Noonan syndrome 3

disease
On this page

Also known as KRAS gene related Noonan syndromeKRAS Noonan syndromeNoonan syndrome caused by mutation in KRASNoonan syndrome type 3NS3

Summary

Noonan syndrome 3 (MONDO:0012371) is a disease caused by KRAS (GenCC Definitive), with 7 cohort genes. The dominant Reactome pathway is Activated NTRK2 signals through FRS2 and FRS3 (4 cohort genes).

At a glance

  • Causal gene: KRAS (GenCC Definitive)
  • Cohort genes: 7
  • ClinVar variants: 74

Clinical features

No curated clinical features (Orphanet) for this disease.

Identifiers

Disease identifiers

FieldValue
Canonical nameNoonan syndrome 3
Mondo IDMONDO:0012371
MeSHC537847
OMIM609942
DOIDDOID:0060581
NCITC176931
UMLSC1860991
MedGen349931
GARD0009885
Is cancer (heuristic)no

Also known as: KRAS gene related Noonan syndrome · KRAS Noonan syndrome · Noonan syndrome 3 · Noonan syndrome caused by mutation in KRAS · Noonan syndrome type 3 · NS3

Data availability: 74 ClinVar variants · 5 GenCC gene-disease records.

Disease family

Classification path: disease › human disease › disease by body system or component › syndromic diseaseNoonan syndromeNoonan syndrome 3

Related subtypes (13): Noonan syndrome 1, Noonan syndrome 2, Noonan syndrome 4, Noonan syndrome 5, Noonan syndrome 6, Noonan syndrome 7, Noonan syndrome 8, Noonan syndrome 9, Noonan syndrome 10, Noonan syndrome 14, Noonan syndrome 11, noonan syndrome 12, Noonan syndrome 13

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

74 retrieved; paginated sample, class counts are floors:

23 pathogenic, 15 uncertain significance, 11 pathogenic/likely pathogenic, 10 conflicting classifications of pathogenicity, 8 likely pathogenic, 4 likely benign, 2 benign/likely benign, 1 benign

ClinVarVariant (HGVS)GeneClassificationReview
984634NM_004859.4(CLTC):c.1912_1916delinsAGA (p.Ala639fs)CLTCPathogenicno assertion criteria provided
12601NM_005343.4(HRAS):c.181C>A (p.Gln61Lys)HRASPathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
12582NM_004985.5(KRAS):c.35G>A (p.Gly12Asp)KRASPathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
12586NM_004985.5(KRAS):c.178G>C (p.Gly60Arg)KRASPathogenicreviewed by expert panel
12587NM_004985.5(KRAS):c.458A>T (p.Asp153Val)KRASPathogenicreviewed by expert panel
12588NM_004985.5(KRAS):c.173C>T (p.Thr58Ile)KRASPathogenicreviewed by expert panel
12589NM_004985.5(KRAS):c.40G>A (p.Val14Ile)KRASPathogenicreviewed by expert panel
12590NM_004985.5(KRAS):c.101C>G (p.Pro34Arg)KRASPathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
12591NM_033360.4(KRAS):c.*9T>GKRASPathogenicno assertion criteria provided
12596NM_004985.5(KRAS):c.13A>G (p.Lys5Glu)KRASPathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
12597NM_033360.4(KRAS):c.178G>A (p.Gly60Ser)KRASPathogeniccriteria provided, multiple submitters, no conflicts
163758NM_004985.5(KRAS):c.466T>A (p.Phe156Ile)KRASPathogeniccriteria provided, multiple submitters, no conflicts
1695421NM_004985.5(KRAS):c.53C>T (p.Ala18Val)KRASPathogeniccriteria provided, single submitter
1695422NM_004985.5(KRAS):c.194_195insGGCAATGAGGGACCAGTACAG (p.Tyr64_Ser65insArgAlaMetArgAspGlnTyr)KRASPathogeniccriteria provided, single submitter
40452NM_004985.5(KRAS):c.65A>G (p.Gln22Arg)KRASPathogenicreviewed by expert panel
40454NM_004985.5(KRAS):c.101C>T (p.Pro34Leu)KRASPathogenicreviewed by expert panel
431103NM_033360.4(KRAS):c.440A>G (p.Lys147Arg)KRASPathogeniccriteria provided, single submitter
45122NM_004985.5(KRAS):c.35G>C (p.Gly12Ala)KRASPathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
637030NM_004985.5(KRAS):c.451-5642A>TKRASPathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
13327NM_002834.5(PTPN11):c.923A>G (p.Asn308Ser)PTPN11Pathogeniccriteria provided, multiple submitters, no conflicts
13333NM_002834.5(PTPN11):c.188A>G (p.Tyr63Cys)PTPN11Pathogenicreviewed by expert panel
13344NM_002834.5(PTPN11):c.1529A>C (p.Gln510Pro)PTPN11Pathogenicreviewed by expert panel
164997NM_002834.5(PTPN11):c.206A>T (p.Glu69Val)PTPN11Pathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
40488NM_002834.5(PTPN11):c.174C>A (p.Asn58Lys)PTPN11Pathogeniccriteria provided, multiple submitters, no conflicts
40494NM_002834.5(PTPN11):c.181G>C (p.Asp61His)PTPN11Pathogeniccriteria provided, multiple submitters, no conflicts
40499NM_002834.5(PTPN11):c.211T>C (p.Phe71Leu)PTPN11Pathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
40507NM_002834.5(PTPN11):c.328G>A (p.Glu110Lys)PTPN11Pathogenic/Likely pathogeniccriteria provided, multiple submitters, no conflicts
40513NM_002834.5(PTPN11):c.417G>C (p.Glu139Asp)PTPN11Pathogenicreviewed by expert panel
40528NM_002834.5(PTPN11):c.853T>C (p.Phe285Leu)PTPN11Pathogeniccriteria provided, multiple submitters, no conflicts
40566NM_002834.5(PTPN11):c.1528C>G (p.Gln510Glu)PTPN11Pathogeniccriteria provided, multiple submitters, no conflicts

