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Article

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

1
Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA
2
The Miami Project to Cure Paralysis, Peggy and Harold Katz Family Drug Discovery Center, Sylvester Comprehensive Cancer Center, Departments of Neurological Surgery and Medicine, University of Miami Miller School of Medicine, Miami, FL 33136, USA
3
Truvitech LLC, Miami, FL 33136, USA
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AstraZeneca, Darwin Building, Cambridge Science Park, Cambridge CB4 0WG, UK
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Institute of Biochemistry 2, Faculty of Medicine, Goethe University Frankfurt, Theodor-Stern-Kai 7, 60438 Frankfurt am Main, Germany
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Buchmann Institute for Molecular Life Sciences, Goethe University Frankfurt, Max-von-Laue-Str. 15, 60438 Frankfurt am Main, Germany
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Max Planck Institute of Biophysics, Max-von-Laue-Str. 3, 60438 Frankfurt am Main, Germany
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Nuffield Department of Medicine, Target Discovery Institute, University of Oxford, Oxford OX3 7FZ, UK
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Boehringer Ingelheim RCV GmbH & Co KG, 1121 Vienna, Austria
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MSD, 33 Avenue Louis Pasteur, Boston, MA 02115, USA
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Novartis Institutes for BioMedical Research, Novartis Campus, 4056 Basel, Switzerland
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Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA 02115, USA
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Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02215, USA
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MRC Oxford Institute for Radiation Oncology, Department of Oncology, University of Oxford, Roosevelt Drive, Oxford OX3 7XB, UK
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Structural Genomics Consortium, Buchmann Institute for Molecular Life Sciences, Goethe University Frankfurt, Max-von-Laue-Straße 15, 60438 Frankfurt am Main, Germany
16
Institute for Pharmaceutical Chemistry, Johann Wolfgang Goethe-University, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany
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Bayer Pharma AG, Drug Discovery, Müllerstrasse 178, 13353 Berlin, Germany
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Oncology Discovery, AbbVie, 1 North Waukegan Road, North Chicago, IL 60064, USA
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Laboratory of Systems Pharmacology, Department of Systems Biology, Harvard Medical School, Boston, MA 02115, USA
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Discovery Network Group, Pfizer Medicine Design, Cambridge, MA 02139, USA
21
Global Research Externalization, Takeda California, Inc., 9625 Towne Center Drive, San Diego, CA 92121, USA
22
GlaxoSmithKline, Chemical Biology, 1250 S Collegeville Rd, Collegeville, PA 19426, USA
*
Author to whom correspondence should be addressed.
Int. J. Mol. Sci. 2021, 22(2), 566; https://doi.org/10.3390/ijms22020566
Received: 8 December 2020 / Accepted: 29 December 2020 / Published: 8 January 2021
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. View Full-Text
Keywords: protein kinase; kinase inhibitor; chemogenomic set; phenotypic screening; small molecules; KCGS; drug discovery; druggable genome; understudied kinase protein kinase; kinase inhibitor; chemogenomic set; phenotypic screening; small molecules; KCGS; drug discovery; druggable genome; understudied kinase
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Figure 1

MDPI and ACS Style

Wells, C.I.; Al-Ali, H.; Andrews, D.M.; Asquith, C.R.M.; Axtman, A.D.; Dikic, I.; Ebner, D.; Ettmayer, P.; Fischer, C.; Frederiksen, M.; Futrell, R.E.; Gray, N.S.; Hatch, S.B.; Knapp, S.; Lücking, U.; Michaelides, M.; Mills, C.E.; Müller, S.; Owen, D.; Picado, A.; Saikatendu, K.S.; Schröder, M.; Stolz, A.; Tellechea, M.; Turunen, B.J.; Vilar, S.; Wang, J.; Zuercher, W.J.; Willson, T.M.; Drewry, D.H. The Kinase Chemogenomic Set (KCGS): An Open Science Resource for Kinase Vulnerability Identification. Int. J. Mol. Sci. 2021, 22, 566. https://doi.org/10.3390/ijms22020566

AMA Style

Wells CI, Al-Ali H, Andrews DM, Asquith CRM, Axtman AD, Dikic I, Ebner D, Ettmayer P, Fischer C, Frederiksen M, Futrell RE, Gray NS, Hatch SB, Knapp S, Lücking U, Michaelides M, Mills CE, Müller S, Owen D, Picado A, Saikatendu KS, Schröder M, Stolz A, Tellechea M, Turunen BJ, Vilar S, Wang J, Zuercher WJ, Willson TM, Drewry DH. The Kinase Chemogenomic Set (KCGS): An Open Science Resource for Kinase Vulnerability Identification. International Journal of Molecular Sciences. 2021; 22(2):566. https://doi.org/10.3390/ijms22020566

Chicago/Turabian Style

Wells, Carrow I., 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, and David H. Drewry. 2021. "The Kinase Chemogenomic Set (KCGS): An Open Science Resource for Kinase Vulnerability Identification" International Journal of Molecular Sciences 22, no. 2: 566. https://doi.org/10.3390/ijms22020566

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