Table 2.
Compd |
Structure |
IC50 [μM]/%[a] |
|
---|---|---|---|
SARS‐CoV PLpro |
SARS‐CoV‐2 PLpro |
||
20 |
|
0.15±0.01 [21] |
|
14 a |
|
45 %[c] |
n.a.[b] |
14 b |
|
n.d. (insoluble)[d] |
|
14 c[e] |
|
n.a.[b] |
|
14 d |
|
14±1 |
n.a.[b] |
14 e |
|
n.a.[c] |
|
14 f |
|
n.a.[b] |
|
14 g |
|
n.d. (insoluble)[d] |
|
14 h[e] |
|
2.9±0.2 |
7.6±0.2 |
14 i |
|
n.a.[b] |
n.a.[b] |
14 j |
|
32±2 |
n.a.[b] |
14 k[e] |
|
4.9±0.3 |
57±1 |
14 l |
|
4.5±0.4 |
|
17 |
|
55 % |
[a] The fluorometric assay was performed in duplicate. Data are reported as mean±standard deviation. Percentage inhibition was measured at 100 μM inhibitor concentration [b]. Compounds with inhibitory effects of less than 50 % at 100 μM compared to DMSO were labelled as not active (n.a.). [c] Percentage inhibition was measured at 10 μM inhibitor concentration with the addition of 0.005 % Brij 35. [d] IC50 values that could not be determined because of limited solubility at 100 μM under the conditions used in the assay are labelled as not determined (n.d.). [e] Compounds could only be obtained with a purity of 85–95 %. To complete the SAR study, the inhibitory effect was nevertheless tested.