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Nanosyn and Amphora Discovery Reach Chemical Genomics Collaboration Milestone: 100,000 Diverse, Purified, Characterized Compounds Delivered by Nanosyn, Novel Drug Leads Identified by Amphora Discovery

Menlo Park, Calif. and Durham, N.C., March 28 /PRNewswire/

On March 18, 2003, Nanosyn delivered its 100,000th purified, characterized compound to Amphora Discovery. Achieving this milestone in fifteen months reaffirms Nanosyn as a leading supplier of high quality compounds to the biotech/pharmaceutical industry. With these purified compounds, Amphora Discovery screened 40 targets, generating over 7 million data points. Amphora Discovery has identified potent, selective leads for several important disease targets including diabetes, rheumatoid arthritis, Crohn's disease, and stroke. Amphora Discovery's precision data allows utilization of all data, positive and negative, enabling chemistry decisions earlier in the drug discovery process. As a result, Amphora has demonstrated the ability to go from target identification through screen development to selective, potent lead molecules in as little as 6 weeks. Amphora Discovery is currently in discussions with large pharma companies for drug discovery partnerships in targets including kinases, phosphatases, proteases, GPCRs and ion channels.

Amphora Discovery has demonstrated that rigorously purified and characterized chemical libraries of known concentration, coupled with high-quality, diverse biological testing methods, accelerate discovery and optimization of selective, potent drug lead molecules, including proprietary leads for targets previously deemed "intractable". As of March 2003, Nanosyn has delivered 100,000 diverse, purified and thoroughly characterized compounds to Amphora Discovery. "We are extremely pleased with Nanosyn's ability to deliver high quality purification and follow-up chemistry. We look forward to a strong continuing relationship in the future," said C. Nicholas Hodge, Ph.D., Co-Founder and Vice President of Chemistry and Technology at Amphora Discovery.

The compound collection that Amphora Discovery has assembled is designed to ensure activity against all of the druggable target classes in the human genome, yet still possess the physical and biological properties that allow rapid optimization of hits into proprietary drug candidates for oral delivery. Amphora Discovery draws from commercially available, semi-exclusive and exclusively synthesized structures in building the library. Each compound that passes Amphora Discovery's initial computational filters for inclusion in the growing library is subjected to Nanosyn's proprietary purification, characterization and quality control process. As a final step that is unique in the industry, Amphora Discovery measures the quantity of compound in the aqueous assay buffer prior to screening.

Upon its founding in late 2001, Amphora Discovery and Nanosyn entered a strategic partnership to participate in the construction a diverse, "drug like" screening library of unprecedented quality. Using their proprietary technology, Nanosyn reached a purification throughput of 15,000 compounds per month by June 2002. During this period Amphora integrated state-of-the-art microfluidic and electrophysiology technology, efficient screening and compound handling operations, and informatics tools. Coupled with knowledge of the purity, identity and concentration of each compound in each screening experiment, the Amphora Discovery engine has generated highly reproducible, accurate structure-activity information from primary screening data that can accelerate the hit-to-lead and lead optimization process by months or even years compared to industry standards. Said Dr. Nikolai Sepetov, Founder and CEO of Nanosyn, "It is very exciting and gratifying to see our chemistry applied so quickly in the drug discovery process. Our collaboration with Amphora has demonstrated that Nanosyn's capabilities can be integrated into an industrialized drug discovery model." In addition to analytical chemistry and purification, Nanosyn has provided Amphora Discovery with designed synthetic libraries, hit expansion and hit-to-lead chemistry support using its proprietary Accelerated Nanoscale Synthesis Technology.

Using purified and characterized libraries and precise, quantitative biology systems, chemistry and biology decisions can be made using the entire body of information present in the initial screen, rather than just a few actives that have been chosen for resynthesis and confirmation in a follow-up screen. Employing this approach, Amphora Discovery has identified multiple proprietary scaffolds with robust structure-activity relationships from primary screening data for every target tested to date. "Access to these datasets permits medicinal chemists to enter lead optimization rapidly with scaffolds that are tuned for critical, disease-specific selectivity and physical property requirements, guaranteeing a higher success rate en route to the clinic," said Hodge. "We refer to this process as Multi-Dimensional Lead Generation, reflecting our ability to use many relevant, highly accurate measurements at the earliest stages of lead selection." Additionally, using the broad selectivity information across all of the targets screened that is available in the Amphora Discovery database, biologists have access to chemical genetics tools for target validation and understanding of the complex pathways that lead to disease.

About Nanosyn

Nanosyn is a chemistry-based company specializing in the design, synthesis and analysis of small organic compounds for pharmaceutical and biotechnology industries. We put special emphases on custom synthesis, 'hit-to-lead' optimization, and development of screening libraries targeted for drug discovery. Nanosyn's unique proprietary technology yields PureQualityTM compounds enabling rapid identification of new drug candidates. For more information, please visit

About Amphora Discovery

Amphora Discovery was formed in September 2001 to exploit opportunities in chemical genomics. By applying high precision screening across biological systems and surrogate therapeutic suitability assays, Amphora Discovery is able to efficiently deliver high quality drug candidates. The senior management has over 50 years of experience in drug discovery including developing world-class lead generation operations. Amphora Discovery is headquartered in Research Triangle Park, NC with additional facilities in Mountain View, CA. For more information, please visit

For more information please contact:

Dr. Olga Issakova
Vice President
Nanosyn, Inc.
3760 Haven Ave.
Menlo Park, CA 94025
Tel: (650) 853-7034
Fax: (650) 853-7033

Cesar Collado
Vice President , Business Development and Commercialization
Amphora Discovery Discovery Corp.
801-4 Capitola Drive
Durham, NC 27713
Tel: (919) 287-6170

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