Fig. 3.

Structures of representative non-tranylcypromine-based KDM1 subfamily inhibitors. Bisguanidines, bisbiguanides, polyamines and (thio)urea-containing compounds (for examples see 21–24) have all been shown to inhibit KDM1 activity in vitro, with some showing effects in cells. A detailed mechanistic/structural understanding of KDM1 inhibition by these compounds is presently not available. Recently, a series of other inhibitors of the KDM1 subfamily have been identified, including Namolin (26), aminothiazoles (27–29), benzohydrazides (30) and a tricyclic pyridine (31).