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Zenobia Therapeutics, Inc. and BioBlocks, Inc. Announce Sale of a Joint Fragment Library Ideal for Screening by All Popular Methods


5/7/2012 11:20:40 AM

LA JOLLA, Calif., May 7, 2012 /PRNewswire/ -- Zenobia Therapeutics, Inc. (Zenobia), the leader in fragment-based lead discovery (FBLD) for CNS diseases and FBLD/structural biology services, and BioBlocks, Inc. (BioBlocks), a leader in medicinal chemistry services and novel building block products, announced today that they are adding a 284 compound fragment library to their product offerings. The library, ZB-Fragment Library 2, is ready for screening by all popular methods, contains soluble, verified protein binders, is shape and functionally diverse, and has an average molecular weight of 161.4 Da. The library was constructed by combining BioBlocks' unique expertise in medicinal chemistry and scaffold design with Zenobia's expertise in FBLD. Vicki Nienaber, Ph.D., President, CSO and founder of Zenobia, reported the first fragment-based crystallographic screening method (Nature Biotechnology 2000) and Robert Meadows, Ph.D. co-founder of Zenobia is an inventor of the SARbyNMR method (Science 1996). Industry veteran BioBlocks medicinal chemists have advanced numerous leads into preclinical and clinical development and have created a lead discovery platform capable of generating high quality patentable leads in a cost and time efficient manner.

"Our customers have experienced an impressive success-rate in identifying valuable hits with Zenobia Fragment Library 1 with many returning to purchase additional copies. Establishing a collaborative relationship with BioBlocks allows us to jointly provide Fragment Library 2 with added core diversity and medicinal chemistry readiness using BioBlocks' unique expertise in creating leads from its building blocks," said Dr. Nienaber. BioBlocks CEO, Dr. Pallai, said, "BioBlocks' core strength is the medicinal chemistry we utilize in collaborative drug discovery programs with our clients. Working with Zenobia allows us to take advantage of their unparalleled capabilities and experience in FBDD and SBDD and combine it with our expertise in fast fragment evolution, lead identification and optimizing compounds for pharmaceutical use. Our collaborative Fragment Library 2 provides a high quality starting point to generate lead compounds. With optimization, the final compounds are significantly more likely to occupy the high probability region of drug space than those developed from a typical HTS hit."

Like Library 1, Library 2 is a small, cherry picked selection of diverse chemotypes and shapes, selected for manageable flexibility and compact interactions with target sites. Fragment functional groups are selected for their medicinal chemistry readiness and pharmaceutical appeal. There is no overlap between Library 1 and Library 2 so screening both will provide a wider variety of initial hits. The compounds are all soluble (200mM in DMSO), so screening with different methods is straightforward.

Through consulting or collaborations, Zenobia and BioBlocks offer structural biology, FBLD and medicinal chemistry expertise in advancing SAR around fragment hits.

About Zenobia

Zenobia provides a commercial fragment library, and access to their structural biology, crystallography and fragment-based lead discovery expertise through partnerships, consulting and collaborations. Zenobia's internal programs combine fragment-based lead discovery with the expertise of biologists and clinicians to find treatments for devastating illnesses for which there is no disease altering treatment such as Parkinson's and Huntington's disease.

About BioBlocks

BioBlocks provides medicinal chemistry expertise to clients in the drug discovery community. In our collaborative projects we optimize partner's hits to leads and preclinical candidates. Our Leap-to-Lead platform addresses fundamental issues in drug discovery the high attrition rate and lack of novelty found in typical HTS hits - by providing an alternative source for high quality tractable leads with multiple possible optimization pathways.

For additional information on BioBlocks, Inc., contact Dr. Peter Pallai at ppallai@bioblocks.com or visit www.bioblocks.com. For additional information on Library 2 please contact fragments@bioblocks.com or Zenobia, please see below.

For additional information on Zenobia Therapeutics, Inc., contact Dr. Vicki Nienaber at vicki@zenobiatherapeutics.com or visit www.zenobiatherapeutics.com. For additional information on Zenobia's Fragment Library 1 or 2, contact Erika Zehm at erika@zenobiatherapeutics.com.

SOURCE Zenobia Therapeutics, Inc.



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