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. 2021 Apr 12;12(5):758–766. doi: 10.1039/d1md00043h

Potency and physicochemical properties of the series 2 with the 4 linkers.

graphic file with name d1md00043h-u6.jpg graphic file with name d1md00043h-u7.jpg graphic file with name d1md00043h-u8.jpg graphic file with name d1md00043h-u9.jpg graphic file with name d1md00043h-u10.jpg
Compound 9 10 11 12
IC50a 478 38 520 146
Log Db >4 4.0 4.0 >4
Solubilityc <0.1 18 11 <0.1
a

IC50 Aβ42 in nM in human H4 cells.

b

Log D determination by high-throughput shake-flask.

c

Solubility expressed in μg mL−1 and measured in Lysa assay.