2. Academic Validation
  3. The Kinase Chemogenomic Set (KCGS): An Open Science Resource for Kinase Vulnerability Identification

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

  • Int J Mol Sci. 2021 Jan 8;22(2):566. doi: 10.3390/ijms22020566.
Carrow I Wells 1,  Hassan Al-Ali 2 3,  David M Andrews 4,  Christopher R M Asquith 1,  Alison D Axtman 1,  Ivan Dikic 5 6 7,  Daniel Ebner 8,  Peter Ettmayer 9,  Christian Fischer 10,  Mathias Frederiksen 11,  Robert E Futrell 1,  Nathanael S Gray 12 13,  Stephanie B Hatch 14,  Stefan Knapp 6 15 16,  Ulrich Lücking 17,  Michael Michaelides 18,  Caitlin E Mills 19,  Susanne Müller 6 15 16,  Dafydd Owen 20,  Alfredo Picado 1,  Kumar S Saikatendu 21,  Martin Schröder 6 15 16,  Alexandra Stolz 5 6 15,  Mariana Tellechea 5 6 15,  Brandon J Turunen 22,  Santiago Vilar 3,  Jinhua Wang 12 13,  William J Zuercher 1,  Timothy M Willson 1,  David H Drewry 1
Affiliations

Affiliations

  • 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, and Departments of Neurological Surgery and Medicine, University of Miami Miller School of Medicine, Miami, FL 33136, USA.
  • 3 Truvitech LLC, Miami, FL 33136, USA.
  • 4 AstraZeneca, Darwin Building, Cambridge Science Park, Cambridge CB4 0WG, UK.
  • 5 Institute of Biochemistry 2, Faculty of Medicine, Goethe University Frankfurt, Theodor-Stern-Kai 7, 60438 Frankfurt am Main, Germany.
  • 6 Buchmann Institute for Molecular Life Sciences, Goethe University Frankfurt, Max-von-Laue-Str. 15, 60438 Frankfurt am Main, Germany.
  • 7 Max Planck Institute of Biophysics, Max-von-Laue-Str. 3, 60438 Frankfurt am Main, Germany.
  • 8 Nuffield Department of Medicine, Target Discovery Institute, University of Oxford, Oxford OX3 7FZ, UK.
  • 9 Boehringer Ingelheim RCV GmbH & Co KG, 1121 Vienna, Austria.
  • 10 MSD, 33 Avenue Louis Pasteur, Boston, MA 02115, USA.
  • 11 Novartis Institutes for BioMedical Research, Novartis Campus, 4056 Basel, Switzerland.
  • 12 Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA 02115, USA.
  • 13 Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02215, USA.
  • 14 MRC Oxford Institute for Radiation Oncology, Department of Oncology, University of Oxford, Roosevelt Drive, Oxford OX3 7XB, UK.
  • 15 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.
  • 17 Bayer Pharma AG, Drug Discovery, Müllerstrasse 178, 13353 Berlin, Germany.
  • 18 Oncology Discovery, AbbVie, 1 North Waukegan Road, North Chicago, IL 60064, USA.
  • 19 Laboratory of Systems Pharmacology, Department of Systems Biology, Harvard Medical School, Boston, MA 02115, USA.
  • 20 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.
PMID: 33429995 DOI: 10.3390/ijms22020566
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), current Version 1.0, is the most highly annotated set of selective kinase inhibitors available to researchers for use in cell-based screens.

Keywords

KCGS; chemogenomic set; drug discovery; druggable genome; kinase inhibitor; phenotypic screening; protein kinase; small molecules; understudied kinase.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-160691
    AURKC Inhibitor