ASSAY MINIATURIZATION FOR ULTRA-HIGH THROUGHPUT SCREENING OF COMBINATORIAL AND DISCRETE COMPOUND LIBRARIES - A 9600-WELL (0.2 MICROLITER) ASSAY SYSTEM

Combinatorial chemistry has opened a new realm of chemical entities in the search for novel therapeutics, Combinatorial chemistry is current ly adding hundreds of thousands of compounds to similar numbers availa ble from yea;rs of synthesis by medicinal chemistry, It is not unreaso nable to expect that over the next several years, nearly a million com pounds will be available for screening against each therapeutic target , The number of potential targets will also be increasing with the adv ances in genomics, With the increasing number of compounds to be scree ned against an increasing number of targets, it is becoming increasing ly difficult and costly to obtain the required amounts of key biologic al material needed to screen these compounds, One obvious solution is to miniaturize the assays so that the biological reagent supply doesn' t need to increase, To this end, we have developed an ultra high throu ghput screening system comprised of a new plate design (9600-well), de tection system, and liquid handling system, This new format is capable of performing assays in as little as 0.2 mu l. The results obtained f rom this system compare favorably to those obtained in the standard 96 -well format.