Table 1 Structure–activity relationship of 4-aminoquinazoline EGFR inhibitors against SARS-CoV-2 PLpro.
From: Bispecific repurposed medicines targeting the viral and immunological arms of COVID-19
| |||||||
|---|---|---|---|---|---|---|---|
Compound number | Generic name | R1 | R2 | R3 | R4 | R5 | IC50 (µM) (range) |
8 | Tarloxotinib | Br | F | N | N |
| 0.3 (0.1–0.5) |
9 | Tarloxotinib (ac) | Br | F | N | N |
| 0.3 (0.1–0.4) |
10 | Pelitinib | Cl | Cl |
|
|
| > 100* |
11 | Afatinib | Cl | Cl | N |
|
| 12 (11–16) |
12 | Dacomitinib | Cl | Cl | N |
|
| 4 (3–5) |
13 | Gefitinib | Cl | Cl | N |
|
| 7 (6–11) |
