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): 269 total — 1 likely-pathogenic
- Phenotypes (HPO): 2
- Druggable target: yes — 42 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_002447
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: 33 — 23 protein_coding, 7 retained_intron, 3 nonsense_mediated_decay
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
RefSeq mRNA: 3 — MANE Select: NM_002447
NM_001244937, NM_001318913, 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.
FANTOM5 promoters (1 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 42284 | 1.3794 | 399 |
Top tissues by expression
286 total, 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 |
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 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): EGR1, HIF1A, IRF6, NFE2L2, NFKB, NFKBIA, RELA, SMAD4, SP1, TXK
miRNA regulators (miRDB)
18 targeting MST1R, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):
| 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 |
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
4 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | mst1rb | ENSDARG00000004871 |
| 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)
Protein
Protein identifiers
Macrophage-stimulating protein receptor — Q04912 (reviewed: Q04912)
Alternative names: CDw136, Protein-tyrosine kinase 8, p185-Ron
All UniProt accessions (6): A0AAQ5BHR6, A0AAQ5BHX4, Q04912, 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 (3): NP_001231866, NP_001305842, 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), 1 shown:
- L-tyrosyl-[protein] + ATP = O-phospho-L-tyrosyl-[protein] + ADP + H(+) (RHEA:10596)
UniProt features (163 total): strand 57, helix 28, sequence variant 20, disulfide bond 11, glycosylation site 8, splice variant 8, turn 7, 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.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 4FWW | X-RAY DIFFRACTION | 1.85 |
| 8ZKD | X-RAY DIFFRACTION | 2.05 |
| 3PLS | X-RAY DIFFRACTION | 2.24 |
| 4QT8 | X-RAY DIFFRACTION | 3 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q04912-F1 | 80.23 | 0.46 |
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): 1208 (proton acceptor)
Ligand- & substrate-binding residues (4): 1088–1096; 1114; 1161–1164; 1212
Post-translational modifications (4): 1238, 1239, 1353, 1360
Disulfide bonds (11): 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): 66, 419, 458, 488, 654, 720, 841, 897
Function
Pathways and Gene Ontology
Reactome pathways
3 pathways
| ID | Pathway |
|---|---|
| R-HSA-8852405 | Signaling by MST1 |
| 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
Rollup of top-2 pathways:
| Category | Pathways |
|---|---|
| Signaling by Receptor Tyrosine Kinases | 1 |
| Signal Transduction | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| 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 |
| 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 |
| protein binding | 1 |
| nucleoside phosphate binding | 1 |
| heterocyclic compound binding | 1 |
Protein interactions and networks
STRING
2840 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| MST1R | MST1 | P26927 | 999 |
| MST1R | HGF | P14210 | 926 |
| MST1R | SRSF1 | Q07955 | 849 |
| MST1R | HYAL2 | Q12891 | 823 |
| MST1R | EGFR | P00533 | 772 |
| MST1R | CTNNB1 | P35222 | 743 |
| MST1R | SPAM1 | P38567 | 742 |
| MST1R | GAB2 | Q9UQC2 | 704 |
