Small-Molecule Inhibitors of GSK-3: Structural Insights and Their Application to Alzheimer's Disease Models

Table 11

Examples of 1,2,5-oxadiazole inhibitors with biological activity against GSK-3, selectivity, X-ray, and reference.

No.	R^1	R^2	IC50 (nM)	Kinase panel	In vivo	X-ray	Year/lit.
103	NH2		β: 410	—	—	—	2003 [123]
104	NH2		β: 100	β + 31	Yes	—	2003 [123]
105	NH2		β: 1160	β + 31	Yes	—	2003 [123]
106	NH2		β: 280	β + 31	Yes	—	2003 [123]
107	NH2		β: 210	β + 3	—	—	2009 [124]
108	NH2		β: 240	β + 3	—	—	2009 [124]
109	NH2		β: 290	β + 3	—	—	2009 [124]

β: GSK-3β.