Combinatorial Chemistry and High Throughput Screening

This chapter explores combinatorial chemistry and high throughput screening. During the 1980s, a rapid increase in molecular biology techniques had resulted in the development of rapid, efficient drug testing systems, known as high throughput screening (HTS). These techniques were able to provide accurate results on extremely small quantities (μg) of test substances. However, in order to be used economically, HTS requires rapid production of very large numbers of test substances which could not be met by traditional synthesis. Combinatorial chemistry was developed to provide new test molecules in sufficient numbers to meet this need. The chapter investigates solid phase synthesis, solution phase synthesis, and polymer-assisted solution phase synthesis. It also considers chemical tagging, deconvolution, purification, combinatorial libraries, and chemogenomics.