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

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ChEMBL ligand: CHEMBL4091762 (DDD107498, DDD-107498, DDD498, M5717, M-5717, MMV121, MMV-121)
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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
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG by IonWorks patch-clamp electrophysiology method B 4.8 pIC50 16000 nM IC50 J Med Chem (2016) 59: 9672-9685 [PMID:27631715]
Plasmodium berghei (target type: ORGANISM) [ChEMBL: CHEMBL612653]
ChEMBL Antiplasmodial activity against Plasmodium berghei ookinete form assessed as growth inhibition incubated for 22 hrs by GFP-based fluorescence microscopic analysis F 8.3 pEC50 5 nM EC50 J Med Chem (2016) 59: 9672-9685 [PMID:27631715]
ChEMBL Antimalarial activity against Plasmodium berghei ookinete form F 8.3 pEC50 5 nM EC50 J Med Chem (2016) 59: 9668-9671 [PMID:27775354]
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]
ChEMBL Antiplasmodial activity against late stage (IV/V) Plasmodium falciparum NF54 gametocytes transfected with GFP-LUC assessed as growth inhibition incubated for 72 hrs by mitotracker Red-CMXROS dye based fluorescence microscopic analysis F 7.62 pEC50 24 nM EC50 J Med Chem (2016) 59: 9672-9685 [PMID:27631715]
ChEMBL Antimalarial activity against Plasmodium falciparum late stage (IV-V) gametocytes F 7.62 pEC50 24 nM EC50 J Med Chem (2016) 59: 9668-9671 [PMID:27775354]
ChEMBL Antimalarial activity against Plasmodium falciparum 3D7 F 9 pEC50 1 nM EC50 J Med Chem (2016) 59: 9668-9671 [PMID:27775354]
ChEMBL Antimalarial activity against drug resistant Plasmodium falciparum D6 F 9 pEC50 <1 nM EC50 J Med Chem (2016) 59: 9668-9671 [PMID:27775354]
ChEMBL Antimalarial activity against drug resistant Plasmodium falciparum V1/S F 9 pEC50 <1 nM EC50 J Med Chem (2016) 59: 9668-9671 [PMID:27775354]
ChEMBL Antimalarial activity against drug resistant Plasmodium falciparum 7G8 F 9 pEC50 <1 nM EC50 J Med Chem (2016) 59: 9668-9671 [PMID:27775354]
ChEMBL Antimalarial activity against drug resistant Plasmodium falciparum TM90C2A F 9 pEC50 <1 nM EC50 J Med Chem (2016) 59: 9668-9671 [PMID:27775354]
ChEMBL Antimalarial activity against drug resistant Plasmodium falciparum K1 F 9 pEC50 <1 nM EC50 J Med Chem (2016) 59: 9668-9671 [PMID:27775354]
ChEMBL Antimalarial activity against drug resistant Plasmodium falciparum W2 F 9 pEC50 <1 nM EC50 J Med Chem (2016) 59: 9668-9671 [PMID:27775354]
ChEMBL Antimalarial activity against drug resistant Plasmodium falciparum NF5 F 9 pEC50 <1 nM EC50 J Med Chem (2016) 59: 9668-9671 [PMID:27775354]
ChEMBL Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in human red blood cells assessed as growth inhibition by SYBR Green fluorescence assay F 9 pEC50 1 nM EC50 J Med Chem (2016) 59: 9672-9685 [PMID:27631715]
ChEMBL Antiplasmodial activity against drug resistant Plasmodium falciparum V1/S by [3H]hypoxanthine incorporation assay F 9.15 pEC50 0.7 nM EC50 J Med Chem (2016) 59: 9672-9685 [PMID:27631715]
ChEMBL Antiplasmodial activity against drug resistant Plasmodium falciparum K1 by [3H]hypoxanthine incorporation assay F 9.4 pEC50 0.4 nM EC50 J Med Chem (2016) 59: 9672-9685 [PMID:27631715]
ChEMBL Antiplasmodial activity against drug resistant Plasmodium falciparum 7G8 by [3H]hypoxanthine incorporation assay F 9.4 pEC50 0.4 nM EC50 J Med Chem (2016) 59: 9672-9685 [PMID:27631715]
ChEMBL Antiplasmodial activity against drug resistant Plasmodium falciparum D6 by [3H]hypoxanthine incorporation assay F 9.4 pEC50 0.4 nM EC50 J Med Chem (2016) 59: 9672-9685 [PMID:27631715]
ChEMBL Antiplasmodial activity against drug resistant Plasmodium falciparum TM90C2A by [3H]hypoxanthine incorporation assay F 9.4 pEC50 0.4 nM EC50 J Med Chem (2016) 59: 9672-9685 [PMID:27631715]
ChEMBL Antiplasmodial activity against drug resistant Plasmodium falciparum W2 by [3H]hypoxanthine incorporation assay F 9.4 pEC50 0.4 nM EC50 J Med Chem (2016) 59: 9672-9685 [PMID:27631715]
ChEMBL Antiplasmodial activity against drug resistant Plasmodium falciparum NF5 by [3H]hypoxanthine incorporation assay F 9.52 pEC50 0.3 nM EC50 J Med Chem (2016) 59: 9672-9685 [PMID:27631715]
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 yoelii (target type: ORGANISM) [ChEMBL: CHEMBL612889]
ChEMBL Antiplasmodial activity against Plasmodium yoelli liver stage forms F 9 pEC50 1 nM EC50 J Med Chem (2016) 59: 9672-9685 [PMID:27631715]
ChEMBL Antimalarial activity against Plasmodium yoelii F 9 pEC50 1 nM EC50 J Med Chem (2016) 59: 9668-9671 [PMID:27775354]
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 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]