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Targeting the Translocator Protein (18 kDa) in Cardiac Diseases: State of the Art and Future Opportunities.
J Med Chem 67: 17-37 (2024)
National Research Council of Italy
Optimization of Selectivity and Pharmacokinetic Properties of Salt-Inducible Kinase Inhibitors that Led to the Discovery of Pan-SIK Inhibitor GLPG3312.
J Med Chem 67: 380-401 (2024)
Galapagos
Fragment Merging, Growing, and Linking Identify New Trypanothione Reductase Inhibitors for Leishmaniasis.
J Med Chem 67: 402-419 (2024)
Sapienza University of Rome
Electrophilic MiniFrags Revealed Unprecedented Binding Sites for Covalent HDAC8 Inhibitors.
J Med Chem 67: 572-585 (2024)
Hun-Ren Research Centre for Natural Sciences
Discovery of Five SOS2 Fragment Hits with Binding Modes Determined by SOS2 X-Ray Cocrystallography.
J Med Chem 67: 774-781 (2024)
Mirati Therapeutics
Screening Ultra-Large Encoded Compound Libraries Leads to Novel Protein-Ligand Interactions and High Selectivity.
J Med Chem 67: 864-884 (2024)
Astrazeneca
Design, Synthesis, and Evaluation of Inhibitors of Hedgehog Acyltransferase.
J Med Chem 67: 1061-1078 (2024)
Imperial College London
Ligand-Based Competition Binding by Real-Time
J Med Chem 67: 1115-1126 (2024)
University of Bologna
First-in-Class Selenium-Containing Potent Serotonin Receptor 5-HT
J Med Chem 67: 1580-1610 (2024)
Jagiellonian University Medical College
Discovery and Preclinical Pharmacology of NX-2127, an Orally Bioavailable Degrader of Bruton's Tyrosine Kinase with Immunomodulatory Activity for the Treatment of Patients with B Cell Malignancies.
J Med Chem 67: 2321-2336 (2024)
Nurix Therapeutics
Discovery of CMX990: A Potent SARS-CoV-2 3CL Protease Inhibitor Bearing a Novel Warhead.
J Med Chem 67: 2369-2378 (2024)
Calibr At Scripps Research Institute
PM534, an Optimized Target-Protein Interaction Strategy through the Colchicine Site of Tubulin.
J Med Chem 67: 2619-2630 (2024)
Unidad Bics
First-in-Class Dual EZH2-HSP90 Inhibitor Eliciting Striking Antiglioblastoma Activity
J Med Chem 67: 2963-2985 (2024)
Taipei Medical University
Synthetic Approaches to Novel Human Carbonic Anhydrase Isoform Inhibitors Based on Pyrrol-2-one Moiety.
J Med Chem 67: 3018-3038 (2024)
Romanian Academy
Antiviral Protein-Protein Interaction Inhibitors.
J Med Chem 67: 3205-3231 (2024)
Wroclaw University
Discovery of 5-Hydroxy-1,4-naphthoquinone (Juglone) Derivatives as Dual Effective Agents Targeting Platelet-Cancer Interplay through Protein Disulfide Isomerase Inhibition.
J Med Chem 67: 3626-3642 (2024)
National Taiwan University
Focused Screening Identifies Different Sensitivities of Human TET Oxygenases to the Oncometabolite 2-Hydroxyglutarate.
J Med Chem 67: 4525-4540 (2024)
University of Oxford
Discovery of the sEH Inhibitor Epoxykynin as a Potent Kynurenine Pathway Modulator.
J Med Chem 67: 4691-4706 (2024)
Max Planck Institute of Molecular Physiology
Discovery of Pyridopyrimidinones that Selectively Inhibit the H1047R PI3Kα Mutant Protein.
J Med Chem 67: 4936-4949 (2024)
Mirati Therapeutics
Discovery of GLPG2737, a Potent Type 2 Corrector of CFTR for the Treatment of Cystic Fibrosis in Combination with a Potentiator and a Type 1 Co-corrector.
J Med Chem 67: 5216-5232 (2024)
Galapagos
Discovery of Clinical Candidate GLPG3970: A Potent and Selective Dual SIK2/SIK3 Inhibitor for the Treatment of Autoimmune and Inflammatory Diseases.
J Med Chem 67: 5233-5258 (2024)
Galapagos