| MST1R | HNRNPA1 | P09651 | 637 |
| MST1R | PLXNB1 | O43157 | 632 |
| MST1R | HYAL1 | Q12794 | 586 |
| MST1R | ATAD1 | Q8NBU5 | 564 |
| MST1R | SEMA3B | Q13214 | 507 |
| MST1R | APEH | P13798 | 506 |
| MST1R | SEMA6A | Q9H2E6 | 503 |
IntAct
38 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| MST1R | MST1 | psi-mi:“MI:0407”(direct interaction) | 0.720 |
| MST1R | MST1 | psi-mi:“MI:0915”(physical association) | 0.720 |
| MST1 | MST1R | psi-mi:“MI:0407”(direct interaction) | 0.720 |
| PLXNB1 | MST1R | psi-mi:“MI:0915”(physical association) | 0.520 |
| PLXNB2 | MST1R | psi-mi:“MI:0915”(physical association) | 0.520 |
| MST1R | PLXNB3 | psi-mi:“MI:0915”(physical association) | 0.520 |
| MST1R | PLXNB1 | psi-mi:“MI:0915”(physical association) | 0.520 |
| MST1R | PLXNB2 | psi-mi:“MI:0915”(physical association) | 0.520 |
| FURIN | MST1R | psi-mi:“MI:0194”(cleavage reaction) | 0.440 |
| MST1R | CBL | psi-mi:“MI:0407”(direct interaction) | 0.440 |
| PKM | MST1R | psi-mi:“MI:0217”(phosphorylation reaction) | 0.440 |
| MST1R | UBL4A | psi-mi:“MI:0914”(association) | 0.420 |
| MST1R | Plxnb1 | psi-mi:“MI:0915”(physical association) | 0.400 |
| YWHAQ | MST1R | psi-mi:“MI:0915”(physical association) | 0.370 |
| ABL1 | psi-mi:“MI:0914”(association) | 0.350 | |
| TMEM106A | QSOX1 | psi-mi:“MI:0914”(association) | 0.350 |
| TMEM106A | TMEM131L | psi-mi:“MI:0914”(association) | 0.350 |
| BTNL2 | TMEM131L | psi-mi:“MI:0914”(association) | 0.350 |
| SFTPC | TMEM131L | psi-mi:“MI:0914”(association) | 0.350 |
| BRICD5 | TMEM131L | psi-mi:“MI:0914”(association) | 0.350 |
| HLA-DRB1 | TMEM131L | psi-mi:“MI:0914”(association) | 0.350 |
| PTCH1 | TMEM131L | psi-mi:“MI:0914”(association) | 0.350 |
| ASIC4 | TMEM131L | psi-mi:“MI:0914”(association) | 0.350 |
| NCR3 | POTEF | psi-mi:“MI:0914”(association) | 0.350 |
| NAAA | HAX1 | psi-mi:“MI:0914”(association) | 0.350 |
| PRG2 | QSOX1 | psi-mi:“MI:0914”(association) | 0.350 |
BioGRID (205): MST1R (Affinity Capture-MS), MST1R (Affinity Capture-MS), MST1R (Affinity Capture-MS), MST1R (Affinity Capture-MS), MST1R (Affinity Capture-MS), PTPRR (Two-hybrid), MST1R (Negative Genetic), MST1R (Negative Genetic), PRKCA (Negative Genetic), MST1R (Negative Genetic), MST1R (Positive Genetic), PRKAB1 (Positive Genetic), MST1R (Positive Genetic), PFKFB4 (Positive Genetic), NPY4R (Positive Genetic)
ESM2 similar proteins: A0A1B0GTW7, A0A1D5NSK0, A0A1L8HYT7, A0A286YEC0, D3ZT86, D3ZWJ9, D4A929, F8W3R9, G7PWZ3, I6M4H4, O08852, O43157, O43278, O75074, O88204, P17813, P49000, P59383, Q04912, Q17R55, Q499Z3, Q4R3B7, Q4TUC0, Q5ND34, Q62190, Q63961, Q6AXX1, Q76MJ5, Q7TN88, Q7TQH7, Q7Z442, Q7Z4F1, Q80W87, Q80YN4, Q866Y3, Q86VZ4, Q8BHW9, Q8BMN4, Q8BYI8, Q8BZT7
Diamond homologs: A0JM20, A0M8R7, A0M8S8, A1X150, F1QVU0, G3V9H8, O02466, O35346, P00519, P00520, P00521, P00522, P00529, P06213, P07949, P08069, P08581, P08941, P09760, P0DV84, P10447, P13368, P14617, P16056, P20806, P22182, P23049, P30530, P33497, P34152, P34925, P35546, P35590, P42684, P55144, P55146, P57097, P70451, P97523, P97793
SIGNOR signaling
9 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 |
Disease & clinical
Clinical variants and AI predictions
ClinVar
269 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 1 |
| Uncertain significance | 192 |
| Likely benign | 27 |
| Benign | 16 |
Top pathogenic / likely-pathogenic (1)
| Variant ID | HGVS | Classification |
|---|---|---|
