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Updated: Sep 11, 2025

Characterization at the Molecular Level using Robust Biochemical Approaches of a New Kinase Protein
Published on: June 30, 2019
High-Quality In Vivo Chemical Probes for Protein Kinases Disclosed in 2024
Ricardo A M Serafim1, Matthias Gehringer2,3,4
1Department of Organic and Pharmaceutical Chemistry, School of Engineering, Institut Químic de Sarrià (IQS), Universitat Ramon Llull (URL), Vía Augusta 390, 08017 Barcelona, Spain.
None:
Protein kinases are highly relevant drug targets, yet a significant fraction of the human kinome remains underexplored. Highly potent and selective small-molecule inhibitors used as chemical probes are invaluable tools for enabling the validation and translation of new kinase targets. This review provides an overview and analysis of the high-quality in vivo chemical probes for protein kinases published and deposited at the Chemical Probes Portal in the year 2024. We discuss the design strategies, molecular mechanism of action, details of their use in vitro and in vivo, as well as their application in target (in)-validation. We also highlight the importance of wisely selecting chemical probes and encourage best practices in using such tool compounds.

