Table 1. In Vitro Activities of Fused Phenylalkanoic Acids.

					FLIPR	binding
compd	X	Y	Z	bond type	human EC50 (μM)a	human Ki (μM)b	rat Ki (μM)b
3	CH2	bond	CH2	single	0.028	0.21	0.52
4	−(CH2)2−	bond	CH2	single	0.023	0.059	3.7
5	−(CH2)3−	bond	CH2	single	0.54	2.4	>10
6	O	bond	CH2	double	1.7	>10	>10
7	O	bond	CH2	single	0.022	0.17	1.1
8	−OCH2−	CH2	bond	single	0.049	0.27	>10
1					0.0057	0.032	0.054

^aAll values are averages of n = 3 in the presence of 0.1% BSA.

^bAll values are averages of n = 2 or 3 in the presence of 0.2% BSA.