Charles River’s unique Retrogenix Cell Microarray Technology identifies primary and secondary (off-target) interactions against human cell surface and secreted proteins with a high degree of accuracy, specificity, and sensitivity. Test articles are profiled against the world’s largest and most high-quality library of human proteins, each expressed in the context of human cells to maximise physiological relevance. Data generated on the platform can be used to identify and confirm new drug targets and receptor interactions, inform and de-risk lead selection by filtering out polyreactive candidates, and provide IND-enabling data for regulatory submissions. This tutorial will provide an overview of the Retrogenix Cell Microarray Platform, optimization to profile different modalities (such as mono- and multi-specific antibodies, proteins, small molecules, and CAR T cells), how the technology has been used by industry partners to simplify, accelerate and de-risk drug discovery and development programs, and how cell microarray data can be used in conjunction with other Charles River technologies. Future developments and technology advancements will also be discussed.