Boehringer Ingelheim Pharmaceuticals, Inc.

Mark E Labadia

Anthony S Prokopowicz

Scott E Jakes

Jessi Marie Wildeson

Martha Priscilla Brown

Jessi Wildeson Jones

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 Kfor the inhibitor compound is derived based on the Kof 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.

Fluorescent probes for use in protein kinase inhibitor binding assay

The invention provides methods relating to a novel 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 Kfor the inhibitor compound is derived based on the Kof 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.

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Brookfield, CT, United States of America

Mark E Labadia