To develop efficacious inhibitors against FTO, Chen’s team conducted a structure-based virtual screening of the 260,000 compounds and validation assays, leading to the identification of two compounds, CS1 and CS2, which displayed strong inhibitory effects against FTO activity and AML cell viability with 10- to 30-fold lower IC50 (Su et al., 2020). Here, FTO is linked to acute myeloid leukemia.