ANYL 40 |
| Increasing attention is being paid to finding privileged structures in small molecule drug discovery and fragment screening techniques are becoming more widespread to identify suitable scaffolds. SPR biosensors have now been validated for fragment screening and with a throughput of 1400 fragments/day/10 ug of protein they have been recognized as an important primary screening technique for use as the first step in a fragment screening campaign. Array based biosensors (e.g. Biacore A100) can confidently measure in a simultaneously mode the binding of 4 fragments to 4 proteins in parallel and provides information on the selectivity of binding and target site specificity that are important criteria in fragment selection. Not only affinities in the range from mM to pM can be measured but also the residence time (off-rate). Examples will be presented of this highly suitable technique for ranking the lead expansion series. |
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Surface Plasmon Resonance
1:30 PM-5:00 PM, Sunday, August 19, 2007 BCEC -- 105, Oral
Division of Analytical Chemistry |