Table 4. In Vitro Binding Data for Benzyl-Oxadiazoles^a.

		NR2B	hERG
compd	R1	Ki (nM)b	IP (nM)c
16	H	6.2	28000
18	2-F	7.6	20000
19	3-F	29	15000
20	4-F	6.5	21000
21	2-CH3	26	3400
22	4-CH3	0.88	20000
23	4-Cl	0.99	7200
24	4-CH2CH3	0.93	6200
25	4-CH(CH3)2	0.98	1500
26	4-CF3	3.7	5100
27	4-CHF2	0.84	4000
28	4-CH2OH	91	>30000
29	4-OCH3	36	8600
30	2-F, 4-CH3	0.83	14000

^aAll values are the geometric mean of at least n = 2 measurements.

^bInhibition of ³H-[(E)-N¹-(2-methoxybenzyl)-cinnamamidine] binding to hNR1a/NR2B receptors expressed in Ltk- cells.⁴³

^cInhibition of MK-499 binding to hERG in HEK293 cells.⁴⁴