ArticleBioorganic & medicinal chemistry letters2013
Small-molecule pyrimidine inhibitors of the cdc2-like (Clk) and dual specificity tyrosine phosphorylation-regulated (Dyrk) kinases: development of chemical probe ML315.
Article in Bioorganic & medicinal chemistry letters, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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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
17 citing papers in PubMed, 50 citations in OpenAlex.
- Identification and Biological Evaluation of a Novel CLK4 Inhibitor Targeting Alternative Splicing in Pancreatic Cancer Using Structure-Based Virtual Screening.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025Article
- Global transcriptome modulation by xenobiotics: the role of alternative splicing in adaptive responses to chemical exposures.Human genomics · 2024Article
- Cdc2-like kinases: structure, biological function, and therapeutic targets for diseases.Signal transduction and targeted therapy · 2023Review
- Discovery of new Cdc2-like kinase 4 (CLK4) inhibitorsRSC advances · 2022Article
- SM04755, a small-molecule inhibitor of the Wnt pathway, as a potential topical treatment for tendinopathy.Journal of orthopaedic research : official publication of the Orthopaedic Research Society · 2021Article
- 5-Methoxybenzothiophene-2-Carboxamides as Inhibitors of Clk1/4: Optimization of Selectivity and Cellular Potency.Molecules (Basel, Switzerland) · 2021Article
- Cdc-Like Kinases (CLKs): Biology, Chemical Probes, and Therapeutic Potential.International journal of molecular sciences · 2020Review
- RNA Splicing: A New Paradigm in Host-Pathogen Interactions.Journal of molecular biology · 2019Review
- Kororamides, Convolutamines, and Indole Derivatives as Possible Tau and Dual-Specificity Kinase Inhibitors for Alzheimer's Disease: A Computational Study.Marine drugs · 2018Article
- Synthesis and Discovery of Estra-1,3,5(10),6,8-pentaene-2,16α-diol.Organic letters · 2018Article
- Pharmacology of Modulators of Alternative Splicing.Pharmacological reviews · 2017Review
- Inhibition of DYRK1A Stimulates Human β-Cell Proliferation.Diabetes · 2016Article
- Synthesis of Thiazolo[5,4-f]quinazolin-9(8H)-ones as Multi-Target Directed Ligands of Ser/Thr Kinases.Molecules (Basel, Switzerland) · 2016Article
- DYRK1A, a Dosage-Sensitive Gene Involved in Neurodevelopmental Disorders, Is a Target for Drug Development in Down Syndrome.Frontiers in behavioral neuroscience · 2016Review
- The Tumor Suppressor NKX3.1 Is Targeted for Degradation by DYRK1B Kinase.Molecular cancer research : MCR · 2015Article
- Synthesis and SAR studies of novel 6,7,8-substituted 4-substituted benzyloxyquinolin-2(1H)-one derivatives for anticancer activity.British journal of pharmacology · 2015Article
- Article
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Authors and funding
9 authors at 4 institutions in 1 country.
Funding
Abstract
Substituted pyrimidine inhibitors of the Clk and Dyrk kinases have been developed, exploring structure-activity relationships around four different chemotypes. The most potent compounds have low-nanomolar inhibitory activity against Clk1, Clk2, Clk4, Dyrk1A and Dyrk1B. Kinome scans with 442 kinases using agents representing three of the chemotypes show these inhibitors to be highly selective for the Clk and Dyrk families. Further off-target pharmacological evaluation with ML315, the most selective agent, supports this conclusion.
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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.