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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
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
David M. Andrews
4AstraZeneca, Darwin Building, Cambridge Science Park, Cambridge, UK
Christopher R. M. Asquith
1Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina, USA
Alison D. Axtman
1Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina, USA
Mirra Chung
5Laboratory of Systems Pharmacology, Department of Systems Biology, Harvard Medical School, Boston, Massachusetts, USA
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
Daniel Ebner
9Nuffield Department of Medicine, Target Discovery Institute, University of Oxford, Oxford, UK
Jonathan M. Elkins
10Structural Genomics Consortium, University of Oxford, Old Road Campus Research Building, Roosevelt Drive, Oxford, UK
Peter Ettmayer
11Boehringer Ingelheim RCV GmbH & Co KG, Vienna, Austria
Christian Fischer
12MSD, 33 Avenue Louis Pasteur, Boston, Massachusetts, USA
Mathias Frederiksen
13Novartis Institutes for BioMedical Research, Novartis Campus, Basel, Switzerland
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
Stephanie Hatch
16MRC Oxford Institute for Radiation Oncology, Department of Oncology, University of Oxford, Roosevelt Drive, Oxford, UK
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
Shudong Lee
16MRC Oxford Institute for Radiation Oncology, Department of Oncology, University of Oxford, Roosevelt Drive, Oxford, UK
Ulrich Lücking
19Bayer Pharma AG, Drug Discovery, Müllerstrasse 178, Berlin, Germany
Michael Michaelides
20Oncology Discovery, AbbVie, 1 North Waukegan Road, North Chicago, Illinois, USA
Caitlin E. Mills
5Laboratory of Systems Pharmacology, Department of Systems Biology, Harvard Medical School, Boston, Massachusetts, USA
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
Dafydd Owen
21Discovery Network Group, Pfizer Medicine Design, Cambridge, Massachusetts, USA
Alfredo Picado
1Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina, USA
Kristijan Ramadan
16MRC Oxford Institute for Radiation Oncology, Department of Oncology, University of Oxford, Roosevelt Drive, Oxford, UK
Kumar S. Saikatendu
22Global Research Externalization, Takeda California, Inc., 9625 Towne Center Drive, San Diego, California, USA
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
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
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
Daniel K. Treiber
23Eurofins DiscoverX Corporation, 42501 Albrae Street, Fremont, California, USA
Brandon J. Turunen
24GlaxoSmithKline, Chemical Biology, 1250 S Collegeville Rd, Collegeville, Pennsylvania, USA
Santiago Vilar
3Truvitech LLC, Miami, Florida, USA
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
William J. Zuercher
1Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina, USA
Timothy M. Willson
1Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina, USA
David H. Drewry
1Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina, USA
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
Copyright
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.
Posted December 23, 2019.
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
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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