MST1R
gene geneOn this page
Also known as CDw136CD136
Summary
MST1R (macrophage stimulating 1 receptor, HGNC:7381) is a protein-coding gene on chromosome 3p21.31, encoding Macrophage-stimulating protein receptor (Q04912). Receptor tyrosine kinase that transduces signals from the extracellular matrix into the cytoplasm by binding to MST1 ligand.
This gene encodes a cell surface receptor for macrophage-stimulating protein (MSP) with tyrosine kinase activity. The mature form of this protein is a heterodimer of disulfide-linked alpha and beta subunits, generated by proteolytic cleavage of a single-chain precursor. The beta subunit undergoes tyrosine phosphorylation upon stimulation by MSP. This protein is expressed on the ciliated epithelia of the mucociliary transport apparatus of the lung, and together with MSP, thought to be involved in host defense. Alternative splicing generates multiple transcript variants encoding different isoforms that may undergo similar proteolytic processing.
Source: NCBI Gene 4486 — RefSeq curated summary.
At a glance
- Gene–disease (curated): nasopharyngeal carcinoma, susceptibility to, 3 (Limited, GenCC)
- GWAS associations: 19
- Clinical variants (ClinVar): 273 total — 1 likely-pathogenic
- GTEx eGene: eQTL in 34 tissues, sQTL in 7 (q < 0.05)
- Phenotypes (HPO): 2
- Drug target: yes — 4 curated mechanism-of-action drugs; 42 molecules with ChEMBL bioactivity (top 1% of genes corpus-wide)
- Approved drugs (ChEMBL mechanism of action): 1 — Crizotinib
- Constraint (gnomAD): pLI 0.00 (LoF-tolerant), LOEUF 0.98 (unconstrained)
- MANE Select transcript:
NM_002447 - Notable: 273 clinical variants but no curated precision-oncology (CIViC) evidence yet
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:7381 |
| Approved symbol | MST1R |
| Name | macrophage stimulating 1 receptor |
| Location | 3p21.31 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | CDw136, CD136 |
| Ensembl gene | ENSG00000164078 |
| Ensembl biotype | protein_coding |
| OMIM | 600168 |
| Entrez | 4486 |
Gene structure
Transcript identifiers
Ensembl transcripts: 38 — 24 protein_coding, 7 nonsense_mediated_decay, 7 retained_intron
MANE Select: ENST00000296474
Transcript support level (Ensembl TSL; 1 = fully mRNA-supported): TSL 1: 6, TSL 2: 1, TSL 3: 2, TSL 4: 1, TSL 5: 3
ENST00000296474, ENST00000344206, ENST00000411578, ENST00000434765, ENST00000440292, ENST00000463789, ENST00000467110, ENST00000468525, ENST00000485044, ENST00000490053, ENST00000493535, ENST00000497001, ENST00000621387, ENST00000714251, ENST00000714252, ENST00000858906, ENST00000858907, ENST00000858908, ENST00000858909, ENST00000858910, ENST00000858911, ENST00000858912, ENST00000858913, ENST00000858914, ENST00000858915, ENST00000858916, ENST00000858917, ENST00000858918, ENST00000858919, ENST00000858920, ENST00000858921, ENST00000858922, ENST00000944850, ENST00001053126, ENST00001053127, ENST00001053128, ENST00001053129, ENST00001145193
RefSeq mRNA: 4 — MANE Select: NM_002447
NM_001244937, NM_001318913, NM_001437543, NM_002447
CCDS: CCDS2807, CCDS58833, CCDS82777
Canonical transcript exons
ENST00000296474 — 20 exons
| Exon | Start | End |
|---|---|---|
| ENSE00003292427 | 49895961 | 49896107 |
| ENSE00003549554 | 49898867 | 49898995 |
| ENSE00003566005 | 49898051 | 49898211 |
| ENSE00003583713 | 49897520 | 49897685 |
| ENSE00003603086 | 49899075 | 49899263 |
| ENSE00003681115 | 49898518 | 49898688 |
| ENSE00004023332 | 49895167 | 49895373 |
| ENSE00004023333 | 49891197 | 49891306 |
| ENSE00004023334 | 49890485 | 49890650 |
| ENSE00004023335 | 49896729 | 49896890 |
| ENSE00004023336 | 49891399 | 49891580 |
| ENSE00004023337 | 49896540 | 49896633 |
| ENSE00004023338 | 49897280 | 49897416 |
| ENSE00004023341 | 49896195 | 49896404 |
| ENSE00004023342 | 49895715 | 49895880 |
| ENSE00004023343 | 49887002 | 49887562 |
| ENSE00004023344 | 49902380 | 49903873 |
| ENSE00004023345 | 49889924 | 49890060 |
| ENSE00004023348 | 49891758 | 49891838 |
| ENSE00004023349 | 49895447 | 49895548 |
Expression profiles
Bgee: expression breadth ubiquitous, 191 present calls, max score 97.15.
FANTOM5 (CAGE): breadth broad, TPM avg 1.3794 / max 95.6933, expressed in 399 samples.
Highest expression (Bgee): mucosa of transverse colon, skin of leg, lower esophagus mucosa, skin of abdomen, rectum.
Genetic regulation across tissues (GTEx eQTL / sQTL)
MST1R is an eGene in GTEx v10 — its expression is genetically regulated (eQTL) in 34 tissues and its splicing (sQTL) in 7 (q < 0.05). Strongest associations first; slope = normalized effect of the lead variant’s alternative allele.
showing 20 of 41 significant tissue × QTL associations:
| Tissue | QTL | q-value | Slope | Lead variant |
|---|---|---|---|---|
| Skin Not Sun Exposed Suprapubic | sqtl | 2.0e-26 | +1.06 | 3:49890070:G:T |
| Skin Sun Exposed Lower leg | sqtl | 2.2e-20 | +0.89 | 3:49890289:A:C |
| Skin Not Sun Exposed Suprapubic | eqtl | 1.8e-18 | +0.21 | 3:49912401:A:T |
| Brain Cerebellum | eqtl | 2.4e-17 | -0.52 | 3:50026991:G:A |
| Skin Sun Exposed Lower leg | eqtl | 1.1e-14 | +0.17 | 3:49887507:T:C |
| Adipose Subcutaneous | eqtl | 4.8e-14 | +0.31 | 3:49904003:G:A |
| Cells Cultured fibroblasts | eqtl | 8.3e-13 | +0.37 | 3:49844916:C:T |
| Brain Cerebellar Hemisphere | eqtl | 8.5e-13 | +0.43 | 3:49872651:T:C |
| Thyroid | eqtl | 4.1e-12 | +0.26 | 3:49904003:G:A |
| Nerve Tibial | eqtl | 8.2e-11 | +0.29 | 3:49912401:A:T |
| Muscle Skeletal | eqtl | 1.4e-10 | +0.26 | 3:49904003:G:A |
| Lung | eqtl | 8.9e-10 | +0.19 | 3:49873722:G:A |
| Artery Tibial | eqtl | 3.2e-09 | -0.32 | 3:50050833:T:C |
| Esophagus Mucosa | sqtl | 3.4e-08 | +0.70 | 3:49923318:C:T |
| Brain Nucleus accumbens basal ganglia | eqtl | 5.9e-08 | -0.39 | 3:50003880:C:T |
| Brain Caudate basal ganglia | eqtl | 1.9e-07 | +0.39 | 3:49934081:C:A |
| Esophagus Muscularis | eqtl | 3.5e-07 | +0.17 | 3:49892782:C:T |
| Testis | sqtl | 3.7e-07 | +0.92 | 3:49891592:C:A |
| Brain Cortex | eqtl | 6.5e-07 | +0.41 | 3:49860567:A:G |
| Artery Aorta | eqtl | 8.6e-07 | +0.30 | 3:49904003:G:A |
FANTOM5 promoters
1 alternative TSS:
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 42284 | 1.3794 | 399 |
Top tissues by expression
showing 100 of 286 tissues by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| mucosa of transverse colon | UBERON:0004991 | 97.15 | gold quality |
| skin of leg | UBERON:0001511 | 94.27 | gold quality |
| lower esophagus mucosa | UBERON:0035834 | 94.06 | gold quality |
| skin of abdomen | UBERON:0001416 | 93.86 | gold quality |
| rectum | UBERON:0001052 | 92.60 | gold quality |
| body of stomach | UBERON:0001161 | 92.04 | gold quality |
| transverse colon | UBERON:0001157 | 91.72 | gold quality |
| small intestine Peyer’s patch | UBERON:0003454 | 91.05 | gold quality |
| zone of skin | UBERON:0000014 | 90.20 | gold quality |
| ileal mucosa | UBERON:0000331 | 90.16 | gold quality |
| gall bladder | UBERON:0002110 | 90.06 | gold quality |
| esophagus mucosa | UBERON:0002469 | 89.40 | gold quality |
| small intestine | UBERON:0002108 | 89.07 | gold quality |
| stomach | UBERON:0000945 | 88.88 | gold quality |
| mucosa of stomach | UBERON:0001199 | 87.84 | gold quality |
| upper lobe of left lung | UBERON:0008952 | 87.10 | gold quality |
| male germ line stem cell (sensu Vertebrata) in testis | CL:0000089 ∩ UBERON:0000473 | 87.02 | gold quality |
| duodenum | UBERON:0002114 | 85.71 | gold quality |
| upper lobe of lung | UBERON:0008948 | 85.35 | gold quality |
| pancreatic ductal cell | CL:0002079 | 85.05 | silver quality |
| intestine | UBERON:0000160 | 84.66 | gold quality |
| colon | UBERON:0001155 | 83.86 | gold quality |
| large intestine | UBERON:0000059 | 83.69 | gold quality |
| fundus of stomach | UBERON:0001160 | 83.56 | gold quality |
| right lung | UBERON:0002167 | 83.47 | gold quality |
| colonic mucosa | UBERON:0000317 | 82.96 | gold quality |
| apex of heart | UBERON:0002098 | 82.96 | gold quality |
| esophagus | UBERON:0001043 | 82.57 | gold quality |
| jejunal mucosa | UBERON:0000399 | 82.10 | gold quality |
| olfactory segment of nasal mucosa | UBERON:0005386 | 81.95 | gold quality |
| vagina | UBERON:0000996 | 81.74 | gold quality |
| right testis | UBERON:0004534 | 81.61 | gold quality |
| left testis | UBERON:0004533 | 81.44 | gold quality |
| mucosa of sigmoid colon | UBERON:0004993 | 81.44 | gold quality |
| minor salivary gland | UBERON:0001830 | 81.19 | gold quality |
| pylorus | UBERON:0001166 | 79.68 | gold quality |
| body of pancreas | UBERON:0001150 | 79.52 | gold quality |
| mouth mucosa | UBERON:0003729 | 79.08 | gold quality |
| vermiform appendix | UBERON:0001154 | 78.65 | gold quality |
| testis | UBERON:0000473 | 77.62 | gold quality |
| sigmoid colon | UBERON:0001159 | 77.61 | gold quality |
| metanephros cortex | UBERON:0010533 | 77.27 | gold quality |
| right lobe of thyroid gland | UBERON:0001119 | 76.89 | gold quality |
| upper arm skin | UBERON:0004263 | 76.82 | gold quality |
| saliva-secreting gland | UBERON:0001044 | 76.73 | gold quality |
| muscle layer of sigmoid colon | UBERON:0035805 | 76.70 | gold quality |
| omental fat pad | UBERON:0010414 | 76.69 | gold quality |
| colonic epithelium | UBERON:0000397 | 76.63 | gold quality |
| peritoneum | UBERON:0002358 | 76.59 | gold quality |
| upper leg skin | UBERON:0004262 | 76.36 | gold quality |
| esophagogastric junction muscularis propria | UBERON:0035841 | 75.90 | gold quality |
| caecum | UBERON:0001153 | 75.32 | gold quality |
| left lobe of thyroid gland | UBERON:0001120 | 75.31 | gold quality |
| lower esophagus | UBERON:0013473 | 75.30 | gold quality |
| lower esophagus muscularis layer | UBERON:0035833 | 75.24 | gold quality |
| pancreas | UBERON:0001264 | 75.07 | gold quality |
| ectocervix | UBERON:0012249 | 74.73 | gold quality |
| adipose tissue of abdominal region | UBERON:0007808 | 74.72 | gold quality |
| nasal cavity epithelium | UBERON:0005384 | 74.45 | silver quality |
| thyroid gland | UBERON:0002046 | 74.07 | gold quality |
| palpebral conjunctiva | UBERON:0001812 | 73.96 | gold quality |
| lung | UBERON:0002048 | 73.88 | gold quality |
| adenohypophysis | UBERON:0002196 | 73.86 | gold quality |
| endocervix | UBERON:0000458 | 73.51 | gold quality |
| urinary bladder | UBERON:0001255 | 73.12 | gold quality |
| ascending aorta | UBERON:0001496 | 72.23 | gold quality |
| thoracic aorta | UBERON:0001515 | 72.00 | gold quality |
| right uterine tube | UBERON:0001302 | 71.81 | gold quality |
| islet of Langerhans | UBERON:0000006 | 71.63 | gold quality |
| cortical plate | UBERON:0005343 | 71.03 | gold quality |
| mucosa of urinary bladder | UBERON:0001259 | 70.86 | silver quality |
| nasal cavity mucosa | UBERON:0001826 | 70.83 | gold quality |
| pituitary gland | UBERON:0000007 | 70.36 | gold quality |
| heart left ventricle | UBERON:0002084 | 70.36 | gold quality |
| tongue squamous epithelium | UBERON:0006919 | 70.03 | gold quality |
| descending thoracic aorta | UBERON:0002345 | 69.61 | gold quality |
| cardiac ventricle | UBERON:0002082 | 69.46 | gold quality |
| tonsil | UBERON:0002372 | 69.18 | gold quality |
| right hemisphere of cerebellum | UBERON:0014890 | 69.17 | gold quality |
| uterine cervix | UBERON:0000002 | 69.13 | gold quality |
| gingival epithelium | UBERON:0001949 | 69.09 | silver quality |
| cervix squamous epithelium | UBERON:0006922 | 68.97 | gold quality |
| skin of hip | UBERON:0001554 | 68.77 | gold quality |
| cerebellar hemisphere | UBERON:0002245 | 68.54 | gold quality |
| left uterine tube | UBERON:0001303 | 68.49 | gold quality |
| smooth muscle tissue | UBERON:0001135 | 68.31 | gold quality |
| cerebellar cortex | UBERON:0002129 | 68.31 | gold quality |
| jejunum | UBERON:0002115 | 68.29 | gold quality |
| cardia of stomach | UBERON:0001162 | 68.18 | gold quality |
| right atrium auricular region | UBERON:0006631 | 68.07 | gold quality |
| prostate gland | UBERON:0002367 | 68.02 | gold quality |
| anatomical system | UBERON:0000467 | 67.54 | gold quality |
| endometrium epithelium | UBERON:0004811 | 67.41 | gold quality |
| right ovary | UBERON:0002118 | 67.37 | gold quality |
| body of uterus | UBERON:0009853 | 67.36 | gold quality |
| squamous epithelium | UBERON:0006914 | 67.05 | silver quality |
| multicellular organism | UBERON:0000468 | 67.03 | gold quality |
| material anatomical entity | UBERON:0000465 | 67.01 | gold quality |
| epithelium of bronchus | UBERON:0002031 | 67.01 | gold quality |
| aorta | UBERON:0000947 | 66.98 | gold quality |
Single-cell (SCXA)
