Figure 3.

Chemical structures of BACE-1 inhibitors developed from fragment hits. The structural formulae of the protonated forms of the compounds bound are shown, and, where determined, IC₅₀ values and crystal structures of complexes with BACE-1 are shown. (a) 2-amino-6-phenethylpyridine; (b) 2-(2-(1H-indol-6-yl)ethyl)-6-aminopyridine; (c) 2-amino-6-(2-(3′-methoxy-[1,1′-biphenyl]-3-yl)ethyl)pyridine; (d) 2-amino-3-((3- (pyridin-3-yl)benzyl)amino)pyridine; (e) 2-amino-3-((3-(5-methoxypyridin-3-yl)benzyl) amino)pyridine; (f) 2-amino-3-((3-(5-propyloxypyridin-3-yl)benzyl)amino)pyridine.