TABLE I.

Binding affinity of compounds

Compounds	IC50/Ki, nM	Binding affinity Relative to PIB	Primary target
PIB	Kd = 3.77a; IC50=3.84b	1	Aβ plaques
	Ki =0.87c
	IC50=10/Ki =6.67d
TAZA	IC50=1.28d	7.81g	Aβ plaques
	Ki =0.84d	4.49h
Dalene (Compound #25 in reference)	Ki =15.2e	(0.21)i	Aβ plaques
Florbetapir	Ki =2.87c	0.30j	Aβ plaques
Florbetaben	Ki =2.22c	0.39j	Aβ plaques
Flutmetamol	Ki =0.74c	1.18j	Aβ plaques
AZD4694 (NAV4694)	Ki =2.3c	0.35j	Aβ plaques
PDB-3 Phenyldiazenyl benzothiazoleg	Ki = 8.24f	(9.85)i	Aβ plaques Tau
	Ki = 0.48k

^aHuman AD brain homogenate kDa using ³H-PIB (Fodero-Tavoletti et al., 2007).

^bHuman AD frontal cortex IC₅₀ using ³H-PIB (Hellstrom-Lindahl et al., 2014).

^cK_i AD brain homogenates using ¹⁸F-florbetapir (Choi et al., 2009).

^dThis work, human hippocampal homogenate using ³H-PIB.

^eK_i using ¹²⁵I-TZDM (Kung et al., 2003; Compound #25 in Patent).

^fK_i measured using thioflavin (Matsumura et al., 2011).

^gCompared to PIB IC₅₀= 10 nM, this work.

^hCompared to kd^a= 3.77 nM in AD brain homogenate using ³H-PIB (Fodero-Tavoletti et al., 2007).

ⁱCompared to affinity measures of SB-13 in the same assay.

^jCompared to K_i = 0.87 nM in AD brain homogenates using ¹⁸F-florbetapir (Choi et al., 2009).

^kK_i measured using thioflavin-S for Tau with Aβ/Tau ratio of >17 (Matsumura et al., 2011).