Noonan syndrome and Noonan-related syndrome

disease
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Summary

Noonan syndrome and Noonan-related syndrome (MONDO:0020297) is a disease (an umbrella term covering 6 Mondo subtypes) caused by RRAS (GenCC Strong), with 19 cohort genes. The dominant Reactome pathway is RAF activation (8 cohort genes).

At a glance

  • Causal gene: RRAS (GenCC Strong)
  • Umbrella term: 6 Mondo subtypes
  • Cohort genes: 19
  • ClinVar variants: 557

Clinical features

No curated clinical features (Orphanet) for this disease.

Identifiers

Disease identifiers

FieldValue
Canonical nameNoonan syndrome and Noonan-related syndrome
Mondo IDMONDO:0020297
MeSHC537846
Orphanet98733
UMLSC5681679
MedGen1826127
GARD0019561
Is cancer (heuristic)no

Data availability: 557 ClinVar variants · 1 GenCC gene-disease record.

Disease family

An umbrella term covering 6 Mondo subtypes.

Classification path: disease › human disease › disease by etiologic mechanism › disease of genetic or genomic mechanism › hereditary diseaseRASopathyNoonan syndrome and Noonan-related syndrome

Related subtypes (3): neurofibromatosis-Noonan syndrome, CBL-related disorder, neurofibromatosis type 1

Subtypes (6): Noonan syndrome with multiple lentigines, Costello syndrome, Noonan syndrome-like disorder with loose anagen hair, Legius syndrome, cardiofaciocutaneous syndrome, Noonan syndrome

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

557 retrieved; paginated sample, class counts are floors:

119 conflicting classifications of pathogenicity, 103 benign, 98 uncertain significance, 76 benign/likely benign, 68 pathogenic, 39 likely benign, 35 pathogenic/likely pathogenic, 19 likely pathogenic

ClinVarVariant (HGVS)GeneClassificationReview
13969NM_004333.6(BRAF):c.1789C>G (p.Leu597Val)BRAFPathogeniccriteria provided, multiple submitters, no conflicts
13973NM_004333.6(BRAF):c.770A>G (p.Gln257Arg)BRAFPathogenicreviewed by expert panel
13974NM_004333.6(BRAF):c.1406G>A (p.Gly469Glu)BRAFPathogenicreviewed by expert panel
13976NM_004333.6(BRAF):c.1495A>G (p.Lys499Glu)BRAFPathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
177775NM_004333.6(BRAF):c.1405G>A (p.Gly469Arg)BRAFPathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
180784NM_004333.6(BRAF):c.739T>C (p.Phe247Leu)BRAFPathogenicreviewed by expert panel
40347NM_004333.6(BRAF):c.735A>C (p.Leu245Phe)BRAFPathogenicreviewed by expert panel
40348NM_004333.6(BRAF):c.735A>T (p.Leu245Phe)BRAFPathogenicreviewed by expert panel
40364NM_004333.6(BRAF):c.1391G>T (p.Gly464Val)BRAFPathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
40366NM_004333.6(BRAF):c.1403T>C (p.Phe468Ser)BRAFPathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
40383NM_004333.6(BRAF):c.1695T>G (p.Asp565Glu)BRAFPathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
55793NM_004333.6(BRAF):c.741T>G (p.Phe247Leu)BRAFPathogenicreviewed by expert panel
13807NM_005188.4(CBL):c.1100A>C (p.Gln367Pro)CBLPathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
12602NM_005343.4(HRAS):c.34G>A (p.Gly12Ser)HRASPathogenicreviewed by expert panel
12603NM_005343.4(HRAS):c.35G>C (p.Gly12Ala)HRASPathogeniccriteria provided, multiple submitters, no conflicts
12604NM_005343.4(HRAS):c.38G>A (p.Gly13Asp)HRASPathogeniccriteria provided, multiple submitters, no conflicts
12606NM_005343.4(HRAS):c.37G>T (p.Gly13Cys)HRASPathogenicreviewed by expert panel
12612NM_005343.4(HRAS):c.35G>A (p.Gly12Asp)HRASPathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
35554NM_005343.4(HRAS):c.37G>C (p.Gly13Arg)HRASPathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
12580NM_004985.5(KRAS):c.38G>A (p.Gly13Asp)KRASPathogeniccriteria provided, multiple submitters, no conflicts
12589NM_004985.5(KRAS):c.40G>A (p.Val14Ile)KRASPathogenicreviewed by expert panel
101038NM_006767.4(LZTR1):c.1397G>A (p.Arg466Gln)LZTR1Pathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
373089NM_006767.4(LZTR1):c.1234C>T (p.Arg412Cys)LZTR1Pathogenicreviewed by expert panel
40744NM_002755.4(MAP2K1):c.371C>T (p.Pro124Leu)MAP2K1Pathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
44588NM_002755.4(MAP2K1):c.275T>G (p.Leu92Arg)MAP2K1Pathogenicreviewed by expert panel
8274NM_030662.4(MAP2K2):c.400T>C (p.Tyr134His)MAP2K2Pathogenicreviewed by expert panel
1070042NM_002524.5(NRAS):c.173C>T (p.Thr58Ile)NRASPathogenicreviewed by expert panel
177778NM_002524.5(NRAS):c.34G>A (p.Gly12Ser)NRASPathogenicreviewed by expert panel
219097NM_002524.5(NRAS):c.35G>C (p.Gly12Ala)NRASPathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
39648NM_002524.5(NRAS):c.35G>A (p.Gly12Asp)NRASPathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts

