Reducing False Positives through the Application of Fluorescence Lifetime Technology: A Comparative Study Using TYK2 Kinase as a Model System

The predominant assay detection methodologies used for enzyme inhibitor identification during early-stage drug discovery are fluorescence-based. Each fluorophore has a characteristic fluorescence decay, known as the fluorescence lifetime, that occurs throughout a nanosecond-to-millisecond timescale....

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Veröffentlicht in:	SLAS discovery 2021-06, Vol.26 (5), p.663-675
Hauptverfasser:	Greenhough, Luke A., Clarke, Gabriella, Phillipou, Alexander N., Mazani, Faith, Karamshi, Bhumika, Rowe, Sam, Rowland, Paul, Messenger, Cassie, Haslam, Carl P., Bingham, Ryan P., Craggs, Peter D.
Format:	Artikel
Sprache:	eng
Schlagworte:	Drug Discovery - methods Drug Discovery - standards Drug Evaluation, Preclinical - methods Drug Evaluation, Preclinical - standards fluorescence lifetime technology (FLT) Fluorescence Resonance Energy Transfer Fluorescent Dyes high-throughput screening (HTS) High-Throughput Screening Assays Mass Spectrometry RapidFire mass spectrometry (RF-MS) Reproducibility of Results Sensitivity and Specificity small-molecule screening time-resolved fluorescence resonance energy transfer (TR-FRET) TYK2 Kinase - antagonists & inhibitors TYK2 Kinase - chemistry
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