DiscoveRx Corporation Expands its GPCR Technology Portfolio to Include Advanced Technologies that Facilitate Lead Optimization and SAR

Release date: 6/1/2010

FREMONT, Calif., June 1, 2010 - DiscoveRx continues to innovate in the field of GPCR signaling assays, tools and services with the introduction of two additional GPCR platforms to facilitate counterscreening, lead optimization and SAR evaluation of compounds identified during a primary screen.

Endocytosis is fundamental to GPCR biology, regulating the amount of cell-surface receptors, helping to transduce signals from the receptor and controlling the recycling or degradation of the receptor itself. Therefore, quantitative analysis of the internalization kinetics of the receptor from the cell surface can lead to the discovery of novel compounds with unique attributes. The PathHunter® Activated GPCR Internalization technology is a non-imaging, non-antibody based platform that provides a direct and quantitative measurement of internalized GPCR localized to intracellular endosomes allowing the fate of unlabeled, activated GPCRs to be monitored in live cells. Unlike other traditional internalization technologies, PathHunter® Assays are simple, non-radioactive chemiluminescent assays that are ideal for studying GPCR receptor recycling and kinetics, determining mechanism of action of lead compounds or identifying novel inhibitors of receptor internalization.

The PathHunter® β-Arrestin Ortholog GPCR assays are fully validated, functional clonal cell lines expressing ortholog GPCRs that have been optimized to detect a full range of compound pharmacologies. With a portfolio of more than 80 ortholog GPCR targets, drug discovery researchers can gain a greater understanding of putative leads, determine mechanism of action, or delineate differential ligand-activated responses of lead compounds prior to testing in expensive animal models. "DiscoveRx has strived to provide cutting edge tools and technologies for the GPCR screening community. The simplicity and robustness of the assays have accelerated the adoption of our HitHunter® cAMP and PathHunter® β-Arrestin recruitment based assays for assay development, primary HTS and secondary screening. Now DiscoveRx is embarking on providing next generation GPCR platforms that help researchers increase their understanding of compound and receptor biology thereby aiding advanced lead optimization and SAR work", said Dr. Tom Wehrman, Senior Director of Research at DiscoveRx. Both assay formats combine a simple, one-step addition protocol and standard chemiluminescent detection and will significantly accelerate drug discovery and development, from early discovery screening through lead optimization and into the preclinical stages.

About DiscoveRx Corporation
Founded in 2000, DiscoveRx is a privately held, venture-backed company headquartered in Fremont, California, with an additional office in Birmingham, England. The Company pioneered the use of β-galactosidase enzyme fragment complementation in biochemical and cell based assays for discovery research, and holds extensive intellectual property in this area. DiscoveRx is dedicated to the development and commercialization of innovative solutions to study GPCRs, Kinases and other major drug target classes, and many of their innovative products have been widely adopted in pharmaceutical and biotech drug screening laboratories worldwide. The Company is also a recipient of two Frost and Sullivan 2008 awards: Award for Innovation in North American Healthcare Market as well as a European Product Line Strategy Award for it's GPCR Cell Based assay portfolio. For more information on DiscoveRx products, please visit

Media Contacts
DiscoveRx Corporation
Sailaja Kuchibhatla
Sr. VP Business Development
42501 Albrae Street
Fremont, CA 94538, USA
tel | 1.510.979.1415 x 104