Plasmodium falciparum glutamate dehydrogenase (GDH) is an attractive target for the rational development of new antimalarial drugs. Enzyme Kinetics assays and molecular modelling technology were used to measure inhibition effects for some ligands on two different GDHs. The study presented in this work provided a base line for future explorations and discoveries of the inhibition selectivity between Plasmodium and human GDH based on bacterial and mammalian animal GDH.