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Binding of I-BET151 and its derivatives to bromodomain proteins measured by ITC. The error of the fit of the binding isotherm is reported. ND: not determined.
| ID | hBRD4, ITC KD | TbBdf2, ITC KD | TbBdf3, ITC KD |
|---|---|---|---|
|
| |||
| I-BET151 | 0.32 ± 0.10 μM | 94 ± 18 μM | 68 ± 9 μM |
| AP-08-188 | 0.68 ± 0.15 μM | No binding | 87 ± 21 μM |
| AP-09-187 | 1.5 ± 0.3 μM | No binding | 100 ± 70 μM |
| AP-09-008 | ND | ND | ND |
| AP-09-191 | No binding | 66 ± 11 μM | 22 ± 11 μM |
