SIRT1 belongs to the class III family of HDACs, which are NAD+ dependent enzymes. SIRT1 modulators have been shown to play a beneficial role in treating diseases such as cancer, diabetes, metabolic disease and inflammation, making them attractive targets for the development of new drugs. The new HTRF® SIRT1 assay, developed by Cisbio Bioassays using its patented HTRF technology, is a homogeneous method for directly measuring SIRT1’s deacetylation activity. This simple and rapid assay offers the advantage of very low enzyme consumption compared to other conventional assays. The HTRF® SIRT1 assay now enables the identification of both inhibitors and activators of SIRT1 activity, and also discriminates polyphenolic compounds.