The discovery of carboline analogs as potent MAPKAP-K2 inhibitors
The discovery of a series of potent, carboline-based MK2 inhibitors is described. These compounds inhibit MK2 with IC50s as low as 10nM, as measured in a DELFIA assay. An X-ray crystal structure reveals that they bind in a region near the p-loop and the hinge region of MK2a.
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Published in | Bioorganic & medicinal chemistry letters Vol. 17; no. 16; pp. 4664 - 4669 |
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Main Authors | , , , , , , , , , , , , , , , , , , , , , |
Format | Journal Article |
Language | English |
Published |
Oxford
Elsevier Ltd
15.08.2007
Elsevier |
Subjects | |
Online Access | Get full text |
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