ABSTRACT
Extracts from natural product sources have been a valuable source of molecular diversity in many drug discovery programs and several therapeutically important drugs have been isolated from natural products. However, the screening of such materials can be very complicated due to fact that they contain a complex mixture of secondary metabolites. Success in identifying new therapeutics using in vitro receptor and enzyme assays is largely dependent upon the proper design and validation of these screening assays. Another key to success is the design of assays with higher throughput so that a large number of extracts can be screened quickly and cost effectively. The advent of combinatorial chemistry methods has also enhanced the importance for high throughput screening methods for testing for bioactivity. This section contains a detailed description of the design and validation of receptor and enzyme assays used to screen combinatorial chemistry reaction products and natural product extracts. In addition, new assay technologies designed to increase assay throughput will also be presented.