| 800321 | NM_002447.4(MST1R):c.1477G>T (p.Asp493Tyr) | Likely pathogenic |
SpliceAI
3675 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 3:49887559:GTACC:G | acceptor_loss | 1.0000 |
| 3:49887560:TACC:T | acceptor_loss | 1.0000 |
| 3:49887561:ACC:A | acceptor_loss | 1.0000 |
| 3:49887562:CCT:C | acceptor_loss | 1.0000 |
| 3:49887563:C:CA | acceptor_loss | 1.0000 |
| 3:49887564:T:A | acceptor_loss | 1.0000 |
| 3:49890481:TCACC:T | donor_loss | 1.0000 |
| 3:49890482:CACCA:C | donor_loss | 1.0000 |
| 3:49890483:ACCAC:A | donor_loss | 1.0000 |
| 3:49890484:CCA:C | donor_gain | 1.0000 |
| 3:49890652:T:C | acceptor_gain | 1.0000 |
| 3:49890652:T:TC | acceptor_gain | 1.0000 |
| 3:49891185:CTGG:C | donor_gain | 1.0000 |
| 3:49891195:A:AC | donor_gain | 1.0000 |
| 3:49891196:C:CC | donor_gain | 1.0000 |
| 3:49891394:CTGA:C | donor_loss | 1.0000 |
| 3:49891395:TGACC:T | donor_loss | 1.0000 |
| 3:49891396:GACC:G | donor_loss | 1.0000 |
| 3:49891398:CCCG:C | donor_gain | 1.0000 |
| 3:49895223:T:TA | donor_gain | 1.0000 |
| 3:49895263:G:C | donor_gain | 1.0000 |
| 3:49895374:C:CC | acceptor_gain | 1.0000 |
| 3:49895457:T:TA | donor_gain | 1.0000 |
| 3:49897417:CTA:C | acceptor_loss | 1.0000 |
| 3:49898207:TGGAA:T | acceptor_gain | 1.0000 |
| 3:49898208:GGAA:G | acceptor_gain | 1.0000 |
| 3:49898212:C:CC | acceptor_gain | 1.0000 |
| 3:49898685:AAAC:A | acceptor_gain | 1.0000 |
| 3:49898686:AAC:A | acceptor_gain | 1.0000 |
| 3:49898689:C:CC | acceptor_gain | 1.0000 |
AlphaMissense
9011 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 3:49891768:C:A | K1114N | 0.997 |
| 3:49891768:C:G | K1114N | 0.997 |
| 3:49890060:A:G | W1271R | 0.996 |
| 3:49890060:A:T | W1271R | 0.996 |
| 3:49890521:G:C | S1258R | 0.996 |
| 3:49890521:G:T | S1258R | 0.996 |
| 3:49890523:T:G | S1258R | 0.996 |
| 3:49890538:A:G | W1253R | 0.996 |
| 3:49890538:A:T | W1253R | 0.996 |
| 3:49890039:A:G | W1278R | 0.995 |
| 3:49890039:A:T | W1278R | 0.995 |
| 3:49890503:A:C | F1264L | 0.995 |
| 3:49890503:A:T | F1264L | 0.995 |
| 3:49890505:A:G | F1264L | 0.995 |
| 3:49890032:A:G | L1280P | 0.994 |
| 3:49890536:C:A | W1253C | 0.993 |
| 3:49890536:C:G | W1253C | 0.993 |
| 3:49890630:A:T | V1222D | 0.993 |
| 3:49891287:A:G | L1185P | 0.993 |
| 3:49891775:G:T | A1112D | 0.993 |
| 3:49902927:A:C | F228C | 0.993 |
| 3:49887540:A:G | W1324R | 0.992 |
| 3:49887540:A:T | W1324R | 0.992 |
| 3:49891823:A:T | V1096D | 0.992 |
| 3:49891831:A:C | F1093L | 0.992 |
| 3:49891831:A:T | F1093L | 0.992 |
| 3:49891833:A:G | F1093L | 0.992 |
| 3:49891829:C:T | G1094E | 0.991 |
| 3:49903182:C:G | C143S | 0.991 |
| 3:49903183:A:T | C143S | 0.991 |
dbSNP variants (sampled 300 via entrez): RS1000195236 (3:49892506 G>A,C), RS1000283859 (3:49898473 C>T), RS1000344143 (3:49890965 A>G), RS1000572102 (3:49890928 G>A), RS1000592373 (3:49898370 T>G), RS1000602560 (3:49901954 A>C,G,T), RS1000884012 (3:49904327 G>T), RS1001079569 (3:49904611 G>A,T), RS1001193344 (3:49894282 G>C), RS1001245372 (3:49894106 T>C), RS1001339313 (3:49887842 C>T), RS1001464861 (3:49898065 G>A,T), RS1001672888 (3:49897569 T>A), RS1001709515 (3:49900871 G>A), RS1001963672 (3:49903908 G>A,C,T)
Disease associations
OMIM: gene MIM:600168 | disease phenotypes: MIM:617075, MIM:254500
GenCC curated gene-disease
| Disease | Classification | Inheritance |
|---|---|---|
| nasopharyngeal carcinoma, susceptibility to, 3 | Limited | Autosomal dominant |