Genes & proteins

Mendelian disease overlap and somatic drivers

GenCC: 4 · Orphanet: 65 · 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
RRASStrongAutosomal dominantNoonan syndrome and Noonan-related syndrome4

Orphanet rare-disease linkage (cohort genes)

GeneOrphanet IDRare disease
RRASOrphanet:648Noonan syndrome
RRASOrphanet:86834Juvenile myelomonocytic leukemia
RIT1Orphanet:648Noonan syndrome
BRAFOrphanet:1340Cardiofaciocutaneous syndrome
BRAFOrphanet:146Differentiated thyroid carcinoma
BRAFOrphanet:251615Pilomyxoid astrocytoma
BRAFOrphanet:389Langerhans cell histiocytosis
BRAFOrphanet:500Noonan syndrome with multiple lentigines
BRAFOrphanet:54595Craniopharyngioma
BRAFOrphanet:58017Classic hairy cell leukemia
BRAFOrphanet:626Large/giant congenital melanocytic nevus
BRAFOrphanet:648Noonan syndrome
BRAFOrphanet:840Syringocystadenoma papilliferum
BRAFOrphanet:96253Cushing disease
SOS1Orphanet:2024Hereditary gingival fibromatosis
SOS1Orphanet:648Noonan syndrome
SOS2Orphanet:648Noonan syndrome
CBLOrphanet:363972Noonan syndrome-like disorder with juvenile myelomonocytic leukemia
CBLOrphanet:648Noonan syndrome
CBLOrphanet:86834Juvenile myelomonocytic leukemia
CBLOrphanet:98850Aggressive systemic mastocytosis
SHOC2Orphanet:2701Noonan syndrome-like disorder with loose anagen hair
SPRED1Orphanet:137605Legius syndrome
LRRC56Orphanet:244Primary ciliary dyskinesia
HRASOrphanet:146Differentiated thyroid carcinoma
HRASOrphanet:2612Linear nevus sebaceus syndrome
HRASOrphanet:2874Phakomatosis pigmentokeratotica
HRASOrphanet:3071Costello syndrome
HRASOrphanet:79414Woolly hair nevus
KRASOrphanet:1333Familial pancreatic carcinoma
KRASOrphanet:1340Cardiofaciocutaneous syndrome
KRASOrphanet:144Lynch syndrome
KRASOrphanet:146Differentiated thyroid carcinoma
KRASOrphanet:2396Encephalocraniocutaneous lipomatosis
KRASOrphanet:251615Pilomyxoid astrocytoma
KRASOrphanet:2612Linear nevus sebaceus syndrome
KRASOrphanet:268114RAS-associated autoimmune leukoproliferative disease
KRASOrphanet:3339Oculoectodermal syndrome
KRASOrphanet:648Noonan syndrome
KRASOrphanet:86834Juvenile myelomonocytic leukemia
LZTR1Orphanet:251576Gliosarcoma
LZTR1Orphanet:251579Giant cell glioblastoma
LZTR1Orphanet:2678Familial isolated café-au-lait macules
LZTR1Orphanet:648Noonan syndrome
LZTR1Orphanet:93921Full schwannomatosis
MAP2K1Orphanet:1340Cardiofaciocutaneous syndrome
MAP2K1Orphanet:389Langerhans cell histiocytosis
MAP2K2Orphanet:1340Cardiofaciocutaneous syndrome
MAP2K2Orphanet:638Neurofibromatosis-Noonan syndrome
NRASOrphanet:146Differentiated thyroid carcinoma

Cohort genes → proteins

19 cohort genes, 18 distinct canonical proteins.

