Table 1.

In vitro evaluation of LSD1 inhibition by the LSD1 inhibitor 1 a, prodrugs 1 b–g and negative controls 2 a, 2 c and 2 f using a Peroxidase‐coupled assay. Most of the prodrugs are >100 times less potent than parent drug 1 a. Determination of higher IC₅₀ values were not possible due to poor solubility. n.i.=inhibition≤10 %.

	#	LSD1 inhibition in vitro IC50 [μM]	Potency window prodrug/1 a
LSD1 inhibitor	1 a	0.094±0.017
prodrugs	1 b	n.i. at 10 μM	>110
	1 c	n.i. at 10 μM	>110
	1 d	5.23±0.48	58±12
	1 e	26.18±5.55	288±81
	1 f	n.i. at 10 μM	>110
	1 g	30.50±0.92	335±61
negative controls	2 a	n.i. at 10 μM	>110
	2 c	n.i. at 10 μM	>110
	2 f	n.i. at 10 μM	>110