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

Table 5

Staurosporine and organometallic inhibitors with biological activity against GSK-3, selectivity, X-ray and reference.

No.	X	R^1			R^2	IC50 (nM)	Kinase panel	In vivo	X-ray	Year/lit.
31	CH2					β: 15	β + 2	—	1Q3D	1977, 1994, 2001, and 2003 [31, 56–58]
No.	R^3	R^4	R^5	R^6	R^7	IC50/𝐾𝑖 (nM)	Kinase Panel	In vivo	X-ray	Year/lit.
32	H	H			H	α: 3; β: 10	α & β + 8	Yes	—	2004 [59]
33	OH	Br			H	α: 0.35^a; β: 0.55^a	α & β + 55	Yes	—	2006 [60]
34	OH	H			F	β: 0.04^a; (0.005^b)	—	—	2JLD	2008 [61]
35	OH	H			H	α: 0.5^a; β: 1.00^a	—	—	3M1S	2011 [62]
36	H	H			NH2	α: 0.9^a; β: 6^a	α & β + 100	—	3PUP	2011 [22]

^a IC₅₀ value; ^b𝐾_𝑖 value; α: GSK-3α; β: GSK-3β.