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Rothenaigner, I. ; Hadian, K.

Brief Guide: Experimental strategies for high-quality hit selection from small-molecule screening campaigns.

SLAS Discov. 26, 851-854 (2021)
Verlagsversion DOI PMC
Open Access Gold (Paid Option)
Creative Commons Lizenzvertrag
Small-molecule screening is a powerful approach to identify modulators of either specific biological targets or cellular pathways with phenotypic endpoints. A myriad of assay technologies are available to assess the activity of enzymes, monitor protein-protein interactions, measure transcription factor activity in reporter assays, or detect cellular features and activities using high-content imaging. A common challenge during small-molecule screening is, however, the presence of hit compounds generating assay interference, thereby producing false-positive hits. Thus, efforts are needed to uncover such interferences to prioritize high-quality hits for further analysis. This process encompasses (1) computational approaches to flag undesirable compounds, and (2) the use of experimental approaches like counter, orthogonal, and cellular fitness screens to identify and eliminate artifacts. In this brief guide, we provide an overview for first-time users, highlighting experimental screening strategies to prioritize high-quality bioactive hits from high-throughput screening/high-content screening (HTS/HCS) campaigns.
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Publikationstyp Artikel: Journalartikel
Dokumenttyp Review
Korrespondenzautor
Schlagwörter Cellular Health ; Counter Assay ; False-positive Exclusion ; High-content Screening ; High-throughput Screening ; Hit Triaging ; Orthogonal Assay; Frequent Hitters; Assay; Identification
ISSN (print) / ISBN 2472-5552
e-ISSN 2472-5560
Zeitschrift SLAS Discovery
Quellenangaben Band: 26, Heft: 7, Seiten: 851-854 Artikelnummer: , Supplement: ,
Verlag Sage
Verlagsort Thousand Oaks, Calif.
Nichtpatentliteratur Publikationen
Begutachtungsstatus Peer reviewed
Institut(e) Institute of Molecular Toxicology and Pharmacology (TOXI)