Targeting TDP-43 phosphorylation by Casein Kinase-1δ inhibitors: a novel strategy for the treatment of frontotemporal dementia

Table 2 Overview of the compounds used in this study

Compound	Structure	% inhition CK-1δ	IC₅₀ [μM]	Pe (10⁻⁶ cm.s⁻¹)	BBB prediction
IGS-2.7		>60	0.023 ± 0.002	11.3 ± 2.0	CNS+
IGS-3.27		>60	0.047 ± 0.005	4.4 ± 2.9	CNS+

The % inhibition of CK-1δ activity was determined in vitro in presence of a fixed concentration of 10 μM of the compounds. IC_50: half maximal concentration of both compounds inhibiting CK-1δ activity. Pe: effective permeability (data from PAMPA assay). BBB prediction. Compounds were classified as CNS+ when they present a permeability >3.74 × 10⁻⁶ cm · s⁻¹ [20]. Values shown are the mean ± SD

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