The new library is the first in a series planned by the two companies that will be sold under the Peakexplorer brand, with two additional GPCR-focussed collections due to be launched before the end of the year. It is intended for use in screening of GPCR targets by pharmaceutical and biotechnology companies.
GPCRs are cell surface targets to which drugs bind to cause changes in intracellular function. As a class, GPCRs are historically the single richest receptor target for drug discovery, and account for the activity of nearly 60 per cent of all prescription drugs on the market today. Medications that treat conditions regulated by GPCRs cover most therapeutic areas and represent tens of billions in annual sales worldwide.
However, the potential for GPCR-based drugs remains largely untapped since only about 200 of these important drug targets are functionally known, in part because their study requires the use of complex call-based assays. It is estimated that there may be as many as 200 additional so-called 'orphan' GPCRs (those whose function is unknown). As a result, most major pharmaceutical companies today have active GPCR drug discovery programs.
The first Peakexplorer library - Peakexplorer G1 - contains over 1,000 diverse compounds generated using De Novo's computational drug design platform SkelGen. De Novo synthesised around 15 million virtual structures in the programme, and Peakdale used its chemistry and synthesis expertise to make the most promising candidates.