jejunal mucosa, tendon of biceps brachii
OTX262broadmarkersecondary oocyte, oocyte, pigmented layer of retina
PROP14yespituitary gland, adenohypophysis, bone marrow cell

Protein interactions among cohort

Intra-cohort edges: 4.

Hub genes (top 10 by interactor count)

SymbolInteractor count
WWOX5,892
GATA44,994
SOX94,935
MAP3K14,414
SOS13,625
DHX373,123
SRY2,835
OTX22,368
NR5A12,146
ZFPM21,437

Intra-cohort edges

ABSources
GATA4NR5A1biogrid_interaction
GATA4ZFPM2biogrid_interaction, string_interaction
NR5A1SOX9biogrid_interaction, string_interaction
NR5A1SRYstring_interaction

Structural data

PDB: 8 · AlphaFold-only: 3 · No structure: 0

Cohort genes with PDB structures (top 30)

SymbolUniProtPDB entries
SOS1Q0788991
SRYQ0506610
NR5A1Q132856
GATA4P436943
SOX9P484361
WWOXQ9NZC71
DHX37Q8IY371
MAP3K1Q132331

AlphaFold-only cohort genes (top 30 by pLDDT)

SymbolUniProtpLDDT
PROP1O7536070.74
OTX2P3224360.99
ZFPM2Q8WW3851.93

Function

Pathway analysis

Distinct Reactome pathways touched by cohort: 183. Enrichment computed across 11 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
Transcriptional regulation of testis differentiation5356.9×1e-10NR5A1, SOX9, SRY, ZFPM2, GATA4
Developmental Lineage of Multipotent Pancreatic Progenitor Cells2120.2×0.011SOX9, GATA4
FCERI mediated MAPK activation269.2×0.021SOS1, MAP3K1
Developmental Lineage of Pancreatic Acinar Cells260.1×0.021SOX9, GATA4
Fc epsilon receptor (FCERI) signaling254.4×0.021SOS1, MAP3K1
Deactivation of the beta-catenin transactivating complex246.6×0.022SOX9, SRY
Developmental Lineage of Pancreatic Ductal Cells245.7×0.022SOX9, GATA4
Downstream signaling of activated FGFR21571.0×0.036SOS1
Downstream signaling of activated FGFR31571.0×0.036SOS1
Downstream signaling of activated FGFR41380.7×0.040SOS1
Signaling by ERBB2 in Cancer1228.4×0.040SOS1
Signaling by EGFRvIII in Cancer1228.4×0.040SOS1
Formation of lateral plate mesoderm1228.4×0.040GATA4
Signaling by Ligand-Responsive EGFR Variants in Cancer1190.3×0.040SOS1
Signaling by NTRK2 (TRKB)1163.1×0.040SOS1
Signaling by PDGFR in disease1163.1×0.040SOS1
SOS-mediated signalling1142.8×0.040SOS1
IGF1R signaling cascade1142.8×0.040SOS1
Activated NTRK3 signals through RAS1126.9×0.040SOS1
Signaling by EGFR in Cancer1114.2×0.040SOS1
EGFR Transactivation by Gastrin1114.2×0.040SOS1
SHC-related events triggered by IGF1R1114.2×0.040SOS1
Signaling by FGFR31114.2×0.040SOS1
Negative regulation of activity of TFAP2 (AP-2) family transcription factors1114.2×0.040WWOX
Activated NTRK2 signals through RAS1114.2×0.040SOS1
Signaling by NTRK3 (TRKC)1114.2×0.040SOS1
Signaling by KIT in disease1114.2×0.040SOS1
FLT3 signaling in disease1114.2×0.040SOS1
Formation of the posterior neural plate1114.2×0.040OTX2
IRS-mediated signalling1103.8×0.040SOS1

GO biological processes by enrichment

Over-representation of cohort genes vs the genome-wide background (hypergeometric test, Benjamini-Hochberg FDR; fold = observed/expected over 11 annotated cohort genes). Counts and members are kept as ground-truth; sorted by enrichment.

GO termCohort genesFoldFDRSample cohort genes
positive regulation of male gonad development5766.0×3e-12NR5A1, SOX9, SRY, ZFPM2, DHX37
negative regulation of female gonad development2766.0×2e-04NR5A1, ZFPM2
positive regulation of transcription by RNA polymerase II79.5×2e-04NR5A1, SOX9, SRY, WWOX, ZFPM2, GATA4, OTX2
Sertoli cell differentiation2278.6×0.001NR5A1, SOX9
intestinal epithelial cell differentiation2278.6×0.001SOX9, GATA4
male sex determination2255.3×0.001NR5A1, SRY
male gonad development342.6×0.001NR5A1, SOX9, GATA4
Fc-epsilon receptor signaling pathway2133.2×0.003SOS1, MAP3K1
aortic valve morphogenesis278.6×0.008SOX9, GATA4
hair follicle development269.6×0.009SOS1, SOX9
positive regulation of DNA-templated transcription410.2×0.010SOX9, SRY, GATA4, OTX2
negative regulation of immune system process1766.0×0.014SOX9
right ventricular cardiac muscle tissue morphogenesis1766.0×0.014ZFPM2
atrial septum secundum morphogenesis1766.0×0.014GATA4
primary sex determination1766.0×0.014NR5A1
hypophysis morphogenesis1766.0×0.014PROP1
epithelial cell proliferation involved in prostatic bud elongation1766.0×0.014SOX9
regulation of cell proliferation involved in tissue homeostasis1766.0×0.014SOX9
regulation of branching involved in lung morphogenesis1766.0×0.014SOX9
cell proliferation involved in heart morphogenesis1766.0×0.014SOX9
regulation of epithelial cell proliferation involved in lung morphogenesis1766.0×0.014SOX9
cellular response to transforming growth factor beta stimulus250.2×0.014SOX9, WWOX
epidermal growth factor receptor signaling pathway245.1×0.014SOS1, SOX9
cellular response to mechanical stimulus239.3×0.014SOX9, MAP3K1
heart valve formation1510.7×0.014SOX9
neural crest cell fate specification1510.7×0.014SOX9
male germ-line sex determination1510.7×0.014SOX9
embryonic heart tube anterior/posterior pattern specification1510.7×0.014GATA4
intrahepatic bile duct development1510.7×0.014SOX9
bronchus cartilage development1510.7×0.014SOX9

