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What do we miss? The detergent Triton-X 100 added to avoid compound aggregation can affect assay results in an unpredictable manner.

What do we miss? The detergent Triton-X 100 added to avoid compound aggregation can affect assay results in an unpredictable manner.
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Ehlert FGR, Linde K, Diederich WE,


Ehlert FGR, Linde K, Diederich WE, (click to view)

Ehlert FGR, Linde K, Diederich WE,

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ChemMedChem 2017 07 26() doi 10.1002/cmdc.201700329

Abstract

In this study we show that the detergent Triton X-100 being widely used in screening campaigns significantly reduces the binding affinities of some known specific inhibitors of HIV-1 protease and the well-established model protease endothiapepsin in a fluorescence-based assay. Surprisingly, other structurally related inhibitors remain entirely unaffected. In consequence, those compounds that were affected would most likely have been misclassified as unspecific binders although they actually are true positives, hence being considered excellent starting points for the further hit optimization.

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