Evidence partition

SubsetGenes
multi_evidence19

Cohort genes (full)

SymbolHGNCEnsemblUniProtNameEvidence
RRASHGNC:10447ENSG00000126458P10301Ras-related protein R-Rasgencc
RIT1HGNC:10023ENSG00000143622Q92963GTP-binding protein Rit1clinvar
BRAFHGNC:1097ENSG00000157764P15056Serine/threonine-protein kinase B-rafclinvar
SOS1HGNC:11187ENSG00000115904Q07889Son of sevenless homolog 1clinvar
SOS2HGNC:11188ENSG00000100485Q07890Son of sevenless homolog 2clinvar
CBLHGNC:1541ENSG00000110395P22681E3 ubiquitin-protein ligase CBLclinvar
SHOC2HGNC:15454ENSG00000108061Q9UQ13Leucine-rich repeat protein SHOC-2clinvar
SPRED1HGNC:20249ENSG00000166068Q7Z699Sprouty-related, EVH1 domain-containing protein 1clinvar
LRRC56HGNC:25430ENSG00000161328Q8IYG6Leucine-rich repeat-containing protein 56clinvar
FRA11BHGNC:3837fragile site, folic acid type, rare, fra(11)(q23.3)clinvar
HRASHGNC:5173ENSG00000174775P01112GTPase HRasclinvar
KRASHGNC:6407ENSG00000133703P01116GTPase KRasclinvar
LZTR1HGNC:6742ENSG00000099949Q8N653Leucine-zipper-like transcriptional regulator 1clinvar
MAP2K1HGNC:6840ENSG00000169032Q02750Dual specificity mitogen-activated protein kinase kinase 1clinvar
MAP2K2HGNC:6842ENSG00000126934P36507Dual specificity mitogen-activated protein kinase kinase 2clinvar
MKRN2HGNC:7113ENSG00000075975Q9H000E3 ubiquitin-protein ligase makorin-2clinvar
NRASHGNC:7989ENSG00000213281P01111GTPase NRasclinvar
PTPN11HGNC:9644ENSG00000179295Q06124Tyrosine-protein phosphatase non-receptor type 11clinvar
RAF1HGNC:9829ENSG00000132155P04049RAF proto-oncogene serine/threonine-protein kinaseclinvar

Cohort function summary

Lead sentence per gene, UniProt-curated.

SymbolProtein nameFunction (lead sentence)
RRASRas-related protein R-RasGTP-binding protein with GTPase activity, likely involved in the regulation of MAPK signaling pathway and thereby controlling multiple cellular processes.
RIT1GTP-binding protein Rit1Plays a crucial role in coupling NGF stimulation to the activation of both EPHB2 and MAPK14 signaling pathways and in NGF-dependent neuronal differentiation.
BRAFSerine/threonine-protein kinase B-rafProtein kinase involved in the transduction of mitogenic signals from the cell membrane to the nucleus.
SOS1Son of sevenless homolog 1Promotes the exchange of Ras-bound GDP by GTP.
SOS2Son of sevenless homolog 2Acts as guanine nucleotide exchange factor (GEF) for RAS proteins.
CBLE3 ubiquitin-protein ligase CBLE3 ubiquitin-protein ligase that acts as a negative regulator of many signaling pathways by mediating ubiquitination of cell surface receptors.
SHOC2Leucine-rich repeat protein SHOC-2Core component of the SHOC2-MRAS-PP1c (SMP) holophosphatase complex that regulates activation of the MAPK pathway.
SPRED1Sprouty-related, EVH1 domain-containing protein 1Tyrosine kinase substrate that inhibits growth-factor-mediated activation of MAP kinase.
LRRC56Leucine-rich repeat-containing protein 56Required for the assembly of dynein arms.
HRASGTPase HRasInvolved in the activation of Ras protein signal transduction.
KRASGTPase KRasRas proteins bind GDP/GTP and possess intrinsic GTPase activity.
LZTR1Leucine-zipper-like transcriptional regulator 1Substrate-specific adapter of a BCR (BTB-CUL3-RBX1) E3 ubiquitin-protein ligase complex that mediates ubiquitination of Ras (K-Ras/KRAS, N-Ras/NRAS and H-Ras/HRAS).
MAP2K1Dual specificity mitogen-activated protein kinase kinase 1Dual specificity protein kinase which acts as an essential component of the MAP kinase signal transduction pathway.
MAP2K2Dual specificity mitogen-activated protein kinase kinase 2Catalyzes the concomitant phosphorylation of a threonine and a tyrosine residue in a Thr-Glu-Tyr sequence located in MAP kinases.
MKRN2E3 ubiquitin-protein ligase makorin-2E3 ubiquitin ligase catalyzing the covalent attachment of ubiquitin moieties onto substrate proteins.
NRASGTPase NRasRas proteins bind GDP/GTP and possess intrinsic GTPase activity.
PTPN11Tyrosine-protein phosphatase non-receptor type 11Acts downstream of various receptor and cytoplasmic protein tyrosine kinases to participate in the signal transduction from the cell surface to the nucleus.
RAF1RAF proto-oncogene serine/threonine-protein kinaseSerine/threonine-protein kinase that acts as a regulatory link between the membrane-associated Ras GTPases and the MAPK/ERK cascade, and this critical regulatory link functions as a switch determining cell fate decisions including prolifer…

