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. Author manuscript; available in PMC: 2022 Apr 5.
Published in final edited form as: Eur J Med Chem. 2021 Feb 3;215:113252. doi: 10.1016/j.ejmech.2021.113252

Table 2.

RIPK2 and ALK2 kinases, and NOD2 cell (HEKBlue) signaling inhibitory activities of 21- 28.

graphic file with name nihms-1669616-t0011.jpg
Compound R1 R2 Kinase IC50 (μM) RIPK2/NOD2
Cell Assay
IC50 (μM)
RIPK2 ALK2
21 H Me 0.0105 ± 0.002 0.284 ± 0.356 0.014 ± 0.004
22 H Et ~ 30 nM 0.004 ± 0.005 0.015 ± 0.005
23 H CH2CH2OH ~ 30 nM 0.018 ± 0.024 0.27 ± 0.22
24 2,6-di-Cl CH2CH2OMe 0.128 ± 0.001 0.018 ± 0.019 0.013 ± 0.007
25 2,6-di-Cl CH2Ph 0.021 ± 0.003 0.008 ± 0.004 0.009 ± 0.003
26 2,6-di-Cl i-Bu 0.005 ± 0.002 0.009 ± 0.005 0.003 ± 0.0005
27 2,6-di-Cl CH2Ph-3-SO2Me 0.025 ± 0.008 0.092 ± 0.005 0.005 ± 0.005
28 2,6-di-Cl CH2Ph-4-SO2Me 0.021 ± 0.007 ND 0.094 ± 0.004

ND: Not determined; IC50 values are shown as the mean of two or more determinations ± standard deviation, unless otherwise indicated.