Detected in 2 experiment(s), a significant marker in 1.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | yes | 6.00 |
| E-CURD-53 | no | 158.90 |
HPA expression
RNA tissue specificity: Tissue enhanced
showing 60 of 69 HPA tissues / cells by nTPM:
| Tissue / cell | Axis | nTPM | Protein (IHC) |
|---|---|---|---|
| Skin 1 | tissue | 30.2 | medium |
| Stomach 1 | tissue | 25.5 | medium |
| Duodenum | tissue | 18.2 | medium |
| Small intestine | tissue | 16.1 | medium |
| Colon | tissue | 12.1 | medium |
| Rectum | tissue | 10.3 | medium |
| Gallbladder | tissue | 6.4 | high |
| Vagina | tissue | 5.6 | low |
| Urinary bladder | tissue | 5.3 | medium |
| Lung | tissue | 5.2 | high |
| Thymus | tissue | 4.8 | |
| Esophagus | tissue | 3.6 | medium |
| Appendix | tissue | 3.6 | medium |
| Tonsil | tissue | 3.2 | medium |
| Breast | tissue | 1.8 | medium |
| Testis | tissue | 1.8 | medium |
| Lymph node | tissue | 1.6 | medium |
| Salivary gland | tissue | 1.6 | medium |
| Cervix | tissue | 1.5 | medium |
| Pancreas | tissue | 1.4 | medium |
| Pituitary gland | tissue | 1.1 | |
| Smooth muscle | tissue | 1.0 | medium |
| Thyroid gland | tissue | 0.9 | high |
| Adipose tissue | tissue | 0.8 | medium |
| Skeletal muscle | tissue | 0.8 | medium |
| Choroid plexus | tissue | 0.8 | |
| Hippocampus | tissue | 0.8 | medium |
| Fallopian tube | tissue | 0.8 | medium |
| Heart muscle | tissue | 0.7 | medium |
| Endometrium 1 | tissue | 0.6 | medium |
| Nucleus accumbens | tissue | 0.6 | |
| Prostate | tissue | 0.6 | medium |
| Seminal vesicle | tissue | 0.5 | medium |
| Epididymis | tissue | 0.5 | medium |
| Placenta | tissue | 0.5 | high |
| Spleen | tissue | 0.5 | low |
| Postcentral gyrus | tissue | 0.5 | |
| Ovary | tissue | 0.4 | high |
| Locus coeruleus | tissue | 0.4 | |
| Tongue | tissue | 0.3 | |
| Kidney | tissue | 0.3 | medium |
| Frontal cortex | tissue | 0.2 | |
| Superior colliculi | tissue | 0.2 | |
| Spinal cord | tissue | 0.2 | |
| Prefrontal cortex | tissue | 0.1 | |
| Cerebral cortex | tissue | 0.1 | medium |
| Retina | tissue | 0.1 | |
| Parathyroid gland | tissue | 0.1 | medium |
| Motor cortex | tissue | 0.1 | |
| Midbrain | tissue | 0.1 | |
| Thalamus | tissue | 0.1 | |
| Substantia nigra | tissue | 0.1 | |
| Liver | tissue | 0.1 | medium |
| Bone marrow | tissue | 0.1 | low |
| Hippocampal formation | tissue | 0.1 | |
| Entorhinal cortex | tissue | 0.1 | |
| Retrosplenial and cingulate cortex | tissue | 0.1 | |
| Somatosensory cortex | tissue | 0.1 | |
| Retrosplenial cortex | tissue | 0.1 | |
| Temporal cortex | tissue | 0.1 |
Brain sub-regions (HPA Brain Atlas): detected in 188; highest nTPM — Blood vessel (1.0), Cerebellar cortex (0.9), Claustrum (0.9), Inferior frontal gyrus, opercular (0.9), Orbitofrontal gyrus, anterior (0.9).
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): EGR1, HIF1A, IRF6, NFE2L2, NFKB, NFKBIA, RELA, SMAD4, SP1, TXK
miRNA regulators (miRDB)
Targeting MST1R by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific).
18 miRNAs:
| miRNA | Max score | Avg score | miRNA target_count |
|---|---|---|---|
| HSA-MIR-218-5P | 99.93 | 72.22 | 2103 |
| HSA-MIR-6721-5P | 99.93 | 68.92 | 2981 |
| HSA-MIR-4697-3P | 99.89 | 67.09 | 1123 |
| HSA-MIR-659-3P | 99.85 | 70.69 | 1620 |
| HSA-MIR-4766-5P | 99.75 | 69.23 | 2662 |
| HSA-MIR-4284 | 99.36 | 65.25 | 1293 |
| HSA-MIR-633 | 98.35 | 69.45 | 1167 |
| HSA-MIR-4436B-3P | 98.25 | 65.26 | 1494 |
| HSA-MIR-6735-5P | 98.24 | 65.36 | 1488 |
| HSA-MIR-7843-5P | 98.12 | 65.26 | 1421 |
| HSA-MIR-4632-5P | 97.82 | 65.38 | 1470 |
| HSA-MIR-6879-5P | 97.77 | 65.52 | 1521 |
| HSA-MIR-296-5P | 97.61 | 64.02 | 851 |
| HSA-MIR-6781-3P | 97.44 | 66.85 | 970 |
| HSA-MIR-2682-3P | 97.10 | 66.16 | 840 |
| HSA-MIR-874-5P | 96.93 | 63.92 | 1014 |
| HSA-MIR-3126-5P | 96.87 | 65.83 | 912 |
| HSA-MIR-6875-5P | 96.87 | 65.49 | 958 |
Functional genomics
gnomAD constraint: pLI 4.11e-28, LOEUF 0.985, missense Z 1.75 — population loss-of-function intolerance (pLI ≥ 0.9 = LoF-intolerant; lower LOEUF = more constrained). gnomAD
Regional missense constraint (gnomAD RMC): no regional variation along ENST00000296474 — one region, missense o/e 0.91.
Literature-anchored findings (GeneRIF, showing 40)
- overexpression of human wild-type RON causes the formation of lung tumors with unique biological characteristics in vivo (PMID:12214279)
- Transgenic mice in which surfactant protein C promoter was used to express human wild-type RON in distal lung epithelial cells developed multiple RON-expressing lung adenomas with distinct morphology & growth pattern which progressed to adenocarcinoma. (PMID:12419829)
- These data suggest that RON expression is altered in certain primary colon cancers. Abnormal accumulation of RON variants may play a role in the progression of certain colorectal cancers in vivo (PMID:12527888)
- HYAL2 receptor protein is associated with the RON receptor tyrosine kinase, rendering it functionally silent. (PMID:12676986)
- immunostaining and Western blot showed Ron in normal kidney and in all oncocytomas but never in renal cell carcinomas or in the renal carcinoma cell line Caki-1; Ron was expressed in phosphorylated, i.e., active, form (PMID:12766581)
- Ron tyrosine kinase receptor desensitization mediated by c-Cbl and its binding partner Grb2. (PMID:12802274)
- These data suggest that coexpression of the MET and RON receptors confer a selective advantage to ovarian cancer cells and might promote ovarian cancer progression. (PMID:12915129)
- Data show that macrophage stimulating protein (MSP) and its receptor (Ron) induce phosphorylation of both Ron and alpha6beta4 integrin, and result in activation of alpha3beta1 integrin. (PMID:12919677)
- the ron-sema domain can suppress the growth of macrophage-stimulating protein-responsive cells in culture (PMID:14597639)
- persistent RON expression and activation cause the loss of epithelial phenotypes (PMID:15001985)
- RON receptor can interact with each of the three members of the class B Plexins and control tumor invasive growth. (PMID:15184888)
- altered expression of RON in colon cancer cells is required to maintain tumorigenic phenotypes (PMID:15378025)
- Data suggest that RON initiates signaling pathways that negatively regulate HIV-1 transcription in monocytes/macrophages, and that HIV-1 suppresses RON function by decreasing protein levels in the brain to assure efficient replication. (PMID:15557181)
- Receptor RON and uts ligand macrophage stimulating protein are involved in the pathophysiology of endometriosis. (PMID:15764806)
- co-expression of RON and MET is associated with aggressive phenotype in node-negative breast cancer patients (PMID:15788670)
- The proto-oncogene, c-Cbl, which modulates ubiquitylation of RON, was increased in glia in both multiple sclerosis brains and experimental autoimmune encephalomyelitis spinal cords (PMID:15929040)
- altered exon usage in the juxtamembrane domain of mouse and human RON regulates receptor activity and signaling specificity (PMID:16166096)
- Mst1r tyrosine kinase-domain deficient-mice have decreased survival times, alterations in cytokine and nitric oxide regulation, and an earlier onset of pulmonary pathology compared with control mice during acute lung injury (PMID:16166746)
- RON activation induced molecular and cellular alterations consistent with epithelial-mesenchymal (EMT) transition. (PMID:17311308)
- These data suggest that high molecular form hyaluronan is broken down by reactive oxygen species to form low-molecular-weight fragments that signal via RHAMM and RON to stimulate beat frequency. (PMID:17395888)
- overexpression of MSP, MT-SP1, and MST1R was a strong independent indicator of both metastasis and death in human breast cancer (PMID:17456594)
- This study reveals for the first time that RON alone is sufficient to induce complete and stabilized EMT in MDCK cells. (PMID:17588532)
- RONdelta170 is a naturally occurring variant with dominant negative activities and has potential for inhibiting RON-mediated tumorigenic activities in colorectal cancer cells. (PMID:17611409)
- RON receptor signaling may contribute to pancreatic carcinogenesis (PMID:17616662)
- high expression of Ron in the colorectal mucosa of ulcerative colitis patients suggests that this receptor might play roles in the pathophysiological background of this disease (PMID:18019691)
- Translocation of c-Met to the nucleus depends upon the adaptor protein Gab1 and importin beta1, and formation of Ca(2+) signals in turn depends upon this translocation (PMID:18073207)
- a clear link between Sp1-dependent RON tyrosine kinase expression and invasion of breast carcinoma cells. (PMID:18165235)
- the linkage disequilibrium with these functional MST1R variants implicate this gene as having a possible role in Crohn Disease pathogenesis. (PMID:18200509)
- RON activation differentially regulates claudin expression in epithelial cells (PMID:18204077)
- RON represses HIV transcription at multiple transcriptional check points including initiation, elongation and chromatin organization. (PMID:18209063)
- We found that RON was over expressed in bladder cancer but RON over expression was not associated with overall survival or other clinical parameters (PMID:18221954)
- loss of Smad4 contributes to aberrant RON expression and cross-talk of Smad4-independent TGF-beta signaling and the RON pathway promotes an invasive phenotype (PMID:18310076)
- The regulation of human RON gene expression by nuclear factor-kappaB; a potential therapeutic role for curcumin in blocking RON tyrosine kinase-mediated invasion of carcinoma cells. (PMID:18593918)
- study demonstrates that HIV-1 Tat targets the receptor tyrosine kinase recepteur d’origine nantais (RON), which negatively regulates inflammation & HIV transcription, for proteosome degradation (PMID:18606710)
- Ron is a critical factor in tumorigenesis. (PMID:18620091)
- RON has 2 alternative SRC-kinase-mediated modes of signaling that can contribute to oncogenic behavior in normal breast epithelial cells: an MSP-dependent increase in cell proliferation & migration and MSP-independent increased cell survival. (PMID:18836480)
- The entire C-terminus is required for RON or RON160-mediated intracellular signaling events leading to various cellular activities. (PMID:18950514)
- RON expression is significant in gastric carcinoma tissue and corresponding paraneoplastic tissue, but is not expressed in normal gastric mucosa. RON expression in gastric carcinoma tissue was not related to patient survival rates. (PMID:19040718)
- Results demonstrate that Ron plays an essential role in maintaining malignant phenotypes of colon cancer cells through regulating mutant PI3K activity. (PMID:19224914)
- RON is involved in mesangial cell proliferation under both physiological and pathological conditions (PMID:19242504)
Cross-species orthologs
3 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | mst1ra | ENSDARG00000060235 |
| mus_musculus | Mst1r | ENSMUSG00000032584 |
| rattus_norvegicus | Mst1r | ENSRNOG00000032618 |
Paralogs (53): INSRR (ENSG00000027644), MUSK (ENSG00000030304), FLT4 (ENSG00000037280), EPHA3 (ENSG00000044524), ROS1 (ENSG00000047936), LTK (ENSG00000062524), ERBB3 (ENSG00000065361), TIE1 (ENSG00000066056), FGFR2 (ENSG00000066468), FGFR3 (ENSG00000068078), EPHA8 (ENSG00000070886), FGFR1 (ENSG00000077782), EPHA6 (ENSG00000080224), TYRO3 (ENSG00000092445), FLT1 (ENSG00000102755), MET (ENSG00000105976), EPHB6 (ENSG00000106123), PDGFRB (ENSG00000113721), EPHA4 (ENSG00000116106), TEK (ENSG00000120156), FLT3 (ENSG00000122025), KDR (ENSG00000128052), EPHB2 (ENSG00000133216), PDGFRA (ENSG00000134853), EPHA7 (ENSG00000135333), IGF1R (ENSG00000140443), NTRK3 (ENSG00000140538), ERBB2 (ENSG00000141736), EPHA2 (ENSG00000142627), EPHA5 (ENSG00000145242), EGFR (ENSG00000146648), EPHA1 (ENSG00000146904), NTRK2 (ENSG00000148053), MERTK (ENSG00000153208), EPHB1 (ENSG00000154928), KIT (ENSG00000157404), FGFR4 (ENSG00000160867), DDR2 (ENSG00000162733), RYK (ENSG00000163785), LMTK2 (ENSG00000164715), RET (ENSG00000165731), AXL (ENSG00000167601), ROR2 (ENSG00000169071), ALK (ENSG00000171094), INSR (ENSG00000171105), ERBB4 (ENSG00000178568), CSF1R (ENSG00000182578), EPHB3 (ENSG00000182580), EPHA10 (ENSG00000183317), ROR1 (ENSG00000185483), EPHB4 (ENSG00000196411), NTRK1 (ENSG00000198400), DDR1 (ENSG00000204580)
Mouse-model phenotypes
Observed phenotypes of the mouse ortholog (MGI:99614) from MGI (Alliance of Genome Resources) — knockout/mutant phenotypes, ranked by annotation count. 20 distinct phenotype terms.
