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LabAutomation 2006 - SLAS

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MP83<br />

Tracy Worzella<br />

Promega Corporation<br />

Madison, Wisconsin<br />

tracy.worzella@promega.com<br />

<strong>LabAutomation</strong><strong>2006</strong><br />

Co-Author(s)<br />

Brad Larson<br />

Promega Corporation<br />

Siegfried Sasshofer<br />

Tecan<br />

High-Throughput Compound Profiling Using Promega Luminescent Assays<br />

on a Tecan Freedom Evo 200 System<br />

We demonstrate the use of Promega’s luminescent HTS assays for profiling a collection of test compounds on a Tecan system. This<br />

profiling example takes a parallel approach to compound analysis by incorporating diverse assay types including cell-based assays for<br />

viability and apoptosis induction, a cell-based GPCR DRD1 assay, cytochrome P450, P-glycoprotein, and kinase assays. Using a panel<br />

of assays, we show that one can obtain a better understanding of drug compound properties in order to better predict off-target activity<br />

and toxicity. To generate the data, a Tecan Freedom Evo 200 with an integrated TeMo was used to dispense cells, serially dilute test<br />

compounds and assemble assays in 384-well format. Luminescence was recorded with a Tecan GENios Pro plate reader. IC50 or EC50<br />

calculations were performed for each compound and assay combination. Results show that data from these assays can be used to<br />

determine multiple compound characteristics for subsequent lead selection or optimization.<br />

MP84<br />

Bradley De Bruler<br />

PfizerDiscovery Technologies<br />

San Diego, California<br />

bradley.debruler@pfizer.com<br />

Co-Author<br />

Tivel, Kathleen<br />

Rapid LCMS Analysis of CombinatorialLlibraries Using Monolithic Columns for<br />

Preparative Scale-Up<br />

Traditional approaches to analyzing combinatorial libraries utilize LC/MS methods with packed columns and short gradients to achieve<br />

fairly rapid results. The ability to develop even faster methods is limited due to high backpressure that prevents significant increases in<br />

flow rate. Monolithic columns are comprised of a single porous rod and have the advantage of greatly reduced backpressure at a given<br />

flow rate compared to particulate columns. Our objective was to dramatically decrease our run time, thus greatly increasing the number of<br />

compounds that can be analyzed in a given time frame. This poster will describe development of analytical scale HPLC methods and their<br />

incorporation into our process for rapid purification of targeted libraries.<br />

144

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