Compound 1a showed a Ki of 9.16–18.85 μM with S-adenosyl methionine (SAM, AdoMet), whereas compound 1b showed a Ki of 3.70–7.06μM with SAM; both inhibitors were found to act allosterically.17 In a subsequent publication, these two compounds(1a and 1b) were reported as first-in-classallosteric inhibitors of DNMT3A, which act by disrupting protein–proteininteractions (PPIs) and induce acute myeloid leukemia cell differentiation(Figure 2).20 Importantly, compounds 1a and 1b are significantly less cytotoxic than FDA-approved inhibitors.21 This evidence concerns the gene DNMT3A and acute myeloid leukemia.