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. 2021 Feb 10;215:113267. doi: 10.1016/j.ejmech.2021.113267

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) Image 24 (4-CH3O)-Ph H Image 25 385.6 ± 36.9
34 (NI-04192) Image 26 Ph i-Pr Image 27 61.0 ± 3.1
35 (NI-09016) Image 28 1H-indol-3-yl i-Pr Image 29 29.5 ± 3.1
36 (NI-18030) Image 30 1H-indol-3-yl i-Pr Image 31 60.1 ± 10.0
37 (NI-09062) Image 32 1H-indol-3-yl i-Pr Image 33 165.1 ± 7.6
38 (NI-23067) Image 34 i-Pr i-Pr Image 35 22.1 ± 1.2
39 (NI-18019) Image 36 i-Pr i-Pr Image 37 99.7 ± 24.7
40 (NI-18020) Image 38 i-Pr i-Pr Image 39 64.1 ± 16.6
41 (NI-09073) Image 40 i-Pr i-Pr Image 41 4701 ± 961
42 (NI-18073) Image 42 i-Pr i-Pr Image 43 41.7 ± 2.5
43 (NI-18060) Image 44 i-Pr i-Pr Image 45 34.8 ± 2.6
44 (NI-09083) Image 46 i-Pr i-Pr Image 47 25.7 ± 3.1
45 (NI-18050) Image 48 i-Pr i-Pr Image 49 31.7 ± 4.9
46 (NI-15020) Image 50 i-Pr i-Pr Image 51 25.3 ± 3.8
47 (NI-18145) Image 52 i-Pr i-Pr Image 53 28.8 ± 3.4
BSc2189 Image 54 i-Pr i-Pr Image 55 34.5 ± 1.7
ONX-0914 58.5 ± 4.3

2.2.3.

a

The compounds were assayed in triplicate with the averaged IC50 ± SEM values shown.