| Mouse phenotype (MP) | Records |
|---|---|
| abnormal macrophage physiology | 3 |
| increased susceptibility to Retroviridae infection | 3 |
| enlarged spleen | 2 |
| increased susceptibility to bacterial infection | 2 |
| abnormal type IV hypersensitivity reaction | 2 |
| abnormal ovary morphology | 1 |
| small ovary | 1 |
| hepatic necrosis | 1 |
| increased inflammatory response | 1 |
| decreased susceptibility to bacterial infection | 1 |
| increased circulating alanine transaminase level | 1 |
| decreased spleen weight | 1 |
| increased acute inflammation | 1 |
| increased interferon-gamma secretion | 1 |
| increased circulating interferon-gamma level | 1 |
| increased susceptibility to endotoxin shock | 1 |
| increased susceptibility to xenobiotic induced morbidity/mortality | 1 |
| embryonic lethality between implantation and somite formation, complete penetrance | 1 |
| decreased susceptibility to Retroviridae infection | 1 |
| decreased superovulation rate | 1 |
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 |
|---|---|---|---|
| Felis catus | A0M8S8 | 100.0% | Diamond |
| Neofelis nebulosa | Q07E37 | 100.0% | Diamond |
| Pan troglodytes | Q2QLF1 | 99.8% | Diamond |
| Gorilla gorilla gorilla | Q2IBF2 | 99.7% | Diamond |
| Pongo abelii | Q2IBD8 | 99.5% | Diamond |
| Papio anubis | A0M8R7 | 99.3% | Diamond |
| Colobus guereza | Q07DZ1 | 99.3% | Diamond |
| Chlorocebus aethiops | Q2IBA6 | 99.3% | Diamond |
| Aotus nancymaae | Q07DV8 | 99.1% | Diamond |
| Nomascus leucogenys | Q07DY1 | 99.1% | Diamond |
| Ateles geoffroyi | Q09YL1 | 99.1% | Diamond |
| Drosophila sechellia | B4HNW4 | 99.0% | Diamond |
| Drosophila simulans | B4QC63 | 99.0% | Diamond |
| Saimiri boliviensis boliviensis | Q09YH7 | 99.0% | Diamond |
| Drosophila persimilis | B4GBH0 | 98.9% | Diamond |
| Drosophila pseudoobscura pseudoobscura | Q290N5 | 98.9% | Diamond |
| Plecturocebus moloch | Q2QLC0 | 98.6% | Diamond |
| Drosophila melanogaster | Q6AWJ9 | 98.5% | Diamond |
| Callithrix jacchus | Q2QLG5 | 97.7% | Diamond |
| Ovis aries | Q09YI9 | 97.5% | Diamond |
| Bos taurus | Q769I5 | 97.5% | Diamond |
| Drosophila erecta | B3NS99 | 97.4% | Diamond |
| Drosophila yakuba | B4P5Q9 | 97.4% | Diamond |
| Muntiacus muntjak | Q09YK0 | 97.4% | Diamond |
| Eulemur macaco macaco | Q2IBG7 | 97.4% | Diamond |
| Microcebus murinus | Q2QL89 | 97.4% | Diamond |
| Mustela putorius furo | Q07E24 | 96.4% | Diamond |
| Canis lupus familiaris | Q75ZY9 | 96.4% | Diamond |
| Xenopus tropicalis | A0JM20 | 95.5% | Diamond |
| Xenopus laevis | Q8QFP9 | 95.5% | Diamond |
| Equus caballus | Q2QLA9 | 94.9% | Diamond |
| Sus scrofa | Q2QLE0 | 94.9% | Diamond |
| Otolemur garnettii | Q2QLH6 | 94.0% | Diamond |
| Atelerix albiventris | Q00PJ8 | 92.0% | Diamond |
| Loxodonta africana | Q108U6 | 91.8% | Diamond |
| Dasypus novemcinctus | Q07E48 | 91.4% | Diamond |
| Oryctolagus cuniculus | Q09YN5 | 91.2% | Diamond |
| Rhinolophus ferrumequinum | Q2IBC0 | 90.1% | Diamond |
| Drosophila ananassae | B3MH43 | 88.7% | Diamond |
| Echinops telfairi | A1X150 | 87.8% | 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 |
|---|---|---|
| SEMA3F-AS1 | ncRNA | 100129060 |
| RBM5-AS1 | ncRNA | 100775107 |
| RBM5 | protein-coding | 10181 |
| SEMA3F | protein-coding | 6405 |
| MON1A | protein-coding | 84315 |
| MIR5193 | ncRNA | 100847079 |
| TRAIP | protein-coding | 10293 |
| UBA7 | protein-coding | 7318 |
| CAMKV | protein-coding | 79012 |
| RBM6 | protein-coding | 10180 |
Protein
Protein identifiers
Macrophage-stimulating protein receptor — Q04912 (reviewed: Q04912)
Alternative names: CDw136, Protein-tyrosine kinase 8, p185-Ron
All UniProt accessions (6): Q04912, A0AAQ5BHR6, A0AAQ5BHX4, H7C074, H7C3Z8, J3KQS7
UniProt curated annotations — full annotation on UniProt →
Function. Receptor tyrosine kinase that transduces signals from the extracellular matrix into the cytoplasm by binding to MST1 ligand. Regulates many physiological processes including cell survival, migration and differentiation. Ligand binding at the cell surface induces autophosphorylation of RON on its intracellular domain that provides docking sites for downstream signaling molecules. Following activation by ligand, interacts with the PI3-kinase subunit PIK3R1, PLCG1 or the adapter GAB1. Recruitment of these downstream effectors by RON leads to the activation of several signaling cascades including the RAS-ERK, PI3 kinase-AKT, or PLCgamma-PKC. RON signaling activates the wound healing response by promoting epithelial cell migration, proliferation as well as survival at the wound site. Also plays a role in the innate immune response by regulating the migration and phagocytic activity of macrophages. Alternatively, RON can also promote signals such as cell migration and proliferation in response to growth factors other than MST1 ligand.
Subunit / interactions. Heterodimer of an alpha chain and a beta chain which are disulfide linked. Binds PLXNB1. Associates with and is negatively regulated by HYAL2. Interacts when phosphorylated with downstream effectors including PIK3R1, PCLG1, GRB2 and GAB1. Interacts with integrin beta1/ITGB1 in a ligand-independent fashion.
Subcellular location. Membrane.
Tissue specificity. Expressed in colon, skin, lung and bone marrow.
Post-translational modifications. Proteolytic processing yields the two subunits. Autophosphorylated in response to ligand binding on Tyr-1238 and Tyr-1239 in the kinase domain leading to further phosphorylation of Tyr-1353 and Tyr-1360 in the C-terminal multifunctional docking site. Ubiquitinated. Ubiquitination by CBL regulates the receptor stability and activity through proteasomal degradation. O-mannosylation of IPT/TIG domains on Thr or Ser residues by TMEM260 is required for protein maturation. O-mannosylated residues are composed of single mannose glycans that are not elongated or modified.
Disease relevance. Nasopharyngeal carcinoma, 3 (NPCA3) [MIM:617075] A form of nasopharyngeal carcinoma, a malignant neoplasm that originates in the nasopharyngeal epithelium and includes 4 subtypes: keratinizing squamous cell, non-keratinizing, basaloid squamous cell, and papillary adenocarcinoma. Disease susceptibility is associated with variants affecting the gene represented in this entry.
Activity regulation. In its inactive state, the C-terminal tail interacts with the catalytic domain and inhibits the kinase activity. Upon ligand binding, the C-terminal tail is displaced and becomes phosphorylated, thus increasing the kinase activity.
Miscellaneous. Lacks part of the extracellular domain, oligomerizes and is constitutively activated. Expressed at higher level in cancer cells.
Similarity. Belongs to the protein kinase superfamily. Tyr protein kinase family.
Isoforms (7)
| UniProt ID | Names | Canonical? |
|---|---|---|
| Q04912-1 | RON | yes |
| Q04912-2 | Delta-RON, sf-RON | |
| Q04912-3 | RON-1 | |
| Q04912-4 | RON-2 | |
| Q04912-5 | RON-3 | |
| Q04912-6 | RON-4 | |
| Q04912-7 | RON-5 |
RefSeq proteins (4): NP_001231866, NP_001305842, NP_001424472, NP_002438* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR000719 | Prot_kinase_dom | Domain |
| IPR001245 | Ser-Thr/Tyr_kinase_cat_dom | Domain |
| IPR001627 | Semap_dom | Domain |
| IPR002165 | Plexin_repeat | Repeat |
| IPR002909 | IPT_dom | Domain |
| IPR008266 | Tyr_kinase_AS | Active_site |
| IPR011009 | Kinase-like_dom_sf | Homologous_superfamily |
| IPR013783 | Ig-like_fold | Homologous_superfamily |
| IPR014756 | Ig_E-set | Homologous_superfamily |
| IPR015943 | WD40/YVTN_repeat-like_dom_sf | Homologous_superfamily |
| IPR016201 | PSI | Domain |
| IPR016244 | Tyr_kinase_HGF/MSP_rcpt | Family |
| IPR017441 | Protein_kinase_ATP_BS | Binding_site |
| IPR020635 | Tyr_kinase_cat_dom | Domain |
| IPR036352 | Semap_dom_sf | Homologous_superfamily |
| IPR039413 | RON_Sema | Domain |
| IPR050122 | RTK | Family |
Pfam: PF01403, PF01437, PF01833, PF07714
Enzyme classification (BRENDA)
- EC 2.7.10.1 — receptor protein-tyrosine kinase (BRENDA: 44 organisms, 214 substrates, 574 inhibitors, 11 Km, 0 kcat entries)
Substrate kinetics (BRENDA)
4 substrates with measured Km, best-characterized 4. Km ranges are aggregated across organisms/conditions.
| Substrate | Km (mM) | Measurements |
|---|---|---|
| ATP | 0.0011–0.129 | 4 |
| AC-DYFE-6-CHLORO-W-NHME | 0.0051 | 1 |
| AC-DYFGW-NHME | 0.07 | 1 |
| YFEW | 0.232 | 1 |
Catalyzed reactions (Rhea)
- L-tyrosyl-[protein] + ATP = O-phospho-L-tyrosyl-[protein] + ADP + H(+) (RHEA:10596)
UniProt features (168 total): strand 57, helix 31, sequence variant 20, disulfide bond 11, turn 9, glycosylation site 8, splice variant 8, domain 5, binding site 4, modified residue 4, chain 3, topological domain 2, sequence conflict 2, signal peptide 1, region of interest 1, active site 1, transmembrane region 1
Structure
Experimental structures (PDB)
4 structures by resolution:
| PDB | Title | Method | Resolution (Å) |
|---|---|---|---|
| 4FWW | Crystal structure of the Sema-PSI extracellular domains of human RON receptor tyrosine … | X-RAY DIFFRACTION | 1.85 |
| 8ZKD | The Crystal Structure of the RON from Biortus. | X-RAY DIFFRACTION | 2.05 |
| 3PLS | RON in complex with ligand AMP-PNP | X-RAY DIFFRACTION | 2.24 |
| 4QT8 | Crystal Structure of RON Sema-PSI-IPT1 extracellular domains in complex with MSP … | X-RAY DIFFRACTION | 3 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q04912-F1 | 80.23 | 0.46 |
Human Protein Atlas
Protein class: Enzymes, ENZYME proteins, Transferases, Kinases, Tyr protein kinases, CD markers, Predicted membrane proteins, Predicted intracellular proteins, Disease related genes, FDA approved drug targets, Small molecule drugs, Human disease related genes
Protein evidence: Evidence at protein level
Subcellular location (HPA, imaging): cytosol
Antibody reliability (HPA): IH enhanced · IF approved
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Catalytic / active sites (1)
| Position | Role |
|---|---|
| 1208 | proton acceptor |
Ligand- & substrate-binding residues (4)
| Position | Role |
|---|---|
| 1088–1096 | ATP |
| 1114 | ATP |
| 1161–1164 | ATP |
| 1212 | ATP |
Post-translational modifications (4)
| Type | Positions |
|---|---|
| Phosphotyrosine | 1238, 1239, 1353, 1360 |
Disulfide bonds (11)
| Type | Positions |
|---|---|
| Disulfide bond | 101–104, 107–162, 135–143, 174–177, 300–367, 385–407, 386–422, 527–545, 533–567, 536–552, 548–558 |
Glycosylation sites (8)
| Type | Positions |
|---|---|
| N-linked (glcnac…) asparagine | 66, 419, 458, 488, 654, 720, 841, 897 |
Function
Pathways and Gene Ontology
Reactome pathways
1 curated (TAS) of 3; 0 disease pathways. Curated-first; evidence = TAS (manually curated) vs IEA (electronic inference).
