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

Table 10

Examples of furopyrimidine inhibitors with biological activity against GSK-3, selectivity, X-ray, and reference.

No.	R^1	R^2	R^3	IC50 (nM)	Kinase panel	In vivo	X-ray	Year/lit.
97		H		β: 5	β + 2	Yes	—	2004 [95]
98		H		β: 32	β + 2	—	—	2004 [95]
99		H		β: 23	β + 2	Yes	—	2004 [95]
100		H		β: 5	β + 24	Yes	PDB n.d.^a	2004 [95]
101			NH2	β: 30	β + 9	Yes	PDB n.d.^a	2008 [96]
102			NH2	β: 23	—	—	—	2008 [96]

^aDocking studies, PDB code (n.d.: not denoted); β: GSK-3β.