ArticleEuropean journal of medicinal chemistry2013
UNC1062, a new and potent Mer inhibitor.
Article in European journal of medicinal chemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 38 papers.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
38 citing papers in PubMed, 65 citations in OpenAlex.
- Purine and Pyrrolopyrimidine-Based Small Molecules as Multitarget Therapeutics.Archiv der Pharmazie · 2026Review
- MerTK inhibition by UNC569 triggers DNA damage and JNK/p38 MAPK cascade-driven apoptosis in pancreatic cancer.Acta biochimica et biophysica Sinica · 2026Article
- Enhancing Chemosensitivity With Quercetin: Mechanistic Insights Into MerTK and Associated Signaling Pathways.Cancer reports (Hoboken, N.J.) · 2025Review
- Discovery of Novel 2-Substituted Aniline Pyrimidine Based Derivatives as Potent Mer/c-Met Dual Inhibitors with Improvement Bioavailability.Biomolecules · 2025Article
- Exploiting structural variability in the kinase back-pocket to modulate polypharmacology of TAM inhibitors.European journal of medicinal chemistry · 2025Article
- UNC9426, a Potent and Orally Bioavailable TYRO3-Specific Inhibitor.Journal of medicinal chemistry · 2025Article
- Novel Compound MMV1804559 from the Global Health Priority Box Exhibits In Vitro and In Vivo Activity againstInternational journal of molecular sciences · 2024Article
- Discovery of pyrazolopyrimidines that selectively inhibit CSF-1R kinase by iterative design, synthesis and screening against glioblastoma cells.RSC medicinal chemistry · 2023Article
- Review
- MERTK Inhibition: Potential as a Treatment Strategy in EGFR Tyrosine Kinase Inhibitor-Resistant Non-Small Cell Lung Cancer.Pharmaceuticals (Basel, Switzerland) · 2021Review
- Development of the phenylpyrazolo[3,4-Theranostics · 2021Article
- Crystal Structure of the Kinase Domain of MerTK in Complex with AZD7762 Provides Clues for Structure-Based Drug Development.International journal of molecular sciences · 2020Article
- Recent developments in anticancer kinase inhibitors based on the pyrazolo[3,4-RSC medicinal chemistry · 2020Review
- MERTK in cancer therapy: Targeting the receptor tyrosine kinase in tumor cells and the immune system.Pharmacology & therapeutics · 2020Review
- Distinct synovial tissue macrophage subsets regulate inflammation and remission in rheumatoid arthritis.Nature medicine · 2020Article
- Small Ones to Fight a Big Problem-Intervention of Cancer Metastasis by Small Molecules.Cancers · 2020Review
- Identification of pAKT as a pharmacodynamic marker for MER kinase in human melanoma G361 cells.Biomarker research · 2020Article
- Targeting Tyro3, Axl and MerTK (TAM receptors): implications for macrophages in the tumor microenvironment.Molecular cancer · 2019Review
- Article
- Review
Corrections and comments
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Authors and funding
18 authors at 3 institutions in 1 country.
Funding
Abstract
Abnormal activation of Mer kinase has been implicated in the oncogenesis of many human cancers including acute lymphoblastic and myeloid leukemia, non-small cell lung cancer, and glioblastoma. We have discovered a new family of small molecule Mer inhibitors, pyrazolopyrimidine sulfonamides, that potently inhibit the kinase activity of Mer. Importantly, these compounds do not demonstrate significant hERG activity in the PatchXpress assay. Through structure-activity relationship studies, 35 (UNC1062) was identified as a potent (IC50 = 1.1 nM) and selective Mer inhibitor. When applied to live tumor cells, UNC1062 inhibited Mer phosphorylation and colony formation in soft agar. Given the potential of Mer as a therapeutic target, UNC1062 is a promising candidate for further drug development.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.