An approach for incorporating preliminary drug discovery research into a biochemistry laboratory is described. During a total of 42 hr (one 3-hr laboratory section a week for 14 weeks), students were exposed to bioinformatics; molecular cloning; protein expression, purification, and characterization; and enzymatic kinetic assays. This research-oriented laboratory not only includes the standard elements of common undergraduate biochemistry laboratory manuals but also emphasizes the logical connections among biochemistry laboratory techniques. Moreover, this approach exposed students to laboratory research and the concept of drug discovery.