- To determine how effective GC376 is at inhibiting the activity of the main protease of SARS-CoV-2, a fluorescence resolution energy transfer assay with a fluorescence protein substrate was used. It was found that GC376 has a potent ability to inhibit the activity of SARS-CoV-2 main protease, with a half-maximal inhibitory concentration of 0.89uM. 

The inhibition efficiency of GC376 on SARS-CoV-2

- IC50 is one of the most often used measures of how potent a drug can inhibit a certain biological process. IC50 is the half-maximal inhibitory concentration, meaning it is the concentration of the drug needed to inhibit 50% of the biological process. The lower the IC50, the stronger the inhibitor is.

Santa Clara University

Important Values to Define when Discussing Protease Inhibitors

Aykul S, Martinez-Hackert E. Determination of half-maximal inhibitory concentration using biosensor-based protein interaction analysis. Anal Biochem. 2016;508:97-103. doi:10.1016/j.ab.2016.06.025

Determination of half-maximal inhibitory concentration using biosensor-based protein interaction analysis

What is IC50?

The Kd is the binding constant, a unit of measurement that demonstrates how tightly a ligand binds to a protein. The lower the Kd value, the tighter the bond is between the ligand and the protein. 

What is Kd?

Te EC50 is the concentration of a drug or other compound that causes a response that is halfway between the baseline and maximum after a desired exposure time. It is commonly referred to as the concentration required to obtain 50% of the effect. It is a good empirical value of the potency of the compound.  

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