MMV048 [Ligand Id: 9726] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2041980 (J3.367.891F, MMV048, MMV-048, Mmv-390048, MMV-390048)
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  • Plasmodium falciparum (isolate K1 / Thailand) in Plasmodium falciparum K1 [ChEMBL: CHEMBL612856]
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  • Plasmodium falciparum phosphatidylinositol 4-kinase beta in Plasmodium cynomolgi [GtoPdb: 2972]
  • Plasmodium falciparum phosphatidylinositol 4-kinase beta in Plasmodium falciparum [GtoPdb: 2972]
  • Plasmodium falciparum phosphatidylinositol 4-kinase beta in Plasmodium falciparum NF54 [GtoPdb: 2972]
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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 B 5 pIC50 >10000 nM IC50 J Med Chem (2019) 62: 10526-10562 [PMID:31385706]
ChEMBL Inhibition of human ERG expressed in CHO cells by IonWorks assay B 5.33 pIC50 4700 nM IC50 J Med Chem (2012) 55: 3479-3487 [PMID:22390538]
Plasmodium cynomolgi (target type: ORGANISM) [ChEMBL: CHEMBL613883]
ChEMBL Antimalarial activity against hypnozoites stage Plasmodium cynomolgi infected in primary rhesus monkey hepatocytes measured on day 5 F 5 pEC50 >10000 nM EC50 J Med Chem (2019) 62: 10526-10562 [PMID:31385706]
ChEMBL Antimalarial activity against schizont stage Plasmodium cynomolgi infected in primary rhesus monkey hepatocytes F 7.19 pEC50 64 nM EC50 J Med Chem (2019) 62: 10526-10562 [PMID:31385706]
ChEMBL Antimalarial activity against hypnozoites stage Plasmodium cynomolgi infected in primary rhesus monkey hepatocytes F 7.21 pEC50 61 nM EC50 J Med Chem (2019) 62: 10526-10562 [PMID:31385706]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antimalarial activity against drug-resistant Plasmodium falciparum Dd2 harboring PI4K S743T mutant F 7.06 pIC50 88 nM IC50 J Med Chem (2018) 61: 4213-4227 [PMID:29665687]
ChEMBL Antiplasmodial activity against multidrug-sensitive Plasmodium falciparum NF54 transfected with GFP-Luc infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation pretreated for 48 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by liquid scintillation counting method F 7.55 pIC50 28 nM IC50 J Med Chem (2021) 64: 2291-2309 [PMID:33573376]
ChEMBL Antiplasmodial activity against Plasmodium falciparum NF54 after 24 to 72 hrs F 7.55 pIC50 28 nM IC50 J Med Chem (2018) 61: 8061-8077 [PMID:29771541]
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum NF54 after 24 hrs by hypoxanthine incorporation assay F 7.55 pIC50 28 nM IC50 J Med Chem (2012) 55: 3479-3487 [PMID:22390538]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 F 7.75 pIC50 17.8 nM IC50 Eur J Med Chem (2013) 66: 314-323 [PMID:23811093]
ChEMBL Antiplasmodial activity against chloroquine-resistant asexual erythrocytic stage of Plasmodium falciparum Dd2 assessed as parasite growth inhibition by lactate dehydrogenase assay F 7.75 pIC50 17.8 nM IC50 J Med Chem (2014) 57: 435-448 [PMID:24354322]
ChEMBL Antiplasmodial activity against chloroquine-sensitive asexual erythrocytic stage of Plasmodium falciparum D10 assessed as parasite growth inhibition by lactate dehydrogenase assay F 8.05 pIC50 9.01 nM IC50 J Med Chem (2014) 57: 435-448 [PMID:24354322]
ChEMBL Antimalarial activity against wild type Plasmodium falciparum Dd2 F 8.28 pIC50 5.2 nM IC50 J Med Chem (2018) 61: 4213-4227 [PMID:29665687]
ChEMBL Antimalarial activity against early stage Plasmodium falciparum gametocytes by luciferase reporter gene assay F 6.67 pEC50 214 nM EC50 J Med Chem (2019) 62: 10526-10562 [PMID:31385706]
ChEMBL Antimalarial activity against late stage Plasmodium falciparum gametocytes by luciferase reporter gene assay F 6.85 pEC50 140 nM EC50 J Med Chem (2019) 62: 10526-10562 [PMID:31385706]
ChEMBL Antimalarial activity against stage 5 Plasmodium falciparum assessed as reduction in oocyst formation in mosquito midgut pretreated 24 hrs before feeding by standard membrane-feeding assay F 6.95 pEC50 111 nM EC50 J Med Chem (2019) 62: 10526-10562 [PMID:31385706]
ChEMBL Antimalarial activity against late stage Plasmodium falciparum gametocytes assessed as reduction in gametogenesis exflagellation after 24 hrs F 7.05 pEC50 90 nM EC50 J Med Chem (2019) 62: 10526-10562 [PMID:31385706]
ChEMBL Ex-vivo antimalarial activity against Plasmodium falciparum serum derived from 40 mg, po treated human after 144 hrs F 7.62 pEC50 24 nM EC50 J Med Chem (2019) 62: 10526-10562 [PMID:31385706]
Plasmodium falciparum (isolate K1 / Thailand) in Plasmodium falciparum K1 (target type: ORGANISM) [ChEMBL: CHEMBL612856]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 after 24 hrs by hypoxanthine incorporation assay F 7.6 pIC50 25 nM IC50 J Med Chem (2012) 55: 3479-3487 [PMID:22390538]
Plasmodium falciparum phosphatidylinositol 4-kinase beta in Plasmodium cynomolgi [GtoPdb: 2972]
GtoPdb Parasite liver stage assay - 5 pIC50 >10000 nM IC50 Sci Transl Med (2017) 9: [PMID:28446690]
GtoPdb Parasite liver stage assay - 7.19 pIC50 64 nM IC50 Sci Transl Med (2017) 9: [PMID:28446690]
GtoPdb Parasite liver stage assay - 7.21 pIC50 61 nM IC50 Sci Transl Med (2017) 9: [PMID:28446690]
Plasmodium falciparum phosphatidylinositol 4-kinase beta in Plasmodium falciparum [GtoPdb: 2972]
GtoPdb - - 6.52 pKd 300 nM Kd Sci Transl Med (2017) 9: [PMID:28446690]
GtoPdb - - 7 pKd 100 nM Kd Sci Transl Med (2017) 9: [PMID:28446690]
GtoPdb Standard membrane feeding assay (SMFA) - 6.95 pIC50 111 nM IC50 Sci Transl Med (2017) 9: [PMID:28446690]
Plasmodium falciparum phosphatidylinositol 4-kinase beta in Plasmodium falciparum NF54 [GtoPdb: 2972]
GtoPdb Parasite gametocyte viability assay - 6.55 pIC50 285 nM IC50 Sci Transl Med (2017) 9: [PMID:28446690]
GtoPdb Parasite gametocyte viability assay - 6.67 pIC50 214 nM IC50 Sci Transl Med (2017) 9: [PMID:28446690]
GtoPdb Parasite gametocyte viability assay - 6.85 pIC50 140 nM IC50 Sci Transl Med (2017) 9: [PMID:28446690]
GtoPdb Parasite growth inhibition assay - 7.55 pIC50 28 nM IC50 Sci Transl Med (2017) 9: [PMID:28446690]

ChEMBL data shown on this page come from version 32:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]