LSPN954 (compound 4i) is an indole peptidomimetic antimalarial agent that exhibits low micromolar activity against both sensitive and multidrug-resistant Plasmodium falciparum strains, while demonstrating low cytotoxicity to human cells and a high selectivity index. It shows a slow-onset inhibitory activity, allowing initial parasite development followed by morphological changes, and its action is not dependent on the inhibition of apicoplast-based isoprenoid biosynthesis. LSPN954 is useful for malaria research.