Table 13.
Examples of bromodomain inhibitors
| Inhibitor | Structure | Potency | Reported target | Reference |
|---|---|---|---|---|
| Compound 2 |  |
1.6 µM | KAT2B | (Zeng et al., 2005) |
| Ischaemin (MS120) |  |
19 µM | CREBBP | (Borah et al., 2011) |
| I-BET-762 (GSK525762A) |  |
50–60 nM | BRD2, BRD3, BRD4, BRDT | (Nicodeme et al., 2010) |
| I-BET-151 (GSK1210151A) |  |
250–800 nM | BRD2, BRD3, BRD4, BRDT | (Seal et al., 2012) |
| JQ1 |  |
50–90 nM | BRD2, BRD3, BRD4, BRDT | (Filippakopoulos et al., 2010) |
| RVX-208 |  |
40 nM – 3 µM | BRD2, BRD3, BRD4, BRDT | (Khmelnitsky et al., 2013) |