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. Author manuscript; available in PMC: 2021 Dec 10.
Published in final edited form as: J Med Chem. 2020 Nov 20;63(23):14626–14646. doi: 10.1021/acs.jmedchem.0c01174

Table 6.

SAR of fluorine substituted 6-aryl substituents

graphic file with name nihms-1655834-t0039.jpg
KinaseSeeker a NanoBRET b
Entry Compound Ar STK17A
(% I)		 STK17B
(% I)		 STK17B
IC50 (nM)		 STK17B
IC50 (nM)
1 11v graphic file with name nihms-1655834-t0040.jpg 8 94 49 ± 7.8 980 ± 410
2 11w graphic file with name nihms-1655834-t0041.jpg 22 90 60 ± 17 1200 ± 370
3 11x graphic file with name nihms-1655834-t0042.jpg 1 83 74 ± 19 820 ± 100
4 11y graphic file with name nihms-1655834-t0043.jpg 0 93 27 ± 5.1 530 ± 450
5 11z graphic file with name nihms-1655834-t0044.jpg 0 94 18 ± 2.6 700 ± 260
6 11aa graphic file with name nihms-1655834-t0045.jpg 0 92 33 ± 5.2 340 ± 40
7 11ab graphic file with name nihms-1655834-t0046.jpg 13 75 280 ± 25 500 ± 100
a

KinaseSeeker split luciferase binding assay. % I, inhibition compared to control (DMSO) at 1 μM, n = 2, data ± 10%. IC50, determined by dose response, n = 2 ± SD.

b

Target engagement determined by NanoBRET assay in HEK293 cells, n = 3 ± SD.