Protein-family classification

Druggable: 7 · Difficult: 4 · Unknown: 8 · Druggable fraction: 0.37

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
Kinase45.8×0.025
Phosphatase14.4×0.603
Scaffold/PPI21.8×0.603
Enzyme (other)21.3×0.718
Transcription factor20.9×0.827
Other/Unknown80.8×0.924

Per-gene assignment

SymbolFamilyDruggable?ECInterPro (top 3)
RRASOther/UnknownnoSmall_GTPase, Small_GTP-bd, Small_GTPase_Ras-type
RIT1Other/UnknownnoSmall_GTPase, Small_GTP-bd, Small_GTPase_Ras-type
BRAFKinaseyes2.7.10.2Prot_kinase_dom, Ser-Thr/Tyr_kinase_cat_dom, PKC_DAG/PE
SOS1Scaffold/PPInoDH_dom, Ras-like_Gua-exchang_fac_N, PH_domain
SOS2Scaffold/PPInoDH_dom, Ras-like_Gua-exchang_fac_N, PH_domain
CBLTranscription factorno2.3.2.27Znf_RING, Adaptor_Cbl_N_hlx, UBA-like_sf
SHOC2Other/UnknownnoLeu-rich_rpt, Leu-rich_rpt_typical-subtyp, LRR_dom_sf
SPRED1Other/UnknownnoWH1/EVH1_dom, Sprouty, PH-like_dom_sf
LRRC56Other/UnknownnoLeu-rich_rpt, Leu-rich_rpt_4, LRR_dom_sf
FRA11BOther/Unknownno
HRASEnzyme (other)yes3.6.5.2Small_GTPase, Small_GTP-bd, Small_GTPase_Ras-type
KRASEnzyme (other)yes3.6.5.2Small_GTPase, Small_GTP-bd, Small_GTPase_Ras-type
LZTR1Other/UnknownnoBTB/POZ_dom, Kelch_1, SKP1/BTB/POZ_sf
MAP2K1Kinaseyes2.7.12.2Prot_kinase_dom, Ser/Thr_kinase_AS, Kinase-like_dom_sf
MAP2K2Kinaseyes2.7.12.2Prot_kinase_dom, Ser/Thr_kinase_AS, Kinase-like_dom_sf
MKRN2Transcription factornoZnf_CCCH, Znf_RING, Znf_RING/FYVE/PHD
NRASOther/UnknownnoSmall_GTPase, Small_GTP-bd, Small_GTPase_Ras-type
PTPN11Phosphataseyes3.1.3.48PTP_cat, Tyr_Pase_dom, SH2
RAF1Kinaseyes2.7.10.2Prot_kinase_dom, Ser-Thr/Tyr_kinase_cat_dom, PKC_DAG/PE

Expression context

Cohort genes with no expression data: 1.

18 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)18
unknown1

Top tissues across cohort

TissueCohort genes
calcaneal tendon3
left testis3
secondary oocyte3
buccal mucosa cell2
colonic epithelium2
trigeminal ganglion2
sural nerve2
ventricular zone2
right testis2
popliteal artery1
right coronary artery1
tibial artery1
leukocyte1
monocyte1
mononuclear cell1
jejunal mucosa1
tendon of biceps brachii1
biceps brachii1
vastus lateralis1
male germ line stem cell (sensu Vertebrata) in testis1

Per-gene tissue summary (top 30)

