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. Author manuscript; available in PMC: 2022 Jan 25.
Published in final edited form as: J Med Chem. 2017 Jan 5;60(2):641–657. doi: 10.1021/acs.jmedchem.6b01474

Table 3.

Selectivity of NSGM 2 and Its Precursor 1j against a Panel of Related Serine Proteasesa

inhibitor enzyme IC50 b (μM) ΔY b,c (%) SId
2 plasmin 7.2 ± 0.6 98 ± 5
thrombin 156 ± 14 77 ± 8 22
FXa ~505 ND 70
FXIa 180 ± 20 93 ± 11 26
FIXa >2000 ND >277
FXIIa >1000 ND >138
trypsin >440 ND >61
chymotrypsin 196 ± 39 92 ± 9 27
1j plasmin 116 ± 9 111 ± 8
thrombin 267 ± 28 91 ± 11 2
FXa 212 ± 30 104 ± 17 2
FXIa 208 ± 32 109 ± 16 2
a

Direct inhibition of human enzymes was measured in appropriate Tris-HCl buffers of pH 7.4 at 37 °C. Inhibition was monitored spectrophotometrically. See Experimental Part for details.

b

Selectivity index.

c

Errors represent ±1 SE.

d

Not determined.