Table 3 TKB245 demonstrates potent SARS-CoV-2^WK521 antiviral activity and favorable cytotoxicity profiles

	TKB245 (µM)		TKB248 (µM)		Nirmatrelvir (µM)		Ensitrelvir fumarate (µM)		Molnupiravir (µM)
Cell line	EC₅₀	CC₅₀	EC₅₀	CC₅₀	EC₅₀	CC₅₀	EC₅₀	CC₅₀	EC₅₀	CC₅₀
VeroE6	0.03 ± 0.02	>100	0.22 ± 0.08	>100	1.02 ± 0.34	>100	0.11 ± 0.05	>100	0.35 ± 0.06	>100
VeroE6 + 2 µM CP100356	0.001 ± 0.001	>100	0.03 ± 0.03	>100	0.025 ± 0.002	>100	-		-	-
HeLa-ACE2-TMPRSS2	0.021 ± 0.008	>100	0.16 ± 0.075	>100	0.24 ± 0.05	>100	0.20 ± 0.03	>100	0.32 ± 0.07	>100
A549-ACE2-TMPRSS2	0.0027 ± 0.0002	>100	0.199 ± 0.005	>100	0.017 ± 0.003	>100	-	-	-	-
HepG2	-	>200	-	>200	-	>200	-	-	-	-

TKB245 inhibited SARS-CoV-2^WK521 replication in VeroE6, HeLa-ACE2-TMPRSS2, and A549-ACE2-TMPRSS2 cells. A P-glycoprotein inhibitor, CP-100356 (efflux inhibitor, EI, 2 µM), was added to inhibit the P-glycoprotein–mediated efflux of TKB245 in VeroE6 cells. Cytotoxicity of TKB245 was evaluated in noninfected cells and was determined with a water-soluble MTT assay. Data from three-four independent assays are shown as arithmetic means (µM) ± 1 S.D. Source data are provided as a Source Data file.

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