HRAS
gene geneOn this page
Summary
HRAS (HRas proto-oncogene, GTPase, HGNC:5173) is a protein-coding gene on chromosome 11p15.5, encoding GTPase HRas (P01112). Signal transducer in the Ras-MAPK signaling pathway that regulates cell proliferation and survival. In precision oncology, BRAF V600E OR NRAS Mutation OR HRAS Mutation OR KRAS Mutation OR NF1 Inactivating Mutation confers sensitivity to Selumetinib in Cancer (CIViC Level B); 8 further curated variant–drug associations are listed below.
This gene belongs to the Ras oncogene family, whose members are related to the transforming genes of mammalian sarcoma retroviruses. The products encoded by these genes function in signal transduction pathways. These proteins can bind GTP and GDP, and they have intrinsic GTPase activity. This protein undergoes a continuous cycle of de- and re-palmitoylation, which regulates its rapid exchange between the plasma membrane and the Golgi apparatus. Mutations in this gene cause Costello syndrome, a disease characterized by increased growth at the prenatal stage, growth deficiency at the postnatal stage, predisposition to tumor formation, cognitive disability, skin and musculoskeletal abnormalities, distinctive facial appearance and cardiovascular abnormalities. Defects in this gene are implicated in a variety of cancers, including bladder cancer, follicular thyroid cancer, and oral squamous cell carcinoma. Multiple transcript variants, which encode different isoforms, have been identified for this gene.
Source: NCBI Gene 3265 — RefSeq curated summary.
At a glance
- Gene–disease (curated): Costello syndrome (Definitive, ClinGen) — +2 more curated relationships
- Clinical variants (ClinVar): 668 total — 21 pathogenic, 23 likely-pathogenic (top 5% of genes corpus-wide)
- Regional missense constraint (gnomAD): 1 of 4 regions constrained (≈7% of expected missense variation)
- GTEx eGene: eQTL in 46 tissues, sQTL in 13 (q < 0.05)
- Phenotypes (HPO): 210
- Drug target: yes — 1 via a complex or family; 4 molecules with ChEMBL bioactivity
- Precision-oncology evidence (CIViC): 9 curated variant–drug associations
- Cancer driver (intOGen): activating (oncogene-like) across 14 cancer types (inferred from mutation patterns)
- Dosage sensitivity (ClinGen): haploinsufficiency no evidence, triplosensitivity no evidence
- Constraint (gnomAD): pLI 0.02 (LoF-tolerant), LOEUF 0.89 (unconstrained)
- MANE Select transcript:
NM_005343 - Interaction hub: 4,618 STRING partners (top 1% of genes corpus-wide)
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:5173 |
| Approved symbol | HRAS |
| Name | HRas proto-oncogene, GTPase |
| Location | 11p15.5 |
| Locus type | gene with protein product |
| Status | Approved |
| Ensembl gene | ENSG00000174775 |
| Ensembl biotype | protein_coding |
| OMIM | 190020 |
| Entrez | 3265 |
Gene structure
Transcript identifiers
Ensembl transcripts: 27 — 21 protein_coding, 4 nonsense_mediated_decay, 1 retained_intron, 1 protein_coding_CDS_not_defined
MANE Select: ENST00000311189 · MANE Plus Clinical: ENST00000417302
Transcript support level (Ensembl TSL; 1 = fully mRNA-supported): TSL 1: 2, TSL 2: 4, TSL 3: 3, TSL 5: 1
ENST00000311189, ENST00000417302, ENST00000397594, ENST00000397596, ENST00000451590, ENST00000462734, ENST00000468682, ENST00000479482, ENST00000482021, ENST00000493230, ENST00000879220, ENST00000879221, ENST00000879222, ENST00000879223, ENST00000879224, ENST00000932528, ENST00000932529, ENST00000932530, ENST00000932531, ENST00000932532, ENST00000979403, ENST00000979404, ENST00001041405, ENST00001041406, ENST00001061984, ENST00001142568, ENST00001142569
RefSeq mRNA: 4 — MANE Select: NM_005343
NM_001130442, NM_001318054, NM_005343, NM_176795
CCDS: CCDS7698, CCDS7699
Canonical transcript exons
ENST00000311189 — 6 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001503789 | 535416 | 535576 |
| ENSE00001529354 | 532242 | 532522 |
| ENSE00003561701 | 532631 | 532755 |
| ENSE00003603244 | 533453 | 533612 |
| ENSE00003921927 | 533766 | 533944 |
| ENSE00004014247 | 534212 | 534375 |
Expression profiles
Bgee: expression breadth ubiquitous, 139 present calls, max score 99.01.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 27.6164 / max 180.9101, expressed in 1811 samples.
Highest expression (Bgee): skin of abdomen, skin of leg, zone of skin, lower esophagus mucosa, putamen.
Genetic regulation across tissues (GTEx eQTL / sQTL)
HRAS is an eGene in GTEx v10 — its expression is genetically regulated (eQTL) in 46 tissues and its splicing (sQTL) in 13 (q < 0.05). Strongest associations first; slope = normalized effect of the lead variant’s alternative allele.
showing 20 of 59 significant tissue × QTL associations:
| Tissue | QTL | q-value | Slope | Lead variant |
|---|---|---|---|---|
| Artery Tibial | eqtl | 2.2e-56 | -0.28 | 11:534242:A:G |
| Nerve Tibial | eqtl | 1.6e-40 | -0.29 | 11:534242:A:G |
| Testis | eqtl | 1.5e-36 | +1.02 | 11:535026:C:T |
| Artery Aorta | eqtl | 9.9e-33 | -0.35 | 11:539646:G:T |
| Esophagus Muscularis | eqtl | 1.1e-29 | -0.28 | 11:534242:A:G |
| Thyroid | eqtl | 1.7e-25 | -0.31 | 11:545276:G:T |
| Lung | eqtl | 6.0e-24 | -0.30 | 11:539648:G:A |
| Adipose Subcutaneous | eqtl | 1.2e-22 | -0.22 | 11:531224:A:G |
| Brain Nucleus accumbens basal ganglia | eqtl | 1.9e-22 | -0.43 | 11:539058:C:T |
| Esophagus Gastroesophageal Junction | eqtl | 6.8e-18 | -0.24 | 11:534242:A:G |
| Brain Caudate basal ganglia | eqtl | 7.1e-16 | -0.37 | 11:531572:G:A |
| Muscle Skeletal | eqtl | 1.4e-15 | -0.17 | 11:547210:T:C |
| Heart Atrial Appendage | eqtl | 7.6e-15 | -0.27 | 11:545276:G:T |
| Brain Putamen basal ganglia | eqtl | 1.4e-14 | -0.40 | 11:540005:C:T |
| Colon Transverse | eqtl | 3.5e-14 | -0.27 | 11:539648:G:A |
| Brain Cortex | eqtl | 5.4e-14 | -0.51 | 11:521462:C:T |
| Cells Cultured fibroblasts | eqtl | 1.3e-13 | -0.12 | 11:555645:T:G |
| Brain Cerebellar Hemisphere | eqtl | 1.6e-13 | -0.19 | 11:531224:A:G |
| Colon Sigmoid | eqtl | 3.7e-13 | -0.20 | 11:534242:A:G |
| Brain Hypothalamus | eqtl | 4.4e-13 | -0.27 | 11:534242:A:G |
FANTOM5 promoters
1 alternative TSS:
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 117775 | 27.6164 | 1811 |
Top tissues by expression
showing 100 of 139 tissues by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| skin of abdomen | UBERON:0001416 | 99.01 | gold quality |
| skin of leg | UBERON:0001511 | 98.93 | gold quality |
| zone of skin | UBERON:0000014 | 98.90 | gold quality |
| lower esophagus mucosa | UBERON:0035834 | 98.90 | gold quality |
| putamen | UBERON:0001874 | 98.55 | gold quality |
| esophagus mucosa | UBERON:0002469 | 98.55 | gold quality |
| caudate nucleus | UBERON:0001873 | 98.38 | gold quality |
| nucleus accumbens | UBERON:0001882 | 98.28 | gold quality |
| hypothalamus | UBERON:0001898 | 97.96 | gold quality |
| temporal lobe | UBERON:0001871 | 97.86 | gold quality |
| amygdala | UBERON:0001876 | 97.85 | gold quality |
| right hemisphere of cerebellum | UBERON:0014890 | 97.84 | gold quality |
| substantia nigra | UBERON:0002038 | 97.77 | gold quality |
| Ammon’s horn | UBERON:0001954 | 97.73 | gold quality |
| vagina | UBERON:0000996 | 97.72 | gold quality |
| cerebellar hemisphere | UBERON:0002245 | 97.71 | gold quality |
| anterior cingulate cortex | UBERON:0009835 | 97.71 | gold quality |
| cerebellum | UBERON:0002037 | 97.67 | gold quality |
| cerebellar cortex | UBERON:0002129 | 97.66 | gold quality |
| right frontal lobe | UBERON:0002810 | 97.63 | gold quality |
| prefrontal cortex | UBERON:0000451 | 97.61 | gold quality |
| brain | UBERON:0000955 | 97.60 | gold quality |
| frontal cortex | UBERON:0001870 | 97.54 | gold quality |
| metanephros cortex | UBERON:0010533 | 97.49 | gold quality |
| cerebral cortex | UBERON:0000956 | 97.45 | gold quality |
| dorsolateral prefrontal cortex | UBERON:0009834 | 97.42 | gold quality |
| Brodmann (1909) area 9 | UBERON:0013540 | 97.42 | gold quality |
| mucosa of transverse colon | UBERON:0004991 | 97.38 | gold quality |
| pituitary gland | UBERON:0000007 | 97.32 | gold quality |
| olfactory segment of nasal mucosa | UBERON:0005386 | 97.29 | gold quality |
| adenohypophysis | UBERON:0002196 | 97.27 | gold quality |
| C1 segment of cervical spinal cord | UBERON:0006469 | 97.26 | gold quality |
| esophagus | UBERON:0001043 | 97.22 | gold quality |
| apex of heart | UBERON:0002098 | 96.94 | gold quality |
| prostate gland | UBERON:0002367 | 96.83 | gold quality |
| right uterine tube | UBERON:0001302 | 96.62 | gold quality |
| primary visual cortex | UBERON:0002436 | 96.58 | gold quality |
| tibial nerve | UBERON:0001323 | 96.39 | gold quality |
| lower esophagus | UBERON:0013473 | 96.18 | gold quality |
| lower esophagus muscularis layer | UBERON:0035833 | 96.18 | gold quality |
| superior frontal gyrus | UBERON:0002661 | 96.09 | gold quality |
| ectocervix | UBERON:0012249 | 96.09 | gold quality |
| minor salivary gland | UBERON:0001830 | 96.06 | gold quality |
| esophagogastric junction muscularis propria | UBERON:0035841 | 95.86 | gold quality |
| fundus of stomach | UBERON:0001160 | 95.73 | gold quality |
| saliva-secreting gland | UBERON:0001044 | 95.72 | gold quality |
| cortex of kidney | UBERON:0001225 | 95.68 | gold quality |
| hindlimb stylopod muscle | UBERON:0004252 | 95.64 | gold quality |
| left coronary artery | UBERON:0001626 | 95.62 | gold quality |
| endocervix | UBERON:0000458 | 95.58 | gold quality |
| right lung | UBERON:0002167 | 95.52 | gold quality |
| body of stomach | UBERON:0001161 | 95.45 | gold quality |
| spleen | UBERON:0002106 | 95.41 | gold quality |
| right lobe of thyroid gland | UBERON:0001119 | 95.40 | gold quality |
| cortical plate | UBERON:0005343 | 95.40 | gold quality |
| heart left ventricle | UBERON:0002084 | 95.38 | gold quality |
| left lobe of thyroid gland | UBERON:0001120 | 95.34 | gold quality |
| transverse colon | UBERON:0001157 | 95.34 | gold quality |
| upper lobe of left lung | UBERON:0008952 | 95.33 | gold quality |
| muscle layer of sigmoid colon | UBERON:0035805 | 95.33 | gold quality |
| right coronary artery | UBERON:0001625 | 95.27 | gold quality |
| ascending aorta | UBERON:0001496 | 95.25 | gold quality |
| thoracic aorta | UBERON:0001515 | 95.22 | gold quality |
| granulocyte | CL:0000094 | 95.17 | gold quality |
| body of uterus | UBERON:0009853 | 95.17 | gold quality |
| popliteal artery | UBERON:0002250 | 95.15 | gold quality |
| tibial artery | UBERON:0007610 | 95.14 | gold quality |
| mammary gland | UBERON:0001911 | 94.92 | gold quality |
| subcutaneous adipose tissue | UBERON:0002190 | 94.92 | gold quality |
| thoracic mammary gland | UBERON:0005200 | 94.92 | gold quality |
| small intestine Peyer’s patch | UBERON:0003454 | 94.87 | gold quality |
| gastrocnemius | UBERON:0001388 | 94.82 | gold quality |
| mucosa of stomach | UBERON:0001199 | 94.80 | gold quality |
| descending thoracic aorta | UBERON:0002345 | 94.74 | gold quality |
| anatomical system | UBERON:0000467 | 94.73 | gold quality |
| material anatomical entity | UBERON:0000465 | 94.71 | gold quality |
| multicellular organism | UBERON:0000468 | 94.71 | gold quality |
| adipose tissue | UBERON:0001013 | 94.65 | gold quality |
| thyroid gland | UBERON:0002046 | 94.65 | gold quality |
| muscle of leg | UBERON:0001383 | 94.51 | gold quality |
| muscle organ | UBERON:0001630 | 94.45 | gold quality |
| omental fat pad | UBERON:0010414 | 94.43 | gold quality |
| colon | UBERON:0001155 | 94.35 | gold quality |
| heart | UBERON:0000948 | 94.28 | gold quality |
| adult mammalian kidney | UBERON:0000082 | 94.27 | gold quality |
| left uterine tube | UBERON:0001303 | 94.25 | gold quality |
| right ovary | UBERON:0002118 | 94.25 | gold quality |
| left ovary | UBERON:0002119 | 94.24 | gold quality |
| stromal cell of endometrium | CL:0002255 | 94.23 | gold quality |
| myometrium | UBERON:0001296 | 94.14 | gold quality |
| right atrium auricular region | UBERON:0006631 | 94.13 | gold quality |
| body of pancreas | UBERON:0001150 | 94.08 | gold quality |
| uterine cervix | UBERON:0000002 | 94.01 | gold quality |
| small intestine | UBERON:0002108 | 93.95 | gold quality |
| ganglionic eminence | UBERON:0004023 | 93.64 | gold quality |
| embryo | UBERON:0000922 | 93.63 | gold quality |
| intestine | UBERON:0000160 | 93.56 | gold quality |
| stomach | UBERON:0000945 | 93.52 | gold quality |
| placenta | UBERON:0001987 | 93.40 | gold quality |
| right lobe of liver | UBERON:0001114 | 93.24 | gold quality |
Single-cell (SCXA)
Detected in 2 experiment(s), a significant marker in 2.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-MTAB-7008 | yes | 87.33 |
| E-ANND-3 | yes | 8.40 |
HPA expression
RNA tissue specificity: Tissue enhanced
showing 60 of 78 HPA tissues / cells by nTPM:
| Tissue / cell | Axis | nTPM | Protein (IHC) |
|---|---|---|---|
| Caudate putamen | tissue | 301.4 | |
| Frontal cortex | tissue | 187.2 | |
| Spinal cord | tissue | 57.8 | |
| Corpus callosum | tissue | 54.9 | |
| Medulla oblongata | tissue | 51.6 | |
| Pons | tissue | 51.1 | |
| Midbrain | tissue | 50.5 | |
| Putamen | tissue | 50.0 | |
| Thalamus | tissue | 48.1 | |
| Superior colliculi | tissue | 46.8 | |
| Cerebral cortex | tissue | 44.5 | medium |
| Motor cortex | tissue | 44.5 | |
| Somatosensory cortex | tissue | 44.2 | |
| Substantia nigra | tissue | 42.8 | |
| Prefrontal cortex | tissue | 39.5 | |
| Basal ganglia | tissue | 39.2 | not detected |
| Occipital cortex | tissue | 39.1 | |
| Hippocampal formation | tissue | 38.7 | |
| Entorhinal cortex | tissue | 37.9 | |
| Hypothalamus | tissue | 37.8 | |
| Retrosplenial cortex | tissue | 37.6 | |
| Temporal cortex | tissue | 37.3 | |
| Ventral forebrain | tissue | 37.2 | |
| Vagina | tissue | 36.7 | not detected |
| Retrosplenial and cingulate cortex | tissue | 36.6 | |
| Insular cortex | tissue | 36.1 | |
| Pituitary gland | tissue | 35.6 | |
| Locus coeruleus | tissue | 34.8 | |
| Periaqueductal gray | tissue | 34.8 | |
| Septum | tissue | 34.4 | |
| Skeletal muscle | tissue | 31.9 | low |
| Amygdala | tissue | 30.1 | |
| Hippocampus | tissue | 29.0 | not detected |
| Heart muscle | tissue | 25.0 | not detected |
| Nucleus accumbens | tissue | 23.9 | |
| Tongue | tissue | 23.4 | |
| Cerebellum | tissue | 22.6 | medium |
| Postcentral gyrus | tissue | 19.5 | |
| Olfactory bulb | tissue | 19.2 | |
| Skin 1 | tissue | 17.4 | low |
| Choroid plexus | tissue | 16.7 | |
| Esophagus | tissue | 12.9 | not detected |
| Parathyroid gland | tissue | 11.9 | medium |
| Adipose tissue | tissue | 11.3 | not detected |
| Urinary bladder | tissue | 11.2 | low |
| Epididymis | tissue | 11.2 | medium |
| Seminal vesicle | tissue | 10.7 | medium |
| Retina | tissue | 9.2 | |
| Tonsil | tissue | 9.0 | low |
| Thymus | tissue | 8.4 | |
| Placenta | tissue | 8.0 | not detected |
| Colon | tissue | 7.9 | high |
| Smooth muscle | tissue | 7.8 | not detected |
| Adrenal gland | tissue | 7.8 | not detected |
| Fallopian tube | tissue | 7.6 | medium |
| Breast | tissue | 7.1 | not detected |
| Ovary | tissue | 6.8 | not detected |
| Prostate | tissue | 6.7 | low |
| Rectum | tissue | 6.2 | high |
| Lung | tissue | 5.7 | not detected |
Brain sub-regions (HPA Brain Atlas): detected in 192; highest nTPM — Ventral spinal cord (57.8), White matter (54.9), Dorsal spinal cord (47.9), Dorsal hippocampus (38.7), Ventral hippocampus (34.5).
