Strategies for Discovering and Derisking Covalent, Irreversible Enzyme Inhibitors

Johnson, Douglas S, Weerapana, Eranthie, Cravatt, Benjamin F·2010·Future Medicinal Chemistry
DOI 10.4155/fmc.10.21

Cited by (425)

Items 401–425 of 425

  1. BindingDB Entry 50002407: Novel indanone derivatives as MAO B/H
    BindingDB · 2020 · UC San Diego
  2. BindingDB Entry 50015538: Characterization of an aromatic trifluoromethyl ketone as a new warhead for covalently reversible kinase inhibitor design.
    BindingDB · 2023 · UC San Diego
  3. BindingDB Entry 50009678: Kinetic Optimization of Lysine-Targeting Covalent Inhibitors of HSP72.
    BindingDB · 2021 · UC San Diego
  4. BindingDB Entry 50000292: Covalent Modifiers: A Chemical Perspective on the Reactivity ofα,β-Unsaturated Carbonyls with Thiols via Hetero-Michael Addition Reactions.
    BindingDB · 2019 · UC San Diego
  5. BindingDB Entry 50043250: 1,2,4-Triazole derivatives as transient inactivators of kallikreins involved in skin diseases.
    BindingDB · 2014 · UC San Diego
  6. BindingDB Entry 50044916: A simple and widely applicable hit validation strategy for protein-protein interaction inhibitors based on a quantitative ligand displacement assay.
    BindingDB · 2016 · UC San Diego
  7. BindingDB Entry 50044711: Structure-Based Design of Reactive Nucleosides for Site-Specific Modification of the A2A Adenosine Receptor.
    BindingDB · 2016 · UC San Diego
  8. BindingDB Entry 50047640: 3-Oxo-hexahydro-1H-isoindole-4-carboxylic Acid as a Drug Chiral Bicyclic Scaffold: Structure-Based Design and Preparation of Conformationally Constrained Covalent and Noncovalent Prolyl Oligopeptidase Inhibitors.
    BindingDB · 2017 · UC San Diego
  9. BindingDB Entry 50006562: Progress toward B-Cell Lymphoma 6 BTB Domain Inhibitors for the Treatment of Diffuse Large B-Cell Lymphoma and Beyond.
    BindingDB · 2024 · UC San Diego
  10. BindingDB Entry 50000622: Discovery of Trifluoromethyl Glycol Carbamates as Potent and Selective Covalent Monoacylglycerol Lipase (MAGL) Inhibitors for Treatment of Neuroinflammation.
    BindingDB · 2019 · UC San Diego
  11. BindingDB Entry 50042799: Identification of selective and potent inhibitors of fibroblast activation protein and prolyl oligopeptidase.
    BindingDB · 2013 · UC San Diego
  12. BindingDB Entry 50044550: Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity.
    BindingDB · 2015 · UC San Diego
  13. BindingDB Entry 50000463: Azetidine and Piperidine Carbamates as Efficient, Covalent Inhibitors of Monoacylglycerol Lipase.
    BindingDB · 2019 · UC San Diego
  14. BindingDB Entry 50039918: Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia.
    BindingDB · 2013 · UC San Diego
  15. BindingDB Entry 50044618: Phenylalanine-Based Inactivator of AKT Kinase: Design, Synthesis, and Biological Evaluation.
    BindingDB · 2015 · UC San Diego
  16. BindingDB Entry 50044947: Design, synthesis and biological evaluation of FLT3 covalent inhibitors with a resorcylic acid core.
    BindingDB · 2016 · UC San Diego
  17. BindingDB Entry 50002718: Synthesis and biological evaluation of curcumin derivatives modified with α-amino boronic acid as proteasome inhibitors.
    BindingDB · 2020 · UC San Diego
  18. BindingDB Entry 50000147: Stilbene Boronic Acids Form a Covalent Bond with Human Transthyretin and Inhibit Its Aggregation.
    BindingDB · 2019 · UC San Diego
  19. BindingDB Entry 50006668: Phenylthiomethyl Ketone-Based Fragments Show Selective and Irreversible Inhibition of Enteroviral 3C Proteases.
    BindingDB · 2020 · UC San Diego
  20. BindingDB Entry 50001159: Chemical Approaches to Intervening in Ubiquitin Specific Protease 7 (USP7) Function for Oncology and Immune Oncology Therapies.
    BindingDB · 2020 · UC San Diego
  21. BindingDB Entry 50010667: Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK).
    BindingDB · 2021 · UC San Diego
  22. BindingDB Entry 50049193: Discovery of 2-((3-Acrylamido-4-methylphenyl)amino)-N-(2-methyl-5-(3,4,5-trimethoxybenzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-BMX-078) as a Highly Potent and Selective Type II Irreversible Bone Marrow Kinase in the X Chromosome (BMX) Kinase Inhibitor.
    BindingDB · 2019 · UC San Diego
  23. BindingDB Entry 50002046: Small molecule inhibitors of anthrax edema factor.
    BindingDB · 2020 · UC San Diego
  24. BindingDB Entry 50018560: JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRAS
    BindingDB · 2024 · UC San Diego
  25. BindingDB Entry 50002518: Design, Synthesis, and Evaluation of Piperazinyl Pyrrolidin-2-ones as a Novel Series of Reversible Monoacylglycerol Lipase Inhibitors.
    BindingDB · 2020 · UC San Diego