Table 2 Potency of EDP-235 against select nirmatrelvir-associated variants

From: The small molecule inhibitor of SARS-CoV-2 3CLpro EDP-235 prevents viral replication and transmission in vivo

 

3CLpro

kcat/Km

IC50 [nM]

3CLpro

[nM]

[(M×s)−1]

EDP-235

Nirmatrelvir

Ancestral

10

4.5 × 104

4

4

L50F

100

3.7 × 104

3

4.4

E166H

100

9.0 ×  102

92

> 10,000

E166V

100

3.6 × 102

113

> 10,000

T21I/E166V

100

7.0 × 102

100

> 10,000

L50F/E166V

10

6.3 × 102

72

> 10,000

L50F/E166A/L167F

40

7.6 × 102

184

1200

  1. FRET assay; data are mean from three individual experiments.
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