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): AP1, BTG2, ESR1, HNRNPAB, MAZ, PAX1, SP1, STAT3, TP53, ZHX2, ZNF362
miRNA regulators (miRDB)
Targeting HRAS by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific).
23 miRNAs:
| miRNA | Max score | Avg score | miRNA target_count |
|---|---|---|---|
| HSA-MIR-3667-3P | 99.99 | 67.17 | 1636 |
| HSA-MIR-4728-5P | 99.85 | 69.39 | 4718 |
| HSA-MIR-6785-5P | 99.82 | 68.68 | 4428 |
| HSA-MIR-149-3P | 99.72 | 68.22 | 3963 |
| HSA-MIR-4699-3P | 99.71 | 70.15 | 3142 |
| HSA-MIR-6883-5P | 99.69 | 68.05 | 3785 |
| HSA-MIR-6513-5P | 99.43 | 67.81 | 1071 |
| HSA-MIR-4292 | 99.16 | 65.57 | 1767 |
| HSA-MIR-6791-5P | 99.16 | 65.92 | 1844 |
| HSA-MIR-6734-3P | 99.15 | 66.27 | 1627 |
| HSA-MIR-6889-3P | 98.84 | 67.35 | 1198 |
| HSA-MIR-6529-3P | 98.68 | 66.76 | 1020 |
| HSA-MIR-1301-3P | 98.64 | 68.27 | 1071 |
| HSA-MIR-5047 | 98.64 | 68.62 | 1035 |
| HSA-MIR-6868-3P | 98.63 | 69.64 | 2259 |
| HSA-MIR-4691-5P | 98.41 | 66.77 | 1343 |
| HSA-MIR-6792-3P | 98.41 | 66.86 | 1359 |
| HSA-MIR-4768-3P | 98.16 | 66.02 | 2330 |
| HSA-MIR-6502-3P | 97.86 | 65.43 | 569 |
| HSA-MIR-4660 | 97.79 | 67.44 | 1328 |
| HSA-MIR-6728-5P | 97.79 | 66.33 | 891 |
| HSA-MIR-4693-5P | 97.35 | 67.02 | 1234 |
| HSA-MIR-1306-5P | 97.11 | 64.04 | 755 |
Functional genomics
gnomAD constraint: pLI 0.0173, LOEUF 0.893, missense Z 1.46 — population loss-of-function intolerance (pLI ≥ 0.9 = LoF-intolerant; lower LOEUF = more constrained). gnomAD
Regional missense constraint (gnomAD)
ENST00000311189 splits into 4 regions with different missense tolerance; 1 is missense-constrained (≈7% of the expected missense variation). Missense variants in a constrained region (low observed/expected) are more likely to be pathogenic. gnomAD
| Region (GRCh38) | Missense obs / exp | o/e | Constrained |
|---|---|---|---|
| 11:532,639–533,803 | 142 / 141.1 | 1.01 | no |
| 11:533,804–534,239 | 51 / 79.0 | 0.65 | no |
| 11:534,240–534,283 | 1 / 17.8 | 0.06 | yes (p 6.9e-05) |
| 11:534,284–534,322 | 10 / 18.0 | 0.56 | no |
ClinGen dosage: haploinsufficiency 0 (no evidence), triplosensitivity 0 (no evidence). ClinGen Gene Dosage Map |
Literature-anchored findings (GeneRIF, showing 40)
- The Tg.AC (v-Ha-ras) transgenic mouse model provides a reporter phenotype of skin papillomas in response to either genotoxic or nongenotoxic carcinogens. (PMID:11695562)
- The Tg.Ac (v-Ha-ras) mouse model was not overly sensitive and possesses utility as an adjunct to the battery of toxicity studies used to establish carcinogenic risk. (PMID:11695563)
- immunohistochemical analysis reveals a protective effect of H-ras expression mediated via apoptosis in node-negative breast cancer patients (PMID:11788888)
- molecular dynamics simulations to show that Ras, a monomeric G protein, can generate mechanical force upon hydrolysis (PMID:11904419)
- Point mutations were identified in DNA from two of the 115 normal individuals. Both mutations resulted in an amino acid substitution at position 12 in H RAS. (PMID:11920220)
- H-Ras/mitogen-activated protein kinase pathway inhibits integrin-mediated adhesion and induces apoptosis in osteoblasts (PMID:11934900)
- H-Ras mutations at the binding site for the GTP nucleotide ring in a human multiple myeloma line leads to transformation and factor-independent cell growth (PMID:12569357)
- HRAS genes are biallelically expressed in multiple fetal and adult tissues both in humans and in mice (PMID:12589428)
- overexpression of PPARalpha or the c-Ha-ras transgene is not associated with the liver tumorigenesis induced by DEHP in rasH2 mice (PMID:12668284)
- steady-state structure of the switch I region of the protein in both the inactive GDP-bound conformation as in the active GTP-bound conformation. (PMID:12717016)
- Ha-ras mutations detected in HPV-induced cervical intraepithelial neoplasia grade II and invasive squamous cell carcinoma (PMID:12878090)
- Results demonstrate the close relationship between Ha-ras expression level and sensitization of 5-flurouracil (5-FU)-treated cells. (PMID:12915131)
- using fragments of the human c-Ha-ras gene containing 8-hydroxyguanine (8-OH-G) in codon 12, evidence for the highly complex biochemical events leading to activation of the oncogene (PMID:14576295)
- the human c-Ha-ras proto-oncogene product does not influence the androgen-dependence of prostate carcinogenesis due to the probasin-mediated SV40 T antigen. (PMID:14662018)
- Ras activates the MAP kinase cascade through simultaneous dual effector interactions: induction of Raf kinase activity and derepression of Raf-MEK complex formation (PMID:14724641)
- When mutated, causes hepatocarcinogenesis in transgenic mice. (PMID:14729607)
- complete loss of p53 is a prerequisite for collaborating with activated Ha-ras to promote bladder tumorigenesis (PMID:14737103)
- H-ras mutations have a role in malignant transformation of aerodigestive spindle cell carcinoma (PMID:14767509)
- a domain of Rap1 acts dominantly on COOH-terminal lipid modification of Ha-Ras, which has been considered to be essential and sufficient for the plasma membrane localization (PMID:15031297)
- Changes in flexibility upon protein-protein complex formation of H-Ras & the Ras-binding domain of C-Raf1 have been investigated using the molecular framework approach FIRST and molecular dynamics simulations of in total approximately 35 ns length. (PMID:15211515)
- ras gene alterations have a specific and early role in the development of follicular type of thyroid tumors in Taiwan. (PMID:15320975)
- Myc rescued cell growth inhibition induced by Ras (PMID:15528212)
- RAS appears to be a pejorative prognostic factor in terms of survival in NSCLC globally, in ADC and when it is studied by PCR. (PMID:15597105)
- No significant correlations were found between mutations in colorect cancer. (PMID:15638373)
- H-Ras-specific activation of Rac-MKK3/6-p38 pathway has a role in invasion and migration of breast epithelial cells (PMID:15677464)
- the mechanism of O2*-mediated Ras guanine nucleotide dissociation is similar to that of NO/O2-mediated Ras guanine nucleotide dissociation (PMID:15684418)
- Ras exists in (at least) two conformational states identifiable by nuclear magnetic resonance spectroscopy: state 2 represents the high-affinity binding state for effectors, while state 1 represents a weak binding state. (PMID:15697248)
- We found mutations in p53, K-ras, and BRAF genes in 35%, 30%, and 4% of tumors, respectively, and observed a minimal or no co-presence of these gene alterations. (PMID:15702478)
- RAS-MEK-ERK1/2 signaling pathway can sensitize cells to TRAIL-induced apoptosis by up-regulating DR4 and DR5 (PMID:15757891)
- reduced Ras activation in cells harbouring the Hepatitis C virus subgenomic replicon (PMID:15784896)
- K-ras mutations are found in plasma after colorectal tumor resection (PMID:15816642)
- the mechanism for Ras-mediated down-regulation of Par-4 is by promoter methylation (PMID:15831492)
- Ras isoforms have distinct and separate cellular and subcellular distribution that may persist even in the malignantly transformed state in pancreatic disease (PMID:15855817)
- In this study, we probe the cellular and molecular mechanisms of RAS-mediated transformation. (PMID:15940260)
- HRAS oncogene could play an important role in the development of cervical cancer, in addition to the presence of HPV, by reducing the G1 phase and accelerating the G1/S transition of infected cells (PMID:15950068)
- N-Ras(L61) transformed cells lack a G0-G1 arrest upon TGF-beta treatment due to absence of p27. (PMID:15963850)
- Ras activity regulates Fbw7-mediated cyclin E proteolysis; impaired cyclin E proteolysis is a mechanism through which Ras mutations promote tumorigenesis. (PMID:15980150)
- RIG1 exerts inhibitory effect at the level of Ras activation, which is independent of Ras subtype but dependent on membrane localization of RIG1. It may be mediated through downregulation of Ras levels and alteration of Ras subcellular distribution. (PMID:16005186)
- studies provide evidence for the existence of human-specific mechanisms that resist Ras/MEK/ERK-mediated transformation (PMID:16007212)
- in primary fibroblasts stabilization of Ras protein by ROS and ERK1/2 amplifies the response of the cells to growth factors and in systemic sclerosis represents a critical factor in the onset and progression of the disease (PMID:16081426)
Cross-species orthologs
7 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | hrasb | ENSDARG00000005651 |
| danio_rerio | hrasa | ENSDARG00000098497 |
| mus_musculus | Hras | ENSMUSG00000025499 |
| rattus_norvegicus | Hras | ENSRNOG00000016611 |
| rattus_norvegicus | Hrasl1 | ENSRNOG00000018301 |
| drosophila_melanogaster | Ras85D | FBGN0003205 |
| caenorhabditis_elegans | WBGENE00002335 |
Paralogs (35): RALA (ENSG00000006451), REM1 (ENSG00000088320), RASL10A (ENSG00000100276), RASD2 (ENSG00000100302), RASL12 (ENSG00000103710), RHEB (ENSG00000106615), RASD1 (ENSG00000108551), RERGL (ENSG00000111404), RAP1A (ENSG00000116473), RASL11A (ENSG00000122035), RAP2C (ENSG00000123728), RAP2A (ENSG00000125249), RRAS (ENSG00000126458), RAP1B (ENSG00000127314), RASL11B (ENSG00000128045), KRAS (ENSG00000133703), RRAS2 (ENSG00000133818), RERG (ENSG00000134533), REM2 (ENSG00000139890), RIT1 (ENSG00000143622), RALB (ENSG00000144118), RIT2 (ENSG00000152214), MRAS (ENSG00000158186), DIRAS3 (ENSG00000162595), GEM (ENSG00000164949), DIRAS2 (ENSG00000165023), RRAD (ENSG00000166592), RHEBL1 (ENSG00000167550), NKIRAS2 (ENSG00000168256), DIRAS1 (ENSG00000176490), RAP2B (ENSG00000181467), ERAS (ENSG00000187682), NKIRAS1 (ENSG00000197885), NRAS (ENSG00000213281), RASL10B (ENSG00000270885)
Mouse-model phenotypes
Observed phenotypes of the mouse ortholog (MGI:96224) from MGI (Alliance of Genome Resources) — knockout/mutant phenotypes, ranked by annotation count. 63 distinct phenotype terms.
| Mouse phenotype (MP) | Records |
|---|---|
| postnatal growth retardation | 2 |
| premature death | 2 |
| abnormal ameloblast morphology | 2 |
| abnormal enamel mineralization | 2 |
| short premaxilla | 1 |
| short maxilla | 1 |
| abnormal frontal bone morphology | 1 |
| abnormal tooth development | 1 |
| malocclusion | 1 |
| hypertension | 1 |
| abnormal heart morphology | 1 |
| heart right ventricle hypertrophy | 1 |
| abnormal cranium morphology | 1 |
| domed cranium | 1 |
| abnormal mammary gland development | 1 |
| mammary gland hyperplasia | 1 |
| abnormal branching of the mammary ductal tree | 1 |
| ataxia | 1 |
| abnormal suckling behavior | 1 |
| abnormal blood vessel morphology | 1 |
| edema | 1 |
| increased mammary adenocarcinoma incidence | 1 |
| hydrocephaly | 1 |
| increased papilloma incidence | 1 |
| increased skin papilloma incidence | 1 |
+38 more (showing top 25).
Additional cross-species homologs
Sequence homologs in species beyond Ensembl Compara’s model organisms, by Diamond local protein alignment (% sequence identity; best hit per species). Lower-identity rows are more distant homologs. The matched accessions’ gene symbols aren’t in biobtree yet, so each row shows the UniProt accession.
| Organism | UniProt | Identity | Method |
|---|---|---|---|
| Pan troglodytes | A5A6J7 | 100.0% | Diamond |
| Coprinopsis cinerea okayama7#130 | A8NU18 | 100.0% | Diamond |
| Drosophila ananassae | B3M185 | 100.0% | Diamond |
| Drosophila erecta | B3NZR4 | 100.0% | Diamond |
| Drosophila persimilis | B4GFJ8 | 100.0% | Diamond |
| Drosophila sechellia | B4HKC7 | 100.0% | Diamond |
| Drosophila yakuba | B4PUP5 | 100.0% | Diamond |
| Crocodylus siamensis | C0HM48 | 100.0% | Diamond |
| Gallus gallus | P08642 | 100.0% | Diamond |
| Cryptococcus deneoformans JEC21 | P0CQ42 | 100.0% | Diamond |
| Cryptococcus deneoformans B-3501A | P0CQ43 | 100.0% | Diamond |
| Candida albicans | P0CY32 | 100.0% | Diamond |
| Bos taurus | P61223 | 100.0% | Diamond |
| Saguinus oedipus | P63320 | 100.0% | Diamond |
| Drosophila simulans | P83831 | 100.0% | Diamond |
| Drosophila mauritiana | P83832 | 100.0% | Diamond |
| Coprinopsis cinerea | Q05058 | 100.0% | Diamond |
| Sus scrofa | Q06AU2 | 100.0% | Diamond |
| Drosophila pseudoobscura pseudoobscura | Q295X7 | 100.0% | Diamond |
| Macaca fascicularis | Q4R9D4 | 100.0% | Diamond |
| Candida albicans SC5314 | Q59XU5 | 100.0% | Diamond |
| Pongo abelii | Q5R4B8 | 100.0% | Diamond |
| Mesocricetus auratus | Q60529 | 100.0% | Diamond |
| Xenopus tropicalis | Q640R7 | 100.0% | Diamond |
| Xenopus laevis | Q7ZXH7 | 100.0% | Diamond |
| Drosophila grimshawi | B4JFU8 | 99.5% | Diamond |
| Drosophila virilis | B4LY29 | 99.5% | Diamond |
| Cavia porcellus | P12825 | 99.5% | Diamond |
| Candida albicans WO-1 | C4YKT4 | 99.0% | Diamond |
| Oryzias latipes | O42277 | 99.0% | Diamond |
| Carassius auratus | P05774 | 99.0% | Diamond |
| Meleagris gallopavo | P79800 | 99.0% | Diamond |
| Monodelphis domestica | Q07983 | 99.0% | Diamond |
| Kryptolebias marmoratus | Q5EFX7 | 99.0% | Diamond |
| Cyprinus carpio | Q9YH38 | 99.0% | Diamond |
| NS.C58 murine sarcoma virus | P23175 | 99.5% | Diamond |
| Moloney murine sarcoma virus | P01113 | 99.0% | Diamond |
| Rasheed rat sarcoma virus | P01114 | 99.0% | Diamond |
| Harvey murine sarcoma virus | P01115 | 98.9% | Diamond |
Genomic neighbors (locus context)
Genes flanking this one on the chromosome (NCBI/Entrez gene neighborhood). Positional context only — some neighbors share regulatory elements (bidirectional promoters, antisense/overlapping transcripts), but chromosomal adjacency is not itself a functional relationship (see Interactions for that).
| Symbol | Type | Entrez |
|---|---|---|
| LMNTD2 | protein-coding | 256329 |
| ANO9 | protein-coding | 338440 |
| RNH1 | protein-coding | 6050 |
| LMNTD2-AS1 | ncRNA | 692247 |
| RASSF7 | protein-coding | 8045 |
| PTDSS2 | protein-coding | 81490 |
| LRRC56 | protein-coding | 115399 |
| SIGIRR | protein-coding | 59307 |
| MIR210HG | ncRNA | 100506211 |
| MIR210 | ncRNA | 406992 |
Protein
Protein identifiers
GTPase HRas — P01112 (reviewed: P01112)
Alternative names: H-Ras-1, Ha-Ras, Transforming protein p21, c-H-ras, p21ras
All UniProt accessions (5): A0A804HJ06, A0A804HKM6, A0A8C8MQR2, P01112, X5D945
UniProt curated annotations — full annotation on UniProt →
Function. Signal transducer in the Ras-MAPK signaling pathway that regulates cell proliferation and survival. Ras proteins bind GDP/GTP and possess intrinsic GTPase activity. Recognized by LZTR1 that mediates its ubiquitination by a BCR (BTB-CUL3-RBX1) E3 ubiquitin-protein ligase complex.
