Bioactivity Comments

The antiparasite activity of UCT943 against all Plasmodium lifecycle stages is provided in the interaction table below. UCT943 inhibits the P. vivax PI4K (PvPI4K) enzyme with a IC50 of 23 nM.

Whole organism assay data
Key to terms and symbols	Click on species/strain names for details	Click column headers to sort
MOA/likely target Sp. Assay description Type Action Value Parameter Concentration range (M) Reference Plasmodium falciparum phosphatidylinositol 4-kinase beta Pb Plasmodium berghei P. berghei (Pb) is a malaria parasite that infects mammals other than humans with the natural mammalian host being the thicket rat (G. surdaster) from Central Africa. Pb is used in rodent model studies of malaria. ✖ Parasite liver stage assay - - 9.0 pIC50 - 1 ⤷ pIC50 9.0 (IC50 9.2x10-10 M) Luciferase bioluminescence assay to measure sporozoite invasion (prophylactic activity) [1] Lifecycle stages: Plasmodium liver stage (sporozoite, hepatic schizont, hepatic merozoite) Plasmodium falciparum phosphatidylinositol 4-kinase beta PfHB3 Plasmodium falciparum HB3 P. falciparum strain HB3 (PfHB3) was cloned from the Honduras I/CDC strain, originally isolated from a patient in Choluteca, Honduras, during an outbreak of urban malaria in January 1980. PfHB3 can be obtained from the European Malaria Reagent Repository or the Malaria Research and Reference Reagent Resource Center (MR4) and is reported to be chloroquine sensitive. ✖ Parasite growth inhibition assay - - 8.4 pIC50 - 1 ⤷ pIC50 8.4 (IC50 3.7x10-9 M) [3H]-hypoxanthine incorporation [1] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont) Plasmodium falciparum phosphatidylinositol 4-kinase beta Pf7G8 Plasmodium falciparum 7G8 P. falciparum strain 7G8 (Pf7G8) was subcloned from the IMTM22 strain by limiting dilution. The original IMTM22 strain was isolated from a 12 year old male near Manaus, Brazil in 1980. Pf7G8 can be obtained from the European Malaria Reagent Repository or the Malaria Research and Reference Reagent Resource Center (MR4). This strain is a gametocyte producer and is reported to be chloroquine-sensitive and pyrimethamine-resistant. ✖ Parasite growth inhibition assay - - 8.4 pIC50 - 1 ⤷ pIC50 8.4 (IC50 4.1x10-9 M) [3H]-hypoxanthine incorporation [1] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont) Plasmodium falciparum phosphatidylinositol 4-kinase beta PfV1/S Plasmodium falciparum V1/S P. falciparum strain V1/S (PfV1/S) is an in vitro culture-adapted clone of V1, that originated in Vietnam. PfV1/S can be obtained from the Malaria Research and Reference Reagent Resource Center (MR4) and is reported to be resistant to chloroquine and quinine. ✖ Parasite growth inhibition assay - - 8.4 pIC50 - 1 ⤷ pIC50 8.4 (IC50 4.2x10-9 M) [3H]-hypoxanthine incorporation [1] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont) Plasmodium falciparum phosphatidylinositol 4-kinase beta PfK1 Plasmodium falciparum K1 P. falciparum strain K1 (PfK1) was isolated in Kanchanaburi, Thailand in 1979. PfK1 can be obtained from the European Malaria Reagent Repository or the Malaria Research and Reference Reagent Resource Center (MR4) and is reported to be a multidrug-resistant strain. ✖ Parasite growth inhibition assay - - 8.3 pIC50 - 1 ⤷ pIC50 8.3 (IC50 4.7x10-9 M) [3H]-hypoxanthine incorporation [1] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont) Plasmodium falciparum phosphatidylinositol 4-kinase beta PfD6 Plasmodium falciparum D6 P. falciparum strain D6 (PfD6) was collected in Sierra Leone. PfD6 can be obtained from the European Malaria Reagent Repository or the Malaria Research and Reference Reagent Resource Center (MR4) and is generally considered drug sensitive with minor mefloquine resistance. ✖ Parasite growth inhibition assay - - 8.3 pIC50 - 1 ⤷ pIC50 8.3 (IC50 5.2x10-9 M) [3H]-hypoxanthine