Table 1.

Inhibition of purified recombinant LSD1 following treatment with 10 μM 3–33, and fold increase in global H3K4me2 levels in Calu-6 human lung adenocarcinoma cells following treatment with carbamimidothioates 5, 8 and 9, aromatic amines 6, 10 and 11 and amidoximes 7 and 12–33 at 10 μM. Each data point is the average of three determinations that in each case differed by less than 5%. ND = not determined.

Structure	Compound	% inhibition of LSD1 at 10 μM	H3K4me2 Fold Increase (48 h)
2d	2d	82.9	5.1
tranylcypromine	3	18.4	ND
pargyline	4	68.8	1.29
	5	24.0	1.94
	8	31.8	1.16
	9	17.3	1.16
	6	0.1	1.1
	10	5.5	1.1
	11	13.4	0.8
	7	31.7	0.62
	12	10.4	1.6
	13	0	7.1
	14	0	0.2
	15	25.3	1.2
	16	0	21.4
	17	5.6	12.44
	18	0	0.6
	19	15.4	1.4
	20	2.0	0.4
	21	0	6.2
	22	30.1	3.7
	23	8.6	2.1
	24	0	5.4
	25	0	0.8
	26	0	7.7
	27	10.4	13.4
	28	4.8	3.1
	29	0	13.1
	30	0	49.0
	31	0.2	6.7
	32	2.1	11.5
	33	16.6	3.1