Subunit / interactions. In its GTP-bound form interacts with PLCE1. Interacts with TBC1D10C. Interacts with RGL3. Interacts with HSPD1. Found in a complex with at least BRAF, HRAS, MAP2K1, MAPK3 and RGS14. Interacts (active GTP-bound form) with RGS14 (via RBD 1 domain). Forms a signaling complex with RASGRP1 and DGKZ. Interacts with RASSF5. Interacts with PDE6D. Interacts with IKZF3. Interacts with RACK1. Interacts with PIK3CG; the interaction is required for membrane recruitment and beta-gamma G protein dimer-dependent activation of the PI3K gamma complex PIK3CG:PIK3R6. Interacts with RAPGEF2. Interacts (active GTP-bound form) with both SHOC2 and PP1c (all isoforms) to form a tertiary complex; SHOC2 and PP1c preferably bind M-Ras/MRAS, but they also bind K-Ras/KRAS, N-Ras/NRAS and H-Ras/HRAS. Interacts (GTP-bound form) with MAPKAP1/SIN1; inhibiting H-Ras/HRAS activity. Interacts (GDP-bound form) with LZTR1; this interaction mediates HRAS ubiquitination by BCR E3 ligase complex.
Subcellular location. Cell membrane. Golgi apparatus. Golgi apparatus membrane Nucleus. Cytoplasm. Perinuclear region.
Tissue specificity. Widely expressed.
Post-translational modifications. Palmitoylated by the ZDHHC9-GOLGA7 complex. A continuous cycle of de- and re-palmitoylation regulates rapid exchange between plasma membrane and Golgi. S-nitrosylated; critical for redox regulation. Important for stimulating guanine nucleotide exchange. No structural perturbation on nitrosylation. The covalent modification of cysteine by 15-deoxy-Delta12,14-prostaglandin-J2 is autocatalytic and reversible. It may occur as an alternative to other cysteine modifications, such as S-nitrosylation and S-palmitoylation. Acetylation at Lys-104 prevents interaction with guanine nucleotide exchange factors (GEFs). Fatty-acylated at Lys-170. Ubiquitinated by the BCR(LZTR1) E3 ubiquitin ligase complex at Lys-170 in a non-degradative manner, leading to inhibit Ras signaling by decreasing Ras association with membranes. (Microbial infection) Glucosylated at Thr-35 by P.sordellii toxin TcsL. Monoglucosylation completely prevents the recognition of the downstream effector, blocking the GTPases in their inactive form, leading to inhibit Ras signaling.
Disease relevance. Costello syndrome (CSTLO) [MIM:218040] A rare condition characterized by prenatally increased growth, postnatal growth deficiency, intellectual disability, distinctive facial appearance, cardiovascular abnormalities (typically pulmonic stenosis, hypertrophic cardiomyopathy and/or atrial tachycardia), tumor predisposition, skin and musculoskeletal abnormalities. The disease is caused by variants affecting the gene represented in this entry. Congenital myopathy with excess of muscle spindles (CMEMS) [MIM:218040] Variant of Costello syndrome. The disease is caused by variants affecting the gene represented in this entry. Thyroid cancer, non-medullary, 2 (NMTC2) [MIM:188470] A form of non-medullary thyroid cancer (NMTC), a cancer characterized by tumors originating from the thyroid follicular cells. NMTCs represent approximately 95% of all cases of thyroid cancer and are classified into papillary, follicular, Hurthle cell, and anaplastic neoplasms. Disease susceptibility is associated with variants affecting the gene represented in this entry. Mutations which change positions 12, 13 or 61 activate the potential of HRAS to transform cultured cells and are implicated in a variety of human tumors. Bladder cancer (BLC) [MIM:109800] A malignancy originating in tissues of the urinary bladder. It often presents with multiple tumors appearing at different times and at different sites in the bladder. Most bladder cancers are transitional cell carcinomas that begin in cells that normally make up the inner lining of the bladder. Other types of bladder cancer include squamous cell carcinoma (cancer that begins in thin, flat cells) and adenocarcinoma (cancer that begins in cells that make and release mucus and other fluids). Bladder cancer is a complex disorder with both genetic and environmental influences. Disease susceptibility is associated with variants affecting the gene represented in this entry. Schimmelpenning-Feuerstein-Mims syndrome (SFM) [MIM:163200] A disease characterized by sebaceous nevi, often on the face, associated with variable ipsilateral abnormalities of the central nervous system, ocular anomalies, and skeletal defects. Many oral manifestations have been reported, not only including hypoplastic and malformed teeth, and mucosal papillomatosis, but also ankyloglossia, hemihyperplastic tongue, intraoral nevus, giant cell granuloma, ameloblastoma, bone cysts, follicular cysts, oligodontia, and odontodysplasia. Sebaceous nevi follow the lines of Blaschko and these can continue as linear intraoral lesions, as in mucosal papillomatosis. The disease is caused by variants affecting the gene represented in this entry.
Activity regulation. Alternates between an inactive form bound to GDP and an active form bound to GTP. Activated by a guanine nucleotide-exchange factor (GEF) and inactivated by a GTPase-activating protein (GAP).
Similarity. Belongs to the small GTPase superfamily. Ras family.
Isoforms (2)
| UniProt ID | Names | Canonical? |
|---|---|---|
| P01112-1 | 1, H-Ras4A, p21 | yes |
| P01112-2 | 2, H-RasIDX, p19 |
RefSeq proteins (4): NP_001123914, NP_001304983, NP_005334, NP_789765 (=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR001806 | Small_GTPase | Family |
| IPR005225 | Small_GTP-bd | Domain |
| IPR020849 | Small_GTPase_Ras-type | Family |
| IPR027417 | P-loop_NTPase | Homologous_superfamily |
Pfam: PF00071
Enzyme classification (BRENDA)
- EC 3.6.5.2 — small monomeric GTPase (BRENDA: 49 organisms, 138 substrates, 55 inhibitors, 5 Km, 1 kcat entries)
Substrate kinetics (BRENDA)
1 substrates with measured Km, best-characterized 1. Km ranges are aggregated across organisms/conditions.
| Substrate | Km (mM) | Measurements |
|---|---|---|
| GTP | — | 0 |
Catalyzed reactions (Rhea)
- GTP + H2O = GDP + phosphate + H(+) (RHEA:19669)
UniProt features (82 total): mutagenesis site 22, sequence variant 19, strand 11, helix 6, binding site 5, modified residue 4, lipid moiety-binding region 4, chain 2, turn 2, initiator methionine 1, glycosylation site 1, cross-link 1, splice variant 1, propeptide 1, region of interest 1, short sequence motif 1
Structure
Experimental structures (PDB)
showing 30 of 256 structures by resolution:
| PDB | Title | Method | Resolution (Å) |
|---|---|---|---|
| 2CE2 | CRYSTAL STRUCTURE ANALYSIS OF A FLUORESCENT FORM OF H-RAS P21 IN COMPLEX WITH GDP | X-RAY DIFFRACTION | 1 |
| 2EVW | Crystal structure analysis of a fluorescent form of H-Ras p21 in complex with R-caged GTP | X-RAY DIFFRACTION | 1.05 |
| 24SQ | Human HRAS WT (GDP-bound) in complex with macrocyclic peptide inhibitor AP6296 | X-RAY DIFFRACTION | 1.08 |
| 8TBG | Tricomplex of RMC-7977, HRAS WT, and CypA | X-RAY DIFFRACTION | 1.2 |
| 2CLD | CRYSTAL STRUCTURE ANALYSIS OF A FLUORESCENT FORM OF H-RAS P21 IN COMPLEX WITH GDP (2) | X-RAY DIFFRACTION | 1.22 |
| 2CL6 | CRYSTAL STRUCTURE ANALYSIS OF A FLUORESCENT FORM OF H-RAS P21 IN COMPLEX WITH S-caged GTP | X-RAY DIFFRACTION | 1.24 |
| 2CL7 | CRYSTAL STRUCTURE ANALYSIS OF A FLUORESCENT FORM OF H-RAS P21 IN COMPLEX WITH GTP | X-RAY DIFFRACTION | 1.25 |
| 5WDQ | H-Ras mutant L120A bound to GMP-PNP at 100K | X-RAY DIFFRACTION | 1.25 |
| 1CTQ | STRUCTURE OF P21RAS IN COMPLEX WITH GPPNHP AT 100 K | X-RAY DIFFRACTION | 1.26 |
| 2CLC | CRYSTAL STRUCTURE ANALYSIS OF A FLUORESCENT FORM OF H-RAS P21 IN COMPLEX WITH GTP (2) | X-RAY DIFFRACTION | 1.3 |
| 3K8Y | Allosteric modulation of H-Ras GTPase | X-RAY DIFFRACTION | 1.3 |
| 3OIW | H-RasG12V with allosteric switch in the “on” state | X-RAY DIFFRACTION | 1.3 |
| 3TGP | Room temperature H-ras | X-RAY DIFFRACTION | 1.31 |
| 4DLR | H-Ras PEG 400/Ca(OAc)2, ordered off | X-RAY DIFFRACTION | 1.32 |
| 3OIU | H-RasQ61L with allosteric switch in the “on” state | X-RAY DIFFRACTION | 1.32 |
| 8BWG | HRas (1-166) Y64 phosphorylation | X-RAY DIFFRACTION | 1.32 |
| 2RGB | Crystal structure of H-RasQ61K-GppNHp | X-RAY DIFFRACTION | 1.35 |
| 5P21 | REFINED CRYSTAL STRUCTURE OF THE TRIPHOSPHATE CONFORMATION OF H-RAS P21 AT 1.35 ANGSTROMS … | X-RAY DIFFRACTION | 1.35 |
| 5WDP | H-Ras mutant L120A bound to GMP-PNP at 277K | X-RAY DIFFRACTION | 1.35 |
| 8CNJ | HRas(1-166) in complex with GDP and BeF3- | X-RAY DIFFRACTION | 1.35 |
| 3I3S | Crystal Structure of H-Ras with Thr50 replaced by Isoleucine | X-RAY DIFFRACTION | 1.36 |
| 2RGE | Crystal structure of H-Ras-GppNHp | X-RAY DIFFRACTION | 1.4 |
| 3RS0 | H-Ras soaked in neat cyclopentanol: one of 10 in MSCS set | X-RAY DIFFRACTION | 1.4 |
| 9PU1 | HRAS complex with UM0140401 compound | X-RAY DIFFRACTION | 1.4 |
| 9PU8 | HRAS complex with UM0140693 compound | X-RAY DIFFRACTION | 1.4 |
| 5E95 | Crystal Structure of Mb(NS1)/H-Ras Complex | X-RAY DIFFRACTION | 1.4 |
| 3L8Z | H-Ras wildtype new crystal form | X-RAY DIFFRACTION | 1.44 |
| 2RGG | Crystal structure of H-RasQ61I-GppNHp, trigonal crystal form | X-RAY DIFFRACTION | 1.45 |
| 8CNN | BeF3 Phospho-HRas GSA complex | X-RAY DIFFRACTION | 1.48 |
| 2QUZ | Crystal Structure of the activating H-RasK117R mutant in Costello Syndrome, bound to … | X-RAY DIFFRACTION | 1.49 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-P01112-F1 | 92.50 | 0.79 |
Antibody-complex structures (SAbDab)
2 antibodies co-crystallized with this protein: 2UZI, 2VH5
Human Protein Atlas
Protein class: Enzymes, ENZYME proteins, Hydrolases, Predicted intracellular proteins, Plasma proteins, RAS pathway related proteins, Cancer-related genes, Candidate cancer biomarkers, Mutated cancer genes, Mutational cancer driver genes, Disease related genes, Potential drug targets, Human disease related genes, Congenital malformations, Congenital malformations of skin, Other congenital malformations
Protein evidence: Evidence at protein level
Subcellular location (HPA, imaging): cytosol; basal body; nucleoplasm
Antibody reliability (HPA): IH supported · IF supported
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Ligand- & substrate-binding residues (5)
| Position | Role |
|---|---|
| 145–147 | GTP |
| 13–18 | GTP |
| 29–35 | GTP |
| 59–60 | GTP |
| 116–119 | GTP |
Post-translational modifications (9)
| Type | Positions |
|---|---|
| N-acetylmethionine | 1 |
| N-acetylthreonine | 2 |
| S-nitrosocysteine | 118 |
| Cysteine methyl ester | 186 |
| S-palmitoyl cysteine | 181, 184 |
| S-(15-deoxy-delta12,14-prostaglandin j2-9-yl)cysteine | 184 |
| S-farnesyl cysteine | 186 |
| Glycyl lysine isopeptide (lys-gly) (interchain with g-cter in ubiquitin) | 170 |
Glycosylation sites (1)
| Type | Positions |
|---|---|
| (microbial infection) o-linked (glc) threonine | 35 |
Mutagenesis-validated functional residues (22)
| Position | Phenotype |
|---|---|
| 17 | dominant negative. prevents plce1 egf-induced recruitment to plasma membrane. no effect on subcellular location of isoform 2. |
| 26 | loss of interaction with plce1; when associated with v-12. |
| 29 | no effect on interaction with plce1; when associated with v-12. |
| 32 | loss of interaction and recruitment to plasma membrane of plce1; when associated with v-12. |
| 34 | no effect on interaction with plce1; when associated with v-12. |
| 35 | loss of interaction with plce1; when associated with v-12. |
| 37 | no effect on interaction with plce1; when associated with v-12. |
| 38 | no effect on interaction with plce1; when associated with v-12. |
| 39 | no effect on interaction with plce1; when associated with v-12. |
| 59 | loss of gtpase activity and creation of an autophosphorylation site. |
| 61 | moderately increased transformation of cultured cell lines. |
| 61 | promotes interaction with shoc2 and pp1c. |
| 61 | strongly increased transformation of cultured cell lines. |
| 83 | gtp-binding activity reduced by factor of 30. |
| 118 | abolishes s-nitrosylation. no stimulation of guanine nucleotide exchange. |
| 119 | loss of gtp-binding activity. |
| 144 | gtp-binding activity reduced by factor of 25. |
| 164–165 | loss of gtp-binding activity. |
| 167–185 | in h-ras-3kr mutant; decreased fatty-acylation. |
| 170 | increased ras signaling due to impaired ubiquitination. |
| 181 | exclusively localized in golgi. non-specifically localized on all endomembranes; when associated with s-184. |
| 184 | loss of s-(15-deoxy-delta12,14-prostaglandin j2-9-yl)cysteine stimulation of ras-gtpase activity. mainly localized in golgi … |
Function
Pathways and Gene Ontology
Reactome pathways
56 curated (TAS) of 142; 37 disease pathways. Curated-first; evidence = TAS (manually curated) vs IEA (electronic inference).