SymbolBgee breadthFANTOM5 breadthSCXATop tissues
RRAS242ubiquitousmarkerright coronary artery, popliteal artery, tibial artery
RIT1268ubiquitousmarkermonocyte, mononuclear cell, leukocyte
BRAF265ubiquitousmarkerbuccal mucosa cell, colonic epithelium, calcaneal tendon
SOS1289ubiquitousmarkercolonic epithelium, jejunal mucosa, tendon of biceps brachii
SOS2298ubiquitousmarkervastus lateralis, biceps brachii, buccal mucosa cell
CBL271ubiquitousmarkerprimordial germ cell in gonad, trigeminal ganglion, male germ line stem cell (sensu Vertebrata) in testis
SHOC2299ubiquitousmarkercalcaneal tendon, sural nerve, bone marrow
SPRED1248ubiquitousmarkerventricular zone, mucosa of sigmoid colon, calcaneal tendon
LRRC56129broadmarkerright uterine tube, right testis, left testis
FRA11B
HRAS139ubiquitousmarkerskin of abdomen, skin of leg, zone of skin
KRAS298ubiquitousmarkertrigeminal ganglion, pylorus, nipple
LZTR1134ubiquitousmarkersural nerve, pituitary gland, adenohypophysis
MAP2K1298ubiquitousmarkersecondary oocyte, oocyte, orbitofrontal cortex
MAP2K2291ubiquitousmarkermucosa of transverse colon, right testis, left testis
MKRN2270ubiquitousmarkersecondary oocyte, left testis, sperm
NRAS278ubiquitousmarkergingival epithelium, epithelium of nasopharynx, secondary oocyte
PTPN11295ubiquitousmarkermedial globus pallidus, dorsal motor nucleus of vagus nerve, globus pallidus
RAF1299ubiquitousmarkergastrocnemius, muscle of leg, ventricular zone

Protein interactions among cohort

Intra-cohort edges: 58.

Hub genes (top 10 by interactor count)

SymbolInteractor count
KRAS14,509
HRAS8,064
NRAS7,598
BRAF7,394
RAF16,574
PTPN116,009
MAP2K15,944
CBL4,575
MAP2K23,789
SOS13,625

Intra-cohort edges

ABSources
BRAFHRASintact, string_interaction
BRAFKRASbiogrid_interaction, intact, string_interaction
BRAFMAP2K1biogrid_interaction, intact, string_interaction
BRAFMAP2K2biogrid_interaction, intact, string_interaction
BRAFNRASbiogrid_interaction, intact, string_interaction
BRAFRAF1biogrid_interaction, intact, string_interaction
BRAFSHOC2string_interaction
BRAFSOS1string_interaction
BRAFSPRED1string_interaction
HRASLZTR1biogrid_interaction
HRASMAP2K1string_interaction
HRASMAP2K2string_interaction
HRASRAF1intact, string_interaction
HRASSHOC2intact, string_interaction
HRASSOS1intact, string_interaction
HRASSOS2string_interaction
KRASLZTR1string_interaction
KRASMAP2K1biogrid_interaction, string_interaction
KRASMAP2K2string_interaction
KRASNRASintact
KRASRAF1intact, string_interaction
KRASSHOC2intact, string_interaction
KRASSOS1string_interaction
KRASSOS2string_interaction
KRASSPRED1string_interaction
LZTR1NRASbiogrid_interaction, intact, string_interaction
LZTR1RIT1biogrid_interaction, intact, string_interaction
LZTR1SHOC2string_interaction
LZTR1SOS1string_interaction
LZTR1SOS2string_interaction
MAP2K1MAP2K2biogrid_interaction, intact, string_interaction
MAP2K1NRASstring_interaction
MAP2K1PTPN11biogrid_interaction, string_interaction
MAP2K1RAF1biogrid_interaction, intact, string_interaction
MAP2K1SHOC2string_interaction
MAP2K2NRASintact, string_interaction
MAP2K2PTPN11string_interaction
MAP2K2RAF1biogrid_interaction, intact
MAP2K2SHOC2string_interaction
MAP2K2SOS1string_interaction
MAP2K2SPRED1string_interaction
MKRN2RAF1string_interaction
NRASPTPN11string_interaction
NRASRAF1biogrid_interaction, intact, string_interaction
NRASSHOC2biogrid_interaction, intact, string_interaction
NRASSOS1string_interaction
NRASSPRED1string_interaction
PTPN11SHOC2string_interaction
PTPN11SOS1biogrid_interaction, string_interaction
PTPN11SOS2string_interaction

Structural data

PDB: 16 · AlphaFold-only: 2 · No structure: 1

Cohort genes with PDB structures (top 30)

SymbolUniProtPDB entries
KRASP01116511
HRASP01112246
BRAFP15056131
PTPN11Q06124115
MAP2K1Q0275094
SOS1Q0788991
RAF1P0404976
NRASP0111135
CBLP2268133
SHOC2Q9UQ1313
SOS2Q0789011
RIT1Q929633
SPRED1Q7Z6993
LZTR1Q8N6533
MAP2K2P365073
RRASP103012

AlphaFold-only cohort genes (top 30 by pLDDT)

SymbolUniProtpLDDT
MKRN2Q9H00071.78
LRRC56Q8IYG656.07

Function

Pathway analysis

Distinct Reactome pathways touched by cohort: 262. Enrichment computed across 19 evidence-associated genes (15 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 15 annotated cohort genes). Counts and members are kept as ground-truth; sorted by enrichment.

