Table 2.

Structures, cLogP and LSD1 residual activity for 3,5-diaminotriazoles 2, 6, 7 and 27–42 at 10 μM. Each data point is the average of 3 determinations ± standard error of the mean. Compounds 34 and 36 were insoluble and thus were not screened for LSD1 inhibition. TCP = tranylcypromine

#	X	R1	R2	R3	R4	cLogP	% LSD1 Activity (10μM)
TCP	--	--	--	--		--	64.2 ± 6.1
2	--	--	--	--		--	33.9 ± 6.7
6	--	H	H	H	H	3.73	15.1 ± 4.7
7	--	--	--	--	--	3.58	25.1 ± 1.9
27	O	H	H	CF3O	H	5.47	61.4 ± 5.6
28	O	H	H	CH3	H	4.94	40.7 ± 6.1
29	O	(CH3)2CH	H	H	CH3	5.97	43.7 ± 3.2
30	O	H	CH3O	H	H	4.36	55.4 ± 5.1
31	O	H	H	(CH3)3C	H	6.27	41.8 ± 8.8
32	O	H	CH3	H	CH3	5.44	32.1 ± 8.8
33	O	H	CF3	H	CF3	6.21	55.1 ± 4.6
34	O	H	H	S-CF3	H	6.11	insolb.
35	O	CF3	H	Br	H	6.19	32.2 ± 5.4
36	O	H	H	S-CH3	H	6.11	insolb.
37	O	CH3O	H	CH3	H	4.51	15.3 ± 3.2
38	O	H	CH3O	H	CH3O	4.45	36.7 ± 8.6
39	O	CH3	CH3	H	H	5.39	19.4 ± 1.9
40	O	H	O-CH2-O		H	4.41	34.2 ± 6.4
41	S	H	H	H	H	4.74	39.2 ± 7.9
42	S	H	CH3O	CH3O	H	4.40	46.8 ± 7.4