BioFocus DPI, a Galapagos company, is launching its latest knowledge base, Kinase SARfari at this week’s World Pharmaceutical Congress. This fully integrated data repository and research workbench focuses on the protein kinase family of drug targets. This powerful tool combines chemical and biological data from internal proprietary and public sources in a single, dynamic system.

Protein kinases are an important class of drug targets often pursued by the pharmaceutical industry because of the vital role they play in regulating cancer and inflammatory diseases. Kinase SARfari enables the user to design compounds and focused libraries against specific protein kinases and rapidly optimize compound discovery through exploration of structure-activity relationships. Through effective integration and mapping of data from diverse biological and chemical sources, Kinase SARfari increases productivity and enhances knowledge discovery. The system comes pre-populated with:

• All human protein kinase sequences and a large collection of model organism orthologs
• Protein kinase clinical candidates and FDA approved drugs
• More than 700 3-D structural domains from the Protein Data Bank (PDB) with complete binding-site focused structural superposition
• Over 14,000 protein kinase compounds and more than 57,000 structure-activity relationship (SAR) screening and ADMET data points from BioFocus DPI’s StARLITe database
• Five binding site definitions based on analysis of known ligand-binding footprints with pre-calculated binding site physicochemical distances

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

Dr. Overington will be presenting this new kinase drug discovery tool at this week’s World Pharmaceutical Congress in Philadelphia (USA). In the talk entitled, “Aligning Target Selection with Compound Design - Leveraging Prior Knowledge for Efficient Discovery”, he will discuss the value of integrating knowledge resources to facilitate effective drug discovery. At the same conference, BioFocus DPI’s Senior Director of Target Discovery, Dr. Richard Janssen, will deliver the presentation “High Content RNAi Screen for Huntington Disease”, where he will address the use of high content screens to identify genes that modulate the survival of cells over-expressing mutant forms of the Huntington protein.

About BioFocus DPI

As the service 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; focused as well as diverse compound libraries; and predictive drug discovery tools. Through full-length cDNA and shRNA constructs, we are able to identify and validate disease-modifying drug targets rapidly. Once a target has been selected, our focused small-molecule, large diversity collection and natural product libraries can be applied to generate hits. These hits can then be further optimized through our expertise 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 eight facilities across Europe and the US. For more information about BioFocus DPI, please visit www.biofocusdpi.com.

More information about Galapagos NV, can be found at www.glpg.com.

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