showing 60 of 142 pathways:
| ID | Pathway | Evidence |
|---|---|---|
| R-HSA-5637810 | Constitutive Signaling by EGFRvIII ⚕ | curated |
| R-HSA-1236382 | Constitutive Signaling by Ligand-Responsive EGFR Cancer Variants ⚕ | curated |
| R-HSA-9634285 | Constitutive Signaling by Overexpressed ERBB2 ⚕ | curated |
| R-HSA-6802955 | Paradoxical activation of RAF signaling by kinase inactive BRAF ⚕ | curated |
| R-HSA-6802953 | RAS signaling downstream of NF1 loss-of-function variants ⚕ | curated |
| R-HSA-6802952 | Signaling by BRAF and RAF1 fusions ⚕ | curated |
| R-HSA-9665348 | Signaling by ERBB2 ECD mutants ⚕ | curated |
| R-HSA-9664565 | Signaling by ERBB2 KD Mutants ⚕ | curated |
| R-HSA-9665686 | Signaling by ERBB2 TMD/JMD mutants ⚕ | curated |
| R-HSA-5655302 | Signaling by FGFR1 in disease ⚕ | curated |
| R-HSA-5655253 | Signaling by FGFR2 in disease ⚕ | curated |
| R-HSA-5655332 | Signaling by FGFR3 in disease ⚕ | curated |
| R-HSA-5655291 | Signaling by FGFR4 in disease ⚕ | curated |
| R-HSA-9703648 | Signaling by FLT3 ITD and TKD mutants ⚕ | curated |
| R-HSA-9703465 | Signaling by FLT3 fusion proteins ⚕ | curated |
| R-HSA-9673770 | Signaling by PDGFRA extracellular domain mutants ⚕ | curated |
| R-HSA-9673767 | Signaling by PDGFRA transmembrane, juxtamembrane and kinase domain mutants ⚕ | curated |
| R-HSA-9656223 | Signaling by RAF1 mutants ⚕ | curated |
| R-HSA-9753510 | Signaling by RAS GAP mutants ⚕ | curated |
| R-HSA-9753512 | Signaling by RAS GTPase mutants ⚕ | curated |
| R-HSA-6802948 | Signaling by high-kinase activity BRAF mutants ⚕ | curated |
| R-HSA-6802946 | Signaling by moderate kinase activity BRAF mutants ⚕ | curated |
| R-HSA-9670439 | Signaling by phosphorylated juxtamembrane, extracellular and kinase domain KIT mutants ⚕ | curated |
| R-HSA-9649948 | Signaling downstream of RAS mutants ⚕ | curated |
| R-HSA-1169092 | Activation of RAS in B cells | curated |
| R-HSA-5621575 | CD209 (DC-SIGN) signaling | curated |
| R-HSA-2424491 | DAP12 signaling | curated |
| R-HSA-186763 | Downstream signal transduction | curated |
| R-HSA-2179392 | EGFR Transactivation by Gastrin | curated |
| R-HSA-3928662 | EPHB-mediated forward signaling | curated |
| R-HSA-9634635 | Estrogen-stimulated signaling through PRKCZ | curated |
| R-HSA-2871796 | FCERI mediated MAPK activation | curated |
| R-HSA-9607240 | FLT3 Signaling | curated |
| R-HSA-5654693 | FRS-mediated FGFR1 signaling | curated |
| R-HSA-5654700 | FRS-mediated FGFR2 signaling | curated |
| R-HSA-5654706 | FRS-mediated FGFR3 signaling | curated |
| R-HSA-5654712 | FRS-mediated FGFR4 signaling | curated |
| R-HSA-179812 | GRB2 events in EGFR signaling | curated |
| R-HSA-5674135 | MAP2K and MAPK activation | curated |
| R-HSA-8851805 | MET activates RAS signaling | curated |
| R-HSA-375165 | NCAM signaling for neurite out-growth | curated |
| R-HSA-5675221 | Negative regulation of MAPK pathway | curated |
| R-HSA-8849471 | PTK6 Regulates RHO GTPases, RAS GTPase and MAP kinases | curated |
| R-HSA-5673000 | RAF activation | curated |
| R-HSA-5673001 | RAF/MAP kinase cascade | curated |
| R-HSA-9648002 | RAS processing | curated |
| R-HSA-5658442 | Regulation of RAS by GAPs | curated |
| R-HSA-5654688 | SHC-mediated cascade:FGFR1 | curated |
| R-HSA-5654699 | SHC-mediated cascade:FGFR2 | curated |
| R-HSA-5654704 | SHC-mediated cascade:FGFR3 | curated |
| R-HSA-5654719 | SHC-mediated cascade:FGFR4 | curated |
| R-HSA-180336 | SHC1 events in EGFR signaling | curated |
| R-HSA-1250347 | SHC1 events in ERBB4 signaling | curated |
| R-HSA-1433557 | Signaling by SCF-KIT | curated |
| R-HSA-210993 | Tie2 Signaling | curated |
| R-HSA-5218921 | VEGFR2 mediated cell proliferation | curated |
| R-HSA-1643685 | Disease ⚕ | — |
| R-HSA-5663202 | Diseases of signal transduction by growth factor receptors and second messengers ⚕ | — |
| R-HSA-9682385 | FLT3 signaling in disease ⚕ | — |
| R-HSA-6802957 | Oncogenic MAPK signaling ⚕ | — |
MSigDB gene sets: 1170 (showing top):
PID_BCR_5PATHWAY, PID_SHP2_PATHWAY, REACTOME_SIGNALING_BY_INSULIN_RECEPTOR, GOBP_RESPONSE_TO_NITROGEN_COMPOUND, GOBP_NEGATIVE_REGULATION_OF_NEURON_APOPTOTIC_PROCESS, GOBP_RESPONSE_TO_IONIZING_RADIATION, BIOCARTA_FMLP_PATHWAY, MODY_HIPPOCAMPUS_POSTNATAL, REACTOME_INNATE_IMMUNE_SYSTEM, GOBP_REGULATION_OF_WOUND_HEALING, BIOCARTA_MAL_PATHWAY, REACTOME_ADAPTIVE_IMMUNE_SYSTEM, REACTOME_CYTOKINE_SIGNALING_IN_IMMUNE_SYSTEM, GOBP_REGULATION_OF_NEURONAL_SYNAPTIC_PLASTICITY, KEGG_MAPK_SIGNALING_PATHWAY
GO Biological Process (31): MAPK cascade (GO:0000165), regulation of transcription by RNA polymerase II (GO:0006357), chemotaxis (GO:0006935), signal transduction (GO:0007165), cell surface receptor signaling pathway (GO:0007166), Ras protein signal transduction (GO:0007265), positive regulation of cell population proliferation (GO:0008284), negative regulation of cell population proliferation (GO:0008285), insulin receptor signaling pathway (GO:0008286), animal organ morphogenesis (GO:0009887), negative regulation of gene expression (GO:0010629), Schwann cell development (GO:0014044), positive regulation of cell migration (GO:0030335), regulation of actin cytoskeleton organization (GO:0032956), regulation of cell population proliferation (GO:0042127), myelination (GO:0042552), positive regulation of MAPK cascade (GO:0043410), positive regulation of transcription by RNA polymerase II (GO:0045944), positive regulation of JNK cascade (GO:0046330), positive regulation of Ras protein signal transduction (GO:0046579), positive regulation of epithelial cell proliferation (GO:0050679), regulation of cell cycle (GO:0051726), adipose tissue development (GO:0060612), positive regulation of ERK1 and ERK2 cascade (GO:0070374), cellular response to gamma radiation (GO:0071480), positive regulation of wound healing (GO:0090303), positive regulation of protein targeting to membrane (GO:0090314), cellular senescence (GO:0090398), regulation of neurotransmitter receptor localization to postsynaptic specialization membrane (GO:0098696), positive regulation of ruffle assembly (GO:1900029), positive regulation of miRNA metabolic process (GO:2000630)
GO Molecular Function (9): GTPase activity (GO:0003924), G protein activity (GO:0003925), GTP binding (GO:0005525), GDP binding (GO:0019003), protein-membrane adaptor activity (GO:0043495), phospholipase C activator activity (GO:0160185), nucleotide binding (GO:0000166), protein binding (GO:0005515), hydrolase activity (GO:0016787)
GO Cellular Component (12): Golgi membrane (GO:0000139), nucleoplasm (GO:0005654), cytoplasm (GO:0005737), endoplasmic reticulum membrane (GO:0005789), Golgi apparatus (GO:0005794), cytosol (GO:0005829), plasma membrane (GO:0005886), perinuclear region of cytoplasm (GO:0048471), glutamatergic synapse (GO:0098978), nucleus (GO:0005634), endomembrane system (GO:0012505), membrane (GO:0016020)
Reactome top-level categories
18 top-level categories:
| Category | Pathways |
|---|---|
| Signaling by ERBB2 | 2 |
| Signaling by EGFR | 2 |
| IRS-mediated signalling | 1 |
| Downstream signaling events of B Cell Receptor (BCR) | 1 |
| Signaling by Ligand-Responsive EGFR Variants in Cancer | 1 |
| Signaling by ERBB4 | 1 |
| Signaling by Receptor Tyrosine Kinases | 1 |
| Signalling to ERKs | 1 |
| Signalling to RAS | 1 |
| Signaling by PDGF | 1 |
| Cell surface interactions at the vascular wall | 1 |
| Gastrin-CREB signalling pathway via PKC and MAPK | 1 |
| DAP12 interactions | 1 |
| IGF1R signaling cascade | 1 |
| Fc epsilon receptor (FCERI) signaling | 1 |
| Axon guidance | 1 |
| EPH-Ephrin signaling | 1 |
| CREB1 phosphorylation through NMDA receptor-mediated activation of RAS signaling | 1 |
GO top-level categories
showing 60 of 72 GO namespaces:
| Category | Terms |
|---|---|
| cellular anatomical structure | 6 |
| cell population proliferation | 3 |
| cytoplasm | 3 |
| transcription by RNA polymerase II | 2 |
| regulation of cellular process | 2 |
| regulation of cell population proliferation | 2 |
| guanyl ribonucleotide binding | 2 |
| anion binding | 2 |
| intracellular membrane-bounded organelle | 2 |
| intracellular signaling cassette | 1 |
| regulation of DNA-templated transcription | 1 |
| response to chemical | 1 |
| taxis | 1 |
| cell communication | 1 |
| cellular process | 1 |
| signaling | 1 |
| cellular response to stimulus | 1 |
| signal transduction | 1 |
| small GTPase-mediated signal transduction | 1 |
| positive regulation of cellular process | 1 |
| negative regulation of cellular process | 1 |
| cell surface receptor protein tyrosine kinase signaling pathway | 1 |
| cellular response to insulin stimulus | 1 |
| anatomical structure morphogenesis | 1 |
| animal organ development | 1 |
| gene expression | 1 |
| regulation of gene expression | 1 |
| negative regulation of macromolecule biosynthetic process | 1 |
| Schwann cell differentiation | 1 |
| glial cell development | 1 |
| cell migration | 1 |
| regulation of cell migration | 1 |
| positive regulation of cell motility | 1 |
| actin cytoskeleton organization | 1 |
| regulation of actin filament-based process | 1 |
| regulation of cytoskeleton organization | 1 |
| axon ensheathment | 1 |
| MAPK cascade | 1 |
| regulation of MAPK cascade | 1 |
| positive regulation of intracellular signal transduction | 1 |
| regulation of transcription by RNA polymerase II | 1 |
| positive regulation of DNA-templated transcription | 1 |
| JNK cascade | 1 |
| positive regulation of MAPK cascade | 1 |
| regulation of JNK cascade | 1 |
| Ras protein signal transduction | 1 |
| regulation of Ras protein signal transduction | 1 |
| positive regulation of small GTPase mediated signal transduction | 1 |
| ribonucleoside triphosphate phosphatase activity | 1 |
| GTPase activity | 1 |
| molecular function regulator activity | 1 |
| purine ribonucleoside triphosphate binding | 1 |
| protein-macromolecule adaptor activity | 1 |
| C-type glycerophospholipase activity | 1 |
| phospholipase activator activity | 1 |
| nucleoside phosphate binding | 1 |
| heterocyclic compound binding | 1 |
| binding | 1 |
| catalytic activity | 1 |
| Golgi apparatus | 1 |
Experimentally-supported GO annotations
GO terms backed by direct experimental evidence (ECO experimental codes) — 30 of 52 annotations. The rest are phylogenetic / computational / electronic (IEA).
30 experimentally-supported GO terms:
Protein interactions and networks
STRING
showing 15 of 4,618 interactions by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| HRAS | BRAF | P15056 | 929 |
| HRAS | TP53 | P04637 | 883 |
| HRAS | MYC | P01106 | 849 |
| HRAS | EGFR | P00533 | 831 |
| HRAS | MAP2K1 | Q02750 | 828 |
| HRAS | PTPN11 | Q06124 | 827 |
| HRAS | PIK3CA | P42336 | 826 |
| HRAS | CDKN2A | P42771 | 821 |
| HRAS | RAF1 | P04049 | 813 |
| HRAS | AKT1 | P31749 | 811 |
| HRAS | SOS1 | Q07889 | 807 |
| HRAS | PTEN | P60484 | 798 |
| HRAS | RALGDS | Q12967 | 773 |
| HRAS | NF1 | P21359 | 745 |
| HRAS | CTNNB1 | P35222 | 741 |
IntAct
Human interaction partners of HRAS in IntAct, one row per partner (best MIscore; records = supporting IntAct interaction records).
showing 30 of 184 partners by confidence:
| Partner | Interaction type | MIscore | Records |
|---|---|---|---|
| RAF1 | physical association | 0.980 | 28 |
| SOS1 | direct interaction | 0.940 | 11 |
| BRAF | direct interaction | 0.940 | 7 |
| RIN1 | physical association | 0.930 | 8 |
| ARAF | direct interaction | 0.850 | 3 |
| RGL1 | direct interaction | 0.740 | 3 |
| MTHFD2 | association | 0.730 | 3 |
| RAP1GDS1 | physical association | 0.690 | 2 |
| RASSF1 | physical association | 0.680 | 7 |
| RALGDS | direct interaction | 0.680 | 3 |
| MRFAP1 | physical association | 0.670 | 3 |
| BLZF1 | physical association | 0.660 | 3 |
| CHMP7 | physical association | 0.660 | 3 |
| RGL2 | association | 0.660 | 3 |
| STIM1 | physical association | 0.660 | 3 |
| NF1 | physical association | 0.600 | 2 |
| RASSF5 | physical association | 0.590 | 4 |
| UBIAD1 | colocalization | 0.580 | 9 |
| FANCI | proximity | 0.570 | 5 |
| RALA | direct interaction | 0.570 | 1 |
| SRC | direct interaction | 0.570 | 1 |
| PCDHGC3 | physical association | 0.560 | 4 |
| AKAP9 | physical association | 0.560 | 3 |
| AP3M2 | physical association | 0.560 | 3 |
| ARHGEF38 | physical association | 0.560 | 3 |
| ATP5IF1 | physical association | 0.560 | 3 |
| AUNIP | physical association | 0.560 | 3 |
| BEX3 | physical association | 0.560 | 3 |
| BRMS1L | physical association | 0.560 | 3 |
| BRPF3 | physical association | 0.560 | 3 |
BioGRID (996 interactions; top human partners by supporting records in a sample of 600 records): RAF1 (Affinity Capture-Western; 13 records), LZTR1 (Affinity Capture-MS; 8 records), BRAF (Affinity Capture-MS; 5 records), MTOR (Proximity Label-MS; 5 records), BSG (Proximity Label-MS; 3 records), F11R (Proximity Label-MS; 3 records), FAM129B (Affinity Capture-Western; 3 records), LYN (Proximity Label-MS; 3 records), MARK2 (Proximity Label-MS; 3 records), MPZL1 (Proximity Label-MS; 3 records), NOTCH1 (Proximity Label-MS; 3 records), NUMB (Proximity Label-MS; 3 records), PI4KA (Proximity Label-MS; 3 records), PVRL2 (Proximity Label-MS; 3 records), RALGDS (Two-hybrid; 3 records)
SIGNOR signaling
showing 35 of 43 signaling interactions:
| A | Effect | B | Mechanism |
|---|---|---|---|
| RIN1 | up-regulates | HRAS | binding |
| HRAS | “up-regulates activity” | BRAF | binding |
| HRAS | up-regulates | BRAF | binding |
| RASGEF1C | up-regulates | HRAS | binding |
| HRAS | up-regulates | ARAF | binding |
| HRAS | “up-regulates activity” | PIK3CB | binding |
| HRAS | up-regulates | PIK3CD | binding |
| HRAS | up-regulates | PIK3CG | binding |
| SOS2 | up-regulates | HRAS | “guanine nucleotide exchange factor” |
| RAPGEF5 | up-regulates | HRAS | “guanine nucleotide exchange factor” |
| RAPGEF6 | up-regulates | HRAS | “guanine nucleotide exchange factor” |
| RASGEF1A | up-regulates | HRAS | binding |
| RASGEF1B | up-regulates | HRAS | binding |
| NF1 | “down-regulates activity” | HRAS | “gtpase-activating protein” |
| HRAS | up-regulates | RAF1 | binding |
| FNTB | “up-regulates activity” | HRAS | |
| FNTA | “up-regulates activity” | HRAS | |
| SRC | “down-regulates activity” | HRAS | phosphorylation |
| PTPN11 | “up-regulates activity” | HRAS | dephosphorylation |
| DAB2IP | “down-regulates activity” | HRAS | “gtpase-activating protein” |
| NF1 | “down-regulates activity” | HRAS | |
| UBIAD1 | “down-regulates activity” | HRAS | binding |
| HRAS | “up-regulates activity” | GATA2 | phosphorylation |
| GOLGA7 | “up-regulates activity” | HRAS | palmitoylation |
| ZDHHC9 | “up-regulates activity” | HRAS | palmitoylation |
| NIBAN2 | “up-regulates activity” | HRAS | binding |
| HRAS | up-regulates | PIK3CA | binding |
| SOS1 | “up-regulates activity” | HRAS | “guanine nucleotide exchange factor” |
| RASA1 | down-regulates | HRAS | binding |
| GNAQ | up-regulates | HRAS | binding |
| PLCE1 | up-regulates | HRAS | “guanine nucleotide exchange factor” |
| HRAS | “up-regulates activity” | JUN | phosphorylation |
| HRAS | “up-regulates activity” | PIK3CA | binding |
| HRAS | “up-regulates activity” | PI3K | binding |
| MVD | “up-regulates quantity by stabilization” | HRAS |
Protein complexes (CORUM) (6)
Experimentally-characterized complexes this protein is a subunit of (★ = the complex contains a known drug target).
6 complexes by size:
| Complex | Subunits | Members |
|---|---|---|
| HRAS-IRAK1-IRAK2-TRAF6 complex | 4 | HRAS, IRAK1, IRAK2, TRAF6 |
| ABL2-HRAS-RIN1 complex | 3 | ABL2, HRAS, RIN1 |
| DGKZ-RASGRP1-HRAS complex | 3 | DGKZ, HRAS, RASGRP1 |
| ★ AURKA-HRAS-RAF1 complex | 3 | HRAS, RAF1, AURKA |
| HRAS-PPP1CC-SHOC2 complex | 3 | HRAS, PPP1CC, SHOC2 |
| ★ HRAS-RAF1 complex | 2 | HRAS, RAF1 |
Enriched among interaction partners
Reactome pathways and GO biological processes over-represented among this gene’s 184 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.
Reactome pathways:
| Pathway | Partners | Fold | FDR |
|---|---|---|---|
| CD28 dependent PI3K/Akt signaling | 7 | 22.2× | 8e-06 |
| RAF activation | 6 | 16.2× | 1e-04 |
| Downstream signal transduction | 5 | 15.3× | 8e-04 |
| Oncogenic MAPK signaling | 7 | 14.0× | 8e-05 |
| FLT3 Signaling | 5 | 13.9× | 1e-03 |
| Signaling by CSF1 (M-CSF) in myeloid cells | 5 | 13.9× | 1e-03 |
| Bacterial Infection Pathways | 5 | 13.5× | 1e-03 |
| Signaling by EGFR | 5 | 13.2× | 1e-03 |
GO biological processes:
| GO term | Partners | Fold | FDR |
|---|---|---|---|
| positive regulation of peptidyl-serine phosphorylation | 5 | 23.2× | 1e-03 |
| mismatch repair | 5 | 19.6× | 1e-03 |
| insulin-like growth factor receptor signaling pathway | 5 | 15.0× | 4e-03 |
| Ras protein signal transduction | 12 | 14.9× | 4e-08 |
| positive regulation of miRNA transcription | 6 | 10.6× | 4e-03 |
| epidermal growth factor receptor signaling pathway | 7 | 10.5× | 1e-03 |
| phosphatidylinositol 3-kinase/protein kinase B signal transduction | 7 | 8.9× | 3e-03 |
| MAPK cascade | 9 | 8.4× | 1e-03 |
Disease & clinical
Cancer significance
From CIViC — curated cancer-variant interpretation:
HRAS is a member of the small GTPase family that upon activation by receptor tyrosine kinases stimulates downstream pathways including RAF-MEK-ERK and PI3K-AKT. In cancer, recurrent gain-of-function mutations at positions G12, G13, and Q61 result in an accumulation of GTP-bound HRAS, constitutive downstream signaling, and transformation. In TCGA, HRAS mutations were found more frequently in head and neck squamous cell carcinoma, bladder urothelial carcinoma, thyroid carcinoma, thymoma, skin cutaneous carcinoma, and pheochromocytoma/paraganglioma. Although development of HRAS inhibitors has not been possible, targeting the enzyme essential for farnesylating HRAS has recently shown benefit in HRAS driven cancers. The farnesyltransferase inhibitor (FTi) tipifarnib has been shown to cause HRAS mislocalization, decrease downstream signaling, and selectively impair proliferation, survival, and transformation of HRAS-mutant cells. Tipifarnib is in clinical development for HRAS-mutant cancers.
