Table 2.
| |||||
---|---|---|---|---|---|
Compound | R1 | IC50 (nM)a | Compound | R2 | IC50 (nM)a |
ML148 | 19 | 14a | phenyl | 22 | |
11a | 22 | 14b | 2-OMe-phenyl | 27 | |
11b | 271 | 14c | 3-Cl-phenyl | 12 | |
11c | 48 | 14d | 3-OMe-phenyl | 19 | |
11d | 68 | 14e | 3-CF3-phenyl | 48 | |
11e | 68 | 14f | 3-iPr-phenyl | 68 | |
11f | 76 | 14g | 3-tBu-phenyl | 171 | |
11g | 1524 | 14h | 4-Me-phenyl | 19 | |
11h | 383 | 14i | 4-Cl-phenyl | 22 | |
11i | 383 | 14j | 4-OMe-phenyl | 19 | |
11j | 429 | 14k | 4-CF3-phenyl | 86 | |
11k | 961 | 14l | 4-tBu-phenyl | 54 | |
11l | 1358 | 14m | tBu | 34 | |
11m | 2710 | 14n | nBu | 68 | |
11n | 3040 |
determined using the HTS enzymatic assay and tested in triplicate.