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. 2020 Oct 16;16(2):340–354. doi: 10.1002/cmdc.202000548

Table 2.

Inhibition of SARS‐CoV PLpro by isoindoline derivatives.

Compd

Structure

IC50 [μM]/%[a]

SARS‐CoV PLpro

SARS‐CoV‐2 PLpro

20

graphic file with name CMDC-16-340-g013.jpg

0.15±0.01 [21]

14 a

graphic file with name CMDC-16-340-g014.jpg

45 %[c]

n.a.[b]

14 b

graphic file with name CMDC-16-340-g015.jpg

n.d. (insoluble)[d]

14 c[e]

graphic file with name CMDC-16-340-g016.jpg

n.a.[b]

14 d

graphic file with name CMDC-16-340-g017.jpg

14±1

n.a.[b]

14 e

graphic file with name CMDC-16-340-g018.jpg

n.a.[c]

14 f

graphic file with name CMDC-16-340-g019.jpg

n.a.[b]

14 g

graphic file with name CMDC-16-340-g020.jpg

n.d. (insoluble)[d]

14 h[e]

graphic file with name CMDC-16-340-g021.jpg

2.9±0.2

7.6±0.2

14 i

graphic file with name CMDC-16-340-g022.jpg

n.a.[b]

n.a.[b]

14 j

graphic file with name CMDC-16-340-g023.jpg

32±2

n.a.[b]

14 k[e]

graphic file with name CMDC-16-340-g024.jpg

4.9±0.3

57±1

14 l

graphic file with name CMDC-16-340-g025.jpg

4.5±0.4

17

graphic file with name CMDC-16-340-g026.jpg

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.