Of note, compound MMV689244 is a fenarimol analogue, identified as a potent inhibitor of Trypsonosoma cruzi during a targeted screening exercise for new drugs for Chagas disease [27–29], during which over 800 fenarimol analogues were synthesized (MMV689244 corresponds to EPL-BS1246 in this library) and addressing, through chemical modification including scaffold-hopping, the few identified liabilities of the fenarimol series notably low solubility, high in vitro metabolism and inhibition of cytochrome P450 3A4/5 (CYP3A4/5). The gene discussed is CYP3A4; the disease is Chagas disease.