Related Experiment Video
Updated: May 31, 2026

08:49
Identification of Mediators of T-cell Receptor Signaling via the Screening of Chemical Inhibitor Libraries
Published on: January 22, 2019
Identification of 2-(4-pyridyl)thienopyridinones as GSK-3β inhibitors
Gabriella Gentile1, Giovanni Bernasconi, Alfonso Pozzan
1Department of Medicinal Chemistry, Neuroscience Centre of Excellence of Drug Discovery, GlaxoSmithKline, Via A Fleming 4, 37135 Verona, Italy. gabriella.gentile@aptuit.com
Bioorganic & Medicinal Chemistry Letters
|July 19, 2011
Abstract:
The discovery of a novel series of 2-(4-pyridyl)thienopyridinone GSK-3β inhibitors is reported. X-ray crystallography reveals its binding mode and enables rationalization of the SAR. The initial optimization of the template for improved cellular activity and predicted CNS penetration is also presented.

