To medicinal chemists, the true utility of privileged structures is the ability to synthesize one library based upon one core scaffold and screen it against a variety of different receptors, yielding several active compounds. This was illustrated using the benzodiazepine scaffold (Figure 2). After developing the synthetic route for the combinatorial synthesis of a series of 1,4-benzodiazepin-2-ones (7), Bunin et al. synthesized a small library of 192 molecules. Screening these compounds against the cholecystokinin A receptor yielded active compounds.32 Subsequently, a larger library of 1680 1,4-benzodiazepines was synthesized and screened against a number of receptor and enzyme targets. Inhibitors of pp60s-src tyrosine kinase and ligands that block an autoimmune DNA-antibody interaction implicated in systemic lupus erythematosus were identified.33