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. 2020 Jul 2;11(8):876–884. doi: 10.1039/d0md00154f

Table 2. Examples of covalent inhibitors in clinical trials.

No. Structure and name Target (therapeutic) Warhead Clinical stage
1 Inline graphicPRN1008 BTK inhibitor α,β-Unsaturated carbonyl III
2 Inline graphicEvobrutinib BTK inhibitor α,β-Unsaturated carbonyl III
3 Inline graphicAMG510 KRAS inhibitor α,β-Unsaturated carbonyl II
4 Inline graphicPoziotinib EGFR inhibitor α,β-Unsaturated carbonyl II
5 Inline graphicPF-06651600 JAK3 inhibitor α,β-Unsaturated carbonyl II
6 Inline graphicRemibrutinib BTK inhibitor α,β-Unsaturated carbonyl II
7 Inline graphicFutibatinib FGFR inhibitor α,β-Unsaturated carbonyl II
8 Inline graphicTirabrutinib BTK inhibitor α,β-Unsaturated propargylamide II
9 Inline graphicSpebrutinib BTK inhibitor α,β-Unsaturated carbonyl II