Table 9.

Synthesized inhibitors and their inhibition constants against furin [189]. Residue numbering, according to Schechter and Berger [228].

No.	P5	P4	P3	P2	P1	P1′–P4′
	1	2	3	4	5	6–9	10	11	12	13–14	C-terminus	Ki, nM	Error, nM
1 a	G	R	C	T	K	SIPP c	I	C	F	PD	OH	35,234	1579
2 b	K	R	C	T	K	SIPP	R	C	H	PD	OH	24.1	0.8
3	G	R	C	R	R	SIPP	R	C	H	PD	OH	1157	10
4	G	R	C	R	K	SIPP	R	C	H	PD	OH	29.3	0.6
5	K	R	C	R	K	SIPP	R	C	H	PD	OH	8.8	0.5
6	R	R	C	R	K	SIPP	R	C	H	PD	OH	9.1	0.3
7	K	R	C	R	K	SIPP	I	C	F	PD	OH	9.8	0.5
8	K	A	C	R	K	SIPP	R	C	H	PD	OH	1301	53
9	K	R	C	R	K	SIPP	R	C	H	PD	OH	2078	62
10	K	R	C	K	K	SIPP	R	C	H	PD	OH	3.8	0.2
11	K	R	C	K	K	SIPP	I	C	F		NH2	0.49	0.04
12	K	R	C	K	K	SIPP	I	C			NH2	0.71	0.04
13	K	R	C	K	K	SIPP	R	C			NH2	4.7	0.1
14	K	R	C	K	K	SIPP	A	C	F		NH2	3.7	0.2
15	K	R	A	R	K	SIPP	R	A	H	PD	OH	2373	87
16	K	R	Aha d	K	K	SIPP	I	Pra e			NH2	21.8	0.6
17	K	R	Aha	K	K	SIPP	I	Pra			NH2	5.0	0.4

^a 1 is SFTI-1. ^b 2 is SDMI-3. ^c SIPP—Ser-Ile-Pro-Pro. ^d Aha—L-azidohomoalanine. ^e Pra—l-propargylglycine.