Inactivation rates of 5 covalent BTK inhibitors.35 The corresponding free energy of activation ΔG‡ values (calculated using transition state theory) are shown for comparison.
| Inhibitor | BTK inactivation rate, kinact (s−1) | Free energy of inactivation ΔG‡ (kcal mol−1) |
|---|---|---|
| Ibrutinib | 2.66 × 10−2 | 19.6 |
| Acalabrutinib | 5.59 × 10−3 | 20.5 |
| Zanubrutinib | 3.33 × 10−2 | 19.5 |
| Spebrutinib | 1.36 × 10−2 | 20.0 |
| Tirabrutinib | 9.72 × 10−2 | 20.2 |