FAST utilizes rapid determination of protein structures to allow both identification and optimization of small molecule fragments that bind to specific targets. FAST is an attractive technology for targets that have not yielded promising leads from high-throughput screening, or HTS. Unlike traditional lead discovery approaches, which require ultra HTS of large numbers of random compounds, FAST optimizes the likelihood of developing a successful drug candidate by focusing on a very small number of low molecular weight, water-soluble fragments, that once identified, can be rapidly optimized by further focused synthesis to enable the delivery of novel, potent and selective modulators of drug targets.

FAST is based upon our proprietary fragment library of approximately 1,000 structurally diverse, low molecular weight compounds. We developed FAST through the integration of a series of technology capabilities, including:

• A high-throughput capability to generate many different crystals of a target protein in parallel;
• The evaluation of our library of fragments and direct visualization of bound fragments utilizing X-ray crystallography;
• The use of novel computational design methods and iterative synthetic chemistry to optimize these fragments into drug-like lead compounds.

We have combined these technologies to generate an efficient platform for drug discovery that delivers lead compounds active against a wide range of targets, while accessing high chemical diversity and the potential for good drug-like properties.