Table 2. SAR of the Benzyl Amine.

Cmpd	R	R′	stereochemistry	Lantha (IC50, nM)a	GAL-4 (EC50, nM)b
9034	H	Et	±	0.37	13 (40%)
30	H	Et	S	3	53 (20%)
31	H	Et	R	0.13	3 (30%)
32	4-F	Me	S	21	638 (40%)
33	4-F	Me	R	0.79	47 (50%)
34	4-OMe	Me	S	0.90	2076 (30%)
35	4-OMe	Me	R	0.54	53 (60%)
1664	4-NO2	Me	S	80	4288 (10%)
36	4-NO2	Me	R	2	503 (75%)
37	4-Br	Me	S	28	516 (20%)
38	4-Br	Me	R	0.73	129 (90%)

^aValues are means of at least two experiments. All standard deviations are <20%.

^bTransactivation at 10 μM.