Genes & proteins

Mendelian disease overlap and somatic drivers

GenCC: 17 · Orphanet: 32 · OMIM-shared: 0 · Dual-evidence (GWAS+Mendelian): 0

GenCC gene–disease validity (cohort genes)

the Disease column is the GenCC-asserted condition — a cohort gene’s strongest validity may be for a related predisposition syndrome.

GeneClassificationInheritanceDiseaseRecords
KRASDefinitiveAutosomal dominantNoonan syndrome 317

Orphanet rare-disease linkage (cohort genes)

GeneOrphanet IDRare disease
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
SOS1Orphanet:2024Hereditary gingival fibromatosis
SOS1Orphanet:648Noonan syndrome
SHOC2Orphanet:2701Noonan syndrome-like disorder with loose anagen hair
CLTCOrphanet:178342Inflammatory myofibroblastic tumor
CLTCOrphanet:178469Autosomal dominant non-syndromic intellectual disability
CLTCOrphanet:319308MiT family translocation renal cell carcinoma
CLTCOrphanet:442835Non-specific early-onset epileptic encephalopathy
HRASOrphanet:146Differentiated thyroid carcinoma
HRASOrphanet:2612Linear nevus sebaceus syndrome
HRASOrphanet:2874Phakomatosis pigmentokeratotica
HRASOrphanet:3071Costello syndrome
HRASOrphanet:79414Woolly hair nevus
PTPN11Orphanet:2499Metachondromatosis
PTPN11Orphanet:500Noonan syndrome with multiple lentigines
PTPN11Orphanet:648Noonan syndrome
PTPN11Orphanet:86834Juvenile myelomonocytic leukemia
RAF1Orphanet:154Familial isolated dilated cardiomyopathy
RAF1Orphanet:251615Pilomyxoid astrocytoma
RAF1Orphanet:500Noonan syndrome with multiple lentigines
RAF1Orphanet:626Large/giant congenital melanocytic nevus
RAF1Orphanet:648Noonan syndrome

Cohort genes → proteins

7 cohort genes, 7 distinct canonical proteins.

Evidence partition

SubsetGenes
multi_evidence7

Cohort genes (full)

SymbolHGNCEnsemblUniProtNameEvidence
KRASHGNC:6407ENSG00000133703P01116GTPase KRasgencc,clinvar
SOS1HGNC:11187ENSG00000115904Q07889Son of sevenless homolog 1clinvar
SHOC2HGNC:15454ENSG00000108061Q9UQ13Leucine-rich repeat protein SHOC-2clinvar
CLTCHGNC:2092ENSG00000141367Q00610Clathrin heavy chain 1clinvar
HRASHGNC:5173ENSG00000174775P01112GTPase HRasclinvar
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)
KRASGTPase KRasRas proteins bind GDP/GTP and possess intrinsic GTPase activity.
SOS1Son of sevenless homolog 1Promotes the exchange of Ras-bound GDP by GTP.
SHOC2Leucine-rich repeat protein SHOC-2Core component of the SHOC2-MRAS-PP1c (SMP) holophosphatase complex that regulates activation of the MAPK pathway.
CLTCClathrin heavy chain 1Clathrin is the major protein of the polyhedral coat of coated pits and vesicles.
HRASGTPase HRasInvolved in the activation of Ras protein signal transduction.
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: 4 · Difficult: 1 · Unknown: 2 · Druggable fraction: 0.57

