CHAPTER 10. Assays to Characterize the Cellular Pharmacology of a Chemical Probe

Chemical probes are bioactive molecules enabling the examination of protein function in cellular systems. Intended as tool compounds, they bind to a specific protein target, thereby conferring either a loss- or gain-of-function phenotype via a clearly defined mechanism of action. Chemical probes represent an excellent means to identify novel and potentially context-dependent functions of a given gene or protein in living systems. Among the many different bespoke functional cellular assays available to interrogate cellular signalling pathways, this chapter focuses on methods that allow for broad profiling of drugs and chemical probes in cells to uncover perturbations and facilitate further characterization of these phenomena.