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. 2021 Jan 28;12(15):5511–5516. doi: 10.1039/d0sc06122k

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