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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 2:

Comparisons of DYRK1A Kd vs DYRK1A-Luc EC50 and MELK Kd versus cytotoxicity (R-Luc CC50) for select 1,5-naphthyridines.

Compound DYRK1A Kd (nM) DYRK1A-Luc EC50 (nM) MELK Kd (nM) R-Luc CC50 (nM)
5 0.12 5 15 64
15 0.16 7 11 186
21 0.075 3 12 51
28 0.22 8 9 165
42 0.6 50 13 5900