The Kinase Chemogenomic Set (KCGS): An Open Science Resource for Kinase Vulnerability Identification

Carrow I Wells; Hassan Al-Ali; David M Andrews; Christopher R M Asquith; Alison D Axtman; Ivan Dikic; Daniel Ebner; Peter Ettmayer; Christian Fischer; Mathias Frederiksen; Robert E Futrell; Nathanael S Gray; Stephanie B Hatch; Stefan Knapp; Ulrich Lücking; Michael Michaelides; Caitlin E Mills; Susanne Müller; Dafydd Owen; Alfredo Picado; Kumar S Saikatendu; Martin Schröder; Alexandra Stolz; Mariana Tellechea; Brandon J Turunen; Santiago Vilar; Jinhua Wang; William J Zuercher; Timothy M Willson; David H Drewry

doi:10.3390/ijms22020566

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The Kinase Chemogenomic Set (KCGS): An Open Science Resource for Kinase Vulnerability Identification

Journal article

Open access

Peer reviewed

The Kinase Chemogenomic Set (KCGS): An Open Science Resource for Kinase Vulnerability Identification

Carrow I Wells, Hassan Al-Ali, David M Andrews, Christopher R M Asquith, Alison D Axtman, Ivan Dikic, Daniel Ebner, Peter Ettmayer, Christian Fischer, Mathias Frederiksen, …

International journal of molecular sciences, Vol.22(2), p.566

2021-01-08

DOI: https://doi.org/10.3390/ijms22020566

PMID: 33429995

Abstract

Small Molecule Libraries - chemistry

Protein Kinase Inhibitors - chemistry

Protein Kinase Inhibitors - therapeutic use

Humans

Protein-Serine-Threonine Kinases - antagonists & inhibitors

Small Molecule Libraries - therapeutic use

Protein-Serine-Threonine Kinases - chemistry

Structure-Activity Relationship

Drug Discovery

We describe the assembly and annotation of a chemogenomic set of protein kinase inhibitors as an open science resource for studying kinase biology. The set only includes inhibitors that show potent kinase inhibition and a narrow spectrum of activity when screened across a large panel of kinase biochemical assays. Currently, the set contains 187 inhibitors that cover 215 human kinases. The kinase chemogenomic set (KCGS), current Version 1.0, is the most highly annotated set of selective kinase inhibitors available to researchers for use in cell-based screens.

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Collaboration types: Industry collaboration; Domestic collaboration; International collaboration
Citation topics: 2 Chemistry; 2.123 Protein Stucture, Folding & Modelling; 2.123.13 Protein Folding
Web Of Science research areas: Biochemistry & Molecular Biology; Chemistry, Multidisciplinary
ESI research areas: Chemistry

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Title: The Kinase Chemogenomic Set (KCGS): An Open Science Resource for Kinase Vulnerability Identification
Creators: Carrow I Wells - Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA
Hassan Al-Ali - Truvitech LLC, Miami, FL 33136, USA
David M Andrews - AstraZeneca, Darwin Building, Cambridge Science Park, Cambridge CB4 0WG, UK
Christopher R M Asquith - Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA
Alison D Axtman - Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA
Ivan Dikic - Max Planck Institute of Biophysics, Max-von-Laue-Str. 3, 60438 Frankfurt am Main, Germany
Daniel Ebner - Nuffield Department of Medicine, Target Discovery Institute, University of Oxford, Oxford OX3 7FZ, UK
Peter Ettmayer - Boehringer Ingelheim RCV GmbH & Co KG, 1121 Vienna, Austria
Christian Fischer - MSD, 33 Avenue Louis Pasteur, Boston, MA 02115, USA
Mathias Frederiksen - Novartis Institutes for BioMedical Research, Novartis Campus, 4056 Basel, Switzerland
Robert E Futrell - Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA
Nathanael S Gray - Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02215, USA
Stephanie B Hatch - MRC Oxford Institute for Radiation Oncology, Department of Oncology, University of Oxford, Roosevelt Drive, Oxford OX3 7XB, UK
Stefan Knapp - Institute for Pharmaceutical Chemistry, Johann Wolfgang Goethe-University, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany
Ulrich Lücking - Bayer Pharma AG, Drug Discovery, Müllerstrasse 178, 13353 Berlin, Germany
Michael Michaelides - Oncology Discovery, AbbVie, 1 North Waukegan Road, North Chicago, IL 60064, USA
Caitlin E Mills - Laboratory of Systems Pharmacology, Department of Systems Biology, Harvard Medical School, Boston, MA 02115, USA
Susanne Müller - Institute for Pharmaceutical Chemistry, Johann Wolfgang Goethe-University, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany
Dafydd Owen - Discovery Network Group, Pfizer Medicine Design, Cambridge, MA 02139, USA
Alfredo Picado - Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA
Kumar S Saikatendu - Global Research Externalization, Takeda California, Inc., 9625 Towne Center Drive, San Diego, CA 92121, USA
Martin Schröder - Institute for Pharmaceutical Chemistry, Johann Wolfgang Goethe-University, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany
Alexandra Stolz - Structural Genomics Consortium, Buchmann Institute for Molecular Life Sciences, Goethe University Frankfurt, Max-von-Laue-Straße 15, 60438 Frankfurt am Main, Germany
Mariana Tellechea - Structural Genomics Consortium, Buchmann Institute for Molecular Life Sciences, Goethe University Frankfurt, Max-von-Laue-Straße 15, 60438 Frankfurt am Main, Germany
Brandon J Turunen - GlaxoSmithKline, Chemical Biology, 1250 S Collegeville Rd, Collegeville, PA 19426, USA
Santiago Vilar - Truvitech LLC, Miami, FL 33136, USA
Jinhua Wang - Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02215, USA
William J Zuercher - Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA
Timothy M Willson - Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA
David H Drewry - Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA
Publication Details: International journal of molecular sciences, Vol.22(2), p.566
Publisher: Switzerland
Grant note: 1R44TR001916-02 / NIH HHS 875510 / Innovative Medicines Initiative 1R01CA218442-01 / NIH HHS 1U24DK116204-01 / NIH HHS
Academic Unit: Miller School of Medicine; Miami Project to Cure Paralysis; UMMG Dept of Neurological Surgery
Language: English
Resource Type: Journal article
PMID: 33429995
Record Identifier: 991031578569302976