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. 2023 Jul 28;66(15):10658–10680. doi: 10.1021/acs.jmedchem.3c00812

Table 2. PMX, PMIV, CatD, and BACE1 Inhibition by Macrocycles 7g–h.

2.2.

# cmpd. Y X PMX, nM PMIV, nM CatD, nM BACE1, nM
1 7g –(CH2)5– O 6.9 ± 0.49 190 1200 6000 ± 300
2 7h –(CH2)2– O 6.8 ± 0.59 200 600 1850 ± 90
3 7i –(CH2)2–O–CH2– CH2 4.6 ± 0.07 81±4 1650±80 22 700 ± 1100
4 7j –(CH2)3– CH2 3.8 ± 0.69 74±4 1370±70 3020 ± 150
5 7k –(CH2)4– CH2 0.4 ± 0.03 17±2 330±20 2030 ± 100