CHAPTER 10: Drugging the Kinome

Kinases are perhaps the most successfully drugged target families of the 21st century, with 35 FDA approved medicines. These drugs only target a very small percentage of the human kinome. Tools that allow exploration of the rest of the kinome will no doubt lead to the identification of new validated kinase drug targets and new approved medicines. In this chapter we describe the progress towards drugging the kinome by talking about 4 groups of kinases: kinases currently targeted by FDA approved drugs, kinases targeted by potent and selective chemical probes, kinases for which there are narrow spectrum inhibitors available (“covered” kinases), and then the remaining kinases for which there are currently no narrow spectrum inhibitors available (“uncovered” kinases). We believe that the scientific community has the motivation, opportunity, and ability to parlay the collective experience and wealth of kinase data available into a set of molecules that cover the entire kinome and can be used to identify the next generation of important therapeutic kinase targets.