Cytokinetics, Inc.

Iconix Pharmaceuticals, Inc.

E3x Bio, Inc.

David Morgans

Bradley Paul Morgan

Pu-Ping Lu

Alex R Muci

Ving J Lee

Erica Anne Kraynack

Matthew Lynn Peterson

Todd Tochimoto

Roger Leger

Jennifer Johnston

Kurt Jarnigan

Kevin Lu

Tohru Fukuyama

Brigit Riley

Provided herein is a novel process for the preparation of an amino-pyrimidine and salts thereof. Also provided herein are novel intermediates used in this process and their preparation.

Process for the preparation of an amino-pyrimidine and intermediates thereof

The present invention provides a screen which exploits mechanism-based activity probes that specifically and covalently modify the active site cysteine thiol residue of E3 Ub ligases including, but not limited to the HECT and RBR family. The activity probes are used to screen for activators and inhibitors of E3 Ub ligases, and to interrogate the functional state of E3 Ub ligases in human disease.

Method for identifying modulators of ubiquitin ligases

Compounds of the invention have the structure D&mdash;L&mdash;A*, where L is a linking moiety that maintains D and A in a configuration compatible with FRET, D is a fluorescent donor moiety capable of causing an acceptor moiety to fluoresce by FRET, and A* is a fluorescent acceptor moiety capable of accepting energy from the donor moiety by FRET and fluorescing only after cleavage of one or more labile groups to provide acceptor A. These compounds are useful as fluorescent substrates for detection of enzymes in vivo.

Hydrolytic enzyme substrates and assay method

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Los Altos, CA, United States of America

David Morgans