From intOGen — cancer-driver classification: activating (oncogene-like) across 14 cancer types — ANGS, BLCA, BRCA, COADREAD, CSCC, HNSC, LUSC, NPC, PGNG, PRAD, PROSTATE, THYM…(+2 more).
intOGen’s role is a computational inference from cohort mutation patterns and may diverge from the gene’s curated/literature role; read it alongside the evidence above.
Genetic variants
Variant evidence for HRAS: 668 ClinVar records (44 pathogenic / likely pathogenic); 13 ClinGen expert-panel interpretations; 7 CIViC cancer variants. Per-variant detail is on Sugi Variant.
ClinVar
668 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 21 |
| Likely pathogenic | 23 |
| Uncertain significance | 273 |
| Likely benign | 264 |
| Benign | 38 |
Top pathogenic / likely-pathogenic (15)
Showing the 15 best-reviewed of 44 pathogenic / likely-pathogenic ClinVar records, ranked by ClinVar review status (expert panel → multiple submitters → single submitter), then by number of submitting labs.
| Variant ID | HGVS | Classification | Review | Submitters |
|---|---|---|---|---|
| 12602 | NM_005343.4(HRAS):c.34G>A (p.Gly12Ser) | Pathogenic | reviewed by expert panel | 50 |
| 12606 | NM_005343.4(HRAS):c.37G>T (p.Gly13Cys) | Pathogenic | reviewed by expert panel | 24 |
| 12610 | NM_005343.4(HRAS):c.173C>T (p.Thr58Ile) | Pathogenic | reviewed by expert panel | 10 |
| 12605 | NM_005343.4(HRAS):c.350A>G (p.Lys117Arg) | Pathogenic | reviewed by expert panel | 6 |
| 40435 | NM_005343.4(HRAS):c.175G>A (p.Ala59Thr) | Likely pathogenic | reviewed by expert panel | 7 |
| 12604 | NM_005343.4(HRAS):c.38G>A (p.Gly13Asp) | Pathogenic | criteria provided, multiple submitters, no conflicts | 22 |
| 12613 | NM_005343.4(HRAS):c.34G>T (p.Gly12Cys) | Pathogenic | criteria provided, multiple submitters, no conflicts | 19 |
| 12600 | NM_005343.4(HRAS):c.35G>T (p.Gly12Val) | Pathogenic | criteria provided, multiple submitters, no conflicts | 13 |
| 12603 | NM_005343.4(HRAS):c.35G>C (p.Gly12Ala) | Pathogenic | criteria provided, multiple submitters, no conflicts | 11 |
| 1209208 | NM_005343.4(HRAS):c.35_36delinsTT (p.Gly12Val) | Pathogenic | criteria provided, multiple submitters, no conflicts | 6 |
| 12608 | NM_005343.4(HRAS):c.187G>A (p.Glu63Lys) | Pathogenic | criteria provided, multiple submitters, no conflicts | 3 |
| 40436 | NM_005343.4(HRAS):c.179G>A (p.Gly60Asp) | Pathogenic | criteria provided, multiple submitters, no conflicts | 3 |
| 391700 | NM_005343.4(HRAS):c.179G>T (p.Gly60Val) | Pathogenic | criteria provided, multiple submitters, no conflicts | 3 |
| 1810343 | NM_005343.4(HRAS):c.176C>G (p.Ala59Gly) | Pathogenic | criteria provided, multiple submitters, no conflicts | 2 |
| 160364 | NM_005343.4(HRAS):c.182A>G (p.Gln61Arg) | Likely pathogenic | criteria provided, multiple submitters, no conflicts | 8 |
Per-variant reference — Sugi Variant
Explore HRAS’s pathogenic and likely-pathogenic variants individually — each with its ClinVar classification and conditions, applied ACMG criteria (ClinGen expert panel, where curated), the calibrated in-silico predictors (AlphaMissense, REVEL, SaProt, conservation), gnomAD frequency, and the predictor-disagreement QC signal — on Sugi Variant.
ClinGen expert-panel interpretations (13)
Expert ACMG interpretations from RASopathy VCEP for Costello syndrome; RASopathy — a higher-authority tier than individual ClinVar submissions.
| Assertion | Variants |
|---|---|
| Pathogenic | 2 |
| Likely Pathogenic | 3 |
| Uncertain Significance | 5 |
| Likely Benign | 1 |
| Benign | 2 |
SpliceAI
Top 10 splice-impact sites by Δscore (adjacent positions with the same effect merged into one range; 30 predictions of 483):
| Position(s) | Effect | Δscore | Sites |
|---|---|---|---|
| 11:532756 | acceptor_gain | 1.0000 | |
| 11:533452 | donor_loss | 1.0000 | |
| 11:533613–533614 | acceptor_loss | 1.0000 | 4 |
| 11:533945–533946 | acceptor_loss | 1.0000 | 5 |
| 11:534210–534211 | donor_loss | 1.0000 | 2 |
| 11:532756–532757 | acceptor_loss | 0.9900 | 3 |
| 11:533275–533276 | donor_loss | 0.9900 | 4 |
| 11:533359–533360 | acceptor_loss | 0.9900 | 6 |
| 11:533451–533452 | donor_loss | 0.9900 | 3 |
| 11:533455 | donor_gain | 0.9900 |
AlphaMissense
852 missense substitutions predicted likely pathogenic (of 1,238 scored), across 154 residues. Top 20 hotspot residues, ranked by the number of likely-pathogenic substitutions (of those reachable by a single-nucleotide change), then by mean score:
| Residue | Likely-pathogenic substitutions | Mean am_pathogenicity | Max am_pathogenicity |
|---|---|---|---|
| M72 | 9 | 0.958 | 0.999 |
| M67 | 9 | 0.938 | 1.000 |
| D57 | 8 | 1.000 | 1.000 |
| D38 | 8 | 0.999 | 1.000 |
| D33 | 8 | 0.998 | 1.000 |
| D119 | 8 | 0.998 | 0.999 |
| D54 | 8 | 0.997 | 0.999 |
| N116 | 8 | 0.991 | 1.000 |
| D69 | 8 | 0.988 | 0.999 |
| F78 | 8 | 0.988 | 1.000 |
| F28 | 8 | 0.987 | 1.000 |
| D47 | 8 | 0.979 | 0.998 |
| F156 | 8 | 0.979 | 0.999 |
| S17 | 8 | 0.958 | 1.000 |
| F82 | 8 | 0.957 | 0.999 |
| D105 | 8 | 0.865 | 0.977 |
| D92 | 8 | 0.799 | 0.954 |
| K16 | 7 | 0.997 | 1.000 |
| E37 | 7 | 0.993 | 0.999 |
| E62 | 7 | 0.989 | 0.998 |
HPA cancer prognostics
RNA cancer specificity: Low cancer specificity
Human Protein Atlas survival analysis — favorable = higher expression predicts better survival.
4 prognostic cancer types:
| Cancer | Prognostic | p-value |
|---|---|---|
| Liver Hepatocellular Carcinoma (TCGA) | unfavorable | 5.53e-06 |
| Cervical Squamous Cell Carcinoma and Endocervical Adenocarcinoma (TCGA) | favorable | 1.08e-05 |
| Liver Hepatocellular Carcinoma (validation) | unfavorable | 0.000348 |
| Pancreatic Adenocarcinoma (validation) | unfavorable | 0.000361 |
Disease associations
OMIM: gene MIM:190020 | disease phenotypes: MIM:218040, MIM:109800, MIM:162900, MIM:188470, MIM:609942, MIM:163950, MIM:163200, MIM:137550, MIM:236750, MIM:108010
GenCC curated gene-disease
3 curated gene-disease records:
| Disease | Classification | Inheritance | Records |
|---|---|---|---|
| Costello syndrome | Definitive | Autosomal dominant | 6 |
| rhabdomyosarcoma | Moderate | Autosomal dominant | |
| Noonan syndrome-like disorder with loose anagen hair | Disputed Evidence | Autosomal dominant |
ClinGen Gene-Disease Validity
Expert-panel classifications — Definitive > Strong > Moderate > Limited > Disputed > Refuted.
2 validity classifications:
| Disease | Classification | Inheritance |
|---|---|---|
| Costello syndrome | Definitive | AD |
| Noonan syndrome-like disorder with loose anagen hair | Disputed | AD |
Genomics England panels (PanelApp)
Clinical diagnostic gene panels including this gene (26 panels, 21 green/diagnostic-grade). Confidence: green = diagnostic, amber = moderate.
26 panels:
| Panel | Rating |
|---|---|
| Adult solid tumours cancer susceptibility | green |
| Childhood solid tumours | green |
| Childhood solid tumours cancer susceptibility | green |
| DDG2P | green |
| Early onset or syndromic epilepsy | green |
| Embryonal tumour of possible germline origin | green |
| Familial rhabdomyosarcoma | green |
| Fetal anomalies | green |
| Fetal hydrops | green |
| IUGR and IGF abnormalities | green |
| Intellectual disability | green |
| Leukodystrophy, childhood onset | green |
| Monogenic short stature | green |
| Mosaic skin disorders - Deep sequencing | green |
| Paediatric disorders | green |
| Paediatric or syndromic cardiomyopathy | green |
| Pigmentary skin disorders | green |
| Primary lymphoedema | green |
| RASopathies | green |
| Sarcoma of possible germline origin | green |
| Unexplained death in infancy and sudden unexplained death in childhood | green |
| Congenital myopathy | amber |
| Hypotonic infant | amber |
| Other rare neuromuscular disorders | amber |
| Sarcoma cancer susceptibility | amber |
| Sarcoma susceptibility | amber |
Mondo (23): Costello syndrome (MONDO:0009026), urinary bladder cancer (MONDO:0001187), nevus, epidermal (MONDO:0008093), myopathy, congenital, with excess of muscle spindles (MONDO:0800299), thyroid cancer, nonmedullary, 2 (MONDO:0008566), Noonan syndrome 3 (MONDO:0012371), spermatocytic seminoma (MONDO:0020513), lip and oral cavity carcinoma (MONDO:0023644), rhabdomyosarcoma (MONDO:0005212), Noonan syndrome 1 (MONDO:0008104), wooly hair nevus (MONDO:0019311), Noonan syndrome and Noonan-related syndrome (MONDO:0020297), RASopathy (MONDO:0021060), linear nevus sebaceous syndrome (MONDO:0008097), large congenital melanocytic nevus (MONDO:0044792), non-immune hydrops fetalis (MONDO:0009369), Noonan syndrome (MONDO:0018997), tumor of salivary gland (MONDO:0021357), vascular malformation (MONDO:0024291), non-small cell lung carcinoma (MONDO:0005233), intramuscular hemangioma (MONDO:0003088), arteriovenous malformations of the brain (MONDO:0007154), Noonan syndrome-like disorder with loose anagen hair (MONDO:0011899)
Orphanet (13): Costello syndrome (Orphanet:3071), Woolly hair nevus (Orphanet:79414), Noonan syndrome (Orphanet:648), Spermatocytic seminoma (Orphanet:99865), RASopathy (Orphanet:536391), Rhabdomyosarcoma (Orphanet:780), Noonan syndrome and Noonan-related syndrome (Orphanet:98733), Linear nevus sebaceus syndrome (Orphanet:2612), Large/giant congenital melanocytic nevus (Orphanet:626), Non-immune hydrops fetalis (Orphanet:363999), Brain arteriovenous malformation (Orphanet:46724), NON RARE IN EUROPE: Bladder cancer (Orphanet:157980), NON RARE IN EUROPE: Non-small cell lung cancer (Orphanet:488201)
HPO phenotypes
showing 60 of 210 phenotypes (HPO-id order):
| HPO | Term |
|---|---|
| HP:0000006 | Autosomal dominant inheritance |
| HP:0000028 | Cryptorchidism |
| HP:0000083 | Renal insufficiency |
| HP:0000085 | Horseshoe kidney |
| HP:0000158 | Macroglossia |
| HP:0000164 | Abnormality of the dentition |
| HP:0000179 | Thick lower lip vermilion |
| HP:0000189 | Narrow palate |
| HP:0000194 | Open mouth |
| HP:0000218 | High palate |
| HP:0000232 | Everted lower lip vermilion |
| HP:0000238 | Hydrocephalus |
| HP:0000256 | Macrocephaly |
| HP:0000260 | Wide anterior fontanel |
| HP:0000267 | Cranial asymmetry |
| HP:0000269 | Prominent occiput |
| HP:0000280 | Coarse facial features |
| HP:0000286 | Epicanthus |
| HP:0000293 | Full cheeks |
| HP:0000307 | Pointed chin |
| HP:0000311 | Round face |
| HP:0000316 | Hypertelorism |
| HP:0000324 | Facial asymmetry |
| HP:0000337 | Broad forehead |
| HP:0000343 | Long philtrum |
| HP:0000347 | Micrognathia |
| HP:0000358 | Posteriorly rotated ears |
| HP:0000369 | Low-set ears |
| HP:0000418 | Narrow nasal ridge |
| HP:0000455 | Broad nasal tip |
| HP:0000463 | Anteverted nares |
| HP:0000465 | Webbed neck |
| HP:0000470 | Short neck |
| HP:0000474 | Thickened nuchal skin fold |
| HP:0000478 | Abnormality of the eye |
| HP:0000483 | Astigmatism |
| HP:0000486 | Strabismus |
| HP:0000494 | Downslanted palpebral fissures |
| HP:0000501 | Glaucoma |
| HP:0000504 | Abnormality of vision |
| HP:0000506 | Telecanthus |
| HP:0000508 | Ptosis |
| HP:0000540 | Hypermetropia |
| HP:0000543 | Optic disc pallor |
| HP:0000545 | Myopia |
| HP:0000563 | Keratoconus |
| HP:0000568 | Microphthalmia |
| HP:0000589 | Coloboma |
| HP:0000602 | Ophthalmoplegia |
| HP:0000612 | Iris coloboma |
| HP:0000629 | Periorbital fullness |
| HP:0000639 | Nystagmus |
| HP:0000682 | Abnormal dental enamel morphology |
| HP:0000768 | Pectus carinatum |
| HP:0000826 | Precocious puberty |
| HP:0000938 | Osteopenia |
| HP:0000951 | Abnormality of the skin |
| HP:0000953 | Hyperpigmentation of the skin |
| HP:0000956 | Acanthosis nigricans |
| HP:0000962 | Hyperkeratosis |
MeSH disease descriptors
11 disease descriptors:
| Descriptor | Name | Tree numbers |
|---|---|---|
| D002289 | Carcinoma, Non-Small-Cell Lung | C04.588.894.797.520.109.220.249; C08.381.540.140.500; C08.785.520.100.220.500 |
| D056685 | Costello Syndrome | C05.660.207.219; C16.131.077.256; C16.320.188 |
| D002538 | Intracranial Arteriovenous Malformations | C10.228.140.300.520; C10.500.190.500; C14.240.850.750.295; C14.240.850.875.500; C14.907.150.295; C14.907.253.560.400; C16.131.240.850.750.295; C16.131.240.850.875.500; C16.131.666.190.500 |
| D009634 | Noonan Syndrome | C05.660.207.690; C14.240.400.787; C14.280.400.787; C16.131.240.400.784; C16.131.621.207.690; C17.300.690 |
| D012208 | Rhabdomyosarcoma | C04.557.450.590.550.660; C04.557.450.795.550.660 |
| D054079 | Vascular Malformations | C14.240.850; C16.131.240.850 |
| C580062 | Epidermal Nevus *(supp.)* | |
| C537846 | Noonan like syndrome *(supp.)* | |
| C537847 | Noonan syndrome 3 *(supp.)* | |
| C564342 | Noonan-Like Syndrome With Loose Anagen Hair *(supp.)* | |
| C572845 | Thyroid cancer, follicular *(supp.)* |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (4): CHEMBL2167 (SINGLE PROTEIN), CHEMBL4524006 (PROTEIN FAMILY), CHEMBL6193817 (PROTEIN-PROTEIN INTERACTION), CHEMBL6195565 (PROTEIN-PROTEIN INTERACTION)
Drugs acting on a complex or family that includes this protein
Curated ChEMBL mechanism-of-action drugs whose target is a protein complex or family of ≤10 members that includes HRAS — the drug acts on the assembly or class, not necessarily on this subunit alone.
1 drugs via a complex or family:
| Drug | Target (ChEMBL) | Members | Max phase |
|---|---|---|---|
| SALIRASIB | RAS | 3 | 2 |
Molecules with ChEMBL bioactivity
Phase ≥1, by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 15,683 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).
4 molecules by phase:
| Molecule | Name | Phase | Patents |
|---|---|---|---|
| CHEMBL298734 | LONAFARNIB | 4 | 13,020 |
| CHEMBL11252 | STALLIMYCIN | 2 | 1,919 |
| CHEMBL351706 | BMS-214662 | 1 | 403 |
| CHEMBL279433 | L-778123 FREE BASE | 1 | 341 |
Clinical evidence (CIViC)
Drug × variant × indication, from 9 curated evidence items; also 1 functional, 1 oncogenic, 1 prognostic. CIViC evidence level: A (validated) → B (clinical) → C (case study) → D (preclinical) → E (inferential).
