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Inhibitory potency against SARS-CoV-2 3CLpro. Optimization of R2.
| Entry | Cmpd | R1 | R2 | Inhibition (%)a | IC50 (μM) |
|---|---|---|---|---|---|
| 1 | 18b |  |
 |
< 5% | ndb |
| 2 | 13k |  |
 |
39 ± 1 | ndb |
| 3 | 13l |  |
-H | 10 ± 15 | ndb |
| 4 | 13m |  |
 |
43 ± 3 | ndb |
| 5 | 13n |  |
 |
23 ± 13 | ndb |
| 6 | 13o |  |
 |
65 ± 3 | ndb |
| 7 | 13p |  |
 |
77 ± 2 | 45.1 ± 18.3 |
| 8 | 13q |  |
 |
< 5% | ndb |
The enzyme activity was measured with 150 nM 3CLpro (114 nM after inhibitor addition) and 50 μM of each potential inhibitor with incubation time of 30 min.
not determined.
