Table 4 Ebselen diselenide derivatives as SARS-CoV-2 nsp14 inhibitors. IC50 was determined in the Py-FLINT assay. Conditions: probe [S1] = 1 μM, SAM cosubstrate [S2] = 20 μM, nsp14 [E] = 40 nM. For inhibition curves see Supplementary Information Fig. S3.

From: Ebselen derivatives inhibit SARS-CoV-2 replication by inhibition of its essential proteins: PLpro and Mpro proteases, and nsp14 guanine N7-methyltransferase

IC50 (µM)

IC50 (µM)

R:

SARS-CoV-2

nsp14

R:

SARS-CoV-2

nsp14

Ebselen

0.35 ± 0.03

29

4.5 ± 1.3

24

0.21 ± 0.02

30

11.5 ± 1.4

25

0.12 ± 0.01

31

0.91 ± 0.10

26

1.82 ± 0.32

32

12.1 ± 1.1

27

0.18 ± 0.04

33

1.06 ± 0.05

28

0.58 ± 0.04

34

2.10 ± 0.58

  1. Significant values are in bold.
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