Combinatorial Chemistry & High Throughput Screening

Rathnam Chaguturu 
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UCSF Small Molecule Discovery Center: Innovation, Collaboration and Chemical Biology in the Bay Area

Author(s): Michelle R. Arkin, Kenny K.H. Ang, Steven Chen, Julia Davies, Connie Merron, Yinyan Tang, Christopher G.M. Wilson, Adam R. Renslo.


The Small Molecule Discovery Center (SMDC) at the University of California, San Francisco, works collaboratively with the scientific community to solve challenging problems in chemical biology and drug discovery. The SMDC includes a high throughput screening facility, medicinal chemistry, and research labs focused on fundamental problems in biochemistry and targeted drug delivery. Here, we outline our HTS program and provide examples of chemical tools developed through SMDC collaborations. We have an active research program in developing quantitative cell-based screens for primary cells and whole organisms; here, we describe whole-organism screens to find drugs against parasites that cause neglected tropical diseases. We are also very interested in target-based approaches for so-called “undruggable”, protein classes and fragment-based lead discovery. This expertise has led to several pharmaceutical collaborations; additionally, the SMDC works with start-up companies to enable their early-stage research. The SMDC, located in the biotech-focused Mission Bay neighborhood in San Francisco, is a hub for innovative small-molecule discovery research at UCSF.

Keywords: Chemical biology, drug discovery, fragment discovery, pharmaceutical industry/academic collaboration, screening, public/private partnership, tropical diseases.

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Article Details

Year: 2014
Page: [333 - 342]
Pages: 10
DOI: 10.2174/1386207317666140323133841
Price: $58