Random screening, drug discovery

One of the earliest approaches to drug discovery was the random screening process. More recently, significant efforts were directed towards... 

Another important method of drug discovery is the random screening of vast numbers of compounds. Each year, for example, the National Cancer Institute screens some 20,000 compounds for anticancer activity. One successful hit was the compound Taxol, shown in Figure 14.4. This compound has significant activity against several forms of cancer, especially ovarian cancer. 

Drug design, based on crystal structures of target incorporated with substrate or inhibitor (primarily for enzymes). More useful for lead optimization than for primary discovery. Can be configured to serve as electronic ( virtual ) random screen. 1980s-present. 

Natural sources are still important sources of lead compounds and new drugs. However, the large diversity of potential natural sources in the world makes the technique of random screening a rather hit or miss process. The screening of local folk remedies (ethnopharmacology) offers the basis of a more systematic approach. In the past this has led to the discovery of many important therapeutic agents, for example, the antimalarial quinine from cinchona bark, the... 

---