A high throughput luminescent assay for glycogen synthase kinase-3beta inhibitors.
A high throughput luminescent assay based on the Kinase-Glo() system (Promega, Madison, WI) has been developed for screening against glycogen synthase kinase-3beta (GSK-3beta). Careful optimization of assay parameters allowed us to develop a robust, reproducible, and sensitive assay. Its usefulness has been demonstrated in a high throughput screening run when screening 55,000 compounds. This campaign yielded five chemical classes of hits, including several highly potent GSK-3beta inhibitors.
Baki
Andrea
A
Chemical and Biotechnological R&D, Gedeon Richter Ltd., Budapest, Hungary.
Bielik
Attila
A
Molnár
László
L
Szendrei
Györgyi
G
Keserü
György M
GM
D002460:Cell Line; D038362:Glycogen Synthase Kinase 3 / Q000037:antagonists & inhibitors*; D000071679:Glycogen Synthase Kinase 3 beta; D008163:Luminescent Measurements / Q000379:methods*; D047428:Protein Kinase Inhibitors / Q000032:analysis* / Q000737:chemistry*
D047428:Protein Kinase Inhibitors; D000071679:Glycogen Synthase Kinase 3 beta; D038362:Glycogen Synthase Kinase 3