Table 1.

Inhibition of human α-thrombin by sulfated benzofurans.^a

	logIC50	IC50 (μM)	HS	ΔYa (%)
9a	−6.17 ± 0.03	0.67 ± 0.04b	1.5 ± 0.2	79 ± 9
9b	−5.69 ± 0.13	2.0 ± 0.6	1.0c	39 ± 2
9c	−3.78 ± 0.07	165 ± 25	2.1 ± 0.5	~94d
9d	–	>500	NAe	NA
9f	−5.23 ± 0.11	5.8 ± 1.5	2.3 ± 1.2	43 ± 3
9g	~ −4.0d	~ 99d	UDf	~ 26d
12	–	>500	NA	NA
13	−4.51 ± 0.06	31 ± 4	3.5 ± 1.2	53 ± 4
14	−4.18 ± 0.17	66 ± 25	1.0c	49 ± 5
17	−3.80 ± 0.15	158 ± 55	1.0c	62 ± 16
23	−3.81 ± 0.13	154 ± 45	1.2 ± 0.3	~ 91d

^aLogistic equation 1 was used to fit the dose-dependence of the residual thrombin activity to obtain logIC₅₀, HS, Y₀, and Y_M values for inhibition in 20 mM Tris-HCl buffer, pH 7.4, containing 100 mM NaCl, 2.5 mM CaCl₂, and 0.1% PEG8000 at 25 °C (see ‘Experimental Procedures’). ΔY = Y_M − Y₀.

^bErrors represent ± 1 S. E.

^cHS was fixed to 1.0 to define the inhibition parameters better.

^dApproximate value because either HS, Y_M or Y₀ was not defined well.

^eNot applicable.

^fUndefined.