Chapter 1. Drugs and their Structural Motifs
Alexander A. Alex, Richard Storer · RSC drug discovery/RSC drug discovery series · 2010
The major focus of the research-based pharmaceutical industry is the discovery of safe, efficacious, new chemical entities (NCEs) for therapeutic targets. The pharmaceutical industry can look back at a history of successful innovations, indicated by the fact that there are currently just over 1,400 unique drugs on the market. This chapter starts with an introduction on the pharmaceutical industry in general, past achievements as well as current challenges, particularly focusing on recent developments in terms of productivity which affect the introduction of new drugs to market. The relationships of those drugs with their biological targets will be reviewed, particularly focusing on biological target space and chemical space, as well as the molecular properties of drugs. Furthermore, examples of chemical substructures which have been associated with a preference for certain biological target classes will be discussed. In addition, examples of marketed drugs bound to their target receptors will be highlighted in the context of binding site shape and properties. The chapter will finish with an outlook on future challenges for drug discovery.