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Title: Design of potent and selective hybrid inhibitors of the mitotic kinase Nek2 : structure−activity relationship, structural biology, and cellular activity
Authors: Innocenti, Paolo
Cheung, Kwai-Ming J.
Solanki, Savade
Mas-Droux, Corine
Rowan, Fiona
Yeoh, Sharon
Boxall, Kathy
Westlake, Maura
Pickard, Lisa
Hardy, Tara
Baxter, Joanne E.
Aherne, G. Wynne
Bayliss, Richard
Fry, Andrew M.
Hoelder, Swen
First Published: 12-Mar-2012
Publisher: American Chemical Society
Citation: Journal of Medicinal Chemistry, 2012, 55 (7), pp. 3228–3241
Abstract: We report herein a series of Nek2 inhibitors based on an aminopyridine scaffold. These compounds have been designed by combining key elements of two previously discovered chemical series. Structure based design led to aminopyridine (R)-21, a potent and selective inhibitor able to modulate Nek2 activity in cells.
DOI Link: 10.1021/jm201683b
ISSN: 0022-2623
eISSN: 1520-4804
Version: Post-print
Status: Peer-reviewed
Type: Journal Article
Rights: Copyright © 2012 American Chemical Society. All rights reserved. Deposited with reference to the publisher’s open access archiving policy.
This document is the Accepted Manuscript version of a Published Work that appeared in final form in Journal of Medicinal Chemistry, copyright © American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see
Appears in Collections:Published Articles, Dept. of Biochemistry

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