Merck + Co., Inc.

Richard T Cummings

Jeffrey Donald Hermes

Peter J Sinclair

Joung L Goulet

Rose M Cubbon

David E Moller

Scott P Salowe

Xingfang Hong

Gaochao Zhou

Barry R Cunningham

James E Thompson

The present invention features alethal factor substrate. The substrate can be used for example to measure lethal factor activity. Preferred substrates contain one or mare detectable labels and have a sufficiently high turnover rate for applications in a high throughput screen.

Reagents for assaying Bacillus anthracis lethal factor protease

Benzimidazo[4,5-f]isoquinolinone derivatives are inhibitors of Janus protein tyrosine kinases (Jak), and as such are useful as immunosuppressants, and in the treatment of diseases including asthma, allergies, autoimmune diseases.

Benzimisazo[4,5-f]isoquinolinone derivatives

Provided is a method of identifying agonists and antagonists of nuclear receptors that comprises measuring agonist-dependent fluorescence resonance energy transfer (FRET) between a fluorescently labeled nuclear receptor or ligand binding domain and fluorescently labeled CREB-binding protein (CBP), p300, other nuclear co-activator, or binding portion thereof. The method is simple, rapid, and inexpensive. Nuclear receptors and nuclear receptor co-activators labeled with fluorescent reagents for use in the above-described method are also provided.

Assays for nuclear receptor agonists and antagonists using fluorescence resonance energy transfer

Growing community of inventors

Fanwood, NJ, United States of America

Richard T Cummings