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High-Throughput 2018, 7(1), 4;

Early Probe and Drug Discovery in Academia: A Minireview

HTS Laboratory, University of Kansas, Lawrence, KS 66045, USA
Received: 27 December 2017 / Revised: 1 February 2018 / Accepted: 2 February 2018 / Published: 9 February 2018
PDF [1577 KB, uploaded 22 February 2018]


Drug discovery encompasses processes ranging from target selection and validation to the selection of a development candidate. While comprehensive drug discovery work flows are implemented predominantly in the big pharma domain, early discovery focus in academia serves to identify probe molecules that can serve as tools to study targets or pathways. Despite differences in the ultimate goals of the private and academic sectors, the same basic principles define the best practices in early discovery research. A successful early discovery program is built on strong target definition and validation using a diverse set of biochemical and cell-based assays with functional relevance to the biological system being studied. The chemicals identified as hits undergo extensive scaffold optimization and are characterized for their target specificity and off-target effects in in vitro and in animal models. While the active compounds from screening campaigns pass through highly stringent chemical and Absorption, Distribution, Metabolism, and Excretion (ADME) filters for lead identification, the probe discovery involves limited medicinal chemistry optimization. The goal of probe discovery is identification of a compound with sub-µM activity and reasonable selectivity in the context of the target being studied. The compounds identified from probe discovery can also serve as starting scaffolds for lead optimization studies. View Full-Text
Keywords: high-throughput screening; assay development; small molecules; drug and probe discovery high-throughput screening; assay development; small molecules; drug and probe discovery

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Roy, A. Early Probe and Drug Discovery in Academia: A Minireview. High-Throughput 2018, 7, 4.

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