ChemBridge Research Laboratories LLC (CRL) announced the successful application of its proprietary design approach and library to discover drug-like small molecule leads against G-protein coupled receptors (GPCR). CRL's newly designed GPCR-Targeted Library therefore addresses the need of the pharmaceutical industry to identify viable lead molecules aimed at this most important drug-target class.

In order to validate this fundamental approach in-house, CRL undertook the synthesis of privileged molecular motifs expressing the desired pharmacophores via specifically designed drug-like templates and target-relevant building blocks. As a result, CRL's scientists were able to identify a proprietary lead acting as an agonist against a certain GPCR.

Dr. Thomas R. Webb, VP of R&D at CRL and ChemBridge Corporation said: "We are pleased to announce the most relevant demonstration of the validity of our targeted library design approach; the direct confirmation of agonist activity against a peptide-ligand binding GPCR. It is well known that such activity is rarely found in standard screening collections of small molecules. We found agonist activity in every compound in a small and tightly focused set of compounds that were designed using our proprietary template and building block approach."

"CRL is now optimizing the lead series further with the aim to enhance drug-relevant properties in parallel", says Dr. Michael Schultz, President and CSO of CRL, "and we are open to discuss this project with pharmaceutical companies interested in a collaboration."

CRL's non-exclusive GPCR Targeted Library was recently launched on the market. Eisai and another undisclosed company currently have access to this cutting-edge research tool for GPCR drug discovery. Deals with several major pharmaceutical companies are under discussion.