High-Throughput Screening (HTS)

The High-Throughput Screening (HTS) facility offers users the ability to screen biological targets against a library of over 100,000 unique chemical compounds in a time-efficient manner. We offer assistance with many of the early drug-discovery stages, including assay development and optimization, robotic screening, data analysis and interpretation, and hit validation. Users interested in structural biology can perform automated screening of their purified protein against hundreds of crystallization conditions.

Overview

High-Throughput Screening (HTS) is one of the most important tools in modern-day drug discovery. The premise of HTS is to automate and miniaturize the assay process, thereby significantly decreasing the cost and time commitments of screening a biological target against thousands of chemical compounds. The HTS facility houses a Tecan Freedom EVO 200 liquid handling robot that is fully capable of assembling and monitoring over 10,000 reactions, in duplicate, in a typical working day. A Tecan Genios Pro spectrophotometer is fully integrated into the robot deck to capture absorbance, fluorescence, and luminescence output from the assays. All assay plates are barcoded in order to automate data collection and to ultimately correlate activity measurements with specific library compounds. Once the screening and data collection are completed, the results are analyzed to generate a structure-activity relationship (SAR) for the screened compounds, identifying chemical trends in the compounds that affect or inhibit the biological target of interest.

The HTS facility currently offers a library of over 85,000 diverse, drug-like compounds available for screening. We are in the process of obtaining another 50,000 synthetic compounds, including over 3,000 marketed drugs, to complement our current collection. Users may contact the facility for more information on the compounds available for screening. Researchers at UIC who wish to deposit novel compounds or natural product fractions into our collection are encouraged to do so.

The Tecan Freedom Evo 200 is also ideally suited to carry out high-throughput protein crystallization. Users can typically screen over 1000 crystallization conditions in under 2 hours. Crystallization plates contain 96 wells, with 3 sitting drop compartments per well, with a 1 µL protein + 1 µL crystallization reagent capacity per compartment. Assembly of the crystallization plates is temperature controlled, and all completed plates are automatically sealed with an optically clear adhesive. The HTS facility is stocked with 12 NeXtal crystallization suites (Qiagen), with each suite containing 96 unique conditions. Users have the option to supply their own crystallization screens in 96 deep-well blocks.