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. IC50: 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