Table 2.

The summary of recently reported Mpro inhibitors.

Compounds	SARS-CoV-2	SARS-CoV-2	Development Stage
	Mpro inhibition (μM)	Antiviral activity (μM)
N3	Kobs/[I]=11,300 ± 800M-1S-1	EC50 = 16.77 ± 1.7	Preclinical; not tested in animals models
Ebselen	IC50 = 0.67 ± 0.09	EC50 = 4.67 ± 0.80	In clinical trials
11a	IC50 = 0.053 ± 0.005	EC50 = 0.53 ± 0.01	Preclinical; Favorable PK in rats and low toxicity in rats and dogs
11b	IC50 = 0.040 ± 0.002	EC50 = 0.72 ± 0.09	Preclinical; Favorable PK in rats
Boceprevir	IC50 = 4.13 ± 0.61 Ki=1.18	EC50 = 1.31 ± 0.58	FDA-approved
			HCV drug
GC-376	IC50 = 0.03 ± 0.008	EC50 = 3.37 ± 1.68	Preclinical; Tested in felines
	K2/KI=40,800M-1S-1
MG-132	IC50 = 3.90 ± 1.01	NT.	Preclinical; Tested in mice
Calpain inhibitor II	IC50 = 0.97 ± 0.27	EC50 = 2.07 ± 0.76	Preclinical; not tested in animals models
	Ki=0.40
Calpain inhibitor XII	IC50 = 0.45 ± 0.06	EC50 = 0.49 ± 0.18	Preclinical; not tested in animals models
	Ki=0.13