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
Phosphatase112.0×0.275
Enzyme (other)23.4×0.275
Kinase14.0×0.378
Scaffold/PPI12.5×0.426
Other/Unknown20.5×0.968

Per-gene assignment

SymbolFamilyDruggable?ECInterPro (top 3)
KRASEnzyme (other)yes3.6.5.2Small_GTPase, Small_GTP-bd, Small_GTPase_Ras-type
SOS1Scaffold/PPInoDH_dom, Ras-like_Gua-exchang_fac_N, PH_domain
SHOC2Other/UnknownnoLeu-rich_rpt, Leu-rich_rpt_typical-subtyp, LRR_dom_sf
CLTCOther/UnknownnoClathrin_H-chain/VPS_repeat, TPR-like_helical_dom_sf, Clathrin_H-chain_linker_core
HRASEnzyme (other)yes3.6.5.2Small_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: 0.

7 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)7
unknown0

Top tissues across cohort

TissueCohort genes
nipple1
pylorus1
trigeminal ganglion1
colonic epithelium1
jejunal mucosa1
tendon of biceps brachii1
bone marrow1
calcaneal tendon1
sural nerve1
Brodmann (1909) area 461
lateral nuclear group of thalamus1
pons1
skin of abdomen1
skin of leg1
zone of skin1
dorsal motor nucleus of vagus nerve1
globus pallidus1
medial globus pallidus1
gastrocnemius1
muscle of leg1

Per-gene tissue summary (top 30)

SymbolBgee breadthFANTOM5 breadthSCXATop tissues
KRAS298ubiquitousmarkertrigeminal ganglion, pylorus, nipple
SOS1289ubiquitousmarkercolonic epithelium, jejunal mucosa, tendon of biceps brachii
SHOC2299ubiquitousmarkercalcaneal tendon, sural nerve, bone marrow
CLTC305ubiquitousmarkerpons, lateral nuclear group of thalamus, Brodmann (1909) area 46
HRAS139ubiquitousmarkerskin of abdomen, skin of leg, zone of skin
PTPN11295ubiquitousmarkermedial globus pallidus, dorsal motor nucleus of vagus nerve, globus pallidus
RAF1299ubiquitousmarkergastrocnemius, muscle of leg, ventricular zone

Protein interactions among cohort

Intra-cohort edges: 11.

Hub genes (top 10 by interactor count)

SymbolInteractor count
KRAS14,509
HRAS8,064
RAF16,574
PTPN116,009
CLTC5,550
SOS13,625
SHOC22,149

Intra-cohort edges

ABSources
HRASRAF1intact, string_interaction
HRASSHOC2intact, string_interaction
HRASSOS1intact, string_interaction
KRASRAF1intact, string_interaction
KRASSHOC2intact, string_interaction
KRASSOS1string_interaction
PTPN11SHOC2string_interaction
PTPN11SOS1biogrid_interaction, string_interaction
RAF1SHOC2biogrid_interaction
RAF1SOS1string_interaction
SHOC2SOS1string_interaction

Structural data

PDB: 7 · AlphaFold-only: 0 · No structure: 0

Cohort genes with PDB structures (top 30)

SymbolUniProtPDB entries
KRASP01116511
HRASP01112246
PTPN11Q06124115
SOS1Q0788991
RAF1P0404976
SHOC2Q9UQ1313
CLTCQ0061010

Function

Pathway analysis

Distinct Reactome pathways touched by cohort: 224. Enrichment computed across 7 evidence-associated genes (7 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 7 annotated cohort genes). Counts and members are kept as ground-truth; sorted by enrichment.

