Fluorescent probes for use in protein kinase inhibitor binding assay

The invention provides methods relating to a screening assay format that can be applied to broad members of the protein kinase gene family. The assay uses a series of labeled, active site probes described herein that can be displaced by an inhibitor agent. The Kd for the inhibitor compound is derive...

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Bibliographische Detailangaben
Hauptverfasser: JAKES SCOTT, BROWN MARTHA PRISCILLA, LABADIA MARK E, PROKOPOWICZ, III ANTHONY S, WILDESON JESSI MARIE
Format: Patent
Sprache:eng
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Beschreibung
Zusammenfassung:The invention provides methods relating to a screening assay format that can be applied to broad members of the protein kinase gene family. The assay uses a series of labeled, active site probes described herein that can be displaced by an inhibitor agent. The Kd for the inhibitor compound is derived based on the Kd of the probe for the kinase and the dose response of the inhibitor agent. The invention also provides active site probes suitable for use with the screening method.