Table 4. Demonstrating Selectivity for Compound 5 and 27.
| protein target | X = O (5) | X = NH (27) |
|---|---|---|
| BRD4-D1 IC50 (μM)a | 3.6 ± 0.05 | 4.5 ± 0.35 |
| BRD4-D1 Kd (μM)b | 1.1 ± 0.63 | 1.2 ± 0.62 |
| BRD4-D2 Kd (μM)b | 0.94 ± 0.48 | 2.1 ± 1.1 |
| SMARCA2 Kd (μM)b | >100 | >100 |
| CBP (μM)b | >100 | 78 ± 48 |
| p38α Kd (μM)c | >200 | >25 |
a
IC50 values were determined by fluorescence anisotropy. Data represents the mean and standard deviation of three independent trials.
b
Kd values were determined by BROMOscan. Data represents the mean and standard error from two independent trials.
c
Kd values were determined by KINOMEscan. Data represents the mean and standard error from two independent trials.