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The Kinase Chemogenomic Set (KCGS): An open science resource for kinase vulnerability identification

View ORCID ProfileCarrow I. Wells, View ORCID ProfileHassan Al-Ali, View ORCID ProfileDavid M. Andrews, View ORCID ProfileChristopher R. M. Asquith, View ORCID ProfileAlison D. Axtman, Mirra Chung, View ORCID ProfileIvan Dikic, View ORCID ProfileDaniel Ebner, View ORCID ProfileJonathan M. Elkins, View ORCID ProfilePeter Ettmayer, Christian Fischer, View ORCID ProfileMathias Frederiksen, View ORCID ProfileNathanael S. Gray, Stephanie Hatch, View ORCID ProfileStefan Knapp, Shudong Lee, View ORCID ProfileUlrich Lücking, Michael Michaelides, Caitlin E. Mills, View ORCID ProfileSusanne Müller, View ORCID ProfileDafydd Owen, View ORCID ProfileAlfredo Picado, View ORCID ProfileKristijan Ramadan, Kumar S. Saikatendu, Martin Schröder, Alexandra Stolz, Mariana Tellechea, Daniel K. Treiber, Brandon J. Turunen, Santiago Vilar, Jinhua Wang, View ORCID ProfileWilliam J. Zuercher, View ORCID ProfileTimothy M. Willson, View ORCID ProfileDavid H. Drewry
doi: https://doi.org/10.1101/2019.12.22.886523
Carrow I. Wells
1Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina, USA
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Hassan Al-Ali
2The Miami Project to Cure Paralysis, Peggy and Harold Katz Family Drug Discovery Center, Sylvester Comprehensive Cancer Center, and Departments of Neurological Surgery and Medicine, University of Miami Miller School of Medicine, Miami, Florida, USA
3Truvitech LLC, Miami, Florida, USA
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David M. Andrews
4AstraZeneca, Darwin Building, Cambridge Science Park, Cambridge, UK
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Christopher R. M. Asquith
1Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina, USA
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Alison D. Axtman
1Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina, USA
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Mirra Chung
5Laboratory of Systems Pharmacology, Department of Systems Biology, Harvard Medical School, Boston, Massachusetts, USA
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Ivan Dikic
6Institute of Biochemistry II, Faculty of Medicine, Goethe University Frankfurt, Theodor-Stern-Kai 7, 60590 Frankfurt am Main, Germany
7Buchmann Institute for Molecular Life Sciences, Goethe University Frankfurt, Max-von-Laue-Str. 15, 60438 Frankfurt am Main, Germany
8Max Planck Institute of Biophysics, Max-von-Laue-Str. 3, 60438 Frankfurt am Main, Germany
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Daniel Ebner
9Nuffield Department of Medicine, Target Discovery Institute, University of Oxford, Oxford, UK
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Jonathan M. Elkins
10Structural Genomics Consortium, University of Oxford, Old Road Campus Research Building, Roosevelt Drive, Oxford, UK
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Peter Ettmayer
11Boehringer Ingelheim RCV GmbH & Co KG, Vienna, Austria
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Christian Fischer
12MSD, 33 Avenue Louis Pasteur, Boston, Massachusetts, USA
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Mathias Frederiksen
13Novartis Institutes for BioMedical Research, Novartis Campus, Basel, Switzerland
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Nathanael S. Gray
14Harvard Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, Massachusetts, USA
15Department of Cancer Biology, Dana−Farber Cancer Institute, Boston, Massachusetts, USA
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Stephanie Hatch
16MRC Oxford Institute for Radiation Oncology, Department of Oncology, University of Oxford, Roosevelt Drive, Oxford, UK
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Stefan Knapp
17Structural Genomics Consortium, Buchmann Institute for Molecular Life Sciences, and Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Straße 15, Frankfurt am Main, Germany
18Institute for Pharmaceutical Chemistry, Johann Wolfgang Goethe-University, Max-von-Laue-Str. 9, D-60438 Frankfurt am Main, Germany
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Shudong Lee
16MRC Oxford Institute for Radiation Oncology, Department of Oncology, University of Oxford, Roosevelt Drive, Oxford, UK
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Ulrich Lücking
19Bayer Pharma AG, Drug Discovery, Müllerstrasse 178, Berlin, Germany
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Michael Michaelides
20Oncology Discovery, AbbVie, 1 North Waukegan Road, North Chicago, Illinois, USA
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Caitlin E. Mills
5Laboratory of Systems Pharmacology, Department of Systems Biology, Harvard Medical School, Boston, Massachusetts, USA
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Susanne Müller
17Structural Genomics Consortium, Buchmann Institute for Molecular Life Sciences, and Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Straße 15, Frankfurt am Main, Germany
18Institute for Pharmaceutical Chemistry, Johann Wolfgang Goethe-University, Max-von-Laue-Str. 9, D-60438 Frankfurt am Main, Germany
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Dafydd Owen
21Discovery Network Group, Pfizer Medicine Design, Cambridge, Massachusetts, USA
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Alfredo Picado
1Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina, USA
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Kristijan Ramadan
16MRC Oxford Institute for Radiation Oncology, Department of Oncology, University of Oxford, Roosevelt Drive, Oxford, UK
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Kumar S. Saikatendu
22Global Research Externalization, Takeda California, Inc., 9625 Towne Center Drive, San Diego, California, USA
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Martin Schröder
17Structural Genomics Consortium, Buchmann Institute for Molecular Life Sciences, and Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Straße 15, Frankfurt am Main, Germany
18Institute for Pharmaceutical Chemistry, Johann Wolfgang Goethe-University, Max-von-Laue-Str. 9, D-60438 Frankfurt am Main, Germany
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Alexandra Stolz
6Institute of Biochemistry II, Faculty of Medicine, Goethe University Frankfurt, Theodor-Stern-Kai 7, 60590 Frankfurt am Main, Germany
7Buchmann Institute for Molecular Life Sciences, Goethe University Frankfurt, Max-von-Laue-Str. 15, 60438 Frankfurt am Main, Germany
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Mariana Tellechea
6Institute of Biochemistry II, Faculty of Medicine, Goethe University Frankfurt, Theodor-Stern-Kai 7, 60590 Frankfurt am Main, Germany
7Buchmann Institute for Molecular Life Sciences, Goethe University Frankfurt, Max-von-Laue-Str. 15, 60438 Frankfurt am Main, Germany
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Daniel K. Treiber
23Eurofins DiscoverX Corporation, 42501 Albrae Street, Fremont, California, USA
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Brandon J. Turunen
24GlaxoSmithKline, Chemical Biology, 1250 S Collegeville Rd, Collegeville, Pennsylvania, USA
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Santiago Vilar
3Truvitech LLC, Miami, Florida, USA
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Jinhua Wang
14Harvard Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, Massachusetts, USA
15Department of Cancer Biology, Dana−Farber Cancer Institute, Boston, Massachusetts, USA
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William J. Zuercher
1Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina, USA
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Timothy M. Willson
1Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina, USA
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David H. Drewry
1Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina, USA
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  • For correspondence: david.drewry@unc.edu
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Abstract

