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Progress towards a public chemogenomic set for protein kinases and a call for contributions

Frederiksen, Mathias and Drewry, David and Wells, Carrow and Andrews, David and Angell, Richard and Al-Ali, Hassan and Axtman, Alison and Capuzzi, Stephen and Elkins, Jonathan and Ettmayer, Peter and Gileadi, Opher and Gray, Nathanael and Hooper, Alice and Knapp, Stefan and Laufer, Stefan and Luecking, Ulrich and Michaelides, Michael and Mueller-Knapp, Susanne and Muratov, Eugene and Denny, Aldrin and Robers, Matt and Saikatendu, Kumar and Trieber, Daniel and Zuercher, William and Willson, Timothy (2017) Progress towards a public chemogenomic set for protein kinases and a call for contributions. PLoS ONE, 12 (8). ISSN 19326203


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.

Item Type: Article
Date Deposited: 19 Dec 2017 00:45
Last Modified: 25 Jan 2019 00:45


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