Renal transport is a central mechanism underlying electrolyte homeostasis, acid base balance and other essential functions of the kidneys in human physiology. Thus, knowledge of the anatomy and physiology of the nephron is essential for the understanding of kidney function in health and disease. However, students find this content difficult to comprehend and retain for a number of reasons, including the amount of detailed information regarding the location of transporters throughout the varying regions of the nephron, the location within the membranes (apical vs. basal) of the epithelial cells lining the tubules, the directionality of solute transport resulting in secretion or reabsorption, hormone regulation, and drug targeting. Much of this material lends itself to rote memorization for learning. Incorporation of active learning activities in conjunction with more traditional approaches to teaching in the classroom have proven to be more effective for student learning and retention compared with lecture alone. Active learning methods promote higher-order objectives on Bloom's taxonomy, such as analysis, synthesis, and evaluation. This article introduces an active learning exercise with the objectives of facilitating the learning of: (1) nephron anatomy; (2) transporter secretion and reabsorptive functions; (3) regulation of transporter activity by hormones; (4) the mechanism of action of various therapeutic drugs that target renal transporters directly or indirectly; and (5) the applicability of the content to "real world" clinical scenarios.