An Unprecedented Industry-Academia Alliance to Accelerate GPCR Deorphanization Efforts

Release date: 9/6/2011

Fremont, California – Tuesday, September 6, 2011 - NC-IUPHAR and DiscoveRx announce that they have formed an alliance to accelerate progress on understanding the functions of orphan G Protein-coupled receptors (GPCRs) and their signalling mechanisms. The goal of this unprecedented relationship is to have researchers worldwide gain greater knowledge and ultimately expedite the process of deorphanizing a whole set of putative disease targets.  The results of their collaboration will be communicated through the IUPHAR Database at by indicating clearly where sufficient evidence exists that an endogenous ligand modulates receptor function directly.

GPCRs are a large family of proteins expressed on the surface of cells and are the target of approximately 30% of current medicinal drugs. About 130 GPCR receptors still remain for which the endogenous ligand (the natural signal used in the body to activate the GPCR) has not yet been identified. These receptors are referred to as “orphan receptors” and are the subject of extensive research. One of the most exciting challenges in pharmacology today is the identification of functional ligands for orphan GPCRs, a promising set of targets for the development of new medicines. There has been rapid progress in developing methodologies to address this problem. Most recently, DiscoveRx has developed the PathHunter® β-Arrestin platform, which consists of an industry leading panel of over 98 cell lines expressing orphan GPCRs and provides a unique, powerful and proven  method to deorphanize GPCRs. These cell lines have been successfully deployed by a number of drug discovery companies to deorphanize some important disease related orphan GPCR’s.

Reciprocal links between IUPHAR-DB and the DiscoveRx websites have been established, enabling users of DiscoveRx products to access cutting-edge information on orphan GPCRs in the IUPHAR-DB and to provide a portal for IUHPAR-DB users to access information on DiscoveRx products. To receive updates about the ongoing developments, enroll at no cost with IUPHAR-DB RSS feeds or e-mails by visiting

About DiscoveRx Corporation
Founded in 2000, DiscoveRx is a privately held, venture-backed company headquartered in Fremont, California, with additional offices in San Diego, California and Birmingham, England. The Company pioneered the use of β-galactosidase enzyme fragment complementation in biochemical and cell based assays for discovery research in fields of receptor biology, 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 and solutions have been widely adopted in academic, pharmaceutical and biotech drug screening laboratories worldwide. In October 2010, it completed its acquisition of the KINOMEscan division ( of Ambit Biosciences thereby becoming a key solution provider for kinase drug discovery profiling and screening. The Company is also a recipient of multiple Frost and Sullivan awards. For more information on DiscoveRx products and services, please visit

About NC-IUPHAR (The International Union of Basic and Clinical Pharmacology Committee on Receptor Nomenclature and Drug Classification)
NC-IUPHAR is an international committee whose mission is to support biomedical research by providing to the international scientific community guidelines on the nomenclature of key receptors including GPCRs, ion channels, and drug binding sites.  These guidelines are published in the journal “Pharmacological Reviews” and are made freely available through the IUPHAR Database (IUPHAR-DB), which is developed and maintained at the University of Edinburgh.

IUPHAR-DB is a popular online reference resource which currently covers the products of 616 human and rodent genes from four protein families: G protein-coupled receptors, voltage- and ligand-gated ion channels, and nuclear hormone receptors. The nomenclature guidelines, receptor classifications, and basic information on selected receptor ligands are formulated or collected by subcommittees of experts in the field. Today there are over 60 NC-IUPHAR subcommittees totalling approximately 700 scientists who volunteer their time to work on this project. The entire operation is overseen and directed by the NC-IUPHAR Committee, chaired by Dr. Michael Spedding. For GPCRs, NC-IUPHAR defines progress in this field via its evolving pharmacology group, chaired by Dr. Anthony Davenport and via its GPCR group chaired by Dr. Rick Neubig. The database committee, responsible for IUPHAR-DB, is chaired by Dr. Tony Harmar.  These groups curate knowledge on receptors, issues guidelines on pharmacology and disseminate this information via the IUPHAR Database. Earlier this year IUPHAR and the British Pharmacological Society (BPS) signed an agreement to work jointly in producing the long-standing BPS publication Guide for Receptors and Channels (GRAC) and the IUPHAR-DB.

Media Contacts
DiscoveRx Corporation
Sailaja Kuchibhatla
Sr. VP Business Development
42501 Albrae Street
Fremont, CA 94538
tel | 510.979.1415 x 104

Professor Michael Spedding