Table 1. SAR of Indane Substitution.
compd | *stereochemistry | R1 | R2 | p300 HAT IC50 (μM) |
---|---|---|---|---|
4 | R,S | H | H | 1.6 |
9 | R,S | CN | H | 2.5 |
10 | R,S | H | CN | 27.8 |
11 | R,S | CONH2 | H | 4.86 |
12 | R,S | H | CONH2 | 17.9 |
13 | R,S | OMe | H | 1.6 |
14 | R,S | CH2 OH | H | 14.0 |
15 | R,S | cyclopropyl | H | 1.71 |
16 | R,S | NHCOMe | H | 0.78 |
17 | S | NHCO2-Me | H | 1.0 |
18 | S | NHSO2-Me | H | 16.0 |
19 | S | NHCONH-Me | H | 0.24 |