3 pathways:
| ID | Pathway | Evidence |
|---|---|---|
| R-HSA-8852405 | Signaling by MST1 | curated |
| R-HSA-162582 | Signal Transduction | — |
| R-HSA-9006934 | Signaling by Receptor Tyrosine Kinases | — |
MSigDB gene sets: 195 (showing top):
GOBP_SINGLE_FERTILIZATION, GOBP_REGULATION_OF_PHOSPHORYLATION, MODULE_255, GOBP_RESPONSE_TO_PEPTIDE, JAEGER_METASTASIS_DN, MODULE_64, GOBP_POSITIVE_REGULATION_OF_MAPK_CASCADE, MODULE_317, GOCC_CELL_SURFACE, GOBP_REGULATION_OF_TRANSFERASE_ACTIVITY, GOBP_VESICLE_MEDIATED_TRANSPORT, HERNANDEZ_MITOTIC_ARREST_BY_DOCETAXEL_2_DN, KANG_FLUOROURACIL_RESISTANCE_DN, MARTINEZ_RB1_TARGETS_UP, GOBP_POSITIVE_REGULATION_OF_CATALYTIC_ACTIVITY
GO Biological Process (16): phagocytosis (GO:0006909), defense response (GO:0006952), signal transduction (GO:0007165), cell surface receptor protein tyrosine kinase signaling pathway (GO:0007169), single fertilization (GO:0007338), nervous system development (GO:0007399), positive regulation of cell population proliferation (GO:0008284), response to virus (GO:0009615), cell migration (GO:0016477), positive regulation of MAP kinase activity (GO:0043406), innate immune response (GO:0045087), positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction (GO:0051897), immune system process (GO:0002376), protein phosphorylation (GO:0006468), macrophage colony-stimulating factor signaling pathway (GO:0038145), semaphorin-plexin signaling pathway (GO:0071526)
GO Molecular Function (11): transmembrane receptor protein tyrosine kinase activity (GO:0004714), macrophage colony-stimulating factor receptor activity (GO:0005011), ATP binding (GO:0005524), enzyme binding (GO:0019899), nucleotide binding (GO:0000166), protein kinase activity (GO:0004672), protein tyrosine kinase activity (GO:0004713), protein binding (GO:0005515), kinase activity (GO:0016301), transferase activity (GO:0016740), semaphorin receptor activity (GO:0017154)
GO Cellular Component (6): stress fiber (GO:0001725), vacuole (GO:0005773), plasma membrane (GO:0005886), cell surface (GO:0009986), signaling receptor complex (GO:0043235), membrane (GO:0016020)
Reactome top-level categories
2 top-level categories:
| Category | Pathways |
|---|---|
| Signaling by Receptor Tyrosine Kinases | 1 |
| Signal Transduction | 1 |
GO top-level categories
58 GO namespaces:
| Category | Terms |
|---|---|
| cellular anatomical structure | 2 |
| endocytosis | 1 |
| response to stress | 1 |
| cell communication | 1 |
| cellular process | 1 |
| signaling | 1 |
| regulation of cellular process | 1 |
| cellular response to stimulus | 1 |
| enzyme-linked receptor protein signaling pathway | 1 |
| fertilization | 1 |
| system development | 1 |
| animal gross anatomical part developmental process | 1 |
| cell population proliferation | 1 |
| regulation of cell population proliferation | 1 |
| positive regulation of cellular process | 1 |
| response to other organism | 1 |
| cell motility | 1 |
| MAP kinase activity | 1 |
| regulation of MAP kinase activity | 1 |
| positive regulation of MAPK cascade | 1 |
| positive regulation of protein serine/threonine kinase activity | 1 |
| immune response | 1 |
| defense response to symbiont | 1 |
| phosphatidylinositol 3-kinase/protein kinase B signal transduction | 1 |
| regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction | 1 |
| positive regulation of intracellular signal transduction | 1 |
| biological_process | 1 |
| phosphorylation | 1 |
| protein modification process | 1 |
| cytokine-mediated signaling pathway | 1 |
| cellular response to macrophage colony-stimulating factor stimulus | 1 |
| cell surface receptor signaling pathway | 1 |
| protein tyrosine kinase activity | 1 |
| transmembrane receptor protein kinase activity | 1 |
| transmembrane receptor protein tyrosine kinase activity | 1 |
| macrophage colony-stimulating factor signaling pathway | 1 |
| adenyl ribonucleotide binding | 1 |
| purine ribonucleoside triphosphate binding | 1 |
| anion binding | 1 |
| protein binding | 1 |
| nucleoside phosphate binding | 1 |
| heterocyclic compound binding | 1 |
| kinase activity | 1 |
| phosphotransferase activity, alcohol group as acceptor | 1 |
| catalytic activity, acting on a protein | 1 |
| protein kinase activity | 1 |
| binding | 1 |
| transferase activity, transferring phosphorus-containing groups | 1 |
| catalytic activity | 1 |
| transmembrane signaling receptor activity | 1 |
| semaphorin-plexin signaling pathway | 1 |
| actomyosin | 1 |
| contractile actin filament bundle | 1 |
| cytoplasm | 1 |
| intracellular membrane-bounded organelle | 1 |
| membrane | 1 |
| cell periphery | 1 |
| protein-containing complex | 1 |
Experimentally-supported GO annotations
GO terms backed by direct experimental evidence (ECO experimental codes) — 5 of 33 annotations. The rest are phylogenetic / computational / electronic (IEA).
5 experimentally-supported GO terms:
| GO term | NS | Evidence |
|---|---|---|
| positive regulation of MAP kinase activity | BP | direct assay |
| positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction | BP | direct assay |
| response to virus | BP | direct assay |
| cell surface | CC | high-throughput assay |
| enzyme binding | MF | physical interaction |
Protein interactions and networks
STRING
showing 15 of 1,122 interactions by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| MST1R | MST1 | P26927 | 965 |
| MST1R | HYAL2 | Q12891 | 788 |
| MST1R | HGF | P14210 | 764 |
| MST1R | SRSF1 | Q07955 | 750 |
| MST1R | SPAM1 | P38567 | 746 |
| MST1R | APEH | P13798 | 695 |
| MST1R | HNRNPA1 | P09651 | 636 |
| MST1R | HYAL1 | Q12794 | 582 |
| MST1R | SEMA3B | Q13214 | 442 |
| MST1R | RNF123 | Q5XPI4 | 441 |
| MST1R | ST14 | Q9Y5Y6 | 439 |
| MST1R | UBA7 | P41226 | 438 |
| MST1R | INAVA | Q3KP66 | 438 |
| MST1R | SEMA6A | Q9H2E6 | 437 |
| MST1R | MKNK2 | Q9HBH9 | 427 |
IntAct
Human interaction partners of MST1R in IntAct, one row per partner (best MIscore; records = supporting IntAct interaction records).
11 partners by confidence:
| Partner | Interaction type | MIscore | Records |
|---|---|---|---|
| MST1 | direct interaction | 0.720 | 5 |
| PLXNB1 | physical association | 0.520 | 3 |
| PLXNB2 | physical association | 0.520 | 2 |
| PLXNB3 | physical association | 0.520 | 2 |
| CBL | direct interaction | 0.440 | 1 |
| FURIN | cleavage reaction | 0.440 | 1 |
| PKM | phosphorylation reaction | 0.440 | 1 |
| UBL4A | association | 0.420 | 1 |
| YWHAQ | physical association | 0.370 | 1 |
| YWHAZ | association | 0.350 | 1 |
| SHTN1 | proximity | 0.270 | 1 |
BioGRID (206 interactions; top human partners by supporting records): BAG6 (Affinity Capture-MS; 2 records), CBL (Affinity Capture-Western; 2 records), CDC37 (Affinity Capture-MS; 2 records), GAB1 (Affinity Capture-Western; 2 records), GRB2 (Reconstituted Complex; 2 records), HSPA1B (Affinity Capture-MS; 2 records), PPP1CA (Biochemical Activity; 2 records), STUB1 (Biochemical Activity; 2 records), UBL4A (Affinity Capture-MS; 2 records), ADCY7 (Co-fractionation), AGGF1 (Proximity Label-MS), AIMP1 (Proximity Label-MS), AKAP1 (Proximity Label-MS), AKT1 (Biochemical Activity), ALDH6A1 (Co-fractionation)
SIGNOR signaling
9 signaling interactions:
| A | Effect | B | Mechanism |
|---|---|---|---|
| AKT | up-regulates | MST1R | phosphorylation |
| N-[4-[(2-amino-3-chloro-4-pyridinyl)oxy]-3-fluorophenyl]-4-ethoxy-1-(4-fluorophenyl)-2-oxo-3-pyridinecarboxamide | down-regulates | MST1R | “chemical inhibition” |
| N-[[3-fluoro-4-[[2-(1-methyl-4-imidazolyl)-7-thieno[3,2-b]pyridinyl]oxy]anilino]-sulfanylidenemethyl]-2-phenylacetamide | down-regulates | MST1R | “chemical inhibition” |
| MK-2461 | down-regulates | MST1R | “chemical inhibition” |
| AKT1 | up-regulates | MST1R | phosphorylation |
| MST1R | “up-regulates activity” | CTNNB1 | phosphorylation |
| EGFR | “up-regulates activity” | MST1R | phosphorylation |
| MST1 | up-regulates | MST1R | binding |
| MST1R | “up-regulates activity” | ABL1 | phosphorylation |
Protein complexes (CORUM) (1)
Experimentally-characterized complexes this protein is a subunit of (★ = the complex contains a known drug target).
1 complexes by size:
| Complex | Subunits | Members |
|---|---|---|
| ★ MET-MST1R complex | 2 | MET, MST1R |
Ligand–receptor pairs (CellPhoneDB) (1)
Curated ligand–receptor partners (cell-cell communication), distinct from the protein–protein interactions above.
1 ligand–receptor pairs:
| Partner | This gene’s role | Signaling class |
|---|---|---|
| MST1 | receptor |
Disease & clinical
Genetic variants
Variant evidence for MST1R: 273 ClinVar records (1 pathogenic / likely pathogenic); 19 GWAS associations. Per-variant detail is on Sugi Variant.
ClinVar
273 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 1 |
| Uncertain significance | 195 |
| Likely benign | 27 |
| Benign | 16 |
Top pathogenic / likely-pathogenic (1)
Showing all 1 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 |
|---|---|---|---|---|
| 800321 | NM_002447.4(MST1R):c.1477G>T (p.Asp493Tyr) | Likely pathogenic | no assertion criteria provided | 1 |
Per-variant reference — Sugi Variant
Explore MST1R’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.
SpliceAI
Top 10 splice-impact sites by Δscore (adjacent positions with the same effect merged into one range; 28 predictions of 1,921):
| Position(s) | Effect | Δscore | Sites |
|---|---|---|---|
| 3:49887563–49887564 | acceptor_loss | 1.0000 | 5 |
| 3:49890484 | donor_loss | 1.0000 | |
| 3:49890652 | acceptor_gain | 1.0000 | |
| 3:49891397–49891398 | donor_loss | 1.0000 | 5 |
| 3:49895263 | donor_gain | 1.0000 | |
| 3:49897417–49897418 | acceptor_loss | 1.0000 | 5 |
| 3:49898689–49898690 | acceptor_loss | 1.0000 | 3 |
| 3:49890483–49890484 | donor_loss | 0.9900 | 5 |
| 3:49890651 | acceptor_gain | 0.9900 | |
| 3:49890658 | acceptor_gain | 0.9900 |
AlphaMissense
1,976 missense substitutions predicted likely pathogenic (of 9,011 scored), across 540 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 |
|---|---|---|---|
| M1196 | 9 | 0.878 | 0.966 |
| M1254 | 9 | 0.857 | 0.960 |
| D1269 | 8 | 0.963 | 0.982 |
| H1206 | 8 | 0.953 | 0.989 |
| F228 | 8 | 0.949 | 0.993 |
| D1208 | 8 | 0.946 | 0.986 |
| F350 | 8 | 0.940 | 0.984 |
| F1128 | 8 | 0.936 | 0.990 |
| D1226 | 8 | 0.932 | 0.978 |
| N1213 | 8 | 0.929 | 0.969 |
| F1227 | 8 | 0.927 | 0.985 |
| F1093 | 8 | 0.921 | 0.992 |
| D437 | 8 | 0.914 | 0.959 |
| F764 | 8 | 0.894 | 0.981 |
| F1334 | 8 | 0.892 | 0.975 |
| F1188 | 8 | 0.868 | 0.973 |
| D176 | 8 | 0.860 | 0.953 |
| F511 | 8 | 0.848 | 0.954 |
| F253 | 8 | 0.830 | 0.952 |
| C143 | 7 | 0.975 | 0.991 |
HPA cancer prognostics
RNA cancer specificity: Low cancer specificity
Human Protein Atlas survival analysis — favorable = higher expression predicts better survival.
