ABSTRACT
Certain enzymes are important molecular targets for drug discovery and many drug discovery programs include enzyme targets in primary screening assays. Generally, these assays utilize partially purified or purified human enzymes and involve the measurement of product formation by a variety of assay methods including radiometric, colorimetric, and fluorometric assays. The following sections detail important considerations for developing and validating enzyme assays for synthetic compounds and screening natural product extracts. In addition, an example of development and validation of a specific enzyme assay is presented to serve as an example.