9 predictive associations by evidence level:
| Variant | Therapy | Indication | Effect | Level | CIViC |
|---|---|---|---|---|---|
| BRAF V600E OR NRAS Mutation OR HRAS Mutation OR KRAS Mutation OR NF1 Inactivating Mutation | Selumetinib | Cancer | Sensitivity/Response | CIViC B | EID11696 |
| BRAF V600E OR NRAS Mutation OR HRAS Mutation OR KRAS Mutation OR NF1 Mutation | Selumetinib | Cancer | Sensitivity/Response | CIViC B | EID11681 |
| HRAS Mutation | Tipifarnib | Bladder Urothelial Carcinoma | Sensitivity/Response | CIViC B | EID9632 |
| HRAS Mutation | Tipifarnib | Head And Neck Squamous Cell Carcinoma | Sensitivity/Response | CIViC B | EID9633 |
| HRAS G13D | Vemurafenib | Skin Squamous Cell Carcinoma | Resistance | CIViC C | EID3851 |
| HRAS G13D | Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor | Colorectal Cancer | Resistance | CIViC C | EID699 |
| HRAS Q61L OR HRAS Q61R OR HRAS G12V | Binimetinib + Mirdametinib + MTOR Kinase Inhibitor AZD8055 + Everolimus + Selumetinib | Cancer | Sensitivity/Response | CIViC D | EID700 |
| HRAS G13D | Cetuximab | Colorectal Cancer | Resistance | CIViC D | EID3852 |
| HRAS G13R | Vemurafenib | Thyroid Gland Carcinoma | Resistance | CIViC D | EID3853 |
Clinical-actionability assertions (CIViC AMP/ASCO/CAP)
Curated AMP/ASCO/CAP tier assertions — the clinical-actionability classification (Tier I highest) for this gene’s variants, distilling the CIViC evidence above into a tiered call.
1 CIViC assertions:
| Molecular profile | Disease | Therapy | Type | AMP tier | Significance |
|---|---|---|---|---|---|
| HRAS G13R | Cancer | Oncogenic | Oncogenic |
CIViC curated variants (7)
Named clinical variants curated in CIViC for this gene (the catalogue beneath the predictive evidence above):
Q61R, G13R (missense variant), G12V, Q61, G13D (missense variant), Mutation (coding transcript variant), Q61L (missense variant).
PharmGKB: 1 entry (CPIC guideline: no)
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: enzyme — RAS subfamily
Most potent curated ligand interactions (1 total), top 1:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| lonafarnib | Inhibition | 8.72 | pIC50 |
Binding affinities (BindingDB)
66 measured of 94 human assays (116 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value | Patent |
|---|---|---|---|
| (R)-3-Benzyl-1-(3H-imidazol-4-ylmethyl)-4-(thiophene-2-sulfonyl)-2,3,4,5-tetrahydro-1H-benzo[e][1,4]diazepine-7-carbonitrile | IC50 | 1.35 nM | |
| 4-{5-[4-(3-Chloro-phenyl)-3-oxo-piperazin-1-ylmethyl]-imidazol-1-ylmethyl}-benzonitrile | IC50 | 2 nM | |
| 5-{4-[Bis-(2-chloro-ethyl)-amino]-benzoylamino}-1H-benzoimidazole-2-carboxylic acid (5-{5-[5-(2-carbamimidoyl-ethylcarbamoyl)-1-methyl-1H-pyrrol-3-ylcarbamoyl]-1-methyl-1H-pyrrol-3-ylcarbamoyl}-1-methyl-1H-pyrrol-3-yl)-amide; hydrochloride | IC50 | 15 nM | |
| 5-{4-[Bis-(2-chloro-ethyl)-amino]-benzoylamino}-1-methyl-1H-indole-2-carboxylic acid (5-{5-[5-(2-carbamimidoyl-ethylcarbamoyl)-1-methyl-1H-pyrrol-3-ylcarbamoyl]-1-methyl-1H-pyrrol-3-ylcarbamoyl}-1-methyl-1H-pyrrol-3-yl)-amide; hydrochloride | IC50 | 15 nM | |
| 5-{4-[Bis-(2-chloro-ethyl)-amino]-benzoylamino}-benzofuran-2-carboxylic acid (5-{5-[5-(2-carbamimidoyl-ethylcarbamoyl)-1-methyl-1H-pyrrol-3-ylcarbamoyl]-1-methyl-1H-pyrrol-3-ylcarbamoyl}-1-methyl-1H-pyrrol-3-yl)-amide; hydrochloride | IC50 | 15 nM | |
| 5-{4-[Bis-(2-chloro-ethyl)-amino]-benzoylamino}-1H-indole-2-carboxylic acid (5-{5-[5-(2-carbamimidoyl-ethylcarbamoyl)-1-methyl-1H-pyrrol-3-ylcarbamoyl]-1-methyl-1H-pyrrol-3-ylcarbamoyl}-1-methyl-1H-pyrrol-3-yl)-amide; hydrochloride | IC50 | 15 nM | |
| 5-[Bis-(2-chloro-ethyl)-amino]-benzofuran-2-carboxylic acid (5-{5-[5-(2-carbamimidoyl-ethylcarbamoyl)-1-methyl-1H-pyrrol-3-ylcarbamoyl]-1-methyl-1H-pyrrol-3-ylcarbamoyl}-1-methyl-1H-pyrrol-3-yl)-amide; hydrochloride | IC50 | 15 nM | |
| 5-[Bis-(2-chloro-ethyl)-amino]-1-methyl-1H-indole-2-carboxylic acid (5-{5-[5-(2-carbamimidoyl-ethylcarbamoyl)-1-methyl-1H-pyrrol-3-ylcarbamoyl]-1-methyl-1H-pyrrol-3-ylcarbamoyl}-1-methyl-1H-pyrrol-3-yl)-amide; hydrochloride | IC50 | 20 nM | |
| 5-[Bis-(2-chloro-ethyl)-amino]-1H-indole-2-carboxylic acid (5-{5-[5-(2-carbamimidoyl-ethylcarbamoyl)-1-methyl-1H-pyrrol-3-ylcarbamoyl]-1-methyl-1H-pyrrol-3-ylcarbamoyl}-1-methyl-1H-pyrrol-3-yl)-amide; hydrochloride | IC50 | 20 nM | |
| CHEMBL4456044 | KD | 51 nM | |
| [(S)-1-((4-Benzyloxy-benzyl)-{[(1-phenyl-cyclobutylmethyl)-carbamoyl]-methyl}-carbamoyl)-2-(3H-imidazol-4-yl)-ethyl]-carbamic acid benzyl ester | IC50 | 88 nM | |
| CHEMBL5174384 | IC50 | 100 nM | |
| CHEMBL5171806 | IC50 | 100 nM | |
| 1-[4-((S)-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)-piperazin-1-yl]-2-pyridin-4-yl-ethanone | IC50 | 140 nM | |
| [(S)-1-{(4-Benzyloxy-benzyl)-[(2-methyl-2-phenyl-propylcarbamoyl)-methyl]-carbamoyl}-2-(3H-imidazol-4-yl)-ethyl]-carbamic acid benzyl ester | IC50 | 180 nM | |
| [(S)-1-((4-Benzyloxy-benzyl)-{[(1-phenyl-cyclopropylmethyl)-carbamoyl]-methyl}-carbamoyl)-2-(3H-imidazol-4-yl)-ethyl]-carbamic acid benzyl ester | IC50 | 180 nM | |
| [(S)-1-{(4-Benzyloxy-benzyl)-[(2-cyano-2-phenyl-ethylcarbamoyl)-methyl]-carbamoyl}-2-(3H-imidazol-4-yl)-ethyl]-carbamic acid benzyl ester | IC50 | 190 nM | |
| [(S)-1-{(4-Benzyloxy-benzyl)-[((S)-2-phenyl-propylcarbamoyl)-methyl]-carbamoyl}-2-(3H-imidazol-4-yl)-ethyl]-carbamic acid benzyl ester | IC50 | 300 nM | |
| [(S)-1-{(4-Benzyloxy-benzyl)-[(2-phenyl-propylcarbamoyl)-methyl]-carbamoyl}-2-(3H-imidazol-4-yl)-ethyl]-carbamic acid benzyl ester | IC50 | 310 nM | |
| [(S)-1-((4-Benzyloxy-benzyl)-{[(1-phenyl-cyclopentylmethyl)-carbamoyl]-methyl}-carbamoyl)-2-(3H-imidazol-4-yl)-ethyl]-carbamic acid benzyl ester | IC50 | 330 nM | |
| [(S)-1-{(4-Benzyloxy-benzyl)-[(2-phenyl-butylcarbamoyl)-methyl]-carbamoyl}-2-(3H-imidazol-4-yl)-ethyl]-carbamic acid benzyl ester | IC50 | 400 nM | |
| [(S)-1-{(4-Benzyloxy-benzyl)-[((R)-2-phenyl-propylcarbamoyl)-methyl]-carbamoyl}-2-(3H-imidazol-4-yl)-ethyl]-carbamic acid benzyl ester | IC50 | 570 nM | |
| [(S)-1-{(4-Benzyloxy-benzyl)-[((R)-1-methyl-2-phenyl-ethylcarbamoyl)-methyl]-carbamoyl}-2-(3H-imidazol-4-yl)-ethyl]-carbamic acid benzyl ester | IC50 | 710 nM | |
| CHEMBL6172941 | IC50 | 870 nM | |
| 1-[(2R,6S)-6-(tert-Butyl-dimethyl-silanyloxymethyl)-4-(2-nitro-benzenesulfonyl)-morpholin-2-yl]-4-chloro-6-methoxy-3-methyl-1H-pyrazolo[3,4-b]quinoline | IC50 | 1000 nM | |
| (8S)-13-(5-ethyl-6-fluoro-1H-benzo[f]indazol-4-yl)-14-fluoro-17-[[(6Z,8S)-6-(fluoromethylidene)-2,3,5,7-tetrahydro-1H-pyrrolizin-8-yl]methoxy]-6,10-dioxa-2,12,16,18-tetrazatetracyclo[9.7.1.02,8.015,19]nonadeca-1(18),11,13,15(19),16-pentaene | IC50 | 1280 nM | US-12466840: Small molecule inhibitors of KRAS proteins |
| 3-[(3aS,4R,6R,6aR)-6-(4-Chloro-6-methoxy-3-methyl-pyrazolo[3,4-b]quinolin-1-yl)-2-thioxo-tetrahydro-furo[3,4-d][1,3]dioxol-4-yloxy]-3-hydroxy-1-phenyl-propan-1-one | IC50 | 1500 nM | |
| CHEMBL6165011 | KD | 2000 nM | |
| (8S)-13-(5-ethyl-6-fluoro-3-methyl-2H-benzo[f]indazol-4-yl)-14-fluoro-17-[[(6Z,8S)-6-(fluoromethylidene)-2,3,5,7-tetrahydro-1H-pyrrolizin-8-yl]methoxy]-6,10-dioxa-2,12,16,18-tetrazatetracyclo[9.7.1.02,8.015,19]nonadeca-1(18),11,13,15(19),16-pentaene | IC50 | 2180 nM | US-12466840: Small molecule inhibitors of KRAS proteins |
| Ophirapstanol Trisulfate | IC50 | 2550 nM | |
| CHEMBL5592316 | EC50 | 2600 nM | |
| (8S)-13-(5-ethyl-6-fluoro-1H-indazol-4-yl)-14-fluoro-17-[[(2R,8S)-2-fluoro-1,2,3,5,6,7-hexahydropyrrolizin-8-yl]methoxy]-6,10-dioxa-2,12,16,18-tetrazatetracyclo[9.7.1.02,8.015,19]nonadeca-1(18),11,13,15(19),16-pentaene | IC50 | 2740 nM | US-12466840: Small molecule inhibitors of KRAS proteins |
| (E)-5-[(2R,6R)-6-(4-Chloro-6-methoxy-3-methyl-pyrazolo[3,4-b]quinolin-1-yl)-4-(4-nitro-phenylsulfanyl)-morpholin-2-yl]-pent-3-en-2-one | IC50 | 3000 nM | |
| CHEMBL6149416 | KD | 4100 nM | |
| [(S)-1-[(4-Benzyloxy-benzyl)-(phenethylcarbamoyl-methyl)-carbamoyl]-2-(1H-imidazol-4-yl)-ethyl]-carbamic acid benzyl ester | IC50 | 4300 nM | |
| (8S)-13-[6-chloro-5-(1-fluorocyclopropyl)-1H-indazol-4-yl]-14-fluoro-17-[[(6Z,8S)-6-(fluoromethylidene)-2,3,5,7-tetrahydro-1H-pyrrolizin-8-yl]methoxy]-6,10-dioxa-2,12,16,18-tetrazatetracyclo[9.7.1.02,8.015,19]nonadeca-1(18),11,13,15(19),16-pentaene | IC50 | 4680 nM | US-12466840: Small molecule inhibitors of KRAS proteins |
| (E)-4-[(2R,6R)-6-(4-Chloro-6-methoxy-3-methyl-pyrazolo[3,4-b]quinolin-1-yl)-4-(2-nitro-phenylsulfanyl)-morpholin-2-yl]-1-phenyl-but-2-en-1-one | IC50 | 4700 nM | |
| CHEMBL1387422 | EC50 | 5000 nM | |
| 1-[(2R,6S)-6-(tert-Butyl-dimethyl-silanyloxymethyl)-4-(4-nitro-benzenesulfonyl)-morpholin-2-yl]-4-chloro-6-methoxy-3-methyl-1H-pyrazolo[3,4-b]quinoline | IC50 | 5000 nM | |
| (8S)-13-(5-ethyl-6-fluoro-3-methyl-2H-benzo[f]indazol-4-yl)-14-fluoro-17-[[(2R,8S)-2-fluoro-1,2,3,5,6,7-hexahydropyrrolizin-8-yl]methoxy]-6,10-dioxa-2,12,16,18-tetrazatetracyclo[9.7.1.02,8.015,19]nonadeca-1(18),11,13,15(19),16-pentaene | IC50 | 5520 nM | US-12466840: Small molecule inhibitors of KRAS proteins |
| [(S)-1-{(4-Benzyloxy-benzyl)-[((S)-1-methyl-2-phenyl-ethylcarbamoyl)-methyl]-carbamoyl}-2-(3H-imidazol-4-yl)-ethyl]-carbamic acid benzyl ester | IC50 | 6300 nM | |
| [(2S,6R)-6-(4-Chloro-6-methoxy-3-methyl-pyrazolo[3,4-b]quinolin-1-yl)-4-(4-nitro-phenylsulfanyl)-morpholin-2-yl]-methanol | IC50 | 6700 nM | |
| (E)-4-[(2R,6R)-6-(4-Chloro-6-methoxy-3-methyl-pyrazolo[3,4-b]quinolin-1-yl)-4-(4-nitro-benzenesulfonyl)-morpholin-2-yl]-1-phenyl-but-2-en-1-one | IC50 | 7000 nM | |
| (E)-4-[(2R,6R)-6-(4-Chloro-6-methoxy-3-methyl-pyrazolo[3,4-b]quinolin-1-yl)-4-(4-nitro-phenylsulfanyl)-morpholin-2-yl]-1-phenyl-but-2-en-1-one | IC50 | 7400 nM | |
| Benzodiazepine-Distamycin Hybrid | IC50 | 8000 nM | |
| [(2S,6R)-6-(4-Chloro-6-methoxy-3-methyl-pyrazolo[3,4-b]quinolin-1-yl)-4-(4-nitro-benzenesulfonyl)-morpholin-2-yl]-methanol | IC50 | 8000 nM | |
| (E)-3-[(2S,3S,4R,5R)-5-(4-Chloro-6-methoxy-3-methyl-pyrazolo[3,4-b]quinolin-1-yl)-3,4-dihydroxy-tetrahydro-furan-2-yloxy]-1-phenyl-propenone | IC50 | 10000 nM | |
| 5-(4-chloro-6-methoxy-3-methyl-1H-pyrazolo[3,4-b]quinolin-1-yl)-3,4-di(phenylcarbonyloxy)-2-phenylcarbonyloxymethyl-(2R,3R,4R,5R)-tetrahydrofuran | IC50 | 10000 nM | |
| 5-(4-chloro-6-methoxy-3-methyl-1H-pyrazolo[3,4-b]quinolin-1-yl)-3,4-di(2-furylcarbonyloxy)-2-(2-furylcarbonyloxymethyl)-(2R,3R,4R,5R)-tetrahydrofuran | IC50 | 10500 nM | |
| [(2S,6R)-4-Benzenesulfonyl-6-(4-chloro-6-methoxy-3-methyl-pyrazolo[3,4-b]quinolin-1-yl)-morpholin-2-yl]-methanol | IC50 | 12000 nM |
ChEMBL bioactivities
50 potent at pChembl≥5 of 71 total, top 49 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 8.89 | IC50 | 1.3 | nM | BMS-214662 |
| 8.80 | Ki | 1.6 | nM | L-778123 FREE BASE |
| 8.72 | IC50 | 1.9 | nM | CHEMBL66699 |
| 7.82 | IC50 | 15 | nM | CHEMBL554247 |
| 7.82 | IC50 | 15 | nM | CHEMBL552690 |
| 7.82 | IC50 | 15 | nM | CHEMBL554353 |
| 7.82 | IC50 | 15 | nM | CHEMBL540313 |
| 7.82 | IC50 | 15 | nM | CHEMBL554189 |
| 7.70 | IC50 | 20 | nM | CHEMBL552863 |
| 7.70 | IC50 | 20 | nM | CHEMBL536328 |
| 7.29 | Kd | 51 | nM | CHEMBL4456044 |
| 7.16 | IC50 | 70 | nM | LONAFARNIB |
| 7.06 | IC50 | 88 | nM | CHEMBL326352 |
| 7.00 | IC50 | 100 | nM | CHEMBL5171806 |
| 6.75 | IC50 | 180 | nM | CHEMBL407445 |
| 6.75 | IC50 | 180 | nM | CHEMBL431440 |
| 6.72 | IC50 | 190 | nM | CHEMBL115943 |
| 6.70 | IC50 | 200 | nM | BAY-293 |
| 6.70 | IC50 | 200 | nM | STALLIMYCIN |
| 6.52 | IC50 | 300 | nM | CHEMBL115669 |
| 6.51 | IC50 | 310 | nM | CHEMBL324827 |
| 6.48 | IC50 | 330 | nM | CHEMBL326127 |
| 6.40 | IC50 | 400 | nM | CHEMBL112512 |
| 6.39 | IC50 | 410 | nM | BAY-293 |
| 6.24 | IC50 | 570 | nM | CHEMBL114281 |
| 6.15 | IC50 | 710 | nM | CHEMBL325073 |
| 6.00 | IC50 | 1000 | nM | CHEMBL304462 |
| 5.82 | IC50 | 1500 | nM | CHEMBL304862 |
| 5.70 | Kd | 2000 | nM | CHEMBL6165011 |
| 5.58 | EC50 | 2600 | nM | CHEMBL5592316 |
| 5.52 | IC50 | 3000 | nM | CHEMBL59515 |
| 5.41 | Kd | 3920 | nM | CHEMBL6172941 |
| 5.39 | Kd | 4100 | nM | CHEMBL6149416 |
| 5.38 | IC50 | 4120 | nM | BAY-294 |
| 5.37 | IC50 | 4300 | nM | CHEMBL102955 |
| 5.33 | IC50 | 4700 | nM | CHEMBL61161 |
| 5.30 | EC50 | 5000 | nM | CHEMBL1387422 |
| 5.30 | IC50 | 5000 | nM | CHEMBL64328 |
| 5.26 | Kd | 5500 | nM | CHEMBL3218192 |
| 5.20 | IC50 | 6300 | nM | CHEMBL324345 |
| 5.17 | IC50 | 6700 | nM | CHEMBL300769 |
| 5.16 | IC50 | 7000 | nM | CHEMBL304474 |
| 5.13 | IC50 | 7400 | nM | CHEMBL294285 |
| 5.11 | Kd | 7800 | nM | CHEMBL3218193 |
| 5.10 | IC50 | 8000 | nM | CHEMBL102341 |
| 5.10 | IC50 | 8000 | nM | CHEMBL303105 |
| 5.02 | Kd | 9500 | nM | CHEMBL3218191 |
| 5.00 | IC50 | 1e+04 | nM | CHEMBL303512 |
| 5.00 | IC50 | 1e+04 | nM | CHEMBL304637 |
PubChem BioAssay actives
33 with measured affinity, of 100 total; 32 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.
