Apparent activity in high-throughput screening: origins of compound-dependent assay interference.

By Natasha Thorne, D. Auld, James Inglese. 2010

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QSAR-Based Virtual Screening: Advances and Applications in Drug Discovery (2018, background): “However, the hit rate of HTS ranges between 0.01% and 0.1% and this highlights the frequently encountered limitation that most of the screened compounds are routinely reported as inactive toward the desired bioactivity (Thorne et al., 2010).”
Integrated Model of Chemical Perturbations of a Biological Pathway Using 18 In Vitro High-Throughput Screening Assays for the Estrogen Receptor. (2015, background): “Conceptually, assay interference (Auld et al. , 2008; Baell and Holloway, 2010; Bruns and Watson, 2012; Thorne et al. , 2010) is a phenomenon whereby assays designed to measure binding to a protein or perturbation of a given pathway may produce false signals when the target protein itself, or other…”
SLC Transporters as Therapeutic Targets: Emerging Opportunities (2015, neutral): “Use of an orange or red fluorophore as the substrate also helps to avoid this interference, as fluorescence and spurious light emissions from test compounds have been found to be more likely to occur at shorter wavelengths 50 .”