Cardiff University | Prifysgol Caerdydd ORCA
Online Research @ Cardiff 
WelshClear Cookie - decide language by browser settings

From PIM1 to PI3Kδ via GSK3β: Target hopping through the kinome

Henley, Zoë A., Bax, Benjamin D. ORCID:, Inglesby, Laura M., Champigny, Aurélie, Gaines, Simon, Faulder, Paul, Le, Joelle, Thomas, Daniel A., Washio, Yoshiaki and Baldwin, Ian R. 2017. From PIM1 to PI3Kδ via GSK3β: Target hopping through the kinome. ACS Medicinal Chemistry Letters 8 (10) , pp. 1093-1098. 10.1021/acsmedchemlett.7b00296

Full text not available from this repository.


Selective inhibitors of phosphoinositide 3-kinase delta are of interest for the treatment of inflammatory diseases. Initial optimization of a 3-substituted indazole hit compound targeting the kinase PIM1 focused on improving selectivity over GSK3β through consideration of differences in the ATP binding pockets. Continued kinase cross-screening showed PI3Kδ activity in a series of 4,6-disubstituted indazole compounds, and subsequent structure–activity relationship exploration led to the discovery of an indole-containing lead compound as a potent PI3Kδ inhibitor with selectivity over the other PI3K isoforms.

Item Type: Article
Date Type: Published Online
Status: Published
Schools: Biosciences
Publisher: American Chemical Society
ISSN: 1948-5875
Date of First Compliant Deposit: 8 May 2018
Date of Acceptance: 5 September 2017
Last Modified: 23 Oct 2022 13:38

Citation Data

Cited 15 times in Scopus. View in Scopus. Powered By Scopus® Data

Actions (repository staff only)

Edit Item Edit Item