Table 1.

Biochemical profile of active site bridging inhibitors of human tryptase

	Compound	Tryptase Ki, nM	Selectivity
			Trypsin	Plasmin
X = 3-SO2	8a: n = 7	800	×15	×12
	8b: n = 6	105	×34	×25
	8c: n = 5	80	×31	×12
	8d: n = 4	30	×60	×2
	8e: n = 3	15	×180	×49
	8f: n = 2	27	×192	×74
	17	98	×31	×102
X = 4-SO2	9a: n = 7	1,500	—	—
	9b: n = 6	3,150	—	—
	9c: n = 5	250	×32	×40
	9d: n = 4	12,500	—	—
	9e: n = 3	800	×5	×8
	9f: n = 2	1,500	—	—
X = 3-CO	10a: n = 7	78	×15	×110
	10b: n = 6	10	×170	×1,000
	10c: n = 5	7	×130	×1,000
	10d: n = 4	9	×120	×1,400
	10e: n = 3	20	×120	×1,400
	10f: n = 2	350	×6	×131
X = 4-CO	11a: n = 7	1	×1,500	×4,000
	11b: n = 6	<0.01	×650,000	×800,000
	11c: n = 5	<0.01	×100,000	×450,000
	11d: n = 4	0.20	×7,500	×60,000
	11e: n = 3	0.50	×5,000	×23,000
	11f: n = 2	50	×28	×130
	18	375	×2	×27