plasmodium pi4k inhibitor

MMV390048 is an antimalarial agent and is a representative of a new chemical class of Plasmodium PI4K inhibitor (Kdapp=0.3 μM). MMV390048 binds to the ATP binding site of Plasmodium PI4K and does not bind to other P. falciparum and human kinases apart from human PIP4K2C, thus alleviating potential kinase-mediated safety concerns.

UCT943 is an inhibitor of Plasmodium falciparum PI4K (IC50 = 23 nM).

PI4K-IN-3 (Compound 27) is an orally effective PI4K inhibitor with an IC50 of 1.9 nM for Plasmodium vivax PI4K. It does not inhibit the hERG channel and is non-cytotoxic to mammalian cells. This compound shows notable selectivity for human MINK1 and MAP4K4 kinases but has lower selectivity for human PI3Kα and PI4Kβ. PI4K-IN-3 exhibits potent antimalarial activity, significantly reducing parasitemia in NSG mouse models infected with Plasmodium falciparum.

BQR-695 (NVP-BQR695) is a phosphatidylinositol 4-kinase (PI4K) inhibitor with IC50s of 80 and 3.5 nM for human PI4KIIIβ and Plasmodium variant of PI4KIIIβ, respectively.

KDU691 is a PI4K inhibitor.

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

BRD73842 is an inhibitor of Plasmodium PI4K.