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Drug Discov Today. 2010 Sep;15(17-18):749-56. doi: 10.1016/j.drudis.2010.06.006. Epub 2010 Jun 18.

Drug profiling: knowing where it hits.

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  • 1Conway Institute of Biomolecular & Biomedical Research, School of Medicine and Medical Science, University College Dublin, Belfield, Dublin 4, Ireland.


Off-target hits of drugs can lead to serious adverse effects or, conversely, to unforeseen alternative medical utility. Selectivity profiling against large panels of potential targets is essential for the drug discovery process to minimize attrition and maximize therapeutic utility. Lately, it has become apparent that drug promiscuity (polypharmacology) goes well beyond target families; therefore, lowering the profiling costs and expanding the coverage of targets is an industry-wide challenge to improve predictions. Here, we review current and promising drug profiling alternatives and commercial solutions in these exciting emerging fields.

Copyright © 2010 Elsevier Ltd. All rights reserved.

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