Figure 1.

Discovery of KDOAM-25

(A) KDOAM-21 is a weak KDM4/5 inhibitor. KDOAM-20 and -25 are potent and selective inhibitors of KDM5B over KDM4C.

(B) KDOAM-25 was tested against a panel of 15 2-OG oxygenases (black text) including a representative from each of the lysine demethylases sub-families (blue branches). KDOAM-25 only inhibits the KDM5 sub-family members of KDM5A-D with potencies <100 nM (box).

*All IC₅₀ values are an average of at least two independent determinations (Table S1); ^‡Not Determined.