#FocusOnCovalentDrugs was a great meeting with talks covering diverse aspects of targeted covalent inhibitor discovery ranging from warhead development and #chemoproteomics to very advanced PK/PD topics. Thank you so much to the organizers for inviting me and to everyone for the fruitful discussions

Inspiring talk by Matthias Gehringer at #FocusOnCovalentDrugs. He gave an insightful overview of covalent warheads that are described in the literature for various amino acids and applications. A very balanced discussion of the respective advantages and challenges.
pubs.acs.org/doi/10.1021/...

Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal Chemistry and Chemical Biology Targeted covalent inhibitors (TCIs) are designed to bind poorly conserved amino acids by means of reactive groups, the so-called warheads. Currently, targeting noncatalytic cysteine residues with acrylamides and other α,β-unsaturated carbonyl compounds is the predominant strategy in TCI development. The recent ascent of covalent drugs has stimulated considerable efforts to characterize alternative warheads for the covalent-reversible and irreversible engagement of noncatalytic cysteine residues as well as other amino acids. This Perspective article provides an overview of warheads—beyond α,β-unsaturated amides—recently used in the design of targeted covalent ligands. Promising reactive groups that have not yet demonstrated their utility in TCI development are also highlighted. Special emphasis is placed on the discussion of reactivity and of case studies illustrating applications in medicinal chemistry and chemical biology.

Fanboy moment for me today at #FocusOnCovalentDrugs. Hearing Matthias Gehringer present for the first time. His reviews on covalent warheads are a must-read in my group for many years now.

#ChemSky #ChemBio #DrugDiscovery #covalent

pubs.acs.org/doi/10.1021/...
pubs.acs.org/doi/10.1021/...

Amazing talk by Sebastian Essig at #FocusOnCovalentDrugs. He talked about covalent drug discovery with a focus on characterizing novel warheads. Great insights into library design, reactivity profiling and #chemoproteomics for global analysis of selectivity.

It was great to be able to present some of our work at #FocusOnCovalentDrugs. I talked about our work on cysteine profiling (onlinelibrary.wiley.com/doi/full/10....), the profiling of diverse electrophiles (chemrxiv.org/engage/chemr...) as well as some very new unpublished data.

A great talk by Joel Rüegger of the group of @mvdstelt.bsky.social at #FocusOnCovalentDrugs. He talked about his amazing work in the @led3hub.bsky.social on the CellEKT platform for profiling target engagement of kinase inhibitors in living cells. (1/5) www.mcponline.org/article/S153...

#FocusOnCovalentDrugs is off to a great start with an inspiring talk by Marcus Bantscheff. He talked about the various #chemoproteomics technologies that his group is applying to better understand the targets of small molecule drugs. Interesting insights into #ABPP and #TPP. (1/2)
#chemsky #ChemBio

Matthias Wittwer and Sherri Dudal open the DMDG meeting #FocusOnCovalentDrugs. Very much looking forward to a full day of exciting science. Thank you so much to the organizers for putting together an amazing program and inviting me to present. www.dmdg.org/events/20250...

Excited to be at the meeting "Focusing on Targeted Covalent Drugs" #FocusOnCovalentDrugs by the DMDG. Looking forward to engaging with the many TCI aficionados as well as discussing our science and TCI development in the pharmaceutical industry.
#chemsky #ChemBio
www.dmdg.org/events/20250...