Ambit Biosciences Publishes Comprehensive Profiling Data for Kinase Inhibitors in Nature Biotechnology and Significantly Expands KINOMEscan™ Profiling Panel

SAN DIEGO - January 8, 2008 – Ambit Biosciences today announced the publication in Nature Biotechnology of kinase profiling data for 38 well-known kinase inhibitors, obtained using Ambit’s high-throughput KINOMEscan™ profiling technology. The study also details a novel approach for quantifying the interactions between compounds and the human kinome. This approach enables the systematic analysis of high-throughput kinase profiling data, which dramatically improves the efficiency of selecting and optimizing the highest quality drug candidates from kinase-focused compound libraries.

The Ambit study was published in an article titled, “A Quantitative Analysis of Kinase Inhibitor Selectivity,” in the January 2008 edition of Nature Biotechnology. The article is currently available online, and the data set from the study can be viewed at www.ambitbio.com/technology/publications.

In the study, Ambit scientists profiled 38 different kinase inhibitors, including approved drugs and preclinical compounds, against a panel of 317 kinases. To enable a global analysis of the data, the scientists generated “selectivity scores” for each compound – an unbiased, quantitative measurement for how selectively a compound interacts with the human kinome. The selectivity score is determined by dividing the number of kinases that bind a compound by the total number of kinases screened. Using this method, promiscuous compounds, or those that interact with a large proportion of kinases screened, are assigned higher selectivity scores, while more selective compounds, or those that interact with few kinases, are assigned lower selectivity scores. These scores, and the promiscuity-selectivity rankings that flow from them, give scientists a quantitative tool for selecting drug leads from large compound libraries.

"Kinase inhibitors have tremendous potential to treat a variety of diseases that plague humankind," said Wendell Wierenga, Ph.D., executive vice president of R&D for Ambit. "However, determining how compounds interact with the human kinome presents a major challenge for drug developers, as certain kinase interactions can significantly impact a compound’s therapeutic and side-effect profile. Ambit’s kinase profiling technology provides a wealth of interaction data to help guide drug discovery and optimization efforts."

Additionally, Ambit announced that it has significantly expanded its commercial KINOMEscan profiling panel to greater than 400 kinases, including therapeutically relevant lipid, mutant, and atypical kinases. The continued expansion of the KINOMEscan panel further enhances the opportunity to uncover new targets for existing kinase inhibitors and enables more complete characterization of compounds before they are advanced toward clinical studies.

"With the industry-leading panel of kinases we have assembled, we can offer drug developers a much broader picture of their compounds’ effects on the human kinome," said Scott Salka, CEO of Ambit. "Publication of this most recent paper emphasizes not only the utility of our KINOMEscan technology, but also our commitment to developing innovative tools to help our partners interpret the valuable data we generate."

About KINOMEscan™

KINOMEscan™ is the industry's most comprehensive high-throughput system for screening compound libraries against large numbers of human kinases. KINOMEscan employs proprietary active-site dependent competition binding assays to determine how compounds bind to both intended and unintended kinases. In addition to helping keep discovery programs on target, KINOMEscan screens can opportunistically identify unanticipated interactions that can expand the therapeutic utility of compounds or serve as advanced starting points for new programs. Ambit's largest panel, scanMAX™, with greater than 400 assays, is the world's largest kinase profiling panel.

Ambit's KINOMEscan Division provides custom kinase profiling services to drug companies in addition to supporting the company's separate, internal drug development programs. KINOMEscan is a key component of Ambit's partnerships with Roche, Bristol-Myers Squibb, GlaxoSmithKline, Cephalon, and others. The technology has been featured in papers published in Nature Biotechnology and The Proceedings of the National Academy of Sciences of the United States of America. For more information, please visit www.kinomescan.com.

About Ambit Biosciences

Ambit Biosciences is a privately-held biopharmaceutical company engaged in the discovery and development of small molecule kinase inhibitors for the treatment of cancer. The company also markets the industry's most comprehensive kinase profiling service through its KINOMEscan™ Division. KINOMEscan is a proprietary technology designed to screen small molecule libraries against large numbers of human kinases. Ambit has multiple drug candidates in pre-clinical and clinical development, including AC220, a selective class III receptor tyrosine kinase inhibitor currently in Phase I for treatment of acute myeloid leukemia. The company has partnerships with Roche, Bristol-Myers Squibb, GlaxoSmithKline, Cephalon, and other leading organizations. For more information, please visit www.ambitbio.com.

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