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 PicadoKumar S. Saikatendu, Martin Schröder, Alexandra Stolz, Mariana Tellechea, Brandon J. Turunen, Santiago Vilar, Jinhua Wang, William J. Zuercher, Timothy M. Willson, David H. Drewry

Research output: Contribution to journalArticlepeer-review

1 Scopus citations

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.

Original languageEnglish (US)
Article number566
Pages (from-to)1-18
Number of pages18
JournalInternational journal of molecular sciences
Volume22
Issue number2
DOIs
StatePublished - Jan 2 2021

Keywords

  • Chemogenomic set
  • Drug discovery
  • Druggable genome
  • KCGS
  • Kinase inhibitor
  • Phenotypic screening
  • Protein kinase
  • Small molecules
  • Understudied kinase

ASJC Scopus subject areas

  • Catalysis
  • Molecular Biology
  • Spectroscopy
  • Computer Science Applications
  • Physical and Theoretical Chemistry
  • Organic Chemistry
  • Inorganic Chemistry

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