| Compound | Assay | Type | Value | Unit |
|---|---|---|---|---|
| (3R)-3-benzyl-1-(1H-imidazol-5-ylmethyl)-4-thiophen-2-ylsulfonyl-3,5-dihydro-2H-1,4-benzodiazepine-7-carbonitrile | 1893917: Inhibition of HRAS (unknown origin) farnesylation | ic50 | 0.0013 | uM |
| 4-[[5-[[4-(3-chlorophenyl)-3-oxopiperazin-1-yl]methyl]imidazol-1-yl]methyl]benzonitrile | 1893894: Binding affinity to HRAS (unknown origin) assessed as inhibition constant | ki | 0.0016 | uM |
| 1-[4-[(2S)-13-chloro-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-yl]piperazin-1-yl]-2-pyridin-4-ylethanone | 1979346: Inhibition of H-Ras (unknown origin) | ic50 | 0.0019 | uM |
| N-[5-[[5-[[5-[(3-amino-3-iminopropyl)carbamoyl]-1-methylpyrrol-3-yl]carbamoyl]-1-methylpyrrol-3-yl]carbamoyl]-1-methylpyrrol-3-yl]-5-[[4-[bis(2-chloroethyl)amino]benzoyl]amino]-1H-benzimidazole-2-carboxamide;hydrochloride | 85480: Tested for 50% inhibition of generation of Human Ha-ras polymerase chain reaction(PCR) products | ic50 | 0.0150 | uM |
| N-[5-[[5-[[5-[(3-amino-3-iminopropyl)carbamoyl]-1-methylpyrrol-3-yl]carbamoyl]-1-methylpyrrol-3-yl]carbamoyl]-1-methylpyrrol-3-yl]-5-[[4-[bis(2-chloroethyl)amino]benzoyl]amino]-1-methylindole-2-carboxamide;hydrochloride | 85480: Tested for 50% inhibition of generation of Human Ha-ras polymerase chain reaction(PCR) products | ic50 | 0.0150 | uM |
| N-(3-amino-3-iminopropyl)-4-[[4-[[4-[[5-[[4-[bis(2-chloroethyl)amino]benzoyl]amino]-1-benzofuran-2-carbonyl]amino]-1-methylpyrrole-2-carbonyl]amino]-1-methylpyrrole-2-carbonyl]amino]-1-methylpyrrole-2-carboxamide;hydrochloride | 85480: Tested for 50% inhibition of generation of Human Ha-ras polymerase chain reaction(PCR) products | ic50 | 0.0150 | uM |
| N-[5-[[5-[[5-[(3-amino-3-iminopropyl)carbamoyl]-1-methylpyrrol-3-yl]carbamoyl]-1-methylpyrrol-3-yl]carbamoyl]-1-methylpyrrol-3-yl]-5-[[4-[bis(2-chloroethyl)amino]benzoyl]amino]-1H-indole-2-carboxamide;hydrochloride | 85480: Tested for 50% inhibition of generation of Human Ha-ras polymerase chain reaction(PCR) products | ic50 | 0.0150 | uM |
| N-(3-amino-3-iminopropyl)-4-[[4-[[4-[[5-[bis(2-chloroethyl)amino]-1-benzofuran-2-carbonyl]amino]-1-methylpyrrole-2-carbonyl]amino]-1-methylpyrrole-2-carbonyl]amino]-1-methylpyrrole-2-carboxamide;hydrochloride | 85480: Tested for 50% inhibition of generation of Human Ha-ras polymerase chain reaction(PCR) products | ic50 | 0.0150 | uM |
| N-[5-[[5-[[5-[(3-amino-3-iminopropyl)carbamoyl]-1-methylpyrrol-3-yl]carbamoyl]-1-methylpyrrol-3-yl]carbamoyl]-1-methylpyrrol-3-yl]-5-[bis(2-chloroethyl)amino]-1-methylindole-2-carboxamide;hydrochloride | 85480: Tested for 50% inhibition of generation of Human Ha-ras polymerase chain reaction(PCR) products | ic50 | 0.0200 | uM |
| N-[5-[[5-[[5-[(3-amino-3-iminopropyl)carbamoyl]-1-methylpyrrol-3-yl]carbamoyl]-1-methylpyrrol-3-yl]carbamoyl]-1-methylpyrrol-3-yl]-5-[bis(2-chloroethyl)amino]-1H-indole-2-carboxamide;hydrochloride | 85480: Tested for 50% inhibition of generation of Human Ha-ras polymerase chain reaction(PCR) products | ic50 | 0.0200 | uM |
| 6-(2,3-dihydro-1,4-benzodioxin-5-yl)-N-[4-[(dimethylamino)methyl]phenyl]-2-methoxypyridin-3-amine | 1582666: Inhibition GST-tagged recombinant HRAS G12V mutant (1 to 166 amino acids) (unknown origin) expressed in Escherichia coli C41(DE3) by SPR assay | kd | 0.0510 | uM |
| Lonafarnib | 79248: Compound was measured for inhibition of H-ras NIH tumor cell line under soft agar assay. | ic50 | 0.0700 | uM |
| benzyl N-[(2S)-3-(1H-imidazol-5-yl)-1-oxo-1-[[2-oxo-2-[(1-phenylcyclobutyl)methylamino]ethyl]-[(4-phenylmethoxyphenyl)methyl]amino]propan-2-yl]carbamate | 79247: Concentration required to inhibit 50% of the cultured colonies of H-Ras-Fcells. | ic50 | 0.0880 | uM |
| methyl (2S)-4-[5-[[[(2R)-2-amino-3-sulfanylpropyl]amino]methyl]-2-phenylphenyl]-2-(2-methylsulfanylethyl)-4-oxobutanoate | 1893906: Inhibition of HRAS (unknown origin) transfected in BALB/c nude mouse incubated for 3 days measured by immunoblot analysis | ic50 | 0.1000 | uM |
| benzyl N-[(2S)-3-(1H-imidazol-5-yl)-1-oxo-1-[[2-oxo-2-[(1-phenylcyclopropyl)methylamino]ethyl]-[(4-phenylmethoxyphenyl)methyl]amino]propan-2-yl]carbamate | 79247: Concentration required to inhibit 50% of the cultured colonies of H-Ras-Fcells. | ic50 | 0.1800 | uM |
| benzyl N-[(2S)-3-(1H-imidazol-5-yl)-1-[[2-[(2-methyl-2-phenylpropyl)amino]-2-oxoethyl]-[(4-phenylmethoxyphenyl)methyl]amino]-1-oxopropan-2-yl]carbamate | 79247: Concentration required to inhibit 50% of the cultured colonies of H-Ras-Fcells. | ic50 | 0.1800 | uM |
| benzyl N-[(2S)-1-[[2-[(2-cyano-2-phenylethyl)amino]-2-oxoethyl]-[(4-phenylmethoxyphenyl)methyl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]carbamate | 79247: Concentration required to inhibit 50% of the cultured colonies of H-Ras-Fcells. | ic50 | 0.1900 | uM |
| N-[5-[[5-[(3-amino-3-iminopropyl)carbamoyl]-1-methylpyrrol-3-yl]carbamoyl]-1-methylpyrrol-3-yl]-4-formamido-1-methylpyrrole-2-carboxamide | 85480: Tested for 50% inhibition of generation of Human Ha-ras polymerase chain reaction(PCR) products | ic50 | 0.2000 | uM |
| benzyl N-[(2S)-3-(1H-imidazol-5-yl)-1-oxo-1-[[2-oxo-2-[[(2S)-2-phenylpropyl]amino]ethyl]-[(4-phenylmethoxyphenyl)methyl]amino]propan-2-yl]carbamate | 79247: Concentration required to inhibit 50% of the cultured colonies of H-Ras-Fcells. | ic50 | 0.3000 | uM |
| benzyl N-[(2S)-3-(1H-imidazol-5-yl)-1-oxo-1-[[2-oxo-2-(2-phenylpropylamino)ethyl]-[(4-phenylmethoxyphenyl)methyl]amino]propan-2-yl]carbamate | 79247: Concentration required to inhibit 50% of the cultured colonies of H-Ras-Fcells. | ic50 | 0.3100 | uM |
| benzyl N-[(2S)-3-(1H-imidazol-5-yl)-1-oxo-1-[[2-oxo-2-[(1-phenylcyclopentyl)methylamino]ethyl]-[(4-phenylmethoxyphenyl)methyl]amino]propan-2-yl]carbamate | 79247: Concentration required to inhibit 50% of the cultured colonies of H-Ras-Fcells. | ic50 | 0.3300 | uM |
| benzyl N-[(2S)-3-(1H-imidazol-5-yl)-1-oxo-1-[[2-oxo-2-(2-phenylbutylamino)ethyl]-[(4-phenylmethoxyphenyl)methyl]amino]propan-2-yl]carbamate | 79247: Concentration required to inhibit 50% of the cultured colonies of H-Ras-Fcells. | ic50 | 0.4000 | uM |
| benzyl N-[(2S)-3-(1H-imidazol-5-yl)-1-oxo-1-[[2-oxo-2-[[(2R)-2-phenylpropyl]amino]ethyl]-[(4-phenylmethoxyphenyl)methyl]amino]propan-2-yl]carbamate | 79247: Concentration required to inhibit 50% of the cultured colonies of H-Ras-Fcells. | ic50 | 0.5700 | uM |
| benzyl N-[(2S)-3-(1H-imidazol-5-yl)-1-oxo-1-[[2-oxo-2-[[(2R)-1-phenylpropan-2-yl]amino]ethyl]-[(4-phenylmethoxyphenyl)methyl]amino]propan-2-yl]carbamate | 79247: Concentration required to inhibit 50% of the cultured colonies of H-Ras-Fcells. | ic50 | 0.7100 | uM |
| (4S)-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2R)-3-[[4-[[4-[[(2R)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S,3S)-2-[[(2S)-2-acetamido-3-(1H-indol-3-yl)propanoyl]amino]-3-methylpentanoyl]amino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylpentanoyl]amino]-3-[[(2S,3R)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[2-[[(2S)-1,4-diamino-1,4-dioxobutan-2-yl]amino]-2-oxoethyl]amino]-1,4-dioxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-6-carbamimidamido-1-oxohexan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-oxopropyl]sulfanylmethyl]phenyl]methoxymethyl]phenyl]methylsulfanyl]-1-amino-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-4-methylpentanoyl]amino]propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-oxopentanoic acid | 2255380: Binding affinity to HRas (unknown origin) assessed as dissociation constant | kd | 2.0000 | uM |
| methyl 3-amino-4-[4-[[ethyl-[7-[(4-fluorobenzoyl)-propan-2-ylamino]heptanoyl]amino]methyl]piperidin-1-yl]benzoate | 2115760: Induction of Rluc8-tagged and GFP2-tagged H-Ras G12V mutant (unknown origin) disruption extracted from HEK293-EBNA cells assessed as intracellular H-Ras G12V membrane anchorage disruption by measuring effective concentration measured after 24 hrs by BRET assay | ec50 | 2.6000 | uM |
| (2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S,5S,8S,11S,15Z,20S)-20-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S,3S)-2-[[(2S)-2-acetamido-3-(1H-indol-3-yl)propanoyl]amino]-3-methylpentanoyl]amino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-5-(4-carbamimidamidobutyl)-2-(3-carbamimidamidopropyl)-11,20-dimethyl-8-(2-methylpropyl)-3,6,9,21-tetraoxo-1,4,7,10-tetrazacyclohenicos-15-ene-11-carbonyl]amino]-5-carbamimidamidopentanoyl]amino]-4-amino-4-oxobutanoyl]amino]acetyl]amino]butanediamide | 2255380: Binding affinity to HRas (unknown origin) assessed as dissociation constant | kd | 3.9200 | uM |
| (4S)-4-[3-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(3S)-3-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[3-[[2-[(3S,6S,12Z)-6-benzyl-3-(2-carboxyethyl)-2,5,8-trioxo-1,4,7-triazacyclotetradec-12-en-1-yl]acetyl]amino]-3-methylpentanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]-4-methylpentanoyl]amino]-6-[4-(ethenylsulfonylamino)butanoylamino]hexanoyl]amino]hexanoyl]amino]propanoylamino]-5-[[(2S)-4-carboxy-1-[[(2S)-1-[[(2S)-1,4-diamino-1,4-dioxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxobutan-2-yl]amino]-5-oxopentanoic acid | 2255367: Binding affinity to wild-type H-Ras (unknown origin) assessed as dissociation constant by fluorescence polarization assay | kd | 4.1000 | uM |
| benzyl N-[(2S)-3-(1H-imidazol-5-yl)-1-oxo-1-[[2-oxo-2-(2-phenylethylamino)ethyl]-[(4-phenylmethoxyphenyl)methyl]amino]propan-2-yl]carbamate | 79247: Concentration required to inhibit 50% of the cultured colonies of H-Ras-Fcells. | ic50 | 4.3000 | uM |
| 4-[3,4-dimethyl-2-(4-methylphenyl)-7-oxopyrazolo[3,4-d]pyridazin-6-yl]-N-(2-phenylpropyl)butanamide | 2115760: Induction of Rluc8-tagged and GFP2-tagged H-Ras G12V mutant (unknown origin) disruption extracted from HEK293-EBNA cells assessed as intracellular H-Ras G12V membrane anchorage disruption by measuring effective concentration measured after 24 hrs by BRET assay | ec50 | 5.0000 | uM |
| benzyl N-[(2S)-3-(1H-imidazol-5-yl)-1-oxo-1-[[2-oxo-2-[[(2S)-1-phenylpropan-2-yl]amino]ethyl]-[(4-phenylmethoxyphenyl)methyl]amino]propan-2-yl]carbamate | 79247: Concentration required to inhibit 50% of the cultured colonies of H-Ras-Fcells. | ic50 | 6.3000 | uM |
| 4-[3-[[(6aS)-2-methoxy-11-oxo-6a,7,8,9-tetrahydropyrrolo[2,1-c][1,4]benzodiazepin-3-yl]oxy]propanoylamino]-N-[5-[[5-[(3-amino-3-iminopropyl)carbamoyl]-1-methylpyrrol-3-yl]carbamoyl]-1-methylpyrrol-3-yl]-1-methylpyrrole-2-carboxamide | 85481: Inhibition of Ha-ras polymerase-chain reaction product | ic50 | 8.0000 | uM |
CTD chemical–gene interactions
148 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| sodium arsenite | increases expression, decreases reaction, increases response to substance, increases activity, decreases expression | 5 |
| Benzo(a)pyrene | affects methylation, increases expression, decreases methylation, increases response to substance | 4 |
| Estradiol | decreases reaction, increases expression, affects expression, affects reaction, increases response to substance | 4 |
| Methylnitrosourea | increases response to substance, decreases reaction | 4 |
| Urethane | increases reaction, increases response to substance, increases mutagenesis, increases expression | 4 |
| Aflatoxin B1 | affects expression, increases expression | 4 |
| 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one | decreases reaction, increases activity, increases expression | 3 |
| Cisplatin | affects splicing, increases expression, increases reaction, decreases response to substance | 3 |
| Doxorubicin | decreases expression, decreases reaction, increases expression | 3 |
| Valproic Acid | affects expression, increases expression, increases methylation | 3 |
| Simvastatin | increases localization, decreases prenylation, affects localization, decreases farnesylation, increases activity (+4 more) | 3 |
| perfluorooctanoic acid | decreases expression, affects cotreatment, affects expression | 2 |
| 2-amino-1-methyl-6-phenylimidazo(4,5-b)pyridine | affects response to substance, increases expression, increases mutagenesis, affects reaction, increases abundance (+1 more) | 2 |
| perfluorooctane sulfonic acid | affects expression, affects cotreatment, decreases expression | 2 |
| Resveratrol | increases response to substance, affects expression, increases activity, increases reaction, increases expression (+2 more) | 2 |
| Zoledronic Acid | decreases localization, increases expression | 2 |
| Arsenic Trioxide | increases expression, affects cotreatment | 2 |
| Copper | affects cotreatment, increases mutagenesis, decreases reaction | 2 |
| Dactinomycin | increases cleavage, increases reaction, affects cotreatment, increases expression | 2 |
| Lipopolysaccharides | decreases reaction, increases activity, increases localization, increases expression, increases prenylation | 2 |
| Lovastatin | decreases prenylation, decreases localization | 2 |
| Malathion | affects cotreatment, increases expression | 2 |
| Parathion | affects cotreatment, increases expression | 2 |
| Quercetin | decreases expression, increases expression | 2 |
| Tetradecanoylphorbol Acetate | affects reaction, increases phosphorylation, affects cotreatment, increases expression | 2 |
| 9,10-Dimethyl-1,2-benzanthracene | affects reaction, increases response to substance | 2 |
| aristolochic acid I | increases expression | 1 |
| ammonium 2,3,3,3-tetrafluoro-2-(heptafluoropropoxy)-propanoate | affects cotreatment, affects expression | 1 |
| BI-2852 | affects binding | 1 |
| bathocuproine | affects cotreatment, decreases reaction, increases mutagenesis | 1 |
ChEMBL screening assays
48 unique, capped per target: 45 binding, 3 functional
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1009538 | Binding | Inhibition of human recombinant p21RAS by GDPX assay | Ophirapstanol trisulfate, a new biologically active steroid sulfate from the deep water marine sponge Topsentia ophiraphidites. — *J Nat Prod* |
| CHEMBL685869 | Functional | Concentration required to inhibit 50% of the cultured colonies of H-Ras-Fcells. | C-terminal modifications of histidyl-N-benzylglycinamides to give improved inhibition of Ras farnesyltransferase, cellular activity, and anticancer activity in mice. — *J Med Chem* |
Cellosaurus cell lines
505 cell lines: 310 cancer cell line, 149 transformed cell line, 29 spontaneously immortalized cell line, 8 telomerase immortalized cell line, 5 hybrid cell line, 4 induced pluripotent stem cell
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_0046 | HTh83 | Cancer cell line | Male |
| CVCL_0309 | HO-23 | Transformed cell line | Female |
| CVCL_0332 | Hs 578T | Cancer cell line | Female |
| CVCL_0505 | RL95-2 | Cancer cell line | Female |
| CVCL_0554 | T24 | Cancer cell line | Female |
| CVCL_0562 | TRM-6/PDX-1 | Transformed cell line | Sex unspecified |
| CVCL_0586 | YMB-A | Cancer cell line | Female |
| CVCL_0588 | ZR-75-1 | Cancer cell line | Female |
| CVCL_0590 | Kasumi-2 | Cancer cell line | Male |
| CVCL_0U15 | BRN-1 | Transformed cell line | Sex unspecified |
Clinical trials (associated diseases)
Via MONDO — disease-level, not drug-specific.
