Late-stage functionalization with strain-release warheads enables tunable covalent inhibition https://covalentmodifiers.blogspot.com/2026/07/late-stage-functionalization-with.html

Peptidic Phosphonates as Irreversible Covalent Inhibitors of Plasmodium falciparum Serine Protease PfSUB1. https://covalentmodifiers.blogspot.com/2026/07/peptidic-phosphonates-as-irreversible.html

CHARMM-GUI Covalent Ligand Docker as a Web-based Molecular Docking Platform for Covalent Ligands https://covalentmodifiers.blogspot.com/2026/07/charmm-gui-covalent-ligand-docker-as.html

Covalent remodeling of CRBN creates a non-canonical neosubstrate interface with NTAQ1 https://covalentmodifiers.blogspot.com/2026/07/covalent-remodeling-of-crbn-creates-non.html

A covalent irreversible inhibitor binds in two mutually exclusive conformations to the active-site cysteine residue of human aldehyde dehydrogenase 1A3 https://covalentmodifiers.blogspot.com/2026/07/a-covalent-irreversible-inhibitor-binds.html

A covalent inhibitor targeting Cys-349 of LIMK1 confers selectivity over LIMK2 https://covalentmodifiers.blogspot.com/2026/07/a-covalent-inhibitor-targeting-cys-349.html

Machine learning-guided discovery of covalent sortase A inhibitors targeting MRSA virulence https://covalentmodifiers.blogspot.com/2026/07/machine-learning-guided-discovery-of.html

A chemoproteomic atlas of the human purine interactome for regioselective ligand discovery https://covalentmodifiers.blogspot.com/2026/06/a-chemoproteomic-atlas-of-human-purine.html

Characterization of the Second-Generation Covalent Fragment Library (CovLib Gen2): Thiol Reactivity Profiling and p53-Y220C Rescue https://covalentmodifiers.blogspot.com/2026/05/characterization-of-second-generation.html

Accelerating SuFEx Reactions via Aryl Fluorosulfate Structural Engineering for Enhanced Covalent Targeted Cancer Therapy https://covalentmodifiers.blogspot.com/2026/05/accelerating-sufex-reactions-via-aryl.html

Covalent Inhibitors of Monoacylglycerol Lipase Induce Conformational Changes and Proteasomal Degradation https://covalentmodifiers.blogspot.com/2026/05/covalent-inhibitors-of-monoacylglycerol.html

Development and Structural Characterization of UTE-156, a Covalent Inhibitor of the VCP/p97 AAA+ ATPase https://covalentmodifiers.blogspot.com/2026/05/development-and-structural.html

Nitro-Diphenyl Ethers as Emerging Cysteine-Targeting Covalent Warheads Enable Identification of Novel Target LDLRAP1 for Anticoronaviral Activity https://covalentmodifiers.blogspot.com/2026/05/nitro-diphenyl-ethers-as-emerging.html

Shifting the PPARγ conformational ensemble toward a transcriptionally repressive state improves covalent inhibitor efficacy https://covalentmodifiers.blogspot.com/2026/05/shifting-ppar-conformational-ensemble.html

Don’t Lose Your (War)head: Structure–Activity Relationships of Covalent Warheads as Substrates for GST-Catalyzed Glutathione Conjugation https://covalentmodifiers.blogspot.com/2026/05/dont-lose-your-warhead.html

Deciphering covalent kinase inhibitor binding landscape through structural kinome profiling https://covalentmodifiers.blogspot.com/2026/04/deciphering-covalent-kinase-inhibitor.html

Data-driven design of chiral covalent fragments using highthroughput chemoproteomics and machine learning https://covalentmodifiers.blogspot.com/2026/04/data-driven-design-of-chiral-covalent.html

Electrophilic compound screening identifies GPX4-dependent ferroptosis as a senescence vulnerability https://covalentmodifiers.blogspot.com/2026/04/electrophilic-compound-screening.html

A Novel Covalent Inhibitor Fragment for the SARS-CoV-2 Main Protease Identified by Target-Specific Deep Learning https://covalentmodifiers.blogspot.com/2026/05/a-novel-covalent-inhibitor-fragment-for.html

Efficacy and safety of branebrutinib (BMS-986195), an irreversible Bruton's tyrosine kinase inhibitor, for the treatment of rheumatoid arthritis: a phase 2a, randomised, double-blind, placebo-controlled study https://covalentmodifiers.blogspot.com/2026/05/efficacy-and-safety-of-branebrutinib.html

A Fragment Screen Identifies Acrylamide Covalent Inhibitors of the TEAD•YAP Protein-Protein Interaction https://covalentmodifiers.blogspot.com/2026/03/a-fragment-screen-identifies-acrylamide.html

Discovery of Covalent Ligands with AlphaFold3 https://covalentmodifiers.blogspot.com/2026/03/discovery-of-covalent-ligands-with.html

Acrylamide Bioisosterism: Alkenyl Aromatic Heterocycles as Reactivity-Tunable Warheads for Covalent BTK Inhibitors https://covalentmodifiers.blogspot.com/2026/03/acrylamide-bioisosterism-alkenyl.html

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 https://covalentmodifiers.blogspot.com/2026/03/covalent-jak3-inhibitors-based-on-2.html

A Global Ligandability Map of Tryptoline Butynamide Stereoprobes Identifies Covalent Inhibitors of the Actin Maturation Protease ACTMAP https://covalentmodifiers.blogspot.com/2026/03/a-global-ligandability-map-of.html

Development and Structural Characterization of UTE-156, a Covalent Inhibitor of the VCP/p97 AAA+ ATPase https://covalentmodifiers.blogspot.com/2026/03/development-and-structural.html

Discovery and Characterization of Divarasib (GDC-6036), a Potent Covalent Inhibitor of KRAS G12C https://covalentmodifiers.blogspot.com/2026/03/discovery-and-characterization-of.html

A Tandem Bioorthogonal Retro-Cope and Cope Elimination for the Activation of Covalent Inhibitors with an Acrylamide or Vinylsulfonamide Warhead in Live Cells https://covalentmodifiers.blogspot.com/2026/02/a-tandem-bioorthogonal-retro-cope-and.html

Discovery of a Potent, Selective, and In Vivo Efficacious Covalent Inhibitor for Lysine Methyltransferase SETD8 https://covalentmodifiers.blogspot.com/2026/02/discovery-of-potent-selective-and-in.html

Exploiting human fucosyltransferase 8 allostery with a covalent inhibitor for core fucosylation suppression https://covalentmodifiers.blogspot.com/2026/02/exploiting-human-fucosyltransferase-8.html