ArticleACS medicinal chemistry letters2015
Fragment-based discovery of type I inhibitors of maternal embryonic leucine zipper kinase.
Article in ACS medicinal chemistry letters, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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The trial behind it
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Who cites it
16 citing papers in PubMed.
- A novel approach for enhancing the potency of kinase inhibitors using topological water networks.Journal of cheminformatics · 2026Article
- Frags2Drugs: A Novel In Silico Fragment-Based Approach to the Discovery of Kinase Inhibitors.Pharmaceuticals (Basel, Switzerland) · 2026Article
- A Perspective on the Strategic Application of Deconstruction-Reconstruction in Drug Discovery.Journal of medicinal chemistry · 2025Review
- Diversified ring expansion of saturated cyclic amines enabled by azlactone insertion.Nature chemistry · 2024Article
- Discovery of first-in-class PROTACs targeting maternal embryonic leucine zipper kinase (MELK) for the treatment of Burkitt lymphoma.RSC medicinal chemistry · 2024Article
- FGDB: a comprehensive graph database of ligand fragments from the Protein Data Bank.Database : the journal of biological databases and curation · 2022Article
- Consensus Virtual Screening Identified [1,2,4]Triazolo[1,5-b]isoquinolines As MELK Inhibitor Chemotypes.ChemMedChem · 2022Article
- Enigmatic MELK: The controversy surrounding its complex role in cancer.The Journal of biological chemistry · 2020Review
- Arrestin-3 interaction with maternal embryonic leucine-zipper kinase.Cellular signalling · 2019Article
- Article
- CRISPR/Cas9 mutagenesis invalidates a putative cancer dependency targeted in on-going clinical trials.eLife · 2017Article
- AutoSite: an automated approach for pseudo-ligands prediction-from ligand-binding sites identification to predicting key ligand atoms.Bioinformatics (Oxford, England) · 2016Article
- MELK-T1, a small-molecule inhibitor of protein kinase MELK, decreases DNA-damage tolerance in proliferating cancer cells.Bioscience reports · 2015Article
- Perspective on computational and structural aspects of kinase discovery from IPK2014.Biochimica et biophysica acta · 2015Review
- Fragment-Based Discovery of Potent and Selective DDR1/2 Inhibitors.ACS medicinal chemistry letters · 2015Article
- Structure-Based Design of Type II Inhibitors Applied to Maternal Embryonic Leucine Zipper Kinase.ACS medicinal chemistry letters · 2015Article
Corrections and comments
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Authors and funding
20 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Fragment-based drug design was successfully applied to maternal embryonic leucine zipper kinase (MELK). A low affinity (160 μM) fragment hit was identified, which bound to the hinge region with an atypical binding mode, and this was optimized using structure-based design into a low-nanomolar and cell-penetrant inhibitor, with a good selectivity profile, suitable for use as a chemical probe for elucidation of MELK biology.
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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.