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. 2024 Jan 10;15(2):250–257. doi: 10.1021/acsmedchemlett.3c00498

Table 1. Inhibitory Activity of Ligand 1′, PROTACs 1 and 2,a and of Representative SARS-CoV-2 Inhibitors against 3CLPro.

compd IC50 (μM)
Ligand 1′ 1.35 ± 0.34
PROTAC 1 21.2 ± 5.8
PROTAC 2 N/A
representative 3CLProinhibitors reported IC50 (μM)
GC-37641,44,45 0.19 ± 0.04
GC-37345 0.40 ± 0.05
Nirmatrelvir46 0.051 ± 0.01
Boceprevir47,48 5.40 ± 1.53
Dalcetrapib-thiol49 14.4 ± 3.3
a

Mean from three different assays, errors were in the range of 5–10% of the reported values; IC50 values were retrieved from dose–response assays as the concentration of compound required for 50% inhibition, as estimated by nonlinear correlation using GraphPad Prism software.