PathwayCohort genesFoldFDRSample cohort genes
Activated NTRK2 signals through FRS2 and FRS34543.8×5e-09KRAS, SOS1, HRAS, PTPN11
Signaling by FLT3 ITD and TKD mutants4435.1×8e-09KRAS, SOS1, HRAS, PTPN11
Tie2 Signaling4343.5×1e-08KRAS, SOS1, HRAS, PTPN11
FRS-mediated FGFR3 signaling4310.8×2e-08KRAS, SOS1, HRAS, PTPN11
FRS-mediated FGFR4 signaling4283.7×2e-08KRAS, SOS1, HRAS, PTPN11
FRS-mediated FGFR1 signaling4261.0×2e-08KRAS, SOS1, HRAS, PTPN11
FRS-mediated FGFR2 signaling4251.0×2e-08KRAS, SOS1, HRAS, PTPN11
Downstream signal transduction4217.5×4e-08KRAS, SOS1, HRAS, PTPN11
FLT3 Signaling4197.8×5e-08KRAS, SOS1, HRAS, PTPN11
RAF activation4191.9×5e-08KRAS, SHOC2, HRAS, RAF1
SOS-mediated signalling3611.8×1e-07KRAS, SOS1, HRAS
Signaling by SCF-KIT4141.9×1e-07KRAS, SOS1, HRAS, PTPN11
Activated NTRK3 signals through RAS3543.8×2e-07KRAS, SOS1, HRAS
EGFR Transactivation by Gastrin3489.4×2e-07KRAS, SOS1, HRAS
SHC-related events triggered by IGF1R3489.4×2e-07KRAS, SOS1, HRAS
Activated NTRK2 signals through RAS3489.4×2e-07KRAS, SOS1, HRAS
MET activates RAS signaling3444.9×3e-07KRAS, SOS1, HRAS
Signaling by FGFR4 in disease3407.9×4e-07KRAS, SOS1, HRAS
Constitutive Signaling by Overexpressed ERBB23407.9×4e-07KRAS, SOS1, HRAS
Signaling by PDGFRA transmembrane, juxtamembrane and kinase domain mutants3376.5×4e-07KRAS, SOS1, HRAS
Signaling by PDGFRA extracellular domain mutants3376.5×4e-07KRAS, SOS1, HRAS
GRB2 events in EGFR signaling3326.3×6e-07KRAS, SOS1, HRAS
Erythropoietin activates RAS3326.3×6e-07KRAS, SOS1, HRAS
SHC1 events in ERBB4 signaling3305.9×7e-07KRAS, SOS1, HRAS
SHC1 events in EGFR signaling3305.9×7e-07KRAS, SOS1, HRAS
Constitutive Signaling by EGFRvIII3305.9×7e-07KRAS, SOS1, HRAS
Signalling to RAS3287.9×7e-07KRAS, SOS1, HRAS
Insulin receptor signalling cascade3287.9×7e-07KRAS, SOS1, HRAS
Signaling by ERBB2 ECD mutants3287.9×7e-07KRAS, SOS1, HRAS
GRB2 events in ERBB2 signaling3271.9×9e-07KRAS, SOS1, HRAS

GO biological processes by enrichment

Over-representation of cohort genes vs the genome-wide background (hypergeometric test, Benjamini-Hochberg FDR; fold = observed/expected over 7 annotated cohort genes). Counts and members are kept as ground-truth; sorted by enrichment.

GO termCohort genesFoldFDRSample cohort genes
Schwann cell development3451.4×2e-06SOS1, HRAS, RAF1
neurotrophin TRK receptor signaling pathway3451.4×2e-06SOS1, PTPN11, RAF1
fibroblast growth factor receptor signaling pathway3122.4×9e-05SOS1, SHOC2, PTPN11
myelination3107.8×1e-04SOS1, HRAS, RAF1
insulin receptor signaling pathway395.0×1e-04SOS1, HRAS, RAF1
Ras protein signal transduction388.1×1e-04KRAS, SOS1, HRAS
MAPK cascade365.7×3e-04KRAS, HRAS, RAF1
cytokine-mediated signaling pathway356.0×4e-04KRAS, SOS1, PTPN11
regulation of long-term neuronal synaptic plasticity2283.2×4e-04KRAS, HRAS
positive regulation of Rac protein signal transduction2185.2×9e-04KRAS, SOS1
insulin-like growth factor receptor signaling pathway2141.6×0.001SOS1, RAF1
homeostasis of number of cells within a tissue2126.7×0.002KRAS, PTPN11
response to mineralocorticoid12407.4×0.005KRAS
negative regulation of cortisol secretion12407.4×0.005PTPN11
negative regulation of growth hormone secretion12407.4×0.005PTPN11
cellular response to growth hormone stimulus12407.4×0.005SHOC2
epidermal growth factor receptor signaling pathway270.8×0.005SOS1, PTPN11
neuron apoptotic process252.9×0.006KRAS, HRAS
microvillus organization11203.7×0.008PTPN11
intestinal epithelial cell migration11203.7×0.008PTPN11
death-inducing signaling complex assembly11203.7×0.008RAF1
multicellular organism growth239.1×0.009SOS1, PTPN11
cerebellar cortex formation1802.5×0.010PTPN11
forebrain astrocyte development1802.5×0.010KRAS
positive regulation of miRNA metabolic process1802.5×0.010HRAS
response to isolation stress1601.9×0.010KRAS
regulation of type I interferon-mediated signaling pathway1601.9×0.010PTPN11
clathrin coat disassembly1601.9×0.010CLTC
negative regulation of hyaluronan biosynthetic process1601.9×0.010CLTC
midbrain morphogenesis1601.9×0.010SOS1