Mondo (2): nasopharyngeal carcinoma, susceptibility to, 3 (MONDO:0014902), plasma cell myeloma (MONDO:0009693)
Orphanet (3): Nasopharyngeal carcinoma (Orphanet:150), Multiple myeloma (Orphanet:29073), AL amyloidosis (Orphanet:85443)
HPO phenotypes
2 total (2 of 2 shown, HPO-id order):
| HPO | Term |
|---|---|
| HP:0000006 | Autosomal dominant inheritance |
| HP:0100630 | Neoplasia of the nasopharynx |
GWAS associations
19 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST001725_77 | Inflammatory bowel disease | 1.000000e-47 |
| GCST002548_9 | Ulcerative colitis | 8.000000e-07 |
| GCST003795_3 | Age at first birth | 5.000000e-15 |
| GCST005951_49 | Body mass index | 1.000000e-08 |
| GCST006044_2 | Age at first birth | 2.000000e-06 |
| GCST006045_5 | Age at first birth | 6.000000e-10 |
| GCST006920_7 | Regular attendance at a gym or sports club | 6.000000e-10 |
| GCST006922_9 | Regular attendance at a religious group | 3.000000e-08 |
| GCST007044_11 | Extremely high intelligence | 4.000000e-08 |
| GCST007559_24 | Sleep duration (short sleep) | 3.000000e-08 |
| GCST008129_41 | Body mass index | 9.000000e-26 |
| GCST010002_422 | Refractive error | 4.000000e-14 |
| GCST010698_80 | Subcortical volume (min-P) | 3.000000e-24 |
| GCST010699_110 | Brain morphology (min-P) | 4.000000e-08 |
| GCST010701_52 | Cortical surface area (MOSTest) | 1.000000e-16 |
| GCST010702_36 | Subcortical volume (MOSTest) | 1.000000e-10 |
| GCST010703_262 | Brain morphology (MOSTest) | 2.000000e-13 |
| GCST010988_142 | Adult body size | 2.000000e-37 |
| GCST011122_43 | Walking pace | 6.000000e-16 |
EFO canonical traits (5, from GWAS)
| 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)
| 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)
Molecules with ChEMBL bioactivity
42 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 155,553 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).
| Molecule | Name | Phase | Patents |
|---|---|---|---|
| CHEMBL1173655 | AFATINIB | 4 | 15,144 |
| CHEMBL180022 | NERATINIB | 4 | 9,404 |
| CHEMBL1834657 | INFIGRATINIB PHOSPHATE | 4 | 285 |
| CHEMBL1852688 | INFIGRATINIB | 4 | 2,209 |
| CHEMBL189963 | PALBOCICLIB | 4 | 13,102 |
| CHEMBL1983268 | ENTRECTINIB | 4 | 3,510 |
| CHEMBL2103830 | FOSTAMATINIB | 4 | 3,841 |
| CHEMBL2105717 | CABOZANTINIB | 4 | 11,177 |
| CHEMBL24828 | VANDETANIB | 4 | 42,230 |
| CHEMBL288441 | BOSUTINIB | 4 | 12,255 |
| CHEMBL3301622 | GILTERITINIB | 4 | 2,395 |
| CHEMBL601719 | CRIZOTINIB | 4 | 14,403 |
| CHEMBL223360 | LINIFANIB | 3 | 3,925 |
| CHEMBL415049 | BARASERTIB | 3 | 2,371 |
| CHEMBL491473 | CEDIRANIB | 3 | 9,098 |
| CHEMBL522892 | DOVITINIB | 3 | 4,944 |
| CHEMBL603469 | LESTAURTINIB | 3 | |
| CHEMBL1230609 | FORETINIB | 2 | 3,096 |
| CHEMBL1738757 | REBASTINIB | 2 | 1,478 |
| CHEMBL1822792 | MK-2461 | 2 | 686 |
| CHEMBL1967878 | CENISERTIB | 2 | |
| CHEMBL1980297 | ILORASERTIB | 2 | |
| CHEMBL215152 | DEFOSBARASERTIB | 2 | |
| CHEMBL253969 | OSI-632 | 2 | |
| CHEMBL3039525 | GOLVATINIB | 2 | |
| CHEMBL3545307 | MERESTINIB | 2 | |
| CHEMBL3989914 | GLESATINIB | 2 | |
| CHEMBL460702 | BMS-777607 | 2 | |
| CHEMBL475251 | R-406 | 2 | |
| CHEMBL564829 | MILCICLIB | 2 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
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)
7 measured of 9 human assays (9 total across all organisms); most potent 7 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value | Patent |
|---|---|---|---|