2 prognostic cancer types:
| Cancer | Prognostic | p-value |
|---|---|---|
| Lung Adenocarcinoma (validation) | unfavorable | 3.86e-05 |
| Thyroid Carcinoma (TCGA) | favorable | 0.000659 |
Disease associations
OMIM: gene MIM:600168 | disease phenotypes: MIM:254500
GenCC curated gene-disease
1 curated gene-disease records:
| Disease | Classification | Inheritance | Records |
|---|---|---|---|
| nasopharyngeal carcinoma, susceptibility to, 3 | Limited | Autosomal dominant |
Mondo (2): plasma cell myeloma (MONDO:0009693), nasopharyngeal carcinoma, susceptibility to, 3 (MONDO:0014902)
Orphanet (2): Multiple myeloma (Orphanet:29073), AL amyloidosis (Orphanet:85443)
HPO phenotypes
2 phenotypes (HPO-id order):
| HPO | Term |
|---|---|
| HP:0000006 | Autosomal dominant inheritance |
| HP:0100630 | Neoplasia of the nasopharynx |
GWAS associations
19 associations:
| Study | Trait | p-value |
|---|---|---|
| GCST001725_77 | Inflammatory bowel disease | 1e-47 |
| GCST010988_346 | Adult body size | 2e-37 |
| GCST008129_64 | Body mass index | 9e-26 |
| GCST010698_7 | Subcortical volume (min-P) | 3e-24 |
| GCST010701_11 | Cortical surface area (MOSTest) | 1e-16 |
| GCST011122_18 | Walking pace | 6e-16 |
| GCST003795_3 | Age at first birth | 5e-15 |
| GCST010002_422 | Refractive error | 4e-14 |
| GCST010703_214 | Brain morphology (MOSTest) | 2e-13 |
| GCST010702_18 | Subcortical volume (MOSTest) | 1e-10 |
| GCST006045_5 | Age at first birth | 6e-10 |
| GCST006920_7 | Regular attendance at a gym or sports club | 6e-10 |
| GCST005951_59 | Body mass index | 1e-8 |
| GCST006922_9 | Regular attendance at a religious group | 3e-8 |
| GCST007559_12 | Sleep duration (short sleep) | 3e-8 |
| GCST007044_11 | Extremely high intelligence | 4e-8 |
| GCST010699_3 | Brain morphology (min-P) | 4e-8 |
| GCST002548_9 | Ulcerative colitis | 8e-7 |
| GCST006044_2 | Age at first birth | 2e-6 |
EFO canonical traits (from GWAS)
5 canonical traits:
| EFO ID | Trait name |
|---|---|
| EFO:0009101 | age at first birth measurement |
| EFO:0004340 | body mass index |
| EFO:0009592 | social interaction measurement |
| EFO:0004337 | intelligence |
| EFO:0004346 | neuroimaging measurement |
MeSH disease descriptors
1 disease descriptors:
| Descriptor | Name | Tree numbers |
|---|---|---|
| D009101 | Multiple Myeloma | C04.557.595.500; C14.907.454.460; C15.378.147.780.650; C15.378.463.515.460; C20.683.515.845; C20.683.780.650 |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL2689 (SINGLE PROTEIN)
Drugs by curated mechanism of action (ChEMBL)
Drugs whose curated ChEMBL mechanism of action targets the MST1R protein itself — single-protein targets only (drugs acting on a protein family or complex that merely includes it are excluded). Includes antibodies and oligonucleotides that bioactivity screening does not capture.
4 curated-mechanism drugs:
| Drug | Modality | Max phase |
|---|---|---|
| CRIZOTINIB | Small molecule | 4 |
| GLESATINIB | Small molecule | 2 |
| NARNATUMAB | Antibody | 2 |
| MK-8033 | Small molecule | 1 |
Molecules with ChEMBL bioactivity
Phase ≥1, by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 159,040 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).
42 molecules by phase:
| Molecule | Name | Phase | Patents |
|---|---|---|---|
| CHEMBL601719 | CRIZOTINIB | 4 | 15,133 |
| CHEMBL1173655 | AFATINIB | 4 | 15,878 |
| CHEMBL288441 | BOSUTINIB | 4 | 12,869 |
| CHEMBL2105717 | CABOZANTINIB | 4 | 11,799 |
| CHEMBL1983268 | ENTRECTINIB | 4 | 3,737 |
| CHEMBL2103830 | FOSTAMATINIB | 4 | 4,026 |
| CHEMBL3301622 | GILTERITINIB | 4 | 2,542 |
| CHEMBL1852688 | INFIGRATINIB | 4 | 2,298 |
| CHEMBL1834657 | INFIGRATINIB PHOSPHATE | 4 | 330 |
| CHEMBL180022 | NERATINIB | 4 | 9,891 |
| CHEMBL189963 | PALBOCICLIB | 4 | 13,796 |
| CHEMBL24828 | VANDETANIB | 4 | 43,290 |
| CHEMBL415049 | BARASERTIB | 3 | 2,469 |
| CHEMBL491473 | CEDIRANIB | 3 | 9,464 |
| CHEMBL522892 | DOVITINIB | 3 | 5,162 |
| CHEMBL603469 | LESTAURTINIB | 3 | |
| CHEMBL223360 | LINIFANIB | 3 | 4,094 |
| CHEMBL3989914 | GLESATINIB | 2 | 1,584 |
| CHEMBL575448 | BMS-754807 | 2 | 418 |
| CHEMBL460702 | BMS-777607 | 2 | 260 |
| CHEMBL1967878 | CENISERTIB | 2 | |
| CHEMBL215152 | DEFOSBARASERTIB | 2 | |
| CHEMBL1230609 | FORETINIB | 2 | |
| CHEMBL3039525 | GOLVATINIB | 2 | |
| CHEMBL1980297 | ILORASERTIB | 2 | |
| CHEMBL3545307 | MERESTINIB | 2 | |
| CHEMBL564829 | MILCICLIB | 2 | |
| CHEMBL1822792 | MK-2461 | 2 | |
| CHEMBL253969 | OSI-632 | 2 | |
| CHEMBL475251 | R-406 | 2 | |
| CHEMBL1738757 | REBASTINIB | 2 | |
| CHEMBL565612 | SOTRASTAURIN | 2 | |
| CHEMBL572878 | TOZASERTIB | 2 | |
| CHEMBL2323775 | MK-8033 | 1 | |
| CHEMBL574738 | AST-487 | 1 | |
| CHEMBL482967 | CYC-116 | 1 | |
| CHEMBL1908397 | KW-2449 | 1 | |
| CHEMBL49120 | PD-0166285 | 1 | |
| CHEMBL1084546 | PF-00562271 | 1 | |
| CHEMBL4289017 | PF-03814735 | 1 | |
| CHEMBL1980391 | RG-1530 | 1 | |
| CHEMBL3545085 | XL-228 | 1 |
PharmGKB: 1 entry (CPIC guideline: no)
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: catalytic receptor — Type X RTKs: HGF (hepatocyte growth factor) receptor family
Most potent curated ligand interactions (5 total), top 5:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| BMS-777607 | Inhibition | 8.74 | pIC50 |
| compound 19a [PMID: 30503936] | Inhibition | 8.54 | pIC50 |
| MK-2461 | Inhibition | 8.15 | pIC50 |
| merestinib | Inhibition | 7.92 | pIC50 |
| compound 8i [PMID: 22765894] | Inhibition | 6.91 | pIC50 |
Binding affinities (BindingDB)
153 measured of 259 human assays (261 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value | Patent |
|---|---|---|---|
| CHEMBL5430218 | IC50 | 0.16 nM | |
| CHEMBL5427445 | IC50 | 0.26 nM | |
| CHEMBL5419134 | IC50 | 0.28 nM | |
| 1-[2-(4-methylphenyl)-5-tert-butyl-pyrazol-3-yl]-3-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]urea | KD | 0.37 nM | |
| CHEMBL5396164 | IC50 | 0.39 nM | |
| CHEMBL5421161 | IC50 | 0.48 nM | |
| CHEMBL5411457 | IC50 | 0.48 nM | |
| CHEMBL5440908 | IC50 | 0.49 nM | |
| CHEMBL5398932 | IC50 | 0.62 nM | |
| CHEMBL5397231 | IC50 | 0.63 nM | |
| CHEMBL5431928 | IC50 | 0.69 nM | |
| CHEMBL5436390 | IC50 | 0.72 nM | |
| CHEMBL5424053 | IC50 | 0.73 nM | |
| CHEMBL5437130 | IC50 | 0.74 nM | |
| CHEMBL5400656 | IC50 | 0.81 nM | |
| CHEMBL5405709 | IC50 | 0.82 nM | |
| CHEMBL5411204 | IC50 | 0.86 nM | |
| CHEMBL5431851 | IC50 | 0.98 nM | |
| CHEMBL2419669 | IC50 | 1.4 nM | |
| CHEMBL2143592 | IC50 | 1.7 nM | |
| CHEMBL5429072 | IC50 | 1.8 nM | |
| CHEMBL5400847 | IC50 | 2.2 nM | |
| CHEMBL5429366 | IC50 | 2.3 nM | |
| CHEMBL5399763 | IC50 | 2.3 nM | |
| CHEMBL5395573 | IC50 | 2.4 nM | |
| CHEMBL5429043 | IC50 | 2.6 nM | |
| N-{3-fluoro-4-[(7-methoxyquinolin-4-yl)oxy]phenyl}-1-(2-hydroxy-2-methylpropyl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide | IC50 | 2.7 nM | |
| N-(5-Amino-1-(4-methoxybenzyl)-1H-pyrazol-4-yl)-5-(3-(4-chloro-3-(trifluoromethyl)phenyl)ureido)-2-methylbenzamide | IC50 | 2.71 nM | |
| CHEMBL5438831 | IC50 | 2.8 nM | |
| CEP-701 | KD | 3.4 nM | |
| CHEMBL5395266 | IC50 | 3.7 nM | |
| CHEMBL4753082 | IC50 | 3.9 nM | |
| CHEMBL5404435 | IC50 | 4 nM | |
| N-[3-fluoro-4-[(2-oxo-3,4-dihydro-1H-pyrido[2,3-d]pyrimidin-5-yl)oxy]phenyl]-1-phenyl-5-(trifluoromethyl)pyrazole-4-carboxamide | IC50 | 4.3 nM | US-9283225: Pyrido-pyrimidine derivatives |
| CHEMBL5409449 | IC50 | 4.3 nM | |
| 4-[4-[(5-tert-butyl-2-quinolin-6-ylpyrazol-3-yl)carbamoylamino]-3-fluorophenoxy]-N-methylpyridine-2-carboxamide | IC50 | 5.5 nM | |
| CHEMBL5425777 | IC50 | 5.5 nM | |
| 3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-16-one | IC50 | 5.6 nM | US-8822500: Tyrosine kinase inhibitors |
| CHEMBL5394757 | IC50 | 6 nM | |
| Staurosporine, 8 | IC50 | 6.5 nM | |
| Momelotinib | IC50 | 8 nM | US-9469613: (N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide |
| ASP-3026 | IC50 | 10 nM | |
| N-[3-fluoro-4-[(2-oxo-3,4-dihydro-1H-pyrido[2,3-d]pyrimidin-5-yl)oxy]phenyl]-5-methyl-1-phenylpyrazole-4-carboxamide | IC50 | 10 nM | US-9283225: Pyrido-pyrimidine derivatives |
| CHEMBL3582033 | IC50 | 10 nM | |
| CHEMBL3608551 | IC50 | 10 nM | |
| CHEMBL5433417 | IC50 | 10 nM | |
| CHEMBL5403688 | IC50 | 10 nM | |
| N-(3-fluoro-4-(2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yloxy)phenyl)-1-phenyl-5-(trifluoromethyl)-1H-pyrazole-4-carboxamide | IC50 | 12 nM | |
| CHEMBL2376650 | IC50 | 12 nM | |
| CHEBI:72317 | IC50 | 14 nM |
ChEMBL bioactivities
354 potent at pChembl≥5 of 383 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 9.80 | IC50 | 0.16 | nM | CHEMBL5430218 |
| 9.60 | Ki | 0.2512 | nM | CHEMBL1980995 |
| 9.59 | IC50 | 0.26 | nM | CHEMBL5427445 |
| 9.55 | IC50 | 0.28 | nM | CHEMBL5419134 |
| 9.41 | IC50 | 0.39 | nM | CHEMBL5396164 |
| 9.39 | IC50 | 0.41 | nM | CHEMBL5404435 |
| 9.32 | IC50 | 0.48 | nM | CHEMBL5421161 |
| 9.32 | IC50 | 0.48 | nM | CHEMBL5411457 |
| 9.31 | IC50 | 0.49 | nM | CHEMBL5440908 |
| 9.21 | IC50 | 0.62 | nM | CHEMBL5398932 |
| 9.20 | IC50 | 0.63 | nM | CHEMBL5397231 |
| 9.16 | IC50 | 0.69 | nM | CHEMBL5431928 |
| 9.14 | IC50 | 0.73 | nM | CHEMBL5424053 |
| 9.14 | IC50 | 0.72 | nM | CHEMBL5436390 |
| 9.13 | IC50 | 0.74 | nM | CHEMBL5437130 |
| 9.09 | IC50 | 0.82 | nM | CHEMBL5405709 |
| 9.09 | IC50 | 0.81 | nM | CHEMBL5400656 |
| 9.07 | IC50 | 0.86 | nM | CHEMBL5411204 |
| 9.01 | IC50 | 0.98 | nM | CHEMBL5431851 |
| 9.00 | Ki | 1 | nM | CHEMBL2031893 |
| 8.92 | IC50 | 1.2 | nM | MERESTINIB |
| 8.89 | Ki | 1.3 | nM | CHEMBL447602 |
| 8.80 | Ki | 1.585 | nM | CHEMBL1980407 |
| 8.74 | IC50 | 1.8 | nM | BMS-777607 |
| 8.74 | IC50 | 1.8 | nM | CHEMBL4753082 |
| 8.74 | IC50 | 1.82 | nM | CHEMBL5429072 |
| 8.69 | IC50 | 2.05 | nM | FORETINIB |
| 8.69 | IC50 | 2.04 | nM | CHEMBL5395266 |
| 8.67 | IC50 | 2.15 | nM | CHEMBL5400847 |
| 8.65 | IC50 | 2.25 | nM | CHEMBL5399763 |
| 8.64 | IC50 | 2.28 | nM | CHEMBL5429366 |
| 8.62 | IC50 | 2.39 | nM | CHEMBL5409449 |
| 8.62 | IC50 | 2.39 | nM | CHEMBL5395573 |
| 8.59 | IC50 | 2.55 | nM | CHEMBL5429043 |
| 8.55 | IC50 | 2.83 | nM | CHEMBL5438831 |
| 8.54 | IC50 | 2.9 | nM | CHEMBL4587222 |
