Table 2.

Described inhibitors for TMPRSS2 and related TLPs

Name and structure	Ki (nM) in enzymatic assay					Antiviral activity in cell culture	References
	TMPRSS2	HAT	Matriptase	Thrombin	FXa
Peptidomimetic inhibitors
Inhibitor ‘92’	0.9	1700	NA	20	50	Inhibits H1N1 and H3N2 replication in Calu-3 cells	[46•]
Inhibitor ‘5′	20	19	55	3.5	2.4	Inhibits H1N1 and H3N2 replication in HAT-expressing MDCK cells	[47]
Inhibitor ‘1′	NA	0.0084	0.000011	0.637	NA	Inhibits H1N1 replication in Calu-3 cells	[28, 49]
Non-peptidomimetic inhibitors
Bromhexine	0.8	NA	59	>100	NA	Nonea	[52]
0591-5329	0.9	NA	75.3	>100	NA	Nonea	[52]
4401-0077	2.7	NA	>100	>100	NA	Nonea	[52]
4554-5138	1.4	NA	78.3	>100	NA	Nonea	[52]
8008-1235	2.6	NA	>100	>100	NA	Nonea	[52]

NA, not available.

^aLaporte, unpublished data.