. 2015 Dec 22;7(2):177–181. doi: 10.1021/acsmedchemlett.5b00357

Table 1. Protease Panel Results as K_i [μM].

	substitutions		matriptase	hepsin	HGFA	trypsin	thrombin	factor Xa
1	meta	X = 0	0.83	3.4	9.8	0.78	35.9	0.24
2	para	X = 0	48.9	61.2	46.5	35.4	>100	25.5
3	meta	X = 1	13.5	15.1	>100	4.8	>100	49.4
4	para	X = 1	15.4	20.8	39.6	4.8	82.2	22.8
5			40.5	53.1	54.6	5.3	>100	5.4
6	Y = 1 (SRI 31215)		0.53	0.54	0.48	0.43	11.6	0.38
7	Y = 2		0.51	2.12	1.11	2.77	>100	0.40
8a	Z = HO–		0.28	0.21	0.88	0.39	21.9	0.85
8b	Z = HOCH₂–		0.58	0.69	0.23	0.15	7.4	0.25
8c	Z = H₃CO–		0.81	0.76	2.49	0.76	>100	1.23
8d	Z = H₃COCH₂–		0.85	0.92	0.16	0.21	8.1	0.20
8e	Z = PhCH₂O–		1.54	0.76	1.92	0.55	29.7	0.92
8f	Z = PhCH₂OCH₂–		0.85	0.56	0.43	0.10	2.13	0.18
8g	Z = PhC(O)NHCH₂–		0.47	1.1	1.1	0.33	> 100	0.75
8h	Z = PhCH₂C(O)NH–		1.28	1.12	0.38	0.5	42.3	0.74
8i	Z = PhCH₂C(O)NHCH₂–		1.51	0.31	1.08	0.59	>100	1.55
8j	Z = H₃CSO₂NH–		0.33	0.72	0.35	0.42	>100	0.51
8k	Z = PhSO₂NH–		0.52	0.67	0.52	0.34	17	0.61
8l	Z = PhCH₂SO₂NH–		0.35	0.53	0.44	0.31	13.4	0.66
	HAI-1		0.0032	0.0038	0.0034	0.0008	>1.0	>1.0

Table 1. Protease Panel Results as Ki [μM].