Therapeutics

Drug target analysis

Approved (phase 4): 2 · Phase ≥3: 2 · Phased (≥1): 2 · Undrugged: 9

Druggability breadth: 5 of 11 evidence-associated genes (45%) 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
MAP3K1PONATINIB
SOS1IDARUBICIN

Top cohort targets by molecule count

SymbolMoleculesMax phase
MAP3K1314
SOS154
NR5A100
SOX900
SRY00
WWOX00
ZFPM200
DHX3700
GATA400
OTX200

Drugs targeting cohort genes (top 30)

MoleculeMax phaseTargets in cohort
PONATINIB4MAP3K1
SORAFENIB4MAP3K1
RUXOLITINIB4MAP3K1
REGORAFENIB4MAP3K1
BARICITINIB4MAP3K1
BOSUTINIB4MAP3K1
TOVORAFENIB4MAP3K1
RIBOCICLIB4MAP3K1
PAZOPANIB4MAP3K1
DASATINIB4MAP3K1
ERLOTINIB4MAP3K1
CRIZOTINIB4MAP3K1
IDARUBICIN4SOS1
DOXORUBICIN4SOS1
SOTORASIB4SOS1
ADAGRASIB4SOS1
ICOTINIB3MAP3K1
TESEVATINIB3MAP3K1
LESTAURTINIB3MAP3K1
TG100-1152MAP3K1
SCH-9007762MAP3K1
OSI-6322MAP3K1
GOLVATINIB2MAP3K1
RG-5472MAP3K1
DANUSERTIB2MAP3K1
AT-92832MAP3K1
PELITINIB2MAP3K1
GSK-4613641MAP3K1
KW-24491MAP3K1
AV-412 FREE BASE1MAP3K1

Bioactivity and enzyme data

Enzyme cohort genes (≥1 EC): 1.

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

SymbolAssaysType breakdown
SOS1421Binding:409, Functional:12
MAP3K1167Binding:165, ADMET:1, Functional:1
NR5A188Binding:84, Functional:4
GATA45Binding:5
SOX93Binding:3

Cohort enzymes (BRENDA EC)

SymbolEC numbersNames
MAP3K12.7.11.25mitogen-activated protein kinase kinase kinase

Cohort genes with high screening signal

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

SymbolChEMBL assays
MAP3K1167
SOS1421

Pharmacogenomics

Cohort genes with a PharmGKB record: 11; 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)
PONATINIB4MAP3K1
SORAFENIB4MAP3K1
RUXOLITINIB4MAP3K1
REGORAFENIB4MAP3K1
BARICITINIB4MAP3K1
BOSUTINIB4MAP3K1
TOVORAFENIB4MAP3K1
RIBOCICLIB4MAP3K1
PAZOPANIB4MAP3K1
DASATINIB4MAP3K1
ERLOTINIB4MAP3K1
CRIZOTINIB4MAP3K1
IDARUBICIN4SOS1
DOXORUBICIN4SOS1
SOTORASIB4SOS1
ADAGRASIB4SOS1
ICOTINIB3MAP3K1
TESEVATINIB3MAP3K1
LESTAURTINIB3MAP3K1
TG100-1152MAP3K1
SCH-9007762MAP3K1
OSI-6322MAP3K1
GOLVATINIB2MAP3K1
RG-5472MAP3K1
DANUSERTIB2MAP3K1
AT-92832MAP3K1
PELITINIB2MAP3K1
GSK-4613641MAP3K1
KW-24491MAP3K1
AV-412 FREE BASE1MAP3K1

Druggability pyramid

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

TierDefinitionGenesSymbols
AApproved (phase 4 drug)2MAP3K1, SOS1
BPhased (≥1) drug, not yet approved0
CDruggable family + PDB, no drug1NR5A1
DDruggable family + AlphaFold only, no drug0
EDifficult family or no structure, no drug8SOX9, SRY, WWOX, ZFPM2, DHX37, GATA4, OTX2, PROP1

Undrugged target profiles

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

SymbolChEMBL assaysDrugged partners (top 3)
NR5A188
SOX93
SRY0
WWOX0
ZFPM20
DHX370
GATA45
OTX20
PROP10

Clinical trials & evidence

Clinical trials

Clinical trials: 0.