ActiveSite Pharmaceuticals, Inc.

Organization Address
187 Magellan Ave.
San Franicsco, CA 94116

Organization Phone



Organization Description
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 owing to their well-known intractability to HTS, that has mostly limited drug-development for this important class of targets to peptidomimetic approaches that often results in molecules with poor drug-like properties. ActiveSite's approach offers a rapidly deployable alternative for identifying non-peptidic, small molecule, drug-like inhibitors of proteases, and other enzymes, as exemplified by its plasma kallikrein inhibitor program.

Therapeutic Areas
Blood & Lymphatic Diseases; Cardiovascular & Circulatory Disorders; Metabolic/Endocrinology Disorders; Ophthalmology

Clinical Development Stage