Netscape 3, Netscape 4, and MSIE 4. X-ray Crystallography High throughput screening uses robots to test the binding activity of thousands of compounds against a molecular disease target, usually a protein. This binding activity is a measure of the compound's ability to inhibit the activity of the protein, the first step in judging whether the compound is a potentially successful drug candidate. The compounds tested are obtained not only through combinatorial chemistry , but also from other high throughput synthesis methods. As described elsewhere, traditional drug development has been compared to carefully selecting one bullet at a time and carrying out extensive laboratory experiments to fine tune the capability of the bullet to hit the target.
Combinatorial chemistry provides thousands of bullets to shoot at the target all at once.
High throughput screening gives us the ability to find the bullets that hit the target. High throughput screening generally does not identify a drug candidate per se . The primary role of the technology is to detect lead compounds and supply directions for their optimization using other techniques. Many properties critical to the development of a successful drug cannot be assessed by high throughput screening. Given the variety and size of chemical libraries available today, and the need to compare the results from multiple screenings, data collection and management of information are critical elements of high throughput screening.