Table 1. Kinetic Values of the Synthesized Inhibitors.

entry	enzyme	compound	AAa	kinact (10–3 s–1)	KI (μM)	kinact/KI (M–1 s–1)	DRb
1	NE	12a	Val	13.0 ± 3.0	51.0 ± 15.4	255 ± 96	11:89
2		1a (ValP)	Val	0.59 ± 0.04	2.96 ± 0.85	200 ± 59
3	PR3	12a	Val	11.0 ± 1.6	26.5 ± 6.2	415 ± 115	11:89
4		12b	Val	1.75 ± 0.20	83.8 ± 18.3	21 ± 5	54:46
5		1a (ValP)	Val	n.d.c	n.d.c	n.i.d
6	PPE	12a	Val	7.80 ± 0.79	132 ± 19	59 ± 10	11:89
7		1a (ValP)	Val	n.d.c	n.d.c	n.i.d
8	ChT	12a	Val	3.04 ± 0.15	7.42 ± 0.83	409 ± 50	11:89
9		10a	Phg	1.57 ± 0.07	0.46 ± 0.076	(3.4 ± 0.6) × 103	20:80
10		10b	Phg	5.84 ± 0.9	14.5 ± 3.8	404 ± 122	55:45
11		11a	Leu	21.1 ± 2.0	21.6 ± 3.3	978 ± 176	44:56
12		11b	Leu	2.44 ± 0.31	13.0 ± 2.9	188 ± 48	53:47
13		13a	Phe	23.0 ± 1.7	1.40 ± 0.28	(16.4 ± 3.6) × 103	39:61
14		1b (PheP)	Phe	5.63 ± 0.24	0.69 ± 0.07	(8.1 ± 0.9) × 103

^aThe tested compound mimics the indicated amino acid.

^bCompounds were tested as indicated mixtures of diastereomers (either as obtained in the reaction or as a mixture with a DR of approximately 50:50).

^cn.d.: not determined; since no inhibition was seen, these values were not determined.

^dn.i.: no inhibition; no good inhibition was seen in a dilution series between 200 and 26.7 μM.