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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 3.

RIPK2 and ALK2 kinases, and NOD2 cell (HEKBlue) signaling inhibitory activities of methylsulfones 29 – 40.


Compound	R₁	R₂	R₃	Kinase IC₅₀ (μM)		RIPK2 Cell Assay IC50 (μM)
Compound	R₁	R₂	R₃	RIPK2	ALK2	RIPK2 Cell Assay IC50 (μM)
29	2,6-di-Cl	Me	4-SO₂Me	0.014 ± 0.0001	0.136 ± 0.118	0.136 ± 0.016
30	2,6-di-Cl	Me	3-SO₂Me	0.006 ± 0.0001	0.972 ± 0.510	0.022 ± 0.018
31	4-Cl	Me	3-SO₂Me	0.0146 ± 0.005	NI^a	NI^b
32	4-Cl	i-Bu	3-SO₂Me	0.0647 ± 0.024	NI^a	NI^b
33	2-Cl	Me	3-SO₂Me	0.008 ± 0.004	2.516 ± 2.168	0.020 ± 0.005
34	2,4-diCl	Me	3-SO₂Me	0.027 ± 0.013	NI^a	0.878 ± 0.23
35	2,3-di-Cl	Me	3-SO₂Me	0.034 ± 0.011	NI^a	1.23 ± 0.156
36	2-Cl, 4-F	Me	3-SO₂Me	0.017 ± 0.001	NI^a	0.218 ± 0.049
37	2,5-di-Cl	Me	3-SO₂Me	0.022 ± 0.0007	ND	0.73 ± 0.32
38	2-Cl, 4-Me	Me	3-SO₂Me	0.015 ± 0.002	ND	0.48 ± 0.04
39	4-OH	Me	3-SO₂Me	0.016 ± 0.001	24.80	NI^b
40	4-OMe	Me	3-SO₂Me	0.011 ± 0.004	NI^a	NI^b

^a

NI: No inhibition observed at 100 μM

^b

NI: No inhibition observed at 10 μM; ND: Not determined; IC₅₀ values are shown as the mean of two or more determinations ± standard deviation.