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. Author manuscript; available in PMC: 2021 Jan 1.
Published in final edited form as: Bioorg Med Chem. 2019 Nov 11;28(1):115193. doi: 10.1016/j.bmc.2019.115193

Table 1.

Chemical structures of the 1,5-naphthyridines library with measured DYRK1A inhibition potency (DYRK1A-Luc EC50), cytotoxicity (R-Luc CC50) and calculated cytotoxicity to DYRK1A inhibition ratio (Index) in HEK 293 cells are shown.

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a

Calculated by 4-parameter agonist dose response (Graphpad) of the induction of DYRK1A-responsive firefly luciferase to test compound in a HEK293T reporter cell assay (11-point dose curve, n = 4 per concentration).

b

Calculated by 4-parameter inhibitor dose response (Graphpad) to test compound of constitutively-active renilla luciferase in a HEK293T reporter cell assay (11-point dose curve, n = 4 per concentration).

c

Compound did not inhibit renilla luciferase expression by >50% at 10 μM.

d

Compound did not stimulate firefly luciferase expression at 10 μM.