Solubility Issues in Early Discovery and HTS

Abstract

Drug discovery programs begin with target identification and validation for diseases with unmet medical needs (Figure 1). Drug discovery targets that are currently available mostly fall into two categories, with 45% being receptors and 28% being enzymes (Table 1) (Drews, 2000). There are only 483 targets addressed by all drugs in the pharmaceutical industry, which is a relatively small number compared to the estimated 3000–10,000 disease relevant genes (Meisner et al., 2004). It is evident that the drug target universe is far from being fully exploited.