Development of High-Affinity CHD1 Chromodomain Inhibitors.
Greschik H, Friedrich F, Seifert L, Mousavizadeh F, Fiorentino F, Walz J, Zhang L, Li J, Fabbrizi E, Tomassi S, Panahi F, Papenkordt N, Wurnig SL, Osterroth J, Strasser AM, Ruprecht J, Moumbock AFA, Hügle M, Sum M, Peng L, Wang S, Baniahmad AA, Pulido-Cortés L, Timmers HTM, Flaig R, Metzger E, Breit B, Einsle O, Günther S, Rotili D, Mai A, Schüle R, Jung M.
Greschik H, et al.
J Med Chem. 2026 May 28;69(10):12020-12047. doi: 10.1021/acs.jmedchem.5c03690. Epub 2026 May 5.
J Med Chem. 2026.
PMID: 42085696
Free PMC article.
We developed the first submicromolar inhibitors (2n and 2s) that target the H3K4me3 binding site of the CHD1 tCD with K(d) values of 0.15 muM and 0.14 muM, respectively. Co-crystal structures of these quinoline-based compounds revealed aromatic cage interactions and extend …
We developed the first submicromolar inhibitors (2n and 2s) that target the H3K4me3 binding site of the CHD1 tCD with K(d) values of …