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. Author manuscript; available in PMC: 2017 Aug 1.
Published in final edited form as: Curr Opin Chem Biol. 2016 Jun 25;33:135–141. doi: 10.1016/j.cbpa.2016.06.004

Table 2.

Select small molecule, non-peptidomimetic inhibitors of methyllysine reader proteins that engage the aromatic cage where methyllysine binds.

Inhibitor Structure Potency (Assay) Target(s) Peptide Binding Mode Ref.
UNC926 graphic file with name nihms797059t3.jpg L3MBTL1 IC50 = 3.9 μM
L3MBTL1 IC50 = 3.9 μM (Alphascreen)		 L3MBTL1, L3MBTL3 (MBT domains) Cavity insertion 21
UNC1215* graphic file with name nihms797059t4.jpg Kd = 0.12 μM (ITC) L3MBTL3 (MBT domain) Cavity insertion 19
Compound 56 graphic file with name nihms797059t5.jpg Kd = 0.35 μM (ITC) L3MBTL3 (MBT domain) Cavity insertion 13
CF16 graphic file with name nihms797059t6.jpg Kd = 7.3 mM (NMR) Pygo2 (PHD finger) Surface groove 34
MS37452 graphic file with name nihms797059t7.jpg Kd = 29 μM (NMR) CBX7 (Chromodomain) Surface groove 31
*

designates a high-quality chemical probe.