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. 2021 Feb 6;26(4):867. doi: 10.3390/molecules26040867

Table 1.

Enzymatic assays on HsPim-1 and HsPim-2 (ADP-Glo method at 10 μM ATP).

graphic file with name molecules-26-00867-i001.jpg
Entry Compound X HsPim-1
IC50 (µM) 1
HsPim-2
IC50 (µM) 1
1 1 H 0.074 2.10
2 5a 6-F 0.17 0.76
3 5b 7-F 1.24 4.20
4 5c 6-Cl 0.13 0.17
5 5d 7-Cl 2.10 2.40
6 5e 6-Br 0.16 0.58
7 5f 7-Br 0.18 2.20
8 5g 6-CF3 0.20 1.80
9 5h 7-CF3 3.85 6.40
10 SGI-1776 0.05 0.10

1 IC50 on Pim-1/2 kinase activity were calculated from dose−response curves. Each inhibitor concentration was tested in duplicate. Inhibition curves for 5c and 5e are reported in supplementary data. Hs: Homo sapiens. Values are a mean of n ≥ 3 independent experiments. Hs: Homo sapiens.