Table 1.

uPA inhibitory activity of amiloride 1 and 6-substituted amiloride derivatives 3-24, as determined by fluorogenic solution-phase enzyme inhibition assays.¹⁸ Values represent the mean ± SEM (n = 2 individual experiments).*Value taken from reference 18. K_i values were derived from IC₅₀ values using the Cheng-Prusoff method.²⁶

Compound	R	uPA Ki (nM)	Compound	R	uPA Ki (nM)
1		2,433 ± 192*	15		302 ± 4
3		2,498 ± 58
4		2,409 ± 61	16		642 ± 88
5		3,136 ± 30	17		587 ± 44
6		771 ± 22	18		578 ± 36
7		204 ± 14
8		1,626 ± 12	19		3,645 ± 254
9		1,208 ± 20	20		904 ± 93
10		1,259 ± 14	21		287 ± 14
11		776 ± 101
12		499 ± 19	22		439 ± 14
13		482 ± 4	23		350 ± 61
14		1,414 ± 79	24		1,477 ± 38