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J Med Chem. 2015 Feb 26;58(4):1976-91. doi: 10.1021/jm501921k. Epub 2015 Feb 11.

Discovery of highly potent, selective, and efficacious small molecule inhibitors of ERK1/2.

Author information

1
Array BioPharma Inc, 3200 Walnut Street, Boulder, Colorado 80301, United States.

Abstract

Using structure-based design, a novel series of pyridone ERK1/2 inhibitors was developed. Optimization led to the identification of (S)-14k, a potent, selective, and orally bioavailable agent that inhibited tumor growth in mouse xenograft models. On the basis of its in vivo efficacy and preliminary safety profiles, (S)-14k was selected for further preclinical evaluation.

PMID:
25603482
DOI:
10.1021/jm501921k
[Indexed for MEDLINE]

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