CHMFL-PI4K-127 (compound 15g) is a highly selective inhibitor of PfPI4K (Plasmodium falciparum PI4K kinase) with oral activity (IC50=0.9 nM). CHMFL-PI4K-127 shows strong inhibitory activity against Plasmodium falciparum 3D7 (EC50=25.1 nM). CHMFL-PI4K-127 has anti-malaria effect.

CHMFL-PI4K-127 (compound 15g) displays high selectivity against PfPI4K over human lipid and protein kinase [1]. CHMFL-PI4K-127 exhibits EC 50 values of 23–47 nM against a panel of the drug-resistant strains of P. falciparum [1].

CHMFL-PI4K-127 (compound 15g) (Orally; 0-80 mg/kg/day for 7 days; 0-15 mg/kg, once) exhibits the antimalaria efficacy in both blood stage (80 mg/kg) and liver stage (1 mg/kg) of Plasmodium in infected rodent model [1]. Animal Model: Balb/c mice were infected by P. yoelii [1]. Dosage: 0, 60, 80 mg/kg Administration: Orally, daily for 7 days Result: Displayed significant in vivo antimalarial activities in a dose-dependent manner and 80 mg/kg × 7 days treatment generated curative effects. The 60 mg/kg dosage resulted in suppressive effects during the drug treatment but relapsed after stopping treatment. Animal Model: Balb/c mice were infected by P. yoelii [1]. Dosage: 0, 1, 5, 15 mg/kg Administration: Orally, once Result: Provided the full protection and cure at 1 mg/kg with no negligible parasite visible in the liver of all tested mice at 24, 48, 72, 96, 144 and 196 h, indicating true causal prophylactic efficacy.