ELQ-300 [Ligand Id: 10021] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2431810
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  • Plasmodium falciparum cytochrome b in Plasmodium falciparum TM90C2B [GtoPdb: 3087]
  • Plasmodium falciparum cytochrome b in Plasmodium berghei [GtoPdb: 3087]
  • Plasmodium falciparum cytochrome b in Plasmodium cynomolgi [GtoPdb: 3087]
  • Plasmodium falciparum cytochrome b in Plasmodium falciparum NF54 [GtoPdb: 3087]
  • Plasmodium falciparum cytochrome b in Plasmodium falciparum Dd2 [GtoPdb: 3087]
  • Plasmodium falciparum cytochrome b in Plasmodium falciparum D6 [GtoPdb: 3087]
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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 Antimalarial activity against drug-resistant Plasmodium falciparum Dd2 harboring CytB Ile22Leu mutant F 6.83 pIC50 148 nM IC50 J Med Chem (2018) 61: 4213-4227 [PMID:29665687]
ChEMBL Antimalarial activity against wild type Plasmodium falciparum Dd2 F 7.7 pIC50 20 nM IC50 J Med Chem (2018) 61: 4213-4227 [PMID:29665687]
ChEMBL Antimalarial activity against Plasmodium falciparum 3D7 F 8.3 pIC50 5 nM IC50 J Med Chem (2016) 59: 5587-5603 [PMID:26791529]
ChEMBL Antimalarial activity against atovaquone-resistant Plasmodium falciparum TM90C2B F 8.52 pIC50 3 nM IC50 J Med Chem (2016) 59: 5587-5603 [PMID:26791529]
ChEMBL Antimalarial activity against atovaquone-resistant clinical isolate Plasmodium falciparum TM90-C2B infected in human red blood cells assessed as suppression of parasitemia after 72 hrs by SYBR Green I-based fluorescence method F 8.85 pEC50 1.4 nM EC50 J Med Chem (2014) 57: 3818-3834 [PMID:24720377]
ChEMBL Antiparasitic activity against Plasmodium falciparum 3D7 F 8.89 pEC50 1.3 nM EC50 Eur J Med Chem (2019) 181: 111353-111353 [PMID:31525705]
ChEMBL Antiparasitic activity against Plasmodium falciparum D6 F 8.89 pEC50 1.3 nM EC50 Eur J Med Chem (2019) 181: 111353-111353 [PMID:31525705]
ChEMBL Antiparasitic activity against Plasmodium falciparum infected in human PBMC F 8.89 pEC50 