Table 1.
Entry | Structure | Compound ID | Fold-Activationa |
---|---|---|---|
1 | TM-2-51 | 12 | |
2 | TM-2-87 | 2 | |
3 | TM-2-88 | 8.4 | |
4 | TM-2-138 | 3.5 | |
5 | TM-2-97 | 5.6 | |
6 | TM-2-105 | 2.0 | |
7 | TM-2-90 | 3.3 | |
8 | TM-2-101 | 1.1 | |
9 | TM-2-104 | 4.5 | |
10 | TM-2-130 | 1.5 | |
11 | TM-2-131 | 3.0 | |
12 | TM-2-126 | 1.2 | |
13 | TM-2-125 | 1.1 | |
14 | TM-2-107 | 3.0 | |
15 | TM-2-139 | 1.0 |
Defined as the ratio of the initial rate of the HDAC-8 catalyzed reaction in the absence and presence and of 10 μM activator