Table 3.
The cell-based CT-L inhibitory activity of head group modified compounds.
Compound | Cap moiety | P2 | P3 | Head group | CT-La IC50 (nM) |
---|---|---|---|---|---|
33 (NI-01106) | ![]() |
(4-CH3O)-Ph | H | ![]() |
385.6 ± 36.9 |
34 (NI-04192) | ![]() |
Ph | i-Pr | ![]() |
61.0 ± 3.1 |
35 (NI-09016) | ![]() |
1H-indol-3-yl | i-Pr | ![]() |
29.5 ± 3.1 |
36 (NI-18030) | ![]() |
1H-indol-3-yl | i-Pr | ![]() |
60.1 ± 10.0 |
37 (NI-09062) | ![]() |
1H-indol-3-yl | i-Pr | ![]() |
165.1 ± 7.6 |
38 (NI-23067) | ![]() |
i-Pr | i-Pr | ![]() |
22.1 ± 1.2 |
39 (NI-18019) | ![]() |
i-Pr | i-Pr | ![]() |
99.7 ± 24.7 |
40 (NI-18020) | ![]() |
i-Pr | i-Pr | ![]() |
64.1 ± 16.6 |
41 (NI-09073) | ![]() |
i-Pr | i-Pr | ![]() |
4701 ± 961 |
42 (NI-18073) | ![]() |
i-Pr | i-Pr | ![]() |
41.7 ± 2.5 |
43 (NI-18060) | ![]() |
i-Pr | i-Pr | ![]() |
34.8 ± 2.6 |
44 (NI-09083) | ![]() |
i-Pr | i-Pr | ![]() |
25.7 ± 3.1 |
45 (NI-18050) | ![]() |
i-Pr | i-Pr | ![]() |
31.7 ± 4.9 |
46 (NI-15020) | ![]() |
i-Pr | i-Pr | ![]() |
25.3 ± 3.8 |
47 (NI-18145) | ![]() |
i-Pr | i-Pr | ![]() |
28.8 ± 3.4 |
BSc2189 | ![]() |
i-Pr | i-Pr | ![]() |
34.5 ± 1.7 |
ONX-0914 | 58.5 ± 4.3 |
The compounds were assayed in triplicate with the averaged IC50 ± SEM values shown.