Table 1. Thermodynamic Parameters of Formation of Binary and Ternary Complexes between VCB, BRD9 Bromodomain, and Compound 5 Measured by Isothermal Titration Calorimetry (ITC)a.
| syringe | cell | Kd (nM) | ΔH (kcal/mol) | ΔG (kcal/mol) | –TΔS (kcal/mol) | N | α |
|---|---|---|---|---|---|---|---|
| BRD9-BD | 5 | 15 ± 3 | –12.5 ± 0.4 | –10.7 ± 0.1 | 1.8 ± 0.5 | 0.753 ± 0.004 | |
| VCB | 5 | 33 ± 2 | –15.2 ± 0.1 | –10.2 ± 0.1 | 4.9 ± 0.1 | 0.60 ± 0.01 | |
| BRD9-BD:5 | 73 ± 2 | –6.4 ± 0.1 | –9.7 ± 0.1 | –3.3 ± 0.1 | 0.75 ± 0.05 | 0.45 |
a
All ITC titrations were performed at 25 °C. Values reported are the mean ± SEM from at least three independent measurements (n ≥ 3).