WDR5-0102 is an inhibitor targeting WDR5-MLL1 interface (Kdis=7 μM, Kd=4 μM). WDR5-0102 suppresses MLL1 HMT activity, but not human H3K4 metltransferase SETD7 and six other HMTs: G9a, EHMT1, SUV39H2, SETD8, PRMT5[1][2].
[1]. Ye X, et al. The identification of novel small-molecule inhibitors targeting WDR5-MLL1 interaction through fluorescence polarization based high-throughput screening. Bioorg Med Chem Lett. 2019 Feb 15;29(4):638-645.
[2]. Chen X, et al. Targeting WD Repeat-Containing Protein 5 (WDR5): A Medicinal Chemistry Perspective. J Med Chem. 2021 Aug 12;64(15):10537-10556.
















