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.


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.

MeSH terms

  • Drug Discovery*
  • Humans
  • Protein Kinase Inhibitors / chemistry*
  • Protein Kinase Inhibitors / therapeutic use
  • Protein Serine-Threonine Kinases / antagonists & inhibitors
  • Protein Serine-Threonine Kinases / chemistry*
  • Small Molecule Libraries / chemistry*
  • Small Molecule Libraries / therapeutic use
  • Structure-Activity Relationship


  • Protein Kinase Inhibitors
  • Small Molecule Libraries
  • Protein Serine-Threonine Kinases