Table 2.

Non-substate-based BACE1 inhibitors

#	Inhibitor name	Design method	in vitro activity	Cellular activity	in vivo activity	Significance	Reference
11	10d	HTSa	IC50 = 0.11 μM	NA	NA	85 fold selectivity over cathepsin D	Cole et al., 2006 (Wyeth)
12	3a	HTS	Ki = 11 nM	Very efficiently inhibit Aβ40 secretion in CHO cells transfected with Swedish mutant APP	3 hours after oral dosing at 30 mg/kg, 40–70% ↓ plasma Aβ40 in rats	Excellent brain permeability	Baxter et al., 2007 (Johnson & Johnson)
13	compound 29	FBDDb	IC50 = 80 nM	IC50 = 470 nM	NA		Edwards et al., 2007 (AstraZeneca)

^aHTS, high throughput screening