AN ULTRA HIGH THROUGHPUT SYSTEM FOR DRUG DISCOVERY

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This project aims at developing an ultra-high throughput (UHTS; >100,000 compounds / day) assay system for drug discovery. The system will utilize a new sprocket driven carrier tape. The tapes consist of 10 ul wells in a standard 384 well microtiter plate format, arrayed sequentially on a roll of polypropylene tape. These types are being developed for high Capacity easy access compound storage. We propose to use these tapes for low volume (approximately 5ul) assays. In Phase I, we will be developing protease inhibition assays, since proteases are a major therapeutic target. These assays will utilize a highly sensitive chemiluminescence detection method. In Phase I, 384 well sections of the tapes will be placed in an appropriate adapter and luminescence will be detected using a 384 well luminometer. In Phase II, additional chemiluminescence and fluorescence based assays, and instrumentation to automate the assay process will be developed. This system will meet the need in the pharmaceutical industry for UHTS systems, which require only minute amounts of valuable compound libraries. PROPOSED COMMERCIAL APPLICATIONS: Pre-clinical drug discovery is nearly a six billion dollar market. It requires the screening of many hundreds of thousands of compounds per project and limited compound collections must be used for multiple projects. The proposed ultra-high throughput system is aimed at meeting those requirements by providing a low volume assay system that will be capable of screening over 100,000 compounds per day.