incorporation [1] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont) Plasmodium falciparum phosphatidylinositol 4-kinase beta PfNF54 Plasmodium falciparum NF54 P. falciparum strain NF54 (PfNF54) was derived from a patient who had never left the Netherlands. PfNF54 can be obtained from the European Malaria Reagent Repository or the Malaria Research and Reference Reagent Resource Center (MR4) and is sensitive to a panel of antimalarial compounds including chloroquine and pyrimethamine. ✖ Parasite growth inhibition assay - - 8.3 pIC50 - 1 ⤷ pIC50 8.3 (IC50 5.4x10-9 M) [3H]-hypoxanthine incorporation [1] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont) Plasmodium falciparum phosphatidylinositol 4-kinase beta PfDd2 Plasmodium falciparum Dd2 P. falciparum strain Dd2 (PfDd2) is a clone derived from PfW2, following continuous culture in mefloquine. PfW2 was cloned from the Indochina III/CDC isolate, originally derived from a Laotian patient who failed chloroquine therapy. PfDd2 can be obtained from the Malaria Research and Reference Reagent Resource Center (MR4) and is reported to be resistant to chloroquine, pyrimethamine and mefloquine. ✖ Parasite growth inhibition assay - - 8.2 pIC50 - 1 ⤷ pIC50 8.2 (IC50 5.7x10-9 M) [3H]-hypoxanthine incorporation [1] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont) Plasmodium falciparum phosphatidylinositol 4-kinase beta Pc Plasmodium cynomolgi P. cynomolgi (Pc) is a malaria parasite that infects non-human primate species with the natural mammalian host being Asian Old World monkeys. Pc is used as a model for human P. vivax infection because these species are phylogenetically close and share a similar lifecycle, including the dormant liver form (hypnozoite). ✖ Parasite liver stage assay - - >8.0 pIC50 - 1 ⤷ pIC50 >8.0 (IC50 <1x10-8 M) P. cynomolgi assay to assess inhibition of liver stage development (prophylactic activity) [1] Lifecycle stages: Plasmodium liver stage (sporozoite, hepatic schizont, hepatic merozoite) Plasmodium falciparum phosphatidylinositol 4-kinase beta Pf Plasmodium falciparum P. falciparum (Pf) is one of five protozoan parasite species of the genus Plasmodium that cause malaria in humans. Pf is responsible for the majority of malaria related deaths and is the most prevalent species in sub-Saharan Africa. ✖ Parasite dual gamete formation assay (DGFA) - - 7.1 pIC50 - 1 ⤷ pIC50 7.1 (IC50 8x10-8 M) Reports on the functional viability of male and female mature stage V gametocytes [1] Lifecycle stages: Plasmodium mosquito host stage (gametocyte, gamete, zygote, ookinete, oocyst, sporozoite) Plasmodium falciparum phosphatidylinositol 4-kinase beta Pf Plasmodium falciparum P. falciparum (Pf) is one of five protozoan parasite species of the genus Plasmodium that cause malaria in humans. Pf is responsible for the majority of malaria related deaths and is the most prevalent species in sub-Saharan Africa. ✖ Parasite gametocyte viability assay - - 6.9 – 7.2 pIC50 - 1 ⤷ pIC50 7.2 (IC50 6.6x10-8 M) Parasite late stage (IV-V) gametocyte assay using luciferase reporter line [1] Lifecycle stages: Plasmodium sexual blood stage (gametocyte) pIC50 6.9 (IC50 1.34x10-7 M) Parasite early stage (I-III) gametocyte assay using luciferase reporter line [1] Lifecycle stages: Plasmodium sexual blood stage (gametocyte) Plasmodium falciparum phosphatidylinositol 4-kinase beta Pf Plasmodium falciparum P. falciparum (Pf) is one of five protozoan parasite species of the genus Plasmodium that cause malaria in humans. Pf is responsible for the majority of malaria related deaths and is the most prevalent species in sub-Saharan Africa. ✖ Standard membrane feeding assay (SMFA) - - 7.0 pIC50 - 1 ⤷ pIC50 7.0 (IC50 9.6x10-8 M) [1] Lifecycle stages: Plasmodium mosquito host stage (gametocyte, gamete, zygote, ookinete, oocyst, sporozoite)