| FORETINIB | IC50 | 1.9 nM | |
| (3R,4R)-3-methoxy-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 | 3.93 nM | US-10189849: CDK inhibitors |
| 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 |
| 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 |
| N-[4-(6,7-dimethoxyquinolin-4-yl)oxy-3-fluorophenyl]-5-ethyl-1-pyrimidin-5-ylpyrazole-4-carboxamide | IC50 | 30 nM | US-9481668: Quinoline inhibitor of the macrophage stimulating 1 receptor MSTR1 |
| 4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]benzamide | IC50 | 33 nM | |
| 4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide | KD | 1000 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 1597 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 |
| methyleugenol | increases expression | 1 |
| pirinixic acid | increases activity, affects binding, decreases expression | 1 |
| beta-lapachone | decreases expression | 1 |
| tris(1,3-dichloro-2-propyl)phosphate | decreases expression | 1 |
| sodium arsenite | affects cotreatment, decreases expression, increases abundance | 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 | affects cotreatment, decreases expression, increases abundance | 1 |
| Curcumin | increases expression, decreases expression, affects binding, decreases reaction | 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 |
| Okadaic Acid | increases 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)
300 trials via MONDO — disease-level, not drug-specific.
| Trial | Phase | Status | Title |
|---|---|---|---|
| NCT00029224 | PHASE4 | COMPLETED | Treatment With Zoledronic Acid in Patients With Breast Cancer, Multiple Myeloma, and Prostate Cancer With Cancer Related Bone Lesions |
| NCT00104104 | PHASE4 | COMPLETED | A Multiple Myeloma Trial in Patients With Bone Metastases |
| NCT00211211 | PHASE4 | COMPLETED | FREE Study - Fracture Reduction Evaluation |
| NCT00242528 | PHASE4 | WITHDRAWN | Open-label Study, to Evaluate the Safety and Tolerability of Zoledronic Acid in Patients With Bone Lesions Secondary to Multiple Myeloma. |
| NCT00257114 | PHASE4 | COMPLETED | Evaluation of VELCADE Given as Retreatment to Multiple Myeloma Patients for Efficacy, Safety and Tolerability |
| NCT00352703 | PHASE4 | COMPLETED | PROMPT - Palifermin in Reduction of Oral Mucositis in PBSC Transplantation |
| NCT00361140 | PHASE4 | COMPLETED | Busulfan Safety/Efficacy as Conditioning Prior to Hematopoietic Cell Transplantation (HCT) |
| NCT00622505 | PHASE4 | COMPLETED | Zoledronic Acid Treatment (Every 4 or 12 Weeks) to Prevent Skeletal Complications in Advanced Multiple Myeloma Participants |
| NCT00652041 | PHASE4 | COMPLETED | Bortezomib/Adriamycine/Melfalan/Prednisone (VAMP)/Thalidomide/Cyclophosphamide/Dexamethasone (TaCyDex) or Bortezomib/Melfalan/Prednisone (V-MP)/TaCyDex) in Refractary or Relapsed Multiple Myeloma |
| NCT00733538 | PHASE4 | COMPLETED | Stage I Multiple Myeloma Treatment |
| NCT01087008 | PHASE4 | COMPLETED | Zoledronic Acid in Patients With Multiple Myeloma and Asymptomatic Biochemical Relapse |
| NCT01249690 | PHASE4 | UNKNOWN | Efficacy Study of PAD and TAD in Newly Diagnosed Multiple Myeloma |
| NCT01410929 | PHASE4 | WITHDRAWN | Evaluation of Vertebral Compression Fracture Fixation With RF Kyphoplasty in Patients With Multiple Myeloma |
| NCT01731886 | PHASE4 | COMPLETED | Lenalidomide and Dexamethasone With/Without Stem Cell Transplant in Patients With Multiple Myeloma |
