Table 1.
Compound | Structure | IC50, uM | Ki, uMb | k2, min−1b | k−2, min−1b |
---|---|---|---|---|---|
1 | 8e-4c | n/a | n/a | n/a | |
2a | 3d | 24 ± 6.0 | 0.3 ± 0.06 | 0.02 | |
2b | 30d | 140 ± 58 | 0.4 ± 0.1 | 4e-3 | |
3a | ≈ 35 | n/a | n/a | n/a | |
3b | ≈ 6 | n/a | n/a | n/a | |
9 | 7 | 76 ± 20 | 0.2 ± 0.03 | 0.01 | |
10 | 600 | n/a | n/a | n/a | |
15 | 5 | 310 ± 130 | 4.2 ± 1.5 | 0.13 | |
17a | >1000 | n/a | n/a | n/a | |
17b | 70 | n/a | n/a | n/a | |
DIFP | 0.12 | 6.0±1.0 | 1.0 ± 0.1 | 0.13 |