Table 1.

Inhibitory potencies of phosphinic derivatives containing various R₁ residues for NEP and APN                

Compound	X	R1	Y	Ki (nM)*
				NEP†	APN‡
3(A + B)	NH2	CH2Ph	(S)Phe	190 ± 50	2.9 ± 0.8
(C + D)				7,000 ± 900	200 ± 40
4(A + B)	NH2	Ph	(S)Phe	104 ± 7	3.8 ± 0.2
(C + D)				32,000 ± 1,000	320 ± 10
5(A + B)	NH2	CH3	(S)Phe	146 ± 2	2.2 ± 0.2
(C + D)				35,000 ± 1,000	670 ± 90
10§	H	CH2Ph	(S)Phe	100 ± 7	>100,000
11¶	NH2	CH2Ph	H	1,000,000	370 ± 80

^*Values are the mean ± SEM from three independent experiments performed in triplicate of five inhibitor concentrations. 

^†NEP activity was measured by using DGNPA as substrate. 

^‡APN activity was measured by using Ala-p. NA as substrate. 

^§Compound 10 is a mixture of two stereoisomers. 

^¶Compound 11 is a mixture of four stereoisomers.