Pyrrol-1-yl benzoic acid derivatives useful as myc inhibitors
AssigneesDana-Farber Cancer Institute, Inc., Whitehead Institute for Biomedical Research
InventorsJames E. Bradner, Michael R. McKeown, Peter B. Rahl, Richard A. Young, Jason J. Marineau
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Abstract
The present invention provides compounds of Formula (I-A), (I-B), and (I-C), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting Myc (e.g., c-Myc) activity. The present invention further provides methods of using the compounds described herein for treating Myc-mediated disorders (e.g., cancer and other proliferative diseases). The present invention also provides assays for identifying Myc inhibitors.
Claims10
A method for identifying a test compound as a Myc inhibitor comprising:
- (a) combining a nucleic acid labeled with a fluorescence donor with Myc and a Max labeled with a fluorescence acceptor in presence of the test compound;
- (b) detecting the binding of Myc and the labeled Max to the labeled nucleic acid using proximity-based luminescence detection;
- and
- (c) identifying the test compound as a Myc inhibitor when the proximity-based luminescence detection signal is decreased in the presence of the test compound relative to the proximity-based luminescence detection signal in the absence of the test compound.
Dependencies are inferred from the claim text.