In 2007 Enamine in collaboration with UORSY Ltd have launched a joint project in order to establish a systematic chemically validated approach to tangible building blocks that consist of up to 21 heavy atoms and therefore can be used in medicinal chemistry and drug discovery.
The approach is based on three types of well known and optimized organic reactions (reaction sequences) that result in molecules containing one reactive functional group such as NH2, NHR, SH, SR, COOH, C=O, CN, CONHR, SO2Cl, CSNHR etc. Divergent approach was widely used for library construction, leading to a multitude of feasible structures of reactive compounds. Over 1,000 reactions or reaction sequences were used for enumeration of products derived from about 10,000 commercially available and proprietary starting materials available from stock. Currently the database of tangible building blocks exceeds 4.6 million records.
Rigorously validated chemical procedures ensure high feasibility and cost effectiveness of the tangible building blocks. About 9,000 tangible building blocks are synthesized annually with an average lead time of 5 weeks and feasibility of at least 70%. The most of these compounds are selected and ordered by pharma- and biotech companies worldwide at low, fixed prices. Weekly progress reports on the synthesis of the ordered tangible building blocks and fragments are provided to the customers.