Table 1 Thrombin inhibition by 3g in the presence of HirP and UFH a .

From: Allosteric Partial Inhibition of Monomeric Proteases. Sulfated Coumarins Induce Regulation, not just Inhibition, of Thrombin

 

IC50,app (μM) b

ΔY(%) b

HS

IC50,predicted (μM) c

[HirP] (nM)

 0

0.22 ± 0.02

52 ± 2

3.3

0.24

 25

0.33 ± 0.02

58 ± 1

2.4

0.45

 187

0.33 ± 0.06

59 ± 6

2.0

0.67

[UFH] (μM)

 0

0.17 ± 0.02

56 ± 3

1.3

0.17

 11.4

0.29 ± 0.03

66 ± 5

1.7

0.29

 22.8

0.58 ± 0.03

59 ± 3

3.7

0.45

  1. aInhibition was measured at pH 7.4 and 25 °C using chromogenic substrate hydrolysis assay and analyzed using logistic equation 1 to obtain IC50,app, ΔY and HS.
  2. bErrors represent ± 1 SE obtained from non-linear regression of the inhibition profile.
  3. cCalculated using Dixon-Webb relationship (equation 3).
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