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International Journal of Alzheimer’s Disease
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International Journal of Alzheimer’s Disease
/
2012
/
Article
/
Tab 11
/
Review Article
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
IC
50
(nM)
Kinase panel
In vivo
X-ray
Year/lit.
103
NH
2
β
: 410
—
—
—
2003 [
123
]
104
NH
2
β
: 100
β
+ 31
Yes
—
2003 [
123
]
105
NH
2
β
: 1160
β
+ 31
Yes
—
2003 [
123
]
106
NH
2
β
: 280
β
+ 31
Yes
—
2003 [
123
]
107
NH
2
β
: 210
β
+ 3
—
—
2009 [
124
]
108
NH
2
β
: 240
β
+ 3
—
—
2009 [
124
]
109
NH
2
β
: 290
β
+ 3
—
—
2009 [
124
]
β
: GSK-3
β
.