A Fragment Screen Identifies Acrylamide Covalent Inhibitors of the TEAD•YAP Protein-Protein Interaction covalentmodifiers.blogspot.com/2026/03/a-fragment-scree...
3 weeks ago
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Posts by Covalent Modifiers
Discovery of Covalent Ligands with AlphaFold3 covalentmodifiers.blogspot.com/2026/03/discovery-of-cov...
4 weeks ago
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Acrylamide Bioisosterism: Alkenyl Aromatic Heterocycles as Reactivity-Tunable Warheads for Covalent BTK Inhibitors covalentmodifiers.blogspot.com/2026/03/acrylamide-biois...
4 weeks ago
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Covalent JAK3 inhibitors based on 2-arylamino and 7H-pyrrolo[2,3-d]pyrimidine scaffold: design, synthesis, and biological evaluation for the potential treatment of Bortezomib-resistant multiple myeloma covalentmodifiers.blogspot.com/2026/03/covalent-jak3-in...
1 month ago
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A Global Ligandability Map of Tryptoline Butynamide Stereoprobes Identifies Covalent Inhibitors of the Actin Maturation Protease ACTMAP covalentmodifiers.blogspot.com/2026/03/a-global-liganda...
1 month ago
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Development and Structural Characterization of UTE-156, a Covalent Inhibitor of the VCP/p97 AAA+ ATPase covalentmodifiers.blogspot.com/2026/03/development-and-...
1 month ago
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Discovery and Characterization of Divarasib (GDC-6036), a Potent Covalent Inhibitor of KRAS G12C covalentmodifiers.blogspot.com/2026/03/discovery-and-ch...
1 month ago
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A Tandem Bioorthogonal Retro-Cope and Cope Elimination for the Activation of Covalent Inhibitors with an Acrylamide or Vinylsulfonamide Warhead in Live Cells covalentmodifiers.blogspot.com/2026/02/a-tandem-bioorth...
2 months ago
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Discovery of a Potent, Selective, and In Vivo Efficacious Covalent Inhibitor for Lysine Methyltransferase SETD8 covalentmodifiers.blogspot.com/2026/02/discovery-of-pot...
2 months ago
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Exploiting human fucosyltransferase 8 allostery with a covalent inhibitor for core fucosylation suppression covalentmodifiers.blogspot.com/2026/02/exploiting-human...
2 months ago
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Covalent inhibitor design confers activity against both GDP- and GTP-bound forms of KRAS G12C covalentmodifiers.blogspot.com/2026/02/covalent-inhibit...
2 months ago
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Development of a Lysine-Reactive Targeted Covalent Inhibitor (TCI) for the P300/CBP-Associated Factor (PCAF) Bromodomain Through Structure-Based Design covalentmodifiers.blogspot.com/2026/02/development-of-l...
2 months ago
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Covalent Protein Inhibitors via Tyrosine and Tryptophan Conjugation with Cyclic Imine Mannich Electrophiles covalentmodifiers.blogspot.com/2026/02/covalent-protein...
2 months ago
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Chemoproteomics discovery of a CNS-penetrant covalent inhibitor of PIKfyve covalentmodifiers.blogspot.com/2026/02/chemoproteomics-...
2 months ago
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Group Competition Strategy for Covalent Ligand Discovery covalentmodifiers.blogspot.com/2026/01/group-competitio...
2 months ago
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Protein tyrosine phosphatase inactivation by electrophilic tyrosine modification covalentmodifiers.blogspot.com/2026/01/protein-tyrosine...
3 months ago
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Covalent Peptide-Encoded Libraries Enable Discovery of Inhibitors of Epidermal Growth Factor Receptor (EGFR) covalentmodifiers.blogspot.com/2026/01/covalent-peptide...
3 months ago
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Structure-Guided Optimization of 4-Chloro-Pyrazolopyridine Analogs for Covalent PREP Inhibition covalentmodifiers.blogspot.com/2026/01/structure-guided...
3 months ago
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Ninhydrin as a covalent warhead for chemical proteomic-enabled discovery and selective engagement of reactive arginines covalentmodifiers.blogspot.com/2026/01/ninhydrin-as-cov...
3 months ago
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Peptide-based covalent inhibitor of tubulin detyrosination promotes mesenchymal-to-epithelial transition in lung cancer cells covalentmodifiers.blogspot.com/2026/01/peptide-based-co...
3 months ago
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Discovery of a First-in-Class Covalent Allosteric SHP1 Inhibitor with Immunotherapeutic Activity covalentmodifiers.blogspot.com/2025/12/discovery-of-fir...
3 months ago
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Covalent Drug Binding in Live Cells Monitored by Mid-Infrared Quantum Cascade Laser Spectroscopy: Photoactive Yellow Protein as a Model System covalentmodifiers.blogspot.com/2025/12/covalent-drug-bi...
4 months ago
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A practical method for determining the rate of covalent modification of fragments and leads covalentmodifiers.blogspot.com/2025/12/a-practical-meth...
4 months ago
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Stereoselective Degradation of Diacylglycerol Kinases Potentiate T cell Activation and Tumor Cell Cytotoxicity covalentmodifiers.blogspot.com/2025/12/stereoselective-...
4 months ago
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Identification of VVD-214/RO7589831, a Clinical-Stage, Covalent Allosteric Inhibitor of WRN Helicase for the Treatment of MSI-High Cancers covalentmodifiers.blogspot.com/2025/12/identification-o...
4 months ago
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The Development of UM-203, A Reversible Covalent STING Antagonis covalentmodifiers.blogspot.com/2025/12/the-development-...
4 months ago
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A Highly Reactive Cysteine-Targeted Acrylophenone Chemical Probe That Enables Peptide/Protein Bioconjugation and Chemoproteomics Analysis covalentmodifiers.blogspot.com/2025/12/a-highly-reactiv...
4 months ago
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Preclinical characterization of EGT710, an oral non-peptidomimetic reversible covalent SARS-CoV-2 main protease inhibitor covalentmodifiers.blogspot.com/2025/11/preclinical-char...
4 months ago
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Fast and Site-Specific Covalent Targeting of Proteins by Arylfluorosulfate-Modified Aptamers covalentmodifiers.blogspot.com/2025/11/fast-and-site-sp...
4 months ago
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youtu.be/4dC23U9S2Vc?... @dannomura.bsky.social @drug-hunter.bsky.social
5 months ago
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