New technologies such as combinatorial chemistry and automated high- hroughput screening of multiple biological targets have revolutionized the drug discovery process. Additionally the desire to utilize large collections of patient data combined with genetics information will soon drastically change how clinical trials will be performed and assessed. Techniques for analyzing these data are not well defined. For new biological targets it is important to determine which compounds should be screened first and determine the features of small molecules important for biological activity. For clinical trials it is important to determine both clinical and genetic factors that affect both efficacy and safety. Recursive partitioning is a very effective method for summarizing and finding trends in very large data sets. We apply this data mining technique to identify active chemical subclasses during high-throughput screening, defining subpopulations in large patient databases, and untangling complex gene interactions.