N,N-Dimethyl-4-pyrazolo[1,5-b]pyridazin-3-yl-2-pyrimidinamine

DYRK1-IN-1 is a highly selective and ligand-efficient DYRK1A inhibitor. DYRK1-IN-1 inhibits DYRK1A phosphorylation activity with an IC50 value of 220 nM. DYRK1-IN-1 can be used for the research of central nervous system penetrant DYRK1A chemical probe[1].

DYRK1A: 220 nM (IC₅₀); DYRK1A: 3 nM (Kd); DYRK1B: 56 nM (Kd)

[1] Henderson SH, et al. Discovery and Characterization of Selective and Ligand-Efficient DYRK Inhibitors. J Med Chem. 2021;64(15):11709-11728. DOI:10.1021/acs.jmedchem.1c01115