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. 2012 Nov 15;20(22):6630–6639. doi: 10.1016/j.bmc.2012.09.024

Table 1.

Structure activity relationships for the benzimidazole series of CHK2 inhibitors

No. Structure CHK2 IC50 (nM)
1 graphic file with name fx2.gif 55 ± 31 15
2 graphic file with name fx3.gif 640 ± 210 15
3 graphic file with name fx4.gif 1900 ± 610 15
4 graphic file with name fx5.gif 1500 ± 720 15
5 graphic file with name fx6.gif 1400 ± 550 15
6 graphic file with name fx7.gif >10000 15
7 graphic file with name fx8.gif 290 ± 90 15
8 graphic file with name fx9.gif >10000 16
9 graphic file with name fx10.gif 1540 16
10 graphic file with name fx11.gif >10000 16
11 graphic file with name fx12.gif >10000 16
12 graphic file with name fx13.gif >10000 16

Numbering to denote the regiochemistry of benzimidazole methylation is shown for compounds 8 and 9.