Millennium Pharmaceuticals Limited

Benjamin Stone Amidon

Alexandra E Gould

Paul D Greenspan

Sean J Harrison

Christine Ellen Bulawa

David P Cardin

Disclosed are chemical entities that inhibit Uba6, each of which is a compound of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R*is &#x2014;H or &#x2014;CH; and Y is Formula (II) or Formula (III), wherein Ris &#x2014;H, &#x2014;CHor Calkyloxycarbonyl; and R, Rand Rare defined herein; pharmaceutical compositions comprising the chemical entities; and methods of using the chemical entities. These chemical entities are useful for treating disorders, particularly cell proliferation disorders, including cancers.

Indole substituted pyrrolopyrimidinyl inhibitors of Uba6

Disclosed is a yeast cell whose genetic complement includes an inactive allele of the yeast CDC7 gene, a first nucleic acid that encodes a mammalian Cdc7 protein, and a second nucleic acid that encodes a mammalian Dbf4 protein. The yeast cell is dependent on the mammalian Cdc7 and Dbf4 proteins for viability. The yeast cell can be used to identify potential anti-proliferative agents by virtue of their inhibition of the mammalian Cdc7 and Dbf4 proteins. In some embodiments, a control yeast cell which does not depend on Cdc7 for viability is used in a secondary screen.

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Arlington, MA, United States of America

Benjamin Stone Amidon