The development of potent and selective bisarylmaleimide GSK3 inhibitors

3-(Imidazo[1,2-a]pyridin-3-yl)-, its aza-analogs, and 3-(pyrazolo[1,5-a]pyridin-3-yl)-4-(2-acyl-(1,2,3,4-tetrahydro[1,4]diazepino[6,7,1-hi]indol-7-yl))maleimides are very potent inhibitors of GSK3 (⩽5 nM) with >160 to >10,000-fold selectivity versus CDK2/4 and PKCβII.