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Enzyme Inhibition Assay from US Patent US9353089: "Compositions and methods for the treatment of malaria"
Assay data:80 Active, 76 Activity ≤ 1 µM, 82 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Efficacy of ELQ-337 In Vitro from US Patent US10584098: "Quinolone-3-diarylethers"
Assay data:12 Active, 12 Activity ≤ 1 µM, 12 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Fluorescence Resonance Energy Transfer (FRET)-Based Assay from Article 10.3109/14756360903508430: "Characterisation of hydrazides and hydrazine derivatives as novel aspartic protease inhibitors."
Assay data:6 Active, 1 Activity ≤ 1 µM, 6 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Enzyme Inhibition Assay from Article 10.1016/j.bmc.2008.08.012: "Achiral oligoamines as versatile tool for the development of aspartic protease inhibitors."
Assay data:7 Active, 1 Activity ≤ 1 µM, 11 Tested
Enzyme Inhibition Measurements from Article 10.1021/cc0301014: "High-speed optimization of inhibitors of the malarial proteases plasmepsin I and II."
Assay data:34 Active, 34 Activity ≤ 1 µM, 34 Tested
Enzyme Inhibition Measurements from Article 10.1021/jm020951i: "Design and synthesis of plasmepsin I and plasmepsin II inhibitors with activity in Plasmodium falciparum-infected cultured human erythrocytes."
Assay data:15 Active, 10 Activity ≤ 1 µM, 16 Tested
Enzyme Inhibition Measurements from Article 10.1021/jm030933g: "Potent inhibitors of the Plasmodium falciparum enzymes plasmepsin I and II devoid of cathepsin D inhibitory activity."
Assay data:21 Active, 2 Activity ≤ 1 nM, 19 Activity ≤ 1 µM, 24 Tested
Enzyme Inhibition Measurements from Article 10.1021/jm031106i: "Design and synthesis of potent inhibitors of the malaria aspartyl proteases plasmepsin I and II. Use of solid-phase synthesis to explore novel statine motifs."
Assay data:22 Active, 2 Activity ≤ 1 nM, 22 Activity ≤ 1 µM, 22 Tested
Inhibition of N-terminal His6-tagged HGXPRT expressed in Escherichia coli BL21 cells assessed as reduction in NADH absorbance using hypoxanthine as substrate by IMPDH coupled assay
Assay data:3 Active, 2 Activity ≤ 1 nM, 2 Activity ≤ 1 µM, 13 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed Citation
Induction of mitochondrial membrane loss in Plasmodium falciparum 3D7 assessed as reduction in red-green ratio at IC50 concentration incubated for 3 hrs by JC-1 staining based spectrofluorometric analysis
Assay data:4 Tested
SummaryPubMed Citation
Resistance index, ratio of IC50 for antiplasmodial activity against artemisinin partially resistant Plasmodium falciparum harbouring C580Y mutant to IC50 for antiplasmodial activity against Plasmodium falciparum 3D7
Assay data:1 Tested
Antiplasmodial activity against Plasmodium falciparum 3D7 infected in human erythrocytes assessed as accumulation of parasite growth at late trophozoite stage at 1 to 10 uM measured after 56 hrs post-treatment by giemsa staining based microscopic analysis
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed Citation
Antiplasmodial activity against Plasmodium falciparum 3D7 infected in human erythrocytes assessed as merozoite formation by measuring cytokinesis of daughter nuclei 1 to 10 uM measured for 56 hrs by giemsa staining based microscopic analysis
Assay data:2 Tested
Antiplasmodial activity against Plasmodium falciparum 3D7 infected in human erythrocytes assessed as pyknotic trophozoites development at 1 to 10 uM measured for 56 hrs by giemsa staining based microscopic analysis
Assay data:2 Active, 2 Tested
Antiplasmodial activity against Plasmodium falciparum 3D7 infected in human erythrocytes assessed as delay in maturation of rings at 1 to 10 uM measured for 56 hrs by giemsa staining based microscopic analysis
Antiplasmodial activity against Plasmodium falciparum 3D7 infected in human erythrocytes assessed as transition from ring to trophozoite at 1 to 10 uM measured for 56 hrs by giemsa staining based microscopic analysis
Antiplasmodial activity against chloroquine resistant Plasmodium falciparum RKL-9 infected in human erythrocytes assessed as inhibition of parasitemia by SYBR green-I fluorescence based spectrofluorometric analysis
Assay data:4 Active, 3 Activity ≤ 1 µM, 4 Tested
Antiplasmodial activity against artemisinin partially resistant Plasmodium falciparum harbouring C580Y mutant assessed as inhibition of parasitemia
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Resistance index, ratio of IC50 for antiplasmodial activity against chloroquine-resistant Plasmodium falciparum RKL-9 to IC50 for antiplasmodial activity against Plasmodium falciparum 3D7
Inhibition of Plasmodium falciparum Plasmepsin X assessed as inhibition constant using DABCYL-G-PSFVEAPVRGG-EDANS as substrate by fluorescence based assay relative to control
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