Table 3.
SAR data for CK1δ/ε inhibitors with a substituted benzimidazole unit (R5)
![]() | |||||
---|---|---|---|---|---|
№ | R5 | R6 | CK1δ IC50 (nM)[a] | CK1ε IC50 (nM)[a] | MDA-MB-231EC50 (nM)[b] |
36 |
![]() |
N-Me | 1565 | 2955 | - [c] |
37 |
![]() |
O | 1155 | 2095 | - [c] |
38 |
![]() |
NH | 825 | 1840 | - [c] |
39 |
![]() |
N-Me | 335 | 630 | - [c] |
40 |
![]() |
O | 520 | 715 | - [c] |
41 |
![]() |
NH | 430 | 915 | - [c] |
42 |
![]() |
N-Me | 100 | 320 | < 1 |
43 |
![]() |
O | 50 | 105 | 4 |
44 |
![]() |
NH | 80 | 255 | 6 |
45 |
![]() |
N-Me | 610 | 335 | - [c] |
46 |
![]() |
O | 520 | 975 | - [c] |
47 |
![]() |
NH | 625 | 1765 | - [c] |
48 |
![]() |
N-Me | 200 | 660 | 1040 |
49 |
![]() |
O | 175 | 340 | 60 |
Biochemical assay.
Cellular proliferation assay.
Not determined.