The Clinical Kinase Index: Prioritizing Understudied Kinases at Targets for the Treatment of Cancer

Figure 1 Overview of Kinase TDLs (A) There are 634 kinases annotated on Pharos. In total, 8.2% are considered Tclin, and 151 of 634 are considered “understudied”; these represent kinases that bear Tdark, Tbio, and Tchem annotations. (B) Certain groups of kinases are historically understudied. The CMGC group, CAMK group, and “other” group kinases are enriched for understudied kinases, while TKs have been extensively explored.

The Clinical Kinase Index: Prioritizing Understudied Kinases at Targets…

Abstract  The approval of the first kinase inhibitor, Gleevec, ushered in a paradigm shift for oncological treatment-the use of genomic data for targeted, efficacious therapies. Since then, over 48 additional small-molecule kinase inhibitors have been approved, solidifying the case for kinases as a highly druggable and attractive target class. Despite the role deregulated kinase activity plays in cancer, only 8% of the kinome has been effectively “drugged.” Moreover, 24% of the 634 human kinases are understudied. We have developed a comprehensive scoring system that utilizes differential gene expression, pathological parameters, overall survival, and mutational hotspot analysis to rank and prioritize clinically relevant kinases across 17 solid tumor cancers from The Cancer Genome Atlas. We have developed the clinical kinase index (CKI) app ( to facilitate interactive analysis of all kinases in each cancer. Collectively, we report that understudied kinases have potential clinical value as biomarkers or drug targets that warrant further study.


Essegian D, Khurana R, Stathias V, Schürer SC. The Clinical Kinase Index: A Method to Prioritize Understudied Kinases as Drug Targets for the Treatment of Cancer. Cell Rep Med. 2020 Oct 20;1(7):100128. doi: 10.1016/j.xcrm.2020.100128. PMID: 33205077; PMCID: PMC7659504.