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. Author manuscript; available in PMC: 2022 Jun 30.
Published in final edited form as: ACS Chem Biol. 2022 Mar 2;17(3):536–544. doi: 10.1021/acschembio.1c00788

Table 1.

Potency and Selectivity of Takinib Analogues against TAK1 and IRAK4

graphic file with name nihms-1819058-t0008.jpg
R1 R2 R3 TAK1 IC50 nM IRAK4 IC50 nM Ratio
Takinib H H propyl 9 120 13
HS-268 graphic file with name nihms-1819058-t0009.jpg H graphic file with name nihms-1819058-t0010.jpg nt nt
HS-269 graphic file with name nihms-1819058-t0011.jpg H graphic file with name nihms-1819058-t0012.jpg 2.8 8.5 3
HS-275 H graphic file with name nihms-1819058-t0013.jpg propyl 2.6 48 18
HS-276 H graphic file with name nihms-1819058-t0014.jpg propyl 2.5 2,500 1000
HS-277 H graphic file with name nihms-1819058-t0015.jpg graphic file with name nihms-1819058-t0016.jpg 2.4 402 168
HS-278 H graphic file with name nihms-1819058-t0017.jpg graphic file with name nihms-1819058-t0018.jpg 1.6 8.2 5
HS-280 graphic file with name nihms-1819058-t0019.jpg H propyl 3.1 29 9
HS-281 graphic file with name nihms-1819058-t0020.jpg H propyl 1.7 4.2 2
HS-285 H graphic file with name nihms-1819058-t0021.jpg propyl 32 1,120 35