showing 60 of 452 trials:
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT00339118 | Phase 4 | UNKNOWN | EpSSG (European Soft Tissue Sarcoma Study Group) Protocol for Non-Metastatic Rhabdomyosarcoma in Children |
| NCT04854018 | Phase 4 | COMPLETED | Indo-cyanine Green (ICG) in Paediatric Oncology MIS |
| NCT01418118 | Phase 4 | COMPLETED | Assessment of the Effects of Pressors on Graft Blood Flow After Free Tissue Transfer Surgery |
| NCT03017053 | Phase 4 | UNKNOWN | The Optimal Neck Treatments Strategy of Early Oral Cancer Based on Adverse Pathological Factor |
| NCT03684707 | Phase 4 | UNKNOWN | Cancer Chemoprevention by Metformin Hydrochloride Compared to Placebo in Oral Potentially Malignant Lesions |
| NCT00162695 | Phase 3 | TERMINATED | Rhabdomyosarcoma and Malignant Soft Tissue Tumours of Childhood |
| NCT00354835 | Phase 3 | COMPLETED | Combination Chemotherapy and Radiation Therapy in Treating Patients With Newly Diagnosed Rhabdomyosarcoma |
| NCT02567435 | Phase 3 | ACTIVE_NOT_RECRUITING | Combination Chemotherapy With or Without Temsirolimus in Treating Patients With Intermediate Risk Rhabdomyosarcoma |
| NCT04994132 | Phase 3 | ACTIVE_NOT_RECRUITING | A Study to Compare Early Use of Vinorelbine and Maintenance Therapy for Patients With High Risk Rhabdomyosarcoma |
| NCT06836492 | Phase 3 | RECRUITING | A Prospective Clinical Cohort Study on Stratified Treatment of Rhabdomyosarcoma Based on Risk Factors. |
| NCT07466316 | Phase 3 | RECRUITING | A Study Comparing Higher Dose Chemotherapy Over a Shorter Amount of Time to Lower Dose Chemotherapy Plus Maintenance Over a Longer Amount of Time in Patients With Newly Diagnosed Intermediate-Risk Rhabdomyosarcoma (IR RMS) |
| NCT00384891 | Phase 3 | TERMINATED | Hyperthermia Treatment in Conjunction With Mitomycin C Versus Bacillus Calmette-Guérin Immunotherapy (BCG) for Superficial Bladder Cancer |
| NCT03335059 | Phase 3 | TERMINATED | Mitomycin C Intravesical Chemotherapy in Conjunction With Synergo® Radiofrequency-Induced Hyperthermia for Treatment of Carcinoma in Situ Non-Muscle Invasive Bladder Cancer Patients Unresponsive to Bacillus Calmette-Guérin, With or Without Papillary Tumors. |
| NCT04534075 | Phase 3 | COMPLETED | Dietary Fiber During Radiotherapy - a Placebo-controlled Randomized Trial |
| NCT05822934 | Phase 3 | UNKNOWN | Carboplatin-gemcitabine Versus Cisplatin- Gemcitabine as Neoadjuvant Chemotherapy for Treatment of Muscle Invasive Urinary Bladder Cancer |
| NCT00158652 | Phase 3 | COMPLETED | Accelerated Radiotherapy and Concomitant Chemo-radiotherapy in HNSCC |
| NCT00158678 | Phase 3 | COMPLETED | IMRT Plus Cisplatin Versus Conventional Radiotherapy Plus Cisplatin in Stage III-IV HNSCC |
| NCT00402779 | Phase 3 | COMPLETED | Erlotinib Prevention of Oral Cancer (EPOC) |
| NCT00655421 | Phase 3 | UNKNOWN | Oral Cancer Screening in Mumbai, India by Primary Health Care Workers |
| NCT00750503 | Phase 3 | COMPLETED | Workplace Tobacco Cessation And Oral Cancer Screening Study |
| NCT00964977 | Phase 3 | COMPLETED | Effectiveness of Adjuvant Radiotherapy in Small Oropharyngeal Squamous Cell Cancer and Single Lymph Node Metastasis. |
| NCT01039298 | Phase 3 | UNKNOWN | Efficacy of Optically-guided Surgery in the Management of Early-staged Oral Cancer - COOLS TRIAL |
| NCT03685409 | Phase 3 | UNKNOWN | Cancer Chemoprevention by Metformin Hydrochloride in Oral Potentially Malignant Lesions |
| NCT05721755 | Phase 3 | ACTIVE_NOT_RECRUITING | Combining Radiation Therapy With Immunotherapy for the Treatment of Metastatic Squamous Cell Carcinoma of the Head and Neck |
| NCT06589804 | Phase 3 | RECRUITING | Testing the Addition of Anti-Cancer Drug, Cetuximab, to Standard of Care Treatment (Pembrolizumab) for Returning or Spreading Head and Neck Cancer After Previous Treatment |
| NCT06737822 | Phase 3 | RECRUITING | Upfront Surgery Vs Induction Chemotherapy Followed By Surgery In Oral Cancers: |
| NCT07402538 | Phase 3 | NOT_YET_RECRUITING | Surgery With or Without Neoadjuvant Treatment of SBRT Plus Chemoimmunotherapy in Resectable Locally Advanced Oral and HPV-unrelated Oropharyngeal Squamous Cell Carcinoma |
| NCT07441681 | Phase 3 | RECRUITING | Comparing Radiation Plus Cetuximab to Radiation Plus Chemotherapy in People With Head and Neck Cancer Who Cannot Receive Cisplatin |
| NCT07827872 | Phase 3 | NOT_YET_RECRUITING | Neoadjuvant Sintilimab Plus Chemotherapy for cT2N0M0 Oral Squamous Cell Carcinoma |
| NCT00001335 | Phase 2 | COMPLETED | New Therapeutic Strategies for Patients With Ewing’s Sarcoma Family of Tumors, High Risk Rhabdomyosarcoma, and Neuroblastoma |
| NCT00001564 | Phase 2 | COMPLETED | A Pilot Study of Tumor-Specific Peptide Vaccination and IL-2 With or Without Autologous T Cell Transplantation in Recurrent Pediatric Sarcomas |
| NCT00001566 | Phase 2 | COMPLETED | A Pilot Study of Autologous T-Cell Transplantation With Vaccine Driven Expansion of Anti-Tumor Effectors After Cytoreductive Therapy in Metastatic Pediatric Sarcomas |
| NCT00180947 | Phase 2 | UNKNOWN | Study of Vinorelbine and Cyclofosfamide Among Patients With Refractory Tumours or in Relapse |
| NCT00186992 | Phase 2 | ACTIVE_NOT_RECRUITING | Radiation Therapy to Treat Musculoskeletal Tumors |
| NCT00464620 | Phase 2 | COMPLETED | Trial of Dasatinib in Advanced Sarcomas |
| NCT00520936 | Phase 2 | COMPLETED | A Study of Pemetrexed in Children With Recurrent Cancer |
| NCT00668148 | Phase 2 | COMPLETED | A Five-Tier, Open-Label Study of IMC-A12 in Advanced Sarcoma |
| NCT00840047 | Phase 2 | ACTIVE_NOT_RECRUITING | Methionine PET/CT Studies In Patients With Cancer |
| NCT01336803 | Phase 2 | COMPLETED | Differentiation of Bone Sarcomas and Osteomyelitis With Ferumoxytol-Enhanced MRI |
| NCT01355445 | Phase 2 | COMPLETED | Vincristine and Irinotecan With or Without Temozolomide in Children and Adults With Refractory/Relapsed Rhabdomyosarcoma |
| NCT01614795 | Phase 2 | COMPLETED | Cixutumumab and Temsirolimus in Treating Younger Patients With Recurrent or Refractory Sarcoma |
| NCT01807468 | Phase 2 | UNKNOWN | Haploidentical Stem Cell Transplantation and NK Cell Therapy in Patients With High-risk Solid Tumors |
| NCT01871766 | Phase 2 | ACTIVE_NOT_RECRUITING | Risk-Adapted Focal Proton Beam Radiation and/or Surgery in Patients With Low, Intermediate and High Risk Rhabdomyosarcoma Receiving Standard or Intensified Chemotherapy |
| NCT02011126 | Phase 2 | WITHDRAWN | Imetelstat Sodium in Treating Younger Patients With Relapsed or Refractory Solid Tumors |
| NCT02048371 | Phase 2 | COMPLETED | SARC024: A Blanket Protocol to Study Oral Regorafenib in Patients With Selected Sarcoma Subtypes |
| NCT02100891 | Phase 2 | TERMINATED | Phase 2 STIR Trial: Haploidentical Transplant and Donor Natural Killer Cells for Solid Tumors |
| NCT02452554 | Phase 2 | COMPLETED | Lorvotuzumab Mertansine in Treating Younger Patients With Relapsed or Refractory Wilms Tumor, Rhabdomyosarcoma, Neuroblastoma, Pleuropulmonary Blastoma, Malignant Peripheral Nerve Sheath Tumor, or Synovial Sarcoma |
| NCT02509598 | Phase 2 | COMPLETED | A Study of Lymphoseek® as a Lymphoid Tissue Targeting Agent in Pediatric Patients With Melanoma, Rhabdomyosarcoma, or Other Solid Tumors Who Are Undergoing Lymph Node Mapping |
| NCT02624388 | Phase 2 | TERMINATED | Study of Genistein in Pediatric Oncology Patients (UVA-Gen001) |
| NCT02689336 | Phase 2 | WITHDRAWN | Erlotinib in Combination With Temozolomide in Treating Relapsed/Recurrent/Refractory Pediatric Solid Tumors |
| NCT02867592 | Phase 2 | ACTIVE_NOT_RECRUITING | Cabozantinib-S-Malate in Treating Younger Patients With Recurrent, Refractory, or Newly Diagnosed Sarcomas, Wilms Tumor, or Other Rare Tumors |
| NCT02945800 | Phase 2 | COMPLETED | Nab-Paclitaxel and Gemcitabine for Recurrent/Refractory Sarcoma |
| NCT03155620 | Phase 2 | ACTIVE_NOT_RECRUITING | Targeted Therapy Directed by Genetic Testing in Treating Pediatric Patients With Relapsed or Refractory Advanced Solid Tumors, Non-Hodgkin Lymphomas, or Histiocytic Disorders (The Pediatric MATCH Screening Trial) |
| NCT03213652 | Phase 2 | ACTIVE_NOT_RECRUITING | Ensartinib in Treating Patients With Relapsed or Refractory Advanced Solid Tumors, Non-Hodgkin Lymphoma, or Histiocytic Disorders With ALK or ROS1 Genomic Alterations (A Pediatric MATCH Treatment Trial) |
| NCT03213665 | Phase 2 | COMPLETED | Tazemetostat in Treating Patients With Relapsed or Refractory Advanced Solid Tumors, Non-Hodgkin Lymphoma, or Histiocytic Disorders With EZH2, SMARCB1, or SMARCA4 Gene Mutations (A Pediatric MATCH Treatment Trial) |
| NCT03213678 | Phase 2 | COMPLETED | Samotolisib in Treating Patients With Relapsed or Refractory Advanced Solid Tumors, Non-Hodgkin Lymphoma, or Histiocytic Disorders With TSC or PI3K/MTOR Mutations (A Pediatric MATCH Treatment Trial) |
| NCT03213704 | Phase 2 | ACTIVE_NOT_RECRUITING | Larotrectinib in Treating Patients With Relapsed or Refractory Advanced Solid Tumors, Non-Hodgkin Lymphoma, or Histiocytic Disorders With NTRK Fusions (A Pediatric MATCH Treatment Trial) |
| NCT03220035 | Phase 2 | COMPLETED | Vemurafenib in Treating Patients With Relapsed or Refractory Advanced Solid Tumors, Non-Hodgkin Lymphoma, or Histiocytic Disorders With BRAF V600 Mutations (A Pediatric MATCH Treatment Trial) |
| NCT03233204 | Phase 2 | COMPLETED | Olaparib in Treating Patients With Relapsed or Refractory Advanced Solid Tumors, Non-Hodgkin Lymphoma, or Histiocytic Disorders With Defects in DNA Damage Repair Genes (A Pediatric MATCH Treatment Trial) |
| NCT03526250 | Phase 2 | COMPLETED | Palbociclib in Treating Patients With Relapsed or Refractory Rb Positive Advanced Solid Tumors, Non-Hodgkin Lymphoma, or Histiocytic Disorders With Activating Alterations in Cell Cycle Genes (A Pediatric MATCH Treatment Trial) |
Predicted chemistry — Sugi Predict
The predicted patent-compound landscape for HRAS across ~30M SureChEMBL compounds — explore on Sugi Predict.
Related Atlas pages
- Associated diseases: Costello syndrome, Noonan syndrome-like disorder with loose anagen hair, rhabdomyosarcoma, cancer, bladder transitional cell carcinoma, head and neck squamous cell carcinoma, skin squamous cell carcinoma, colorectal cancer, thyroid gland carcinoma
- Biomarker drugs (CIViC) (drugs whose response is associated with variants in this gene — CIViC predictive evidence, not targeting): Selumetinib, Tipifarnib, Vemurafenib, Cetuximab
- Targeted by drugs: Lonafarnib
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): arteriovenous malformations of the brain, bladder transitional cell carcinoma, cancer, colorectal carcinoma, congenital fibrosis of extraocular muscles, Costello syndrome, epidermolytic nevus, head and neck squamous cell carcinoma, hypophosphatemic rickets, intramuscular hemangioma, large congenital melanocytic nevus, linear nevus sebaceous syndrome, lip and oral cavity carcinoma, myopathy, congenital, with excess of muscle spindles, nevus, epidermal, non-immune hydrops fetalis, Noonan syndrome, Noonan syndrome 1, Noonan syndrome 3, Noonan syndrome and Noonan-related syndrome, Noonan syndrome-like disorder with loose anagen hair, parathyroid gland adenoma, phakomatosis pigmentokeratotica, prostate cancer, hereditary, 1, RASopathy, rhabdomyosarcoma, skin squamous cell carcinoma, spermatocytic seminoma, thyroid cancer, nonmedullary, 2, thyroid gland carcinoma, thyroid gland follicular carcinoma, tumor of salivary gland, urinary bladder cancer, vascular malformation, wooly hair nevus