ActiveSite's proprietary technology platform is a novel approach to fragment-based drug discovery, especially applicable to enzymes such as proteases that have proven to be recalcitrant targets in drug discovery.
This technology enables ActiveSite to detect the interaction of drug-like small molecules (from its unique, internally developed library) with the active site of target enzymes without the use of NMR, crystallization or in silico methodology typically used by other fragment-based approaches.
Although the technology is applicable to all enzymes, the company has focused on proteases, an important class of enzymes known to be involved in numerous human diseases. ActiveSite's approach offers a rapidly deployable alternative to high-throughput screening for identifying small molecule, drug-like inhibitors of proteases as exemplified by its plasma kallikrein inhibitor program.
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