| 8.52 | IC50 | 3 | nM | FORETINIB |
| 8.52 | Kd | 3 | nM | FORETINIB |
| 8.51 | IC50 | 3.1 | nM | CHEMBL4171115 |
| 8.46 | IC50 | 3.43 | nM | FORETINIB |
| 8.46 | IC50 | 3.48 | nM | FORETINIB |
| 8.45 | IC50 | 3.54 | nM | FORETINIB |
| 8.44 | IC50 | 3.62 | nM | FORETINIB |
| 8.41 | IC50 | 3.92 | nM | FORETINIB |
| 8.40 | Ki | 3.981 | nM | CENISERTIB |
| 8.37 | IC50 | 4.3 | nM | CHEMBL3899652 |
| 8.26 | IC50 | 5.47 | nM | CHEMBL5425777 |
| 8.26 | IC50 | 5.5 | nM | CRIZOTINIB |
| 8.24 | IC50 | 5.71 | nM | CHEMBL5433417 |
| 8.22 | IC50 | 6 | nM | CHEMBL5394757 |
PubChem BioAssay actives
219 with measured affinity, of 1602 total; 50 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 |
|---|---|---|---|---|
| 4-ethoxy-N-[3-fluoro-4-[2-[5-[(3-methoxyazetidin-1-yl)methyl]-2-pyridinyl]thieno[3,2-b]pyridin-7-yl]oxyphenyl]-1-(4-fluorophenyl)-2-oxopyridine-3-carboxamide | 2015473: Inhibition of N-terminal GST-tagged human recombinant RON (979 to 1400(end) residues) expressed in Sf21 cells incubated for 20 mins followed by ATP addition measured after 60 mins by TR-FRET based LanthaScreen kinase assay | ic50 | 0.0002 | uM |
| 4-ethoxy-N-[3-fluoro-4-[2-[5-[(4-methylpiperazin-1-yl)methyl]-2-pyridinyl]thieno[3,2-b]pyridin-7-yl]oxyphenyl]-1-(4-fluorophenyl)-2-oxopyridine-3-carboxamide | 2015473: Inhibition of N-terminal GST-tagged human recombinant RON (979 to 1400(end) residues) expressed in Sf21 cells incubated for 20 mins followed by ATP addition measured after 60 mins by TR-FRET based LanthaScreen kinase assay | ic50 | 0.0003 | uM |
| 4-ethoxy-N-[3-fluoro-4-[2-[5-[(2-methoxyethylamino)methyl]-2-pyridinyl]thieno[3,2-b]pyridin-7-yl]oxyphenyl]-1-(4-fluorophenyl)-2-oxopyridine-3-carboxamide | 2015473: Inhibition of N-terminal GST-tagged human recombinant RON (979 to 1400(end) residues) expressed in Sf21 cells incubated for 20 mins followed by ATP addition measured after 60 mins by TR-FRET based LanthaScreen kinase assay | ic50 | 0.0003 | uM |
| 4-ethoxy-N-[3-fluoro-4-[2-[5-(morpholin-4-ylmethyl)-2-pyridinyl]thieno[3,2-b]pyridin-7-yl]oxyphenyl]-1-(4-fluorophenyl)-2-oxopyridine-3-carboxamide | 2015473: Inhibition of N-terminal GST-tagged human recombinant RON (979 to 1400(end) residues) expressed in Sf21 cells incubated for 20 mins followed by ATP addition measured after 60 mins by TR-FRET based LanthaScreen kinase assay | ic50 | 0.0004 | uM |
| 4-ethoxy-N-[3-fluoro-4-[2-(1-methylimidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxyphenyl]-1-(4-fluorophenyl)-2-oxopyridine-3-carboxamide | 2015473: Inhibition of N-terminal GST-tagged human recombinant RON (979 to 1400(end) residues) expressed in Sf21 cells incubated for 20 mins followed by ATP addition measured after 60 mins by TR-FRET based LanthaScreen kinase assay | ic50 | 0.0004 | uM |
| N-[4-[2-[5-[(3,3-difluoroazetidin-1-yl)methyl]-2-pyridinyl]thieno[3,2-b]pyridin-7-yl]oxy-3-fluorophenyl]-4-ethoxy-1-(4-fluorophenyl)-2-oxopyridine-3-carboxamide | 2015473: Inhibition of N-terminal GST-tagged human recombinant RON (979 to 1400(end) residues) expressed in Sf21 cells incubated for 20 mins followed by ATP addition measured after 60 mins by TR-FRET based LanthaScreen kinase assay | ic50 | 0.0005 | uM |
| N-[3-fluoro-4-[2-[5-(morpholin-4-ylmethyl)-2-pyridinyl]thieno[3,2-b]pyridin-7-yl]oxyphenyl]-1-(4-fluorophenyl)-2-oxo-4-propoxypyridine-3-carboxamide | 2015473: Inhibition of N-terminal GST-tagged human recombinant RON (979 to 1400(end) residues) expressed in Sf21 cells incubated for 20 mins followed by ATP addition measured after 60 mins by TR-FRET based LanthaScreen kinase assay | ic50 | 0.0005 | uM |
| 4-ethoxy-1-(4-fluorophenyl)-N-[3-fluoro-4-(2-pyridin-2-ylthieno[3,2-b]pyridin-7-yl)oxyphenyl]-2-oxopyridine-3-carboxamide | 2015473: Inhibition of N-terminal GST-tagged human recombinant RON (979 to 1400(end) residues) expressed in Sf21 cells incubated for 20 mins followed by ATP addition measured after 60 mins by TR-FRET based LanthaScreen kinase assay | ic50 | 0.0005 | uM |
| 4-ethoxy-N-[3-fluoro-4-[2-[5-[(3-fluoroazetidin-1-yl)methyl]-2-pyridinyl]thieno[3,2-b]pyridin-7-yl]oxyphenyl]-1-(4-fluorophenyl)-2-oxopyridine-3-carboxamide | 2015473: Inhibition of N-terminal GST-tagged human recombinant RON (979 to 1400(end) residues) expressed in Sf21 cells incubated for 20 mins followed by ATP addition measured after 60 mins by TR-FRET based LanthaScreen kinase assay | ic50 | 0.0006 | uM |
| N-[3-fluoro-4-[2-[5-(morpholin-4-ylmethyl)-2-pyridinyl]thieno[3,2-b]pyridin-7-yl]oxyphenyl]-1-(4-fluorophenyl)-4-(2-methylpropoxy)-2-oxopyridine-3-carboxamide | 2015473: Inhibition of N-terminal GST-tagged human recombinant RON (979 to 1400(end) residues) expressed in Sf21 cells incubated for 20 mins followed by ATP addition measured after 60 mins by TR-FRET based LanthaScreen kinase assay | ic50 | 0.0006 | uM |
| 4-ethoxy-N-[3-fluoro-4-[2-[5-[(4-methoxypiperidin-1-yl)methyl]-2-pyridinyl]thieno[3,2-b]pyridin-7-yl]oxyphenyl]-1-(4-fluorophenyl)-2-oxopyridine-3-carboxamide | 2015473: Inhibition of N-terminal GST-tagged human recombinant RON (979 to 1400(end) residues) expressed in Sf21 cells incubated for 20 mins followed by ATP addition measured after 60 mins by TR-FRET based LanthaScreen kinase assay | ic50 | 0.0007 | uM |
| 4-ethoxy-N-[3-fluoro-4-[2-[5-[(3-methoxypyrrolidin-1-yl)methyl]-2-pyridinyl]thieno[3,2-b]pyridin-7-yl]oxyphenyl]-1-(4-fluorophenyl)-2-oxopyridine-3-carboxamide | 2015473: Inhibition of N-terminal GST-tagged human recombinant RON (979 to 1400(end) residues) expressed in Sf21 cells incubated for 20 mins followed by ATP addition measured after 60 mins by TR-FRET based LanthaScreen kinase assay | ic50 | 0.0007 | uM |
| 4-(2-cyclopropylethoxy)-N-[3-fluoro-4-[2-[5-(morpholin-4-ylmethyl)-2-pyridinyl]thieno[3,2-b]pyridin-7-yl]oxyphenyl]-1-(4-fluorophenyl)-2-oxopyridine-3-carboxamide | 2015473: Inhibition of N-terminal GST-tagged human recombinant RON (979 to 1400(end) residues) expressed in Sf21 cells incubated for 20 mins followed by ATP addition measured after 60 mins by TR-FRET based LanthaScreen kinase assay | ic50 | 0.0007 | uM |
| 4-ethoxy-N-[3-fluoro-4-[2-[5-(morpholin-4-ylmethyl)-2-pyridinyl]thieno[3,2-b]pyridin-7-yl]oxyphenyl]-1-(3-fluorophenyl)-2-oxopyridine-3-carboxamide | 2015473: Inhibition of N-terminal GST-tagged human recombinant RON (979 to 1400(end) residues) expressed in Sf21 cells incubated for 20 mins followed by ATP addition measured after 60 mins by TR-FRET based LanthaScreen kinase assay | ic50 | 0.0007 | uM |
| 4-ethoxy-N-[3-fluoro-4-[2-[5-(morpholin-4-ylmethyl)-2-pyridinyl]thieno[3,2-b]pyridin-7-yl]oxyphenyl]-2-oxo-1-phenylpyridine-3-carboxamide | 2015473: Inhibition of N-terminal GST-tagged human recombinant RON (979 to 1400(end) residues) expressed in Sf21 cells incubated for 20 mins followed by ATP addition measured after 60 mins by TR-FRET based LanthaScreen kinase assay | ic50 | 0.0008 | uM |
| 4-ethoxy-N-[3-fluoro-4-[2-[5-[(3-fluoropyrrolidin-1-yl)methyl]-2-pyridinyl]thieno[3,2-b]pyridin-7-yl]oxyphenyl]-1-(4-fluorophenyl)-2-oxopyridine-3-carboxamide | 2015473: Inhibition of N-terminal GST-tagged human recombinant RON (979 to 1400(end) residues) expressed in Sf21 cells incubated for 20 mins followed by ATP addition measured after 60 mins by TR-FRET based LanthaScreen kinase assay | ic50 | 0.0008 | uM |
| N-[4-[2-[5-[(3,3-difluoropyrrolidin-1-yl)methyl]-2-pyridinyl]thieno[3,2-b]pyridin-7-yl]oxy-3-fluorophenyl]-4-ethoxy-1-(4-fluorophenyl)-2-oxopyridine-3-carboxamide | 2015473: Inhibition of N-terminal GST-tagged human recombinant RON (979 to 1400(end) residues) expressed in Sf21 cells incubated for 20 mins followed by ATP addition measured after 60 mins by TR-FRET based LanthaScreen kinase assay | ic50 | 0.0009 | uM |
| 4-butoxy-N-[3-fluoro-4-[2-[5-(morpholin-4-ylmethyl)-2-pyridinyl]thieno[3,2-b]pyridin-7-yl]oxyphenyl]-1-(4-fluorophenyl)-2-oxopyridine-3-carboxamide | 2015473: Inhibition of N-terminal GST-tagged human recombinant RON (979 to 1400(end) residues) expressed in Sf21 cells incubated for 20 mins followed by ATP addition measured after 60 mins by TR-FRET based LanthaScreen kinase assay | ic50 | 0.0010 | uM |
| N-[4-(6,7-dimethoxyquinolin-4-yl)oxy-3-fluorophenyl]-1,5-dimethyl-3-oxo-2-phenylpyrazole-4-carboxamide | 662101: Inhibition of RON by HTRF assay | ki | 0.0010 | uM |
| N-[3-fluoro-4-[1-methyl-6-(1H-pyrazol-4-yl)indazol-5-yl]oxyphenyl]-1-(4-fluorophenyl)-6-methyl-2-oxopyridine-3-carboxamide | 1533355: Inhibition of RON (unknown origin) by FISH assay | ic50 | 0.0012 | uM |
| 2-(4-fluoroanilino)-5-[5-[6-methoxy-7-(3-morpholin-4-ylpropoxy)quinolin-4-yl]oxy-2-pyridinyl]-3-methylpyrimidin-4-one | 364260: Inhibition of phosphorylated RON | ki | 0.0013 | uM |
| N-[4-[(2-amino-3-chloro-4-pyridinyl)oxy]-3-fluorophenyl]-1-(4-fluorophenyl)-4-methoxy-2-oxopyridine-3-carboxamide | 1691612: Inhibition of Ron (unknown origin) | ic50 | 0.0018 | uM |
| 4-ethoxy-N-[3-fluoro-4-[2-[5-[(4-fluoropiperidin-1-yl)methyl]-2-pyridinyl]thieno[3,2-b]pyridin-7-yl]oxyphenyl]-1-(4-fluorophenyl)-2-oxopyridine-3-carboxamide | 2015473: Inhibition of N-terminal GST-tagged human recombinant RON (979 to 1400(end) residues) expressed in Sf21 cells incubated for 20 mins followed by ATP addition measured after 60 mins by TR-FRET based LanthaScreen kinase assay | ic50 | 0.0018 | uM |
| N-[4-[(2-amino-3-chloro-4-pyridinyl)oxy]-3-fluorophenyl]-4-ethoxy-1-(4-fluorophenyl)-2-oxopyridine-3-carboxamide | 1534900: Inhibition of RON (unknown origin) | ic50 | 0.0018 | uM |
| 1-[(2S)-2-(2,4-difluorophenyl)-4-oxo-1,3-thiazolidin-3-yl]-3-[4-[7-[3-(4-ethylpiperazin-1-yl)propoxy]-6-methoxyquinolin-4-yl]oxy-3,5-difluorophenyl]urea | 1986472: Inhibition of RON (unknown origin) by kinome scan assay | ic50 | 0.0020 | uM |
| 1-N’-[3-fluoro-4-[6-methoxy-7-(3-morpholin-4-ylpropoxy)quinolin-4-yl]oxyphenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide | 1986472: Inhibition of RON (unknown origin) by kinome scan assay | ic50 | 0.0021 | uM |
