Whole organism assay data
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MOA/likely target Sp. Assay description Type Action Value Parameter Concentration range (M) Reference Plasmodium falciparum non-SERCA-type Ca2+ -transporting P-ATPase PfTM90C2B Plasmodium falciparum TM90C2B P. falciparum TM90C2B (PfTM90C2B) is a clinical isolate, first described during a Phase 2 clinical trial to determine atovaquone efficacy in Thailand (PMID:8651372). A point mutation (Y268S) at the Qo site of cytochrome b results in a 3,000-fold loss of atovaquone sensitivity. It is used as a screening tool for the development of new cytochrome b inhibitors. ✖ Parasite growth inhibition assay - - 7.9 pEC50 - 2 ⤷ pEC50 7.9 (EC50 1.3x10-8 M) [3H]-hypoxanthine incorporation [2] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont) Plasmodium falciparum non-SERCA-type Ca2+ -transporting P-ATPase PfTM90C2A Plasmodium falciparum TM90C2A P. falciparum TM90C2A (PfTM90C2A) is a clinical isolate, first described during a Phase 2 clinical trial to determine atovaquone efficacy in Thailand (PMID:8651372). PfTM90C2A is sensitive to atovaquone. ✖ Parasite growth inhibition assay - - 7.8 pEC50 - 2 ⤷ pEC50 7.8 (EC50 1.4x10-8 M) [3H]-hypoxanthine incorporation [2] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont) Plasmodium falciparum non-SERCA-type Ca2+ -transporting P-ATPase Pf3D7 Plasmodium falciparum 3D7 P. falciparum strain 3D7 (Pf3D7) was derived from isolate NF54 by limiting dilution. The complete genome of Pf3D7 has been sequenced (GenBank: LN999946.1). Pf3D7 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 - - 7.7 pEC50 - 2 ⤷ pEC50 7.7 (EC50 1.8x10-8 M) [3H]-hypoxanthine incorporation [2] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont) Plasmodium falciparum non-SERCA-type Ca2+ -transporting P-ATPase PfFCR3 Plasmodium falciparum FCR3 P. falciparum strain FCR3 (PfFCR3) was originally isolated from a patient in The Gambia, West Africa in 1976. PfFCR3 can be obtained from the European Malaria Reagent Repository or the Malaria Research and Reference Reagent Resource Center (MR4). Differences in sensitivity of PfFCR3 clones to chloroquine have been reported, with the original isolate that was chloroquine sensitive rapidly acquiring resistance in culture (PMID: 7031656, PMID: 51801). ✖ Parasite growth inhibition assay - - 7.7 pEC50 - 2 ⤷ pEC50 7.7 (EC50 1.9x10-8 M) [3H]-hypoxanthine incorporation [2] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont) Plasmodium falciparum non-SERCA-type Ca2+ -transporting P-ATPase 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 - - 7.7 pEC50 - 2 ⤷ pEC50 7.7 (EC50 2.2x10-8 M) [3H]-hypoxanthine incorporation [2] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont) Plasmodium falciparum non-SERCA-type Ca2+ -transporting P-ATPase 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 - - 7.5 pEC50 - 2 ⤷ pEC50 7.5 (EC50 3.2x10-8 M) [3H]-hypoxanthine incorporation [2] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont) Plasmodium falciparum non-SERCA-type Ca2+ -transporting P-ATPase 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 - - 7.4 pEC50 - 2 ⤷ pEC50 7.4 (EC50 3.8x10-8 M) [3H]-hypoxanthine incorporation [2] Lifecycle stages: Plasmodium asexual blood stage (erythrocytic merozoite, trophozoite, erythrocytic schizont) Plasmodium falciparum non-SERCA-type Ca2+ -transporting P-ATPase 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 dual gamete formation assay (DGFA) - - 7.1 – 7.4 pEC50 - 2 ⤷ pEC50 7.4 (EC50 3.9x10-8 M) inhibition of gamete formation from mature Stage V male gametocytes [2] Lifecycle stages: Plasmodium sexual blood stage (gametocyte) pEC50 7.1 (EC50 7.4x10-8 M) inhibition of gamete formation from mature Stage V female gametocytes [2] Lifecycle stages: Plasmodium sexual blood stage (gametocyte)