Table 2.
Compd | X | β EC50 nMa | α EC50 nMa | Fold selectivity for β over αb | γ EC50 nMa | Fold selectivity for β over γb | cLogPd |
---|---|---|---|---|---|---|---|
ATRA | - | 1.9 | 1.2 | 0.9 | 0.6 | 0.5 | |
5 | 1.5 | 18c | 28 | 12 | 19 | 5.1 | |
8 | 4200 | 18 | 17 | 0.0043 | 0.0041 | 7.2 | |
9 | 1.4 | 4 | 3 | 2.8 | 2.1 | 7.2 | |
10 | 1.9 | 26 | 11 | 13 | 5.6 | 5.3 | |
11 | 2.5 | 19 | 5.3 | 7.6 | 2 | 5.3 | |
12 | 3.4 | 30 | 6.3 | 9 | 2 | 5.8 | |
13 | 11 | 114 | 83 | 10 | 7.5 | 4.1 |
See Table 1.