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. 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 2.

SAR of cyclo[Asp-P3-Lys] peptides based on 18 with P3 group variations.

Compd Ac-cyclo[Asp-P3-Lys]-
Arg-kbt
HGFA
IC50
(nM)
Matriptase
IC50 (nM)
Hepsin
IC50
(nM)
Factor
Xa IC50
(nM)
Thrombin
IC50 (nM)
18 Leu 8610 2.2 11 2048 8140
22 Gly 4,312 6.3 5.9 6183 >20,000
23 Ala 13,705 2.5 8.8 >20,000 >20,000
24 Val 1,832 3.2 7.8 1514 >20,000
25 Asn 15,837 3.8 10 4653 >20,000
26 Gln 16,108 7.7 22 >20,000 >20,000
27 Thr 11,777 3.7 5.8 13341 >20,000
28 Met 3,240 1.0 5.9 1395 18456
29 Phe 3,173 3.4 17 1530 1090
30 Tyr >20,000 6.1 44 16962 >20,000
32 Ac-cyclo[Asp-Leu-Lys(N-Me)]-Arg-kbt 12,000 1.1 15 678 17100