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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 4.

SAR of polar 6-aryl substituents

graphic file with name nihms-1655834-t0026.jpg
KinaseSeeker a NanoBRET b
Entry Compound Ar STK17A
(% I)		 STK17B
(% I)		 STK17B
IC50 (nM)		 STK17B
IC50 (nM)
1 11k graphic file with name nihms-1655834-t0027.jpg 7 93 23 ± 2.4 >10,000 c
2 11l graphic file with name nihms-1655834-t0028.jpg 24 94 35 ± 4.5 >10,000 c
3 11m graphic file with name nihms-1655834-t0029.jpg 11 95 7 ± 0.72 >10,000 c
4 11n graphic file with name nihms-1655834-t0030.jpg 21 96 13 ± 1.6 1500 ± 210
5 11o graphic file with name nihms-1655834-t0031.jpg 20 92 83 ± 8.4 2900 ± 340
6 11p graphic file with name nihms-1655834-t0032.jpg 37 98 14 ± 1.1 720 ± 60
7 11q graphic file with name nihms-1655834-t0033.jpg 9 93 37 ± 3.5 >10,000 c
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 ± SE.

c

n = 1.