TCMDC-135051 is a potent PfCLK3 inhibitor with IC50 of 40 nM.
TCMDC-135051 rapidly killed P. falciparum at the trophozoite to schizont stages as well as preventing the development of stage V gametocytes and inhibiting the development of liver stage parasites.
TCMDC-135051 also showed equivalent in vitro kinase activity at CLK3 from P. falciparum, Plasmodium berghei (mouse malaria), Plasmodium vivax (human malaria), and Plasmodium knowlesi (monkey and human malaria).
TCMDC-135051 inhibits in live parasite viability (parasiticidal) assays using laboratory strain 3D7 (chloroquine-sensitive) P. falciparum with EC50 of 180 nM.