| NCT01868828 | PHASE4 | UNKNOWN | A Study of PAD Versus Velcade, Cyclophosphamide and Dexamethasone (VCD) Treatment in Subjects With Multiple Myeloma |
| NCT02268890 | PHASE4 | COMPLETED | A Pharmacokinetic Study of Bortezomib in Taiwanese Participants With Multiple Myeloma |
| NCT02286830 | PHASE4 | COMPLETED | Prolonged Protection From Bone Disease in Multiple Myeloma |
| NCT02559154 | PHASE4 | UNKNOWN | Modified Bortezomib-based Combination Therapy for Multiple Myeloma |
| NCT02577783 | PHASE4 | UNKNOWN | PDD vs PAD to Treat Initially Diagnosed MM |
| NCT02773550 | PHASE4 | TERMINATED | Treatment With a Scheme With Low Doses of Bortezomib / Melphalan / Prednisone (MPV) in Patients With Multiple Myeloma |
| NCT02958969 | PHASE4 | COMPLETED | Apixaban for Primary Prevention of Venous Thromboembolism in Patients With Multiple Myeloma |
| NCT03173092 | PHASE4 | TERMINATED | A Study of Ixazomib (NINLARO®) in Combination With Lenalidomide and Dexamethasone (IRD) for the Treatment of Participants With Multiple Myeloma (MM) |
| NCT03619252 | PHASE4 | COMPLETED | Pneumococcal Vaccination of Multiple Myeloma Patients on Novel Agents |
| NCT03768960 | PHASE4 | 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 | PHASE4 | ACTIVE_NOT_RECRUITING | STUDY COMPARING TWO STANDARD TREATMENTS IN AUTOLOGOUS STEM CELL TRANSPLANTATION INELIGIBLE POPULATION AFFECTED BY MULTIPLE MYELOMA |
| NCT03908138 | PHASE4 | UNKNOWN | RDD Versus VDD in Newly Diagnosed Patients With Multiple Myeloma |
| NCT04217967 | PHASE4 | COMPLETED | Ixazomib, Lenalidomide, and Combination for Maintenance in NDMM Patients |
| NCT04952766 | PHASE4 | COMPLETED | Study Evaluating SARS-CoV-2 (COVID-19) Humoral Response After BNT162b2 Vaccine in Immunocompromised Adults Compared to Healthy Adults |
| NCT04989140 | PHASE4 | UNKNOWN | Study of Pomalidomide, Oral Dexamethasone and Ixazomib in Patients With Relapsed MM Who Have Received Lenalidomide |
| NCT05183139 | PHASE4 | 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 | PHASE4 | RECRUITING | A Long-term Study for Participants Previously Treated With Ciltacabtagene Autoleucel |
| NCT05429515 | PHASE4 | NOT_YET_RECRUITING | Effect of HFR-SUPRA in the Treatment of Multiple Myeloma-related Acute Kidney Injury |
| NCT05511428 | PHASE4 | COMPLETED | Home Based Daratumumab Administration for Patients With Multiple Myeloma |
| NCT05545202 | PHASE4 | 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 | PHASE4 | COMPLETED | Alternative Dosing Scheme of Pomalidomide 4 mg Every Other Day Versus Pomalidomide 2 mg and 4 mg Every Day; the POMAlternative Study |
| NCT05722405 | PHASE4 | RECRUITING | Ixazomib Plus Low-dose Lenalidomide Versus Ixazomib Alone for Maintenance Treatment of High Risk Multiple Myeloma |
| NCT05855122 | PHASE4 | UNKNOWN | Safety and ASCT-related Symptom Burden Optimization of Tocilizumab in ASCT Following HD Melphalan Conditioning for Multiple Myeloma Patients |
| NCT05944783 | PHASE4 | NOT_YET_RECRUITING | Bioequivalence Studies of Dasatinib 100 Mg |
| NCT06057402 | PHASE4 | RECRUITING | Elranatamab Post Trial Access Study for Participants With Multiple Myeloma (MM) |
| NCT06251076 | PHASE4 | RECRUITING | Plan Development for Giving Teclistamab in the Outpatient Setting |
Related Atlas pages
- Associated diseases: nasopharyngeal carcinoma, susceptibility to, 3
- 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