PathwayCohort genesFoldFDRSample cohort genes
RAF activation8179.1×4e-15BRAF, SHOC2, HRAS, KRAS, MAP2K1, MAP2K2, NRAS, RAF1
Signaling by high-kinase activity BRAF mutants7148.0×1e-12BRAF, HRAS, KRAS, MAP2K1, MAP2K2, NRAS, RAF1
MAP2K and MAPK activation7133.2×2e-12BRAF, HRAS, KRAS, MAP2K1, MAP2K2, NRAS, RAF1
Signaling by RAF1 mutants7130.0×2e-12BRAF, HRAS, KRAS, MAP2K1, MAP2K2, NRAS, RAF1
Negative regulation of MAPK pathway7123.9×2e-12BRAF, HRAS, KRAS, MAP2K1, MAP2K2, NRAS, RAF1
Signaling by moderate kinase activity BRAF mutants7118.4×2e-12BRAF, HRAS, KRAS, MAP2K1, MAP2K2, NRAS, RAF1
Paradoxical activation of RAF signaling by kinase inactive BRAF7118.4×2e-12BRAF, HRAS, KRAS, MAP2K1, MAP2K2, NRAS, RAF1
Signaling downstream of RAS mutants7118.4×2e-12BRAF, HRAS, KRAS, MAP2K1, MAP2K2, NRAS, RAF1
RAF/MAP kinase cascade936.6×9e-12BRAF, SOS1, SHOC2, SPRED1, HRAS, KRAS, MAP2K1, MAP2K2 (+1 more)
Signaling by BRAF and RAF1 fusions779.5×3e-11BRAF, HRAS, KRAS, MAP2K1, MAP2K2, NRAS, RAF1
Activated NTRK2 signals through FRS2 and FRS35317.2×3e-11SOS1, HRAS, KRAS, NRAS, PTPN11
FLT3 Signaling6138.4×4e-11SOS1, CBL, HRAS, KRAS, NRAS, PTPN11
Signaling by FLT3 ITD and TKD mutants5253.8×1e-10SOS1, HRAS, KRAS, NRAS, PTPN11
Constitutive Signaling by EGFRvIII5237.9×2e-10SOS1, CBL, HRAS, KRAS, NRAS
Signaling by SCF-KIT699.3×3e-10SOS1, CBL, HRAS, KRAS, NRAS, PTPN11
Tie2 Signaling5200.3×3e-10SOS1, HRAS, KRAS, NRAS, PTPN11
Negative feedback regulation of MAPK pathway4507.6×4e-10BRAF, MAP2K1, MAP2K2, RAF1
Constitutive Signaling by Ligand-Responsive EGFR Cancer Variants5190.3×4e-10SOS1, CBL, HRAS, KRAS, NRAS
FRS-mediated FGFR3 signaling5181.3×5e-10SOS1, HRAS, KRAS, NRAS, PTPN11
FRS-mediated FGFR4 signaling5165.5×8e-10SOS1, HRAS, KRAS, NRAS, PTPN11
RAS signaling downstream of NF1 loss-of-function variants4435.1×8e-10SPRED1, HRAS, KRAS, NRAS
FRS-mediated FGFR1 signaling5152.3×1e-09SOS1, HRAS, KRAS, NRAS, PTPN11
FRS-mediated FGFR2 signaling5146.4×1e-09SOS1, HRAS, KRAS, NRAS, PTPN11
SOS-mediated signalling4380.7×1e-09SOS1, HRAS, KRAS, NRAS
Activated NTRK3 signals through RAS4338.4×3e-09SOS1, HRAS, KRAS, NRAS
Downstream signal transduction5126.9×3e-09SOS1, HRAS, KRAS, NRAS, PTPN11
EGFR Transactivation by Gastrin4304.5×4e-09SOS1, HRAS, KRAS, NRAS
SHC-related events triggered by IGF1R4304.5×4e-09SOS1, HRAS, KRAS, NRAS
Activated NTRK2 signals through RAS4304.5×4e-09SOS1, HRAS, KRAS, NRAS
MET activates RAS signaling4276.9×6e-09SOS1, HRAS, KRAS, NRAS

GO biological processes by enrichment

Over-representation of cohort genes vs the genome-wide background (hypergeometric test, Benjamini-Hochberg FDR; fold = observed/expected over 18 annotated cohort genes). Counts and members are kept as ground-truth; sorted by enrichment.

