Table 2.
Data for hybrid inhibitors against Class I and Class IIb HDACs.
Cmpd |
pIC50 a |
|||||
---|---|---|---|---|---|---|
HDAC1b |
HDAC2b |
HDAC3b |
HDAC6b |
HDAC8b,c |
HDAC10c,d |
|
PCI‐34051 (2a) |
4.33 |
<4.0 |
4.24 |
5.15 |
7.29 |
4.38 |
Tubastatin A (1c) |
5.91 |
4.89 |
5.78 |
7.70 |
5.70 |
7.90 |
3a |
6.58 |
5.65 |
5.26 |
7.74 |
7.17 |
8.59 |
3b |
6.21 |
5.27 |
5.16 |
7.12 |
6.78 |
8.55 |
3c |
6.30 |
5.38 |
4.87 |
7.32 |
6.29 |
7.91 |
3d |
6.28 |
5.33 |
5.19 |
7.65 |
7.01 |
8.49 |
3e |
6.09 |
5.15 |
5.18 |
7.35 |
7.18 |
8.52 |
3f |
7.06 |
6.14 |
5.88 |
7.82 |
7.37 |
8.47 |
3g |
6.18 |
5.02 |
5.18 |
7.52 |
7.05 |
8.40 |
[a] See Table S1 for error values associated with these calculations. [b] Enzymatic HDAC‐GloTM I/II assay. [c] Values taken from Table 1. [d] Ligand displacement FRET assay.