M5717 [Ligand Id: 9737] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4091762
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  • Plasmodium falciparum (isolate K1 / Thailand) in Plasmodium falciparum K1 [ChEMBL: CHEMBL612856]
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  • Plasmodium falciparum elongation factor 2 in Plasmodium berghei [GtoPdb: 2975]
  • Plasmodium falciparum elongation factor 2 in Plasmodium falciparum NF54 [GtoPdb: 2975]
  • Plasmodium falciparum elongation factor 2 in Plasmodium falciparum 3D7 [GtoPdb: 2975] [UniProtKB: Q8IKW5]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against erythrocytic stage of chloroquine-sensitive Plasmodium falciparum NF54 assessed as reduction in [3H]hypoxanthine incorporation after 48 hrs by liquid scintillation counting method F 9.89 pIC50 0.13 nM IC50 Bioorg Med Chem (2017) 25: 2251-2259 [PMID:28279559]
Plasmodium falciparum (isolate K1 / Thailand) in Plasmodium falciparum K1 (target type: ORGANISM) [ChEMBL: CHEMBL612856]
ChEMBL Antiplasmodial activity against erythrocytic stage of chloroquine/pyrimethamine-resistant Plasmodium falciparum K1 assessed as reduction in [3H]hypoxanthine incorporation after 48 hrs by liquid scintillation counting method F 9.66 pIC50 0.22 nM IC50 Bioorg Med Chem (2017) 25: 2251-2259 [PMID:28279559]
Plasmodium falciparum elongation factor 2 in Plasmodium berghei [GtoPdb: 2975]
GtoPdb Parasite liver stage assay - 8.78 pEC50 1.65 nM EC50 Nature (2015) 522: 315-20 [PMID:26085270]
Plasmodium falciparum elongation factor 2 in Plasmodium falciparum NF54 [GtoPdb: 2975]
GtoPdb Standard membrane feeding assay (SMFA) - 8 pEC50 10 nM EC50 Nature (2015) 522: 315-20 [PMID:26085270]
GtoPdb Parasite gamete formation assay - 8.74 pEC50 1.8 nM EC50 Nature (2015) 522: 315-20 [PMID:26085270]
GtoPdb Standard membrane feeding assay (SMFA) - 8.74 pEC50 1.8 nM EC50 Nature (2015) 522: 315-20 [PMID:26085270]
GtoPdb Parasite gamete formation assay - 8.92 pEC50 1.2 nM EC50 Nature (2015) 522: 315-20 [PMID:26085270]
Plasmodium falciparum elongation factor 2 in Plasmodium falciparum 3D7 [GtoPdb: 2975] [UniProtKB: Q8IKW5]
GtoPdb Parasite growth inhibition assay - 9 pEC50 1 nM EC50 Nature (2015) 522: 315-20 [PMID:26085270]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]