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. Author manuscript; available in PMC: 2023 Sep 6.
Published in final edited form as: ACS Infect Dis. 2022 Jun 1;8(6):1191–1203. doi: 10.1021/acsinfecdis.2c00172

Table 4.

Compounds having confirmed inhibition of TMPRSS2 in both biochemical assays and in the cellular assay.

Biochemical (fluorogenic) Biochemical (fluorogenic counterassay) Biochemical (mass spectrometry) SARS-CoV-2 PP (Delta) SARS-CoV-2 PP (WA1 + D614G) Calu-3 (cytotoxicity)
Compound Name Structure AC50 (μM) Max Response (%) AC50 (μM) AC50 (μM) Max Response (%) AC50 (μM) Max Response (%) AC50 (μM) Max Response (%) Status for Human Use
Nafamostat mesilate graphic file with name nihms-1922421-t0006.jpg 0.00011 −1.9 0.0002 0.0014 −100% 0.0064 −100% N/D 0% Approved
Camostat graphic file with name nihms-1922421-t0007.jpg 0.0062 −5 0.0055 0.059 −92% 0.05 −95% N/D 0% Approved
PCI-27433 graphic file with name nihms-1922421-t0008.jpg 1.8 61.3 1.4 15.85 −66% 16.5 −66% N/D 0% Clinical Trials
Cmpd 92 (Meyer) graphic file with name nihms-1922421-t0009.jpg 0.41 −5.6 0.28 3.98 92% 2.05 −70% N/D 0% N/T
Cmpd 114 (Meyer) graphic file with name nihms-1922421-t0010.jpg 0.57 −6.2 0.26 15.27 99% 5.35 −88% N/D 0% N/T
Otamixaban graphic file with name nihms-1922421-t0011.jpg 1.64 −1 1.23 18.01 54% 20 −50% N/D 0% Clinical Trials
*

N/D = Not Detected

*

N/T = Not Tested