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. Author manuscript; available in PMC: 2019 Feb 1.
Published in final edited form as: Bioorg Med Chem. 2017 Dec 15;26(3):590–602. doi: 10.1016/j.bmc.2017.12.020

Table 3.

SAR data for CK1δ/ε inhibitors with a substituted benzimidazole unit (R5)

graphic file with name nihms931057u4.jpg
R5 R6 CK1δ IC50 (nM)[a] CK1ε IC50 (nM)[a] MDA-MB-231EC50 (nM)[b]
36 graphic file with name nihms931057t17.jpg N-Me 1565 2955 - [c]
37 graphic file with name nihms931057t17.jpg O 1155 2095 - [c]
38 graphic file with name nihms931057t17.jpg NH 825 1840 - [c]
39 graphic file with name nihms931057t18.jpg N-Me 335 630 - [c]
40 graphic file with name nihms931057t18.jpg O 520 715 - [c]
41 graphic file with name nihms931057t18.jpg NH 430 915 - [c]
42 graphic file with name nihms931057t19.jpg N-Me 100 320 < 1
43 graphic file with name nihms931057t19.jpg O 50 105 4
44 graphic file with name nihms931057t19.jpg NH 80 255 6
45 graphic file with name nihms931057t20.jpg N-Me 610 335 - [c]
46 graphic file with name nihms931057t20.jpg O 520 975 - [c]
47 graphic file with name nihms931057t20.jpg NH 625 1765 - [c]
48 graphic file with name nihms931057t21.jpg N-Me 200 660 1040
49 graphic file with name nihms931057t21.jpg O 175 340 60
[a]

Biochemical assay.

[b]

Cellular proliferation assay.

[c]

Not determined.