The Chemical Probes Portal: an expert review-based public resource to empower chemical probe assessment, selection and use

Author:

Antolin Albert A123ORCID,Sanfelice Domenico123ORCID,Crisp Alisa123,Villasclaras Fernandez Eloy123,Mica Ioan L123,Chen Yi123,Collins Ian143,Edwards Aled53,Müller Susanne673ORCID,Al-Lazikani Bissan83ORCID,Workman Paul143ORCID

Affiliation:

1. Division of Cancer Therapeutics, The Institute of Cancer Research , London , SM2 5NG , UK

2. Department of Data Science, The Institute of Cancer Research , London , SM2 5NG , UK

3. Chemical Probes Portal , www.chemicalprobes.org

4. Centre for Cancer Drug Discovery, The Institute of Cancer Research , London , SM2 5NG , UK

5. Structural Genomics Consortium, University of Toronto , Toronto , ON M5G 1L7 , Canada

6. Institute of Pharmaceutical Chemistry, Goethe University Frankfurt , Frankfurt , 60438, Germany

7. Structural Genomics Consortium, BMLS, Goethe University Frankfurt , Frankfurt , 60438 , Germany

8. Department of Genomics Medicine and the Institute of Data Science in Oncology, MD Anderson Cancer Center , Houston , TX , 77054 , USA

Abstract

Abstract We describe the Chemical Probes Portal (https://www.chemicalprobes.org/), an expert review-based public resource to empower chemical probe assessment, selection and use. Chemical probes are high-quality small-molecule reagents, often inhibitors, that are important for exploring protein function and biological mechanisms, and for validating targets for drug discovery. The publication, dissemination and use of chemical probes provide an important means to accelerate the functional annotation of proteins, the study of proteins in cell biology, physiology, and disease pathology, and to inform and enable subsequent pioneering drug discovery and development efforts. However, the widespread use of small-molecule compounds that are claimed as chemical probes but are lacking sufficient quality, especially being inadequately selective for the desired target or even broadly promiscuous in behaviour, has resulted in many erroneous conclusions in the biomedical literature. The Chemical Probes Portal was established as a public resource to aid the selection and best-practice use of chemical probes in basic and translational biomedical research. We describe the background, principles and content of the Portal and its technical development, as well as examples of its applications and use. The Chemical Probes Portal is a community resource and we therefore describe how researchers can be involved in its content and development.

Funder

Wellcome

The Structural Genomics Consortium

UNC Eshelman School of Pharmacy and Cancer Research UK

Institute of Cancer Research

Cancer Prevention and Research Institute of Texas

Ontario Genomics Institute

Janssen

Merck KGaA

Pfizer

Takeda

German Cancer Research Center

Frankfurt Cancer Institute

European Union's Horizon 2020

Ontario Institute for Cancer Research

Chordoma Foundation

Mark Foundation

Wellcome Trust Sir Henry Wellcome Postdoctoral Fellowship

Publisher

Oxford University Press (OUP)

Subject

Genetics

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