4.7 Article

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

期刊

出版社

MDPI
DOI: 10.3390/ijms22020566

关键词

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

资金

  1. AbbVie
  2. Bayer Pharma AG
  3. Boehringer Ingelheim
  4. Canada Foundation for Innovation
  5. Eshelman Institute for Innovation
  6. Genentech
  7. Genome Canada through Ontario Genomics Institute [OGI-196]
  8. EU/EFPIA/OICR/McGill/KTH/Diamond Innovative Medicines Initiative 2 Joint Undertaking (EUbOPEN) [875510]
  9. Janssen
  10. Merck KGaA
  11. Merck Sharp and Dohme
  12. Novartis Pharma AG
  13. Pfizer
  14. Sao Paulo Research Foundation-FAPESP
  15. Takeda
  16. Wellcome Trust
  17. UNC Lineberger Comprehensive Cancer Center
  18. National Institutes of Health [1R44TR001916-02, 1R01CA218442-01, 1U24DK116204-01]
  19. Foundation for Food and Agriculture Research (FFAR) [A18-2129-S001]
  20. DFG, German Reaseach Foundation [2591307 SFB1177]
  21. PharmAlliance

向作者/读者索取更多资源

The chemogenomic set of protein kinase inhibitors described in this study is a valuable open science resource for studying kinase biology, consisting of 187 inhibitors that target 215 human kinases. It is highly annotated and selective, making it a useful tool for researchers in cell-based screens.
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.

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