GO termCohort genesFoldFDRSample cohort genes
Ras protein signal transduction779.9×4e-10RIT1, RRAS, SOS1, SOS2, HRAS, KRAS, NRAS
Schwann cell development5292.6×5e-10SOS1, HRAS, MAP2K1, MAP2K2, RAF1
MAPK cascade759.6×1e-09BRAF, HRAS, KRAS, MAP2K1, MAP2K2, NRAS, RAF1
face development4178.3×4e-07BRAF, MAP2K1, MAP2K2, RAF1
myelination569.9×4e-07SOS1, HRAS, MAP2K1, MAP2K2, RAF1
thyroid gland development4120.8×1e-06BRAF, MAP2K1, MAP2K2, RAF1
insulin-like growth factor receptor signaling pathway4110.1×2e-06SOS1, MAP2K1, MAP2K2, RAF1
ERBB2-ERBB3 signaling pathway3280.9×4e-06MAP2K1, MAP2K2, RAF1
thymus development474.9×6e-06BRAF, MAP2K1, MAP2K2, RAF1
neurotrophin TRK receptor signaling pathway3175.5×2e-05SOS1, PTPN11, RAF1
insulin receptor signaling pathway449.3×3e-05SOS1, SOS2, HRAS, RAF1
cerebellar cortex formation2624.1×8e-05MAP2K1, PTPN11
positive regulation of axonogenesis396.8×8e-05BRAF, MAP2K1, MAP2K2
regulation of Golgi inheritance2468.1×1e-04MAP2K1, MAP2K2
cytokine-mediated signaling pathway429.0×2e-04SOS1, CBL, KRAS, PTPN11
epithelial cell proliferation involved in lung morphogenesis2374.5×2e-04MAP2K1, MAP2K2
regulation of pro-B cell differentiation2374.5×2e-04SOS1, SOS2
regulation of T cell differentiation in thymus2267.5×3e-04SOS1, SOS2
regulation of axon regeneration2267.5×3e-04MAP2K1, MAP2K2
trachea formation2267.5×3e-04MAP2K1, MAP2K2
ERK1 and ERK2 cascade353.0×3e-04BRAF, MAP2K1, MAP2K2
regulation of early endosome to late endosome transport2234.1×4e-04MAP2K1, MAP2K2
fibroblast growth factor receptor signaling pathway347.6×4e-04SOS1, SHOC2, PTPN11
regulation of stress-activated MAPK cascade2208.1×5e-04MAP2K1, MAP2K2
epidermal growth factor receptor signaling pathway341.3×5e-04BRAF, SOS1, PTPN11
positive regulation of ERK1 and ERK2 cascade418.9×5e-04BRAF, HRAS, MAP2K1, PTPN11
Bergmann glial cell differentiation2170.2×6e-04MAP2K1, PTPN11
positive regulation of protein serine/threonine kinase activity2144.0×8e-04MAP2K1, MAP2K2
regulation of T cell proliferation2117.0×0.001SOS1, SOS2
regulation of long-term neuronal synaptic plasticity2110.1×0.001HRAS, KRAS

Therapeutics

Drug target analysis

Approved (phase 4): 9 · Phase ≥3: 9 · Phased (≥1): 10 · Undrugged: 9

Druggability breadth: 11 of 19 evidence-associated genes (58%) 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
BRAFVEMURAFENIB
SOS1IDARUBICIN
SOS2TACRINE
HRASLONAFARNIB
KRASVEMURAFENIB
MAP2K1VEMURAFENIB
MAP2K2VEMURAFENIB
PTPN11ESTRAMUSTINE PHOSPHATE
RAF1VEMURAFENIB

Top cohort targets by molecule count

SymbolMoleculesMax phase
MAP2K1544
MAP2K2524
BRAF484
RAF1314
KRAS114
PTPN1184
SOS154
HRAS44
SOS214
NRAS11

Drugs targeting cohort genes (top 30)

MoleculeMax phaseTargets in cohort
VEMURAFENIB4BRAF, KRAS, MAP2K1, MAP2K2, RAF1
PONATINIB4BRAF
FEDRATINIB4BRAF, MAP2K1, MAP2K2
SORAFENIB4BRAF, MAP2K1, RAF1
DASATINIB ANHYDROUS4BRAF
RUXOLITINIB4BRAF, MAP2K1, MAP2K2
INFIGRATINIB PHOSPHATE4BRAF
INFIGRATINIB4BRAF
REGORAFENIB4BRAF, RAF1
DABRAFENIB4BRAF, KRAS, RAF1
COBIMETINIB4BRAF, MAP2K1, MAP2K2
NILOTINIB4BRAF, RAF1
ABEMACICLIB4BRAF
ENCORAFENIB4BRAF
TOVORAFENIB4BRAF, RAF1
PAZOPANIB4BRAF, RAF1
DASATINIB4BRAF, MAP2K1, MAP2K2, RAF1
ERLOTINIB4BRAF, RAF1
GEFITINIB4BRAF
IMATINIB4BRAF, RAF1
IDARUBICIN4SOS1
DOXORUBICIN4SOS1
SOTORASIB4KRAS, SOS1
ADAGRASIB4KRAS, SOS1
TACRINE4SOS2
LONAFARNIB4HRAS, KRAS
SELUMETINIB4MAP2K1, MAP2K2
TRAMETINIB4MAP2K1, MAP2K2
BINIMETINIB4MAP2K1, MAP2K2
AXITINIB4MAP2K1, MAP2K2