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) is the most highly annotated set of selective kinase inhibitors available to researchers for use in cell-based screens.

Footnotes

  • http://www.randomactsofkinase.org/

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The copyright holder for this preprint is the author/funder, who has granted bioRxiv a license to display the preprint in perpetuity. It is made available under a CC-BY-NC-ND 4.0 International license.
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Posted December 23, 2019.
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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, Mirra Chung, Ivan Dikic, Daniel Ebner, Jonathan M. Elkins, Peter Ettmayer, Christian Fischer, Mathias Frederiksen, Nathanael S. Gray, Stephanie Hatch, Stefan Knapp, Shudong Lee, Ulrich Lücking, Michael Michaelides, Caitlin E. Mills, Susanne Müller, Dafydd Owen, Alfredo Picado, Kristijan Ramadan, Kumar S. Saikatendu, Martin Schröder, Alexandra Stolz, Mariana Tellechea, Daniel K. Treiber, Brandon J. Turunen, Santiago Vilar, Jinhua Wang, William J. Zuercher, Timothy M. Willson, David H. Drewry
bioRxiv 2019.12.22.886523; doi: https://doi.org/10.1101/2019.12.22.886523
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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, Mirra Chung, Ivan Dikic, Daniel Ebner, Jonathan M. Elkins, Peter Ettmayer, Christian Fischer, Mathias Frederiksen, Nathanael S. Gray, Stephanie Hatch, Stefan Knapp, Shudong Lee, Ulrich Lücking, Michael Michaelides, Caitlin E. Mills, Susanne Müller, Dafydd Owen, Alfredo Picado, Kristijan Ramadan, Kumar S. Saikatendu, Martin Schröder, Alexandra Stolz, Mariana Tellechea, Daniel K. Treiber, Brandon J. Turunen, Santiago Vilar, Jinhua Wang, William J. Zuercher, Timothy M. Willson, David H. Drewry
bioRxiv 2019.12.22.886523; doi: https://doi.org/10.1101/2019.12.22.886523

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