Table 5.
Binding Affinities of Selected Active Compounds for the BET Bromodomains and Non-BET Protein CBP (IC50, nM)a
| bromodomains | 1 | 3 | 50 | 52 | 53 |
|---|---|---|---|---|---|
| BRD4 BD1 | 1,151 ± 132 | 92 ± 11 | 138 ± 14 | 90 ± 9 | 93 ± 12 |
| BRD4 BD2 | 132 ± 14 | 62 ± 9 | 746 ± 89 | 1,093 ± 136 | 1,168 ± 152 |
| BRD2 BD1 | 5,697 ± 675 | 77 ± 8 | 1,254 ± 143 | 835 ± 117 | 742 ± 89 |
| BRD2 BD2 | 246 ± 35 | 54 ± 7 | 1,207 ± 129 | 1,308 ± 149 | 1,376 ± 157 |
| BRD3 BD1 | 3,878 ± 437 | 79 ± 11 | NDb | 2,183 ± 275 | 2,104 ± 272 |
| BRD3 BD2 | 217 ± 26 | 72 ± 8 | NDb | 1,996 ± 257 | 2,018 ± 214 |
| BRDT BD1 | 5,027 ± 639 | 178 ± 19 | NDb | 2,416 ± 284 | 2,217 ± 253 |
| BRDT BD2 | 696 ± 81 | 224 ± 26 | NDb | 1,902 ± 225 | 1,987 ± 226 |
| CBP | >10000 | 9,546 ± 673 | NDb | >10000 | >10000 |
a
Binding affinity was measured using a TR-FRET assay with the isolated bromodomain. Reported as mean of three separate assay runs and IC50 values are calculated using Four Parameters Regression method (https://www.aatbio.com/tools/ic50-calculator/).
b
ND, not determined.