| 4-[2-(dimethylamino)ethoxy]-N-[3-fluoro-4-[2-[5-(morpholin-4-ylmethyl)-2-pyridinyl]thieno[3,2-b]pyridin-7-yl]oxyphenyl]-1-(4-fluorophenyl)-2-oxopyridine-3-carboxamide | 2015473: Inhibition of N-terminal GST-tagged human recombinant RON (979 to 1400(end) residues) expressed in Sf21 cells incubated for 20 mins followed by ATP addition measured after 60 mins by TR-FRET based LanthaScreen kinase assay | ic50 | 0.0022 | uM |
| N-[3,5-difluoro-4-[2-[5-(morpholin-4-ylmethyl)-2-pyridinyl]thieno[3,2-b]pyridin-7-yl]oxyphenyl]-4-ethoxy-1-(4-fluorophenyl)-2-oxopyridine-3-carboxamide | 2015473: Inhibition of N-terminal GST-tagged human recombinant RON (979 to 1400(end) residues) expressed in Sf21 cells incubated for 20 mins followed by ATP addition measured after 60 mins by TR-FRET based LanthaScreen kinase assay | ic50 | 0.0022 | uM |
| N-[3-chloro-4-[2-[5-(morpholin-4-ylmethyl)-2-pyridinyl]thieno[3,2-b]pyridin-7-yl]oxyphenyl]-4-ethoxy-1-(4-fluorophenyl)-2-oxopyridine-3-carboxamide | 2015473: Inhibition of N-terminal GST-tagged human recombinant RON (979 to 1400(end) residues) expressed in Sf21 cells incubated for 20 mins followed by ATP addition measured after 60 mins by TR-FRET based LanthaScreen kinase assay | ic50 | 0.0023 | uM |
| 4-ethoxy-N-[3-fluoro-4-[2-[5-(2-morpholin-4-ylethoxy)-2-pyridinyl]thieno[3,2-b]pyridin-7-yl]oxyphenyl]-1-(4-fluorophenyl)-2-oxopyridine-3-carboxamide | 2015473: Inhibition of N-terminal GST-tagged human recombinant RON (979 to 1400(end) residues) expressed in Sf21 cells incubated for 20 mins followed by ATP addition measured after 60 mins by TR-FRET based LanthaScreen kinase assay | ic50 | 0.0024 | uM |
| 1-[2-(2,4-difluorophenyl)-4-oxo-1,3-thiazolidin-3-yl]-3-[4-[7-[3-(4-ethylpiperazin-1-yl)propoxy]-6-methoxyquinolin-4-yl]oxy-3,5-difluorophenyl]urea | 1986472: Inhibition of RON (unknown origin) by kinome scan assay | ic50 | 0.0024 | uM |
| 1-(4-chlorophenyl)-4-ethoxy-N-[3-fluoro-4-[2-[5-(morpholin-4-ylmethyl)-2-pyridinyl]thieno[3,2-b]pyridin-7-yl]oxyphenyl]-2-oxopyridine-3-carboxamide | 2015473: Inhibition of N-terminal GST-tagged human recombinant RON (979 to 1400(end) residues) expressed in Sf21 cells incubated for 20 mins followed by ATP addition measured after 60 mins by TR-FRET based LanthaScreen kinase assay | ic50 | 0.0026 | uM |
| 4-ethoxy-N-[3-fluoro-4-[2-[5-(2-morpholin-4-ylethyl)-2-pyridinyl]thieno[3,2-b]pyridin-7-yl]oxyphenyl]-1-(4-fluorophenyl)-2-oxopyridine-3-carboxamide | 2015473: Inhibition of N-terminal GST-tagged human recombinant RON (979 to 1400(end) residues) expressed in Sf21 cells incubated for 20 mins followed by ATP addition measured after 60 mins by TR-FRET based LanthaScreen kinase assay | ic50 | 0.0028 | uM |
| 1-[2-(2,6-difluorophenyl)-4-oxo-1,3-thiazolidin-3-yl]-3-[4-[7-[3-(4-ethylpiperazin-1-yl)propoxy]-6-methoxyquinolin-4-yl]oxy-3,5-difluorophenyl]urea | 1533587: Inhibition of Ron (unknown origin) using FAM-labelled peptide and ATP incubated for 10 mins by mobility shift assay | ic50 | 0.0029 | uM |
| N-[4-[(2-amino-3-chloro-4-pyridinyl)oxy]-3-fluorophenyl]-5-(4-fluorophenyl)-4-oxo-1H-pyridine-3-carboxamide | 1276923: Inhibition of Ron (unknown origin) | ic50 | 0.0030 | uM |
| 1-[2-(2,6-difluorophenyl)-4-oxo-1,3-thiazolidin-3-yl]-3-[2-fluoro-4-[6-methoxy-7-(3-pyrrolidin-1-ylpropoxy)quinolin-4-yl]oxyphenyl]urea | 1352741: Inhibition of Ron (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 1 hr by ELISA | ic50 | 0.0031 | uM |
| 4-[[3-fluoro-4-[6-methoxy-7-(3-morpholin-4-ylpropoxy)quinolin-4-yl]oxyphenyl]iminomethyl]-5-methyl-2-[2-(trifluoromethyl)phenyl]-1H-pyrazol-3-one | 1800438: HTRF kinase assay from Article 10.1016/j.bioorg.2014.07.011: “Design, synthesis and pharmacological evaluation of 6,7-disubstituted-4-phenoxyquinoline derivatives as potential antitumor agents.” | ic50 | 0.0042 | uM |
| Crizotinib | 2161836: Inhibition of human N-terminal GST-fused RON cytoplasmic domain (979 to 1400(end) residues) expressed in baculovirus expression system using Srctide as substrate measured after 1 hr by off-chip mobility shift assay relative to control | ic50 | 0.0055 | uM |
| N-[3-fluoro-4-[2-[5-(morpholin-4-ylmethyl)-2-pyridinyl]thieno[3,2-b]pyridin-7-yl]oxyphenyl]-1-(4-fluorophenyl)-4-(1-methylpyrrolidin-3-yl)oxy-2-oxopyridine-3-carboxamide | 2015473: Inhibition of N-terminal GST-tagged human recombinant RON (979 to 1400(end) residues) expressed in Sf21 cells incubated for 20 mins followed by ATP addition measured after 60 mins by TR-FRET based LanthaScreen kinase assay | ic50 | 0.0055 | uM |
| 1-[(2R)-2-(2,4-difluorophenyl)-4-oxo-1,3-thiazolidin-3-yl]-3-[4-[7-[3-(4-ethylpiperazin-1-yl)propoxy]-6-methoxyquinolin-4-yl]oxy-3,5-difluorophenyl]urea | 1986472: Inhibition of RON (unknown origin) by kinome scan assay | ic50 | 0.0057 | uM |
| N-[4-[2-[5-[(4,4-difluoropiperidin-1-yl)methyl]-2-pyridinyl]thieno[3,2-b]pyridin-7-yl]oxy-3-fluorophenyl]-4-ethoxy-1-(4-fluorophenyl)-2-oxopyridine-3-carboxamide | 2015473: Inhibition of N-terminal GST-tagged human recombinant RON (979 to 1400(end) residues) expressed in Sf21 cells incubated for 20 mins followed by ATP addition measured after 60 mins by TR-FRET based LanthaScreen kinase assay | ic50 | 0.0060 | uM |
| 14-(dimethylsulfamoylamino)-5-(1-methylpyrazol-4-yl)-2-oxo-7-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,9,12,14-heptaene | 728081: Inhibition of RON (unknown origin) by TR-FRET assay | ic50 | 0.0070 | uM |
| 14-[[[(2R)-1,4-dioxan-2-yl]methyl-methylsulfamoyl]amino]-5-(1-methylpyrazol-4-yl)-2-oxo-7-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,9,12,14-heptaene | 606069: Inhibition of human Ron | ic50 | 0.0070 | uM |
| 1-[5-(1-methylpyrazol-4-yl)-2-oxo-7-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,9,12,14-heptaen-14-yl]-N-(pyridin-2-ylmethyl)methanesulfonamide | 1534900: Inhibition of RON (unknown origin) | ic50 | 0.0070 | uM |
| N-[3-fluoro-4-(7-methoxyquinolin-4-yl)oxyphenyl]-1-(2-hydroxy-2-methylpropyl)-5-methyl-3-oxo-2-phenylpyrazole-4-carboxamide | 2015471: Inhibition of RON (unknown origin) | ic50 | 0.0090 | uM |
| N-[3-fluoro-4-[2-(1-methylimidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxyphenyl]-1-phenyl-2-(trifluoromethyl)pyrrole-3-carboxamide | 1228792: Inhibition of RON (unknown origin) transfected in 293T cells assessed as autophosporylated level by ELISA | ic50 | 0.0100 | uM |
| 1-(2-hydroxy-2-methylpropyl)-N-[5-(7-methoxyquinolin-4-yl)oxy-2-pyridinyl]-5-methyl-3-oxo-2-phenylpyrazole-4-carboxamide | 662101: Inhibition of RON by HTRF assay | ic50 | 0.0100 | uM |
| N-[3-fluoro-4-[2-(1-methylimidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxyphenyl]-1-phenyl-5-(trifluoromethyl)pyrazole-4-carboxamide | 1241723: Inhibition of human RON | ic50 | 0.0100 | uM |
| N-[2-chloro-4-[2-[5-(morpholin-4-ylmethyl)-2-pyridinyl]thieno[3,2-b]pyridin-7-yl]oxyphenyl]-4-ethoxy-1-(4-fluorophenyl)-2-oxopyridine-3-carboxamide | 2015473: Inhibition of N-terminal GST-tagged human recombinant RON (979 to 1400(end) residues) expressed in Sf21 cells incubated for 20 mins followed by ATP addition measured after 60 mins by TR-FRET based LanthaScreen kinase assay | ic50 | 0.0103 | uM |
| N-[3-fluoro-4-[2-(1-methylimidazol-4-yl)thieno[3,2-b]pyridin-7-yl]oxyphenyl]-1-phenyl-5-(trifluoromethyl)imidazole-4-carboxamide | 1228792: Inhibition of RON (unknown origin) transfected in 293T cells assessed as autophosporylated level by ELISA | ic50 | 0.0130 | uM |
CTD chemical–gene interactions
32 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| bisphenol A | decreases methylation, increases expression | 2 |
| Benzo(a)pyrene | affects methylation, increases expression | 2 |
| Tobacco Smoke Pollution | decreases expression | 2 |
| Aflatoxin B1 | decreases methylation, increases expression | 2 |
| Particulate Matter | affects expression, decreases expression | 2 |
| methyleugenol | increases expression | 1 |
| pirinixic acid | affects binding, decreases expression, increases activity | 1 |
| beta-lapachone | decreases expression | 1 |
| tris(1,3-dichloro-2-propyl)phosphate | decreases expression | 1 |
| sodium arsenite | increases abundance, affects cotreatment, decreases expression | 1 |
| cobaltous chloride | decreases expression | 1 |
| butyraldehyde | increases expression | 1 |
| pyrrolidine dithiocarbamic acid | decreases expression | 1 |
| benzo(e)pyrene | decreases methylation | 1 |
| cupric chloride | increases expression | 1 |
| nickel sulfate | decreases expression, increases expression | 1 |
| pentanal | increases expression | 1 |
| jinfukang | increases expression | 1 |
| NSC 689534 | increases expression | 1 |
| 5H-benzo(4,5)cyclohepta(1,2-b)pyridin-5-one | decreases activity | 1 |
| Arsenic Trioxide | decreases response to substance | 1 |
| Arsenic | increases abundance, affects cotreatment, decreases expression | 1 |
| Curcumin | decreases reaction, increases expression, decreases expression, affects binding | 1 |
| Methapyrilene | decreases methylation | 1 |
| Smoke | decreases expression | 1 |
| Tetrachlorodibenzodioxin | increases expression | 1 |
| Valproic Acid | decreases expression, increases methylation | 1 |
| Vanadium | decreases expression | 1 |
| Asbestos, Crocidolite | decreases expression | 1 |
| Antirheumatic Agents | decreases expression | 1 |
ChEMBL screening assays
384 unique, capped per target: 382 binding, 2 functional
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1006336 | Binding | Inhibition of Tel-fused RON kinase-mediated mouse BaF3 cell proliferation | Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. — *Proc Natl Acad Sci U S A* |
| CHEMBL1964103 | Functional | PUBCHEM_BIOASSAY: Navigating the Kinome. (Class of assay: other) Panel member name: MST1R | PubChem BioAssay data set |
Cellosaurus cell lines
4 cell lines: 3 cancer cell line, 1 spontaneously immortalized cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_C7DA | Abcam A-549 MST1R KO | Cancer cell line | Male |
| CVCL_C7E0 | Abcam HCT 116 MST1R KO | Cancer cell line | Male |
| CVCL_D3UF | MDCK-RE7 | Spontaneously immortalized cell line | Female |
| CVCL_D7VC | Ubigene A-549 MST1R KO | Cancer cell line | Male |
Clinical trials (associated diseases)
Via MONDO — disease-level, not drug-specific.
