Combinatorial Libraries

Combinatorial Libraries

Torrey Pines Institute's drug discovery program is centered on our proprietary "high density" combinatorial libraries, otherwise known as mixture-based combinatorial libraries. The utility of mixture-based combinatorial libraries has been demonstrated in more than 100 separate studies in which active compounds have been identified. These studies have been carried out by more than 50 separate research groups. New enzyme inhibitors, agonists and antagonists to specific receptors, antimicrobial, antifungal and antiviral compounds, and B and T cell epitopes have been identified from such libraries, and have been extensively reviewed.

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HTS and uHTS

Torrey Pines Institute currently has 37 small molecule libraries representing approximately 31 million compounds proportioned into 96-well polypropylene plates. Each plate contains 80 samples (100ul/well) at a concentration of 1 mg/ml. The entire small molecule library collection is made up of 5,915 samples, proportioned into 75 96-well plates.

In Vivo and Other Low Throughput Assays

Torrey Pines Institute has developed a tool, the scaffold ranking library, that provides initial biological information on over 5 million small molecules derived from 30 different scaffolds, from the testing of just 30 samples. From the results of these studies, additional sets of between 30 to 100 samples are prioritized for testing. In previous studies with complex in vivo models, a series of active individual compounds were identified from the testing of only 150 samples.

Future Libraries

Torrey Pines Institute is continually exploring the development of additional high density combinatorial libraries. In developing new libraries consideration is given to several factors including: drug like characteristics, position of library in chemical space (Figure below), diversity of substituents, ease and reproducibility of synthetic scheme.