Journal of Medicinal Chemistry · 2003 · 226 citations · 8 references
Life SciencesPharmacologyDrug DiscoveryEnzymologyStructure-activity RelationshipsChemical InhibitionEnzyme InhibitionLigand BindingAssayEnzyme Inhibition AssaysEnzyme Inhibitor DiscoveryEnzyme Mechanism-based InhibitionInhibitor ScreeningInhibitor SelectivityInhibitor SpecificityMechanism-based Inhibition
The term "promiscuous" inhibitors has been coined for compounds whose inhibition mechanism involves the interaction of aggregates of many compound molecules with the target protein, rather than the binding of individual molecules. This paper demonstrates that promiscuous inhibitors can be differentiated from classical 1:1 inhibitors by the judicious use of detergents, making it possible to configure assays that significantly reduce this undesirable mechanism of inhibition without compromising assay performance.
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Emil B. Lobkovsky, Paul C. Moews, Hong Liu et al. · Proceedings of the National Academy of Sciences · 1993 · 191 citations