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Updated: May 5, 2026

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays
Published on: October 23, 2019
Seeding collaborations to advance kinase science with the GSK Published Kinase Inhibitor Set (PKIS)
David H Drewry, Timothy M Willson, William J Zuercher1
1Department of Chemical Biology, GlaxoSmithKline, 20 T. W. Alexander Drive, STF 209.3, Research Triangle Park, North Carolina, 27709, USA. william.j.zuercher@gsk.com.
Abstract:
To catalyze research on historically untargeted protein kinases, we created the PKIS, an annotated set of 367 small molecule kinase inhibitors. The set has been widely distributed to academic collaborators as an open access tool. It has been used to identify chemical starting points for development of chemical probes for orphan kinases and to investigate kinase signaling in high content phenotypic assays. Access to the set comes with few restrictions other than the requirement that assay results be released into the public domain for the benefit of the entire research community. Examples from the efforts of several collaborators are summarized.
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