showing 60 of 300 trials:
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT00029224 | Phase 4 | COMPLETED | Treatment With Zoledronic Acid in Patients With Breast Cancer, Multiple Myeloma, and Prostate Cancer With Cancer Related Bone Lesions |
| NCT00104104 | Phase 4 | COMPLETED | A Multiple Myeloma Trial in Patients With Bone Metastases |
| NCT00211211 | Phase 4 | COMPLETED | FREE Study - Fracture Reduction Evaluation |
| NCT00242528 | Phase 4 | WITHDRAWN | Open-label Study, to Evaluate the Safety and Tolerability of Zoledronic Acid in Patients With Bone Lesions Secondary to Multiple Myeloma. |
| NCT00257114 | Phase 4 | COMPLETED | Evaluation of VELCADE Given as Retreatment to Multiple Myeloma Patients for Efficacy, Safety and Tolerability |
| NCT00352703 | Phase 4 | COMPLETED | PROMPT - Palifermin in Reduction of Oral Mucositis in PBSC Transplantation |
| NCT00361140 | Phase 4 | COMPLETED | Busulfan Safety/Efficacy as Conditioning Prior to Hematopoietic Cell Transplantation (HCT) |
| NCT00622505 | Phase 4 | COMPLETED | Zoledronic Acid Treatment (Every 4 or 12 Weeks) to Prevent Skeletal Complications in Advanced Multiple Myeloma Participants |
| NCT00652041 | Phase 4 | COMPLETED | Bortezomib/Adriamycine/Melfalan/Prednisone (VAMP)/Thalidomide/Cyclophosphamide/Dexamethasone (TaCyDex) or Bortezomib/Melfalan/Prednisone (V-MP)/TaCyDex) in Refractary or Relapsed Multiple Myeloma |
| NCT00733538 | Phase 4 | COMPLETED | Stage I Multiple Myeloma Treatment |
| NCT01087008 | Phase 4 | COMPLETED | Zoledronic Acid in Patients With Multiple Myeloma and Asymptomatic Biochemical Relapse |
| NCT01249690 | Phase 4 | UNKNOWN | Efficacy Study of PAD and TAD in Newly Diagnosed Multiple Myeloma |
| NCT01410929 | Phase 4 | WITHDRAWN | Evaluation of Vertebral Compression Fracture Fixation With RF Kyphoplasty in Patients With Multiple Myeloma |
| NCT01731886 | Phase 4 | COMPLETED | Lenalidomide and Dexamethasone With/Without Stem Cell Transplant in Patients With Multiple Myeloma |
| NCT01868828 | Phase 4 | UNKNOWN | A Study of PAD Versus Velcade, Cyclophosphamide and Dexamethasone (VCD) Treatment in Subjects With Multiple Myeloma |
| NCT02268890 | Phase 4 | COMPLETED | A Pharmacokinetic Study of Bortezomib in Taiwanese Participants With Multiple Myeloma |
| NCT02286830 | Phase 4 | COMPLETED | Prolonged Protection From Bone Disease in Multiple Myeloma |
| NCT02559154 | Phase 4 | UNKNOWN | Modified Bortezomib-based Combination Therapy for Multiple Myeloma |
| NCT02577783 | Phase 4 | UNKNOWN | PDD vs PAD to Treat Initially Diagnosed MM |
| NCT02773550 | Phase 4 | TERMINATED | Treatment With a Scheme With Low Doses of Bortezomib / Melphalan / Prednisone (MPV) in Patients With Multiple Myeloma |
| NCT02958969 | Phase 4 | COMPLETED | Apixaban for Primary Prevention of Venous Thromboembolism in Patients With Multiple Myeloma |
| NCT03173092 | Phase 4 | TERMINATED | A Study of Ixazomib (NINLARO®) in Combination With Lenalidomide and Dexamethasone (IRD) for the Treatment of Participants With Multiple Myeloma (MM) |
| NCT03619252 | Phase 4 | COMPLETED | Pneumococcal Vaccination of Multiple Myeloma Patients on Novel Agents |
| NCT03768960 | Phase 4 | COMPLETED | A Study of DARZALEX (Daratumumab) In Indian Participants With Relapsed and Refractory Multiple Myeloma, Whose Prior Therapy Included a Proteasome Inhibitor and an Immunomodulatory Agent |
| NCT03829371 | Phase 4 | ACTIVE_NOT_RECRUITING | STUDY COMPARING TWO STANDARD TREATMENTS IN AUTOLOGOUS STEM CELL TRANSPLANTATION INELIGIBLE POPULATION AFFECTED BY MULTIPLE MYELOMA |
| NCT03908138 | Phase 4 | UNKNOWN | RDD Versus VDD in Newly Diagnosed Patients With Multiple Myeloma |
| NCT04217967 | Phase 4 | COMPLETED | Ixazomib, Lenalidomide, and Combination for Maintenance in NDMM Patients |
| NCT04952766 | Phase 4 | COMPLETED | Study Evaluating SARS-CoV-2 (COVID-19) Humoral Response After BNT162b2 Vaccine in Immunocompromised Adults Compared to Healthy Adults |
| NCT04989140 | Phase 4 | UNKNOWN | Study of Pomalidomide, Oral Dexamethasone and Ixazomib in Patients With Relapsed MM Who Have Received Lenalidomide |
| NCT05183139 | Phase 4 | WITHDRAWN | A Multicenter In-class Transition Study of Ixazomib Combined With Pomalidomide and Dexamethasone or With Lenalidomide and Dexamethasone in Adults With Relapsed/Refractory Multiple Myeloma |
| NCT05201781 | Phase 4 | RECRUITING | A Long-term Study for Participants Previously Treated With Ciltacabtagene Autoleucel |
| NCT05429515 | Phase 4 | NOT_YET_RECRUITING | Effect of HFR-SUPRA in the Treatment of Multiple Myeloma-related Acute Kidney Injury |
| NCT05511428 | Phase 4 | COMPLETED | Home Based Daratumumab Administration for Patients With Multiple Myeloma |
| NCT05545202 | Phase 4 | UNKNOWN | A Randomized, Comparative, Double-blind Trial of Pentaisomaltose and Dimethyl Sulphoxide for Cryoprotection of Hematopoietic Stem Cells in Subjects With Multiple Myeloma or Malignant Lymphoma With a Need for Autologous Transplantation |
| NCT05555329 | Phase 4 | COMPLETED | Alternative Dosing Scheme of Pomalidomide 4 mg Every Other Day Versus Pomalidomide 2 mg and 4 mg Every Day; the POMAlternative Study |
| NCT05722405 | Phase 4 | RECRUITING | Ixazomib Plus Low-dose Lenalidomide Versus Ixazomib Alone for Maintenance Treatment of High Risk Multiple Myeloma |
| NCT05855122 | Phase 4 | UNKNOWN | Safety and ASCT-related Symptom Burden Optimization of Tocilizumab in ASCT Following HD Melphalan Conditioning for Multiple Myeloma Patients |
| NCT05944783 | Phase 4 | NOT_YET_RECRUITING | Bioequivalence Studies of Dasatinib 100 Mg |
| NCT06057402 | Phase 4 | RECRUITING | Elranatamab Post Trial Access Study for Participants With Multiple Myeloma (MM) |
| NCT06251076 | Phase 4 | RECRUITING | Plan Development for Giving Teclistamab in the Outpatient Setting |
| NCT06409702 | Phase 4 | RECRUITING | Treatment of High-risk Newly Diagnosed Multiple Myeloma With Minimal Residual Disease Detection |
| NCT06425276 | Phase 4 | COMPLETED | Evaluate Safety and Efficacy of High-dose Melphalan HCL for Injection in MM Patients With Auto-HSC Transplantation |
| NCT07030517 | Phase 4 | ACTIVE_NOT_RECRUITING | A Study to Assess Safety of Teclistamab in Indian Participants With Relapsed and Refractory Multiple Myeloma |
| NCT07094048 | Phase 4 | RECRUITING | Immunoglobulins in Multiple Myeloma Patients Receiving a BCMA-Directed T Cell Engager |
| NCT07101445 | Phase 4 | RECRUITING | Evaluating Premedication Regimens (Methylprednisolone vs Dexamethasone-based) for the Prevention of Systemic and Injection Site Reactions to Motixafortide in Patients With Multiple Myeloma Undergoing Stem Cell Mobilization, PARADE Trial |
| NCT07154537 | Phase 4 | ACTIVE_NOT_RECRUITING | Pneumococcal Conjugated Vaccine 13 (PCV13) for Patients With Multiple Myeloma (MM) |
| NCT07334535 | Phase 4 | NOT_YET_RECRUITING | Isa-VRD in TIE HRMM |
| NCT07474961 | Phase 4 | NOT_YET_RECRUITING | BLOOD-dose: A Platform Trial Evaluating Dose Optimization in Hematological Diseases. |
| NCT00001561 | Phase 3 | COMPLETED | Active Immunization of Sibling Bone Marrow Transplant Donors Against Purified Myeloma Protein of the Recipient Undergoing Allogeneic Bone Marrow Transplantation |
| NCT00002548 | Phase 3 | COMPLETED | SWOG-9321 Melphalan, TBI, and Transplant vs Combo Chemo in Untreated Myeloma |
| NCT00002556 | Phase 3 | COMPLETED | Combination Chemotherapy With or Without High Dose Cyclophosphamide and Recombinant Interferon Alfa-2b in Treating Patients With Previously Untreated Stage I-III Multiple Myeloma |
| NCT00002850 | Phase 3 | COMPLETED | Antibiotic Therapy in Preventing Early Infection in Patients With Multiple Myeloma Who Are Receiving Chemotherapy |
| NCT00005834 | Phase 3 | TERMINATED | S9922 Combination Chemo Plus Filgrastim With or Without Thalidomide in Refractory Multiple Myeloma |
| NCT00037791 | Phase 3 | COMPLETED | Safety and Efficacy of (PN-152,243)/PN-196,444 in the Prevention of Thrombocytopenia |
| NCT00038233 | Phase 3 | COMPLETED | Thalidomide for Multiple Myeloma |
| NCT00048230 | Phase 3 | COMPLETED | PS-341 (VELCADE™) Versus High-Dose Dexamethasone in Patients With Relapsed or Refractory Multiple Myeloma |
| NCT00056160 | Phase 3 | COMPLETED | CC-5013 Plus Dexamethasone Versus Dexamethasone Alone in Previously Treated Subjects With Multiple Myeloma |
| NCT00057564 | Phase 3 | COMPLETED | A Study of Combination Thalidomide Plus Dexamethasone Therapy vs. Dexamethasone Therapy Alone in Previously Untreated Subjects With Multiple Myeloma |
| NCT00063726 | Phase 3 | COMPLETED | A Study of PS-341 Given to Patients With Multiple Myeloma Who Experienced Progressive Disease After Receiving Dexamethasone in M34101-039 |
| NCT00064038 | Phase 3 | COMPLETED | S0232 Dexamethasone With or Without Lenalidomide in Treating Patients With Previously Untreated Stage I, Stage II, or Stage III Multiple Myeloma |
Predicted chemistry — Sugi Predict
The predicted patent-compound landscape for MST1R across ~30M SureChEMBL compounds — explore on Sugi Predict.
Related Atlas pages
- Associated diseases: nasopharyngeal carcinoma, susceptibility to, 3
- Targeted by drugs: Crizotinib
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): nasopharyngeal carcinoma, susceptibility to, 3