Bioactivity and enzyme data

Enzyme cohort genes (≥1 EC): 8.

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

SymbolAssaysType breakdown
BRAF1,442Binding:1400, Functional:37, ADMET:5
MAP2K11,200Binding:1150, Functional:47, ADMET:3
KRAS861Binding:829, Functional:32
RAF1839Binding:803, Functional:31, ADMET:5
MAP2K2615Binding:581, Functional:33, ADMET:1
PTPN11588Binding:585, Functional:2, ADMET:1
SOS1421Binding:409, Functional:12
HRAS48Binding:45, Functional:3
NRAS18Binding:18
SOS210Binding:10
CBL4Binding:2, Toxicity:2

Cohort enzymes (BRENDA EC)

SymbolEC numbersNames
BRAF2.7.10.2, 2.7.11.1non-specific protein-tyrosine kinase, non-specific serine/threonine protein kinase
CBL2.3.2.27RING-type E3 ubiquitin transferase
HRAS3.6.5.2small monomeric GTPase
KRAS3.6.5.2small monomeric GTPase
MAP2K12.7.12.2mitogen-activated protein kinase kinase
MAP2K22.7.12.2mitogen-activated protein kinase kinase
PTPN113.1.3.48protein-tyrosine-phosphatase
RAF12.7.10.2non-specific protein-tyrosine kinase

Cohort genes with high screening signal

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

SymbolChEMBL assays
BRAF1,442
SOS1421
KRAS861
MAP2K11,200
MAP2K2615
PTPN11588
RAF1839

Pharmacogenomics

Cohort genes with a PharmGKB record: 18; 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)
VEMURAFENIB4BRAF, KRAS, MAP2K1, MAP2K2, RAF1
PONATINIB4BRAF
FEDRATINIB4BRAF, MAP2K1, MAP2K2
SORAFENIB4BRAF, MAP2K1, RAF1
DASATINIB ANHYDROUS4BRAF
RUXOLITINIB4BRAF, MAP2K1, MAP2K2
INFIGRATINIB PHOSPHATE4BRAF
INFIGRATINIB4BRAF
REGORAFENIB4BRAF, RAF1
DABRAFENIB4BRAF, KRAS, RAF1
COBIMETINIB4BRAF, MAP2K1, MAP2K2
NILOTINIB4BRAF, RAF1
ABEMACICLIB4BRAF
ENCORAFENIB4BRAF
TOVORAFENIB4BRAF, RAF1
PAZOPANIB4BRAF, RAF1
DASATINIB4BRAF, MAP2K1, MAP2K2, RAF1
ERLOTINIB4BRAF, RAF1
GEFITINIB4BRAF
IMATINIB4BRAF, RAF1
IDARUBICIN4SOS1
DOXORUBICIN4SOS1
SOTORASIB4KRAS, SOS1
ADAGRASIB4KRAS, SOS1
TACRINE4SOS2
LONAFARNIB4HRAS, KRAS
SELUMETINIB4MAP2K1, MAP2K2
TRAMETINIB4MAP2K1, MAP2K2
BINIMETINIB4MAP2K1, MAP2K2
AXITINIB4MAP2K1, MAP2K2

Druggability pyramid

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

TierDefinitionGenesSymbols
AApproved (phase 4 drug)9BRAF, SOS1, SOS2, HRAS, KRAS, MAP2K1, MAP2K2, PTPN11, RAF1
BPhased (≥1) drug, not yet approved1NRAS
CDruggable family + PDB, no drug0
DDruggable family + AlphaFold only, no drug0
EDifficult family or no structure, no drug9RRAS, RIT1, CBL, SHOC2, SPRED1, LRRC56, FRA11B, LZTR1, MKRN2

Undrugged target profiles

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

SymbolChEMBL assaysDrugged partners (top 3)
SHOC20SOS1, NRAS
SPRED10RAF1
RRAS0
RIT10
CBL4
LRRC560
FRA11B0
LZTR10
MKRN20

Clinical trials & evidence

Clinical trials

Clinical trials: 0.