Table 2 TKB245 exerts potent activity against various SARS-CoV-2 variants

From: Identification of SARS-CoV-2 Mpro inhibitors containing P1’ 4-fluorobenzothiazole moiety highly active against SARS-CoV-2

 

Against SARS-CoV-2 variants EC50 (µM)

       

KTKYX00012/ο

TKYVS2037/ο

TKYTS14631/ο

UT-NCD1757-1N/ο

Compound

WK521

QHN001/α

TY8-612/β

Y7-501/γ

K1734/δ

5356/k

BA.1

BA.2

BA.5

BA.2.75

TKB245

0.03 ± 0.02

0.042 ± 0.042

0.028 ± 0.009

0.056 ± 0.045

0.030 ± 0.003

0.020 ± 0.002

0.014 ± 0.001

0.045 ± 0.014

0.019 ± 0.005

0.049 ± 0.005

TKB248

0.22 ± 0.08

0.300 ± 0.001

0.287 ± 0.005

0.228 ± 0.061

0.273 ± 0.036

0.180 ± 0.035

0.282 ± 0.043

0.210 ± 0.087

0.070 ± 0.008

0.430 ± 0.091

Nirmatrelvir

0.94 ± 0.21

1.980 ± 0.559

1.498 ± 0.240

2.494 ± 0.292

1.499 ± 0.078

1.658 ± 0.606

1.047 ± 0.061

1.240 ± 0.125

1.080 ± 0.150

0.967 ± 0.135

  1. Anti-SARS-CoV2 activity by compounds was evaluated with RT-qPCR of viral RNA from culture medium of SARS-CoV2-exposed VeroE6 cells. Each EC50 value was calculated as previously published15. Data from three-four independent assays are shown as arithmetic means ± 1 S.D. Source data are provided as a Source Data file.
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