Table 1.

SAR of 2-amino moiety for ERK5 and LRRK2

Compound ID	R1	Cellular EC50 (ERK5, μM)a	Enzymatic IC50 (ERK5, μM)b	Enzymatic IC50 (LRRK2[G2019S], μM)c
5		0.19 ± 0.04	0.087 ± 0.007	0.026
6		0.24 ± 0.04	0.297 ± 0.014	0.017
7		0.26 ± 0.03	0.233 ± 0.019	0.031
8		0.31 ± 0.06	0.171 ± 0.016	0.07
9		4.68 ± 0.52	1.724 ± 0.221	2.37
10		4.11 ± 0.59	1.253 ± 0.151	>10
11		0.24 ± 0.04	0.364 ± 0.058	0.059
12		>0.5	1.530 ± 0.172	0.256
13		0.24 ± 0.03	0.140 ± 0.009	0.005
14		0.32 ± 0.05	0.338 ± 0.018	0.008
15		0.16 ± 0.04	0.114 ± 0.011	0.004

^aThe required concentration for inhibiting 50% of EGF-stimulated autophosphorylation of ERK5 in HeLa cells.

^bThe required concentration for inhibiting 50% of enzymatic activity of ERK5 using an in vitro assay.

^cThe required concentration for inhibiting 50% of enzymatic activity of LRRK2[G2019S] using an in vitro assay.