Skip to main content
. 2020 Apr 8;38(5):1350–1364. doi: 10.1007/s10637-020-00923-4

Table 2.

Kinetic parameters of α-aminoalkylphosphonate diaryl ester peptidyl derivatives

No. Structure log EC50
[µM]
EC50 [µM] Ki
[µM]
% Inh
(50 µM)
graphic file with name 10637_2020_923_Figb_HTML.gif
R 1 R 2 R 3
23 -CH(CH3)2 -CH3 -CH2CH3 1.535 ± 0.031 34.25 17.00 64.1
24 -CH(CH2)5 -CH3 -CH2CH3 1.313 ± 0.053 20.54 10.19 74.1
25 -CH(CH3)2 -CH3 -CH(CH3)2 1.342 ± 0.026 21.98 10.90 81.8
26 -CH(CH2)5 -CH3 -CH(CH3)2 1.297 ± 0.033 19.83 9.84 85.8
27 -CH(CH3)2 -CH3 -C(CH3)3 1.328 ± 0.039 21.26 10.54 83.3
28 -CH(CH2)5 -CH3 -C(CH3)3 1.427 ± 0.041 26.76 13.27 77.3
29 -CH(CH3)2 -CH3 -H 1.503 ± 0.042 31.86 15.81 62.1
30 -CH(CH2)5 -CH3 -H 1.481 ± 0.060 30.24 15.00 69.0
31 -CH(CH3)2 -CH2CH3 -H 1.580 ± 0.056 37.97 18.84 57.0
32 -CH(CH2)5 -CH2CH3 -H 1.380 ± 0.074 23.97 11.89 71.0
33 -CH(CH3)2 -CH(CH3)2 -H 1.543 ± 0.052 34.96 17.35 58.5
34 -CH(CH2)5 -CH(CH3)2 -H 1.378 ± 0.034 23.85 11.83 70.5
35 -CH(CH3)2 -CH(CH3)CH2CH3 -H 1.251 ± 0.037 17.84 8.84 77.4
36 -CH(CH2)5 -CH(CH3)CH2CH3 -H 1.211 ± 0.036 16.24 8.05 81.4
37 -CH(CH3)2 -CH2CH(CH3)2 -H 1.449 ± 0.062 28.13 13.96 67.4
38 -CH(CH2)5 -CH2CH(CH3)2 -H 1.026 ± 0.051 10.61 5.25 84.2
39 -CH(CH3)2 -CH2CH2SCH3 -H 1.418 ± 0.041 26.20 13.00 65.8
40 -CH(CH2)5 -CH2CH2SCH3 -H 1.420 ± 0.028 26.31 13.05 73.8
41 -CH(CH3)2 -CH2(C6H5) -H -0.884 ± 0.036 0.13 0.05 100.0
42 -CH(CH 2 ) 5 -CH2(C6H5) -H -0.132 ± 0.034 0.74 0.35 100.0
43 -CH(CH3)2 -CH2CH2(C6H5) -H 1.235 ± 0.048 17.17 13.00 85.4
44 -CH(CH2)5 -CH2CH2(C6H5) -H 1.184 ± 0.046 15.27 7.57 86.5