Table 2.
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 |