In a relatively short time, the pharmaceutical industry has witnessed a rapid integration of the CRISPR technology in multiple areas of research, development, therapy, and diagnostics. A unique feature to this system compared with other technologies is the exceptional versatility in adapting to the broad range of needs across the drug discovery pipeline, such as target identification, cell engineering, and in vivo modeling. As a consequence, the CRISPR toolbox has been evolving to address key questions around preclinical and clinical drug development. In this review, we provide a high-level perspective of how CRISPR has impacted several aspects of the drug discovery workflow and the future ahead for this exciting technology.