LATEST NEWS
02.02.2012
San Diego: CalAsia Pharmaceuticals and Professor R. Padmanabhan of Georgetown University announce a collaboration to develop inhibitors of Dengue and West Nile virus protoeases.
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TECHNOLOGY
Development and Optimization of Assays
Crystallography based fragment screening is time consuming and expensive. Therefore, to expedite and make it meaningful, CalAsia has pioneered in developing and optimizing screening assays based on the biological function of the drug targets to identify fragment hits and to screen compounds and compound library for efficacy and selectivity. Screening of fragments using functional assay has multiple advantages over crystallography screening:
- Function based screening of fragments is much faster compared to crystallography methods
- Provides efficacy values of fragments in terms of Ki, Kd, IC50 or EC50
- Minimizes false positives and non-specific binding
- Given the limited size of a typical fragment library, these assays can be formatted for a low to medium throughput
CalAsia Pharmaceuticals has successfully applied this approach in identifying fragment hits for its internal drug discovery programs, where we can routinely measure the binding constants, IC50 and EC50 in low micro- to millimolar ranges for a variety of drug targets.
