The Molecular Targets Program (MTP) is an organizational entity within the Center for Cancer Research (CCR) at NCI. The MTP provides the focus and infrastructure to enable CCR tenured and tenure-track Principal Investigators to initiate and pursue interdisciplinary, applied, collaborative, molecularly targeted drug discovery research within a matrix organizational format that is both supportive of and complementary to the traditional NCI/NIH intramural Lab/Branch organization. The MTP mission statement further defines the new organizational model. The initial goal of the MTP is to facilitate the discovery of compounds that may serve as bioprobes for functional genomics, proteomics and molecular target validation research, as well as leads or candidates for drug development. Compounds of interest include not only classical, drug-like organic small-molecules, but also peptides, proteins, nucleic acids, lipids, carbohydrates and other bioactive chemical classes. Future implementation phases of the MTP concept may support preclinical and clinical development of promising new molecularly targeted investigational drugs.