Skip to main content
. Author manuscript; available in PMC: 2022 Jul 22.
Published in final edited form as: J Med Chem. 2021 Dec 13;64(24):18158–18174. doi: 10.1021/acs.jmedchem.1c01671

Table 1.

Enzyme inhibition activity of cycloamide ketobenzothiazole (kbt) inhibitors.

Compd Structure HGFA
IC50
(nM)		 Matriptase
IC50 (nM)		 Hepsin
IC50
(nM)		 Factor Xa
IC50 (nM)		 Thrombin
IC50 (nM)
15 Ac-cyclo[Lys-Leu-Asp]-Arg-kbt >20,000 20 25 1161 >20,000
16 Ac-cyclo[Lys-Leu-Glu]-Arg-kbt 4,466 4.4 1.7 723 >20,000
17 Ac-cyclo[Lys-Arg-Glu]-Arg-kbt 5046 0.13 0.08 155 >20,000
18 Ac-cyclo[Asp-Leu-Lys]-Arg-kbt 8610 2.2 11 2048 8140
19 Ac-cyclo[Glu-Leu-Lys]-Arg-kbt >20,000 3.1 8.4 1714 >20,000
20 Ac-cyclo[Asp-Leu-Lys]-Arg-kbt-[Val]-amide 5378 11 5.4 118 34
21 Ac-cyclo[Asp-Leu-Lys]-Arg-kt >20,000 41 136 1363 7939