PT  - JOURNAL ARTICLE
AU  - David H. Drewry
AU  - Carrow I. Wells
AU  - David M. Andrews
AU  - Richard Angell
AU  - Hassan Al-Ali
AU  - Alison D. Axtman
AU  - Stephen J. Capuzzi
AU  - Jonathan M. Elkins
AU  - Peter Ettmayer
AU  - Mathias Frederiksen
AU  - Opher Gileadi
AU  - Nathanael Gray
AU  - Alice Hooper
AU  - Stefan Knapp
AU  - Stefan Laufer
AU  - Ulrich Luecking
AU  - Susanne Müller
AU  - Eugene Muratov
AU  - R. Aldrin Denny
AU  - Kumar S. Saikatendu
AU  - Daniel K. Treiber
AU  - William J. Zuercher
AU  - Timothy M. Willson
TI  - Progress Towards a Public Chemogenomic Set for Protein Kinases and a Call for Contributions
AID  - 10.1101/104711
DP  - 2017 Jan 01
TA  - bioRxiv
PG  - 104711
4099  - http://biorxiv.org/content/early/2017/01/31/104711.short
4100  - http://biorxiv.org/content/early/2017/01/31/104711.full
AB  - Protein kinases are highly tractable targets for drug discovery. However, the biological function and therapeutic potential of the majority of the 500+ human protein kinases remains unknown. We have developed physical and virtual collections of small molecule inhibitors, which we call chemogenomic sets, that are designed to inhibit the catalytic function of almost half the human protein kinases. In this manuscript we share our progress towards generation of a comprehensive kinase chemogenomic set (KCGS), release kinome profiling data of a large inhibitor set (Published Kinase Inhibitor Set 2 (PKIS2)), and outline a process through which the community can openly collaborate to create a KCGS that probes the full complement of human protein kinases.