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

Table 12

Examples of 1,3,4-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.
110			β: 65	—	—	3F7Z	2009 [125]
111			β: 44	—	—	—	2009 [125]
112			β: 3.1	—	—	—	2009 [125]
113			β: 3.5	—	—	—	2009 [125]
114			β: 2.3	β + 23	Yes	3F88	2009 [125]
115	Me		β: 140	—	—	—	2009 [126]
116	Me		α: 37; β: 34 (53)^a	β + 22	Yes	3GB2	2009, 2011 [126, 127]
117	Me		β: 190	—	—	—	2009 [126]
118	Me		β: 20	β + 22	Yes	—	2009 [126]
119			β: 17	β + 1	Yes	1UV5^b	2010 [128]
120			β: 53	—	—	—	2010 [128]
121			β: 18	—	—	—	2010 [128]
122			β: 7	—	—	1UV5^b	2010 [128]

^aResults of different publications; ^bdocking studies, PDB code (n.d.: not denoted); β: GSK-3β.