Table 1. Validation of the Halogen Bonding Interaction in Compound 2.
ID | R | IC50 (nM)a | Ki (nM)b |
---|---|---|---|
3 | -H | 1641.3 ± 221.2 | 151.3 ± 20.7 |
4 | -F | 403.4 ± 53.1 | 53.3 + 13.7 |
5 | -Cl | 46.9 ± 4.8 | 6.3 ± 0.9 |
2 | -Br | 35.4 ± 1.7 | 5.8 ± 1.2 |
6 | -I | 23.3 ± 3.7 | 1.7 ± 0.4 |
7 | -CH3 | 459.4 ± 118.2 | 19.8 ± 4.8 |
8 | –OH | n.a.c | 313.5 ± 43.0 |
The IC50 values were determined for each compound (mean ± SEM) from two independent tests.
The Ki values were determined for each compound (mean ± SEM) from three independent tests.
Not active, <50% inhibition at 10 μM concentration.