Table 3. Effect of Nitrogen Atom(s) on BRD4-D1 Affinity.
compound | N atom location | BRD4-D1 IC50 (μM)a |
---|---|---|
22 | 1,2 | 9.7 ± 1.8 |
23 | none | 12 ± 1.1 |
5 | 1 | 3.6 ± 0.05 |
24 | 2 | 97 ± 2.6 |
25 | 3 | >100 |
26 | 4 | >100 |
IC50 values were determined by fluorescence anisotropy. Data represents the mean and standard deviation of three independent trials.