BioFocus DPI, a Galapagos Company, is launching a new version of the GPCR SARfari discovery tool at the American Chemical Society meeting this week in San Diego (USA). Following the success of the Kinase SARfari launched in June, GPCR SARfari now also combines chemical and biological GPCR data from both internal and public sources into a single, dynamic system.

GPCRs play a key role in many human diseases, making them of strategic importance to the pharmaceutical industry. GPCR SARfari enables the user to design compounds and focused libraries against specific GPCRs and rapidly optimize compound discovery through exploration of structure-activity relationships. The system comes pre-populated with:

• Full complement of 297 human Class 1 non-olfactory GPCRs
• Comprehensive names, synonyms and targets for FDA approved drugs
• More than 77,000 bioactive GPCR-focused compounds and more than 300,000 experimental
  end points abstracted from the literature
• Six different binding site views for all 297 GPCRs, enabling comparison and clustering based
  on binding site properties
• Pre-calculated site profiles for each GPCR using almost 500 physicochemical descriptors

Dr. John Overington, Senior Director of Discovery Informatics at BioFocus DPI, said “The key advantage of this latest release of GPCR SARfari is its ability to integrate biological and chemical data from public and proprietary sources. The result is a more powerful, single-sweep, data mining resource that provides a unique insight on GPCR drug discovery.”

Dr. Overington will present this new GPCR drug discovery tool at this week’s ACS meeting in San Diego. In the talk entitled “Large-scale databases applied to chemogenomics” he will discuss the value of integrating knowledge resources to facilitate effective drug discovery.

About BioFocus DPI

As the service business unit for Galapagos NV, an integrated drug discovery company, BioFocus DPI aims to expand our partners’ drug pipelines by accelerating the gene-to-candidate discovery process. We achieve this by offering a biologically-focused discovery platform with three key differentiators:

• target discovery in human primary cells
• hit discovery using focused chemogenomic libraries as well as diverse compound collections
• in silico drug discovery tools

Through a proprietary adenoviral platform with human full-length cDNA and shRNA constructs, we are able to rapidly identify and validate disease-modifying drug targets. Once a target has been selected, our focused small-molecule libraries, large diversity collection and natural product libraries can be applied to generate hits. These hits can then be further optimized through our predictive drug discovery tools applied in medicinal and computational chemistry as well as through our assay development, high throughput screening, and ADME optimization - thereby progressing our partners’ discovery programs. BioFocus DPI has over 300 employees and operates facilities across Europe and the US. For more information about BioFocus DPI, please visit www.biofocusdpi.com.

BioFocus® and SARfari™ are trademarks of Galapagos NV and/or its affiliates