| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1365048 | Bioorganic & Medicinal Chemistry Letters | 2008 | 7 Pages |
Abstract
Checkpoint kinase-1 (Chk1, CHEK1) is a Ser/Thr protein kinase that mediates the cellular response to DNA-damage. A novel class of 2-ureido thiophene carboxamide urea (TCU) Chk1 inhibitors is described. Inhibitors in this chemotype were optimized for cellular potency and selectivity over Cdk1.
Graphical abstractA series of thiophene carboxamide checkpoint kinase inhibitors (3) were discovered through HTS and optimized for cellular potency (12n).Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
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Authors
James W. Janetka, Lynsie Almeida, Susan Ashwell, Patrick J. Brassil, Kevin Daly, Chun Deng, Thomas Gero, Roberta E. Glynn, Candice L. Horn, Stephanos Ioannidis, Paul Lyne, Nicholas J. Newcombe, Vibha B. Oza, Martin Pass, Stephanie K. Springer, Mei Su,