High-Quality In Vivo Chemical Probes for Protein Kinases Disclosed in 2024

Ricardo A.M. Serafim; Matthias Gehringer

doi:10.1021/acsptsci.5c00293

High-Quality In Vivo Chemical Probes for Protein Kinases Disclosed in 2024

Ricardo A.M. Serafim^*
, Matthias Gehringer^*

^*Corresponding author for this work

Research output: Indexed journal article › Review › peer-review

1 Citation (Scopus)

Abstract

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.

Original language	English
Pages (from-to)	2401-2414
Number of pages	14
Journal	ACS Pharmacology and Translational Science
Volume	8
Issue number	8
Early online date	17 Jul 2025
DOIs	https://doi.org/10.1021/acsptsci.5c00293
Publication status	Published - 8 Aug 2025

Keywords

chemical probes
drug discovery
protein kinase inhibitors
target validation
understudied kinome

Access to Document

10.1021/acsptsci.5c00293Licence: CC BY

Cite this

@article{766f396b3c8942a7b3d769467792f241,

title = "High-Quality In Vivo Chemical Probes for Protein Kinases Disclosed in 2024",

abstract = "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.",

keywords = "chemical probes, drug discovery, protein kinase inhibitors, target validation, understudied kinome",

author = "Serafim, \{Ricardo A.M.\} and Matthias Gehringer",

note = "Publisher Copyright: {\textcopyright} 2025 The Authors. Published by American Chemical Society. https://creativecommons.org/licenses/by/4.0/",

year = "2025",

month = aug,

day = "8",

doi = "10.1021/acsptsci.5c00293",

language = "English",

volume = "8",

pages = "2401--2414",

journal = "ACS Pharmacology and Translational Science",

issn = "2575-9108",

publisher = "American Chemical Society",

number = "8",

}

TY - JOUR

T1 - High-Quality In Vivo Chemical Probes for Protein Kinases Disclosed in 2024

AU - Serafim, Ricardo A.M.

AU - Gehringer, Matthias

PY - 2025/8/8

Y1 - 2025/8/8

N2 - 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.

AB - 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.

KW - chemical probes

KW - drug discovery

KW - protein kinase inhibitors

KW - target validation

KW - understudied kinome

UR - https://www.scopus.com/pages/publications/105013497675

UR - https://www.webofscience.com/api/gateway?GWVersion=2&SrcApp=pure_univeritat_ramon_llull&SrcAuth=WosAPI&KeyUT=WOS:001530842200001&DestLinkType=FullRecord&DestApp=WOS_CPL

UR - http://hdl.handle.net/20.500.14342/5518

U2 - 10.1021/acsptsci.5c00293

DO - 10.1021/acsptsci.5c00293

M3 - Review

C2 - 40810168

AN - SCOPUS:105013497675

SN - 2575-9108

VL - 8

SP - 2401

EP - 2414

JO - ACS Pharmacology and Translational Science

JF - ACS Pharmacology and Translational Science

IS - 8

ER -

High-Quality In Vivo Chemical Probes for Protein Kinases Disclosed in 2024

Abstract

Keywords

Access to Document

Other files and links

Fingerprint

Cite this