Therapeutics

Drug target analysis

Approved (phase 4): 5 · Phase ≥3: 5 · Phased (≥1): 5 · Undrugged: 2

Druggability breadth: 6 of 7 evidence-associated genes (86%) 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
KRASVEMURAFENIB
SOS1IDARUBICIN
HRASLONAFARNIB
PTPN11ESTRAMUSTINE PHOSPHATE
RAF1VEMURAFENIB

Top cohort targets by molecule count

SymbolMoleculesMax phase
RAF1314
KRAS114
PTPN1184
SOS154
HRAS44
SHOC200
CLTC00

Drugs targeting cohort genes (top 30)

MoleculeMax phaseTargets in cohort
VEMURAFENIB4KRAS, RAF1
DABRAFENIB4KRAS, RAF1
LONAFARNIB4HRAS, KRAS
SOTORASIB4KRAS, SOS1
ADAGRASIB4KRAS, SOS1
IDARUBICIN4SOS1
DOXORUBICIN4SOS1
ESTRAMUSTINE PHOSPHATE4PTPN11
SORAFENIB4RAF1
REGORAFENIB4RAF1
NILOTINIB4RAF1
TOVORAFENIB4RAF1
PAZOPANIB4RAF1
DASATINIB4RAF1
ERLOTINIB4RAF1
IMATINIB4RAF1
OPNURASIB3KRAS
PLINABULIN3RAF1
AVUTOMETINIB3RAF1
NAPORAFENIB3RAF1
MOTESANIB3RAF1
DIVARASIB2KRAS
GLECIRASIB2KRAS
STALLIMYCIN2HRAS
ENOXOLONE2PTPN11
CEFSULODIN2PTPN11
BATOPROTAFIB2PTPN11
VOCIPROTAFIB2PTPN11
DORAMAPIMOD2RAF1
CI-10402RAF1

Bioactivity and enzyme data

Enzyme cohort genes (≥1 EC): 4.

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

SymbolAssaysType breakdown
KRAS861Binding:829, Functional:32
RAF1839Binding:803, Functional:31, ADMET:5
PTPN11588Binding:585, Functional:2, ADMET:1
SOS1421Binding:409, Functional:12
HRAS48Binding:45, Functional:3
CLTC8Binding:8

Cohort enzymes (BRENDA EC)

SymbolEC numbersNames
KRAS3.6.5.2small monomeric GTPase
HRAS3.6.5.2small monomeric GTPase
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
KRAS861
SOS1421
PTPN11588
RAF1839

Pharmacogenomics

Cohort genes with a PharmGKB record: 7; 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)
VEMURAFENIB4KRAS, RAF1
DABRAFENIB4KRAS, RAF1
LONAFARNIB4HRAS, KRAS
SOTORASIB4KRAS, SOS1
ADAGRASIB4KRAS, SOS1
IDARUBICIN4SOS1
DOXORUBICIN4SOS1
ESTRAMUSTINE PHOSPHATE4PTPN11
SORAFENIB4RAF1
REGORAFENIB4RAF1
NILOTINIB4RAF1
TOVORAFENIB4RAF1
PAZOPANIB4RAF1
DASATINIB4RAF1
ERLOTINIB4RAF1
IMATINIB4RAF1
OPNURASIB3KRAS
PLINABULIN3RAF1
AVUTOMETINIB3RAF1
NAPORAFENIB3RAF1
MOTESANIB3RAF1
DIVARASIB2KRAS
GLECIRASIB2KRAS
STALLIMYCIN2HRAS
ENOXOLONE2PTPN11
CEFSULODIN2PTPN11
BATOPROTAFIB2PTPN11
VOCIPROTAFIB2PTPN11
DORAMAPIMOD2RAF1
CI-10402RAF1

Druggability pyramid

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

TierDefinitionGenesSymbols
AApproved (phase 4 drug)5KRAS, SOS1, HRAS, PTPN11, RAF1
BPhased (≥1) drug, not yet approved0
CDruggable family + PDB, no drug0
DDruggable family + AlphaFold only, no drug0
EDifficult family or no structure, no drug2SHOC2, CLTC

Undrugged target profiles

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

SymbolChEMBL assaysDrugged partners (top 3)
SHOC20SOS1
CLTC8

Clinical trials & evidence

Clinical trials

Clinical trials: 0.