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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 1.

SAR data for CK1δ/ε inhibitors with alkyl and aryl substituents at N9 (R1)

graphic file with name nihms931057u2.jpg
№ R1 CK1δ IC50 (nM)[a] CK1ε IC50 (nM)[a] MDA-MB-231 EC50 (nM)[b]
11 -Me > 10000 > 10000 - [c]
12 -Et 4010 6560 - [c]
SR-3029 (13) graphic file with name nihms931057t1.jpg 44 260 26
14 graphic file with name nihms931057t2.jpg 535 395 - [c]
15 graphic file with name nihms931057t3.jpg 4520 990 - [c]
16 graphic file with name nihms931057t4.jpg 48 80 101
17 graphic file with name nihms931057t5.jpg 53 145 68
18 graphic file with name nihms931057t6.jpg 10 16 38
19 graphic file with name nihms931057t7.jpg 525 250 - [c]
20 graphic file with name nihms931057t8.jpg 110 135 6280
21 graphic file with name nihms931057t9.jpg 230 175 9790
[a]

Biochemical assay.

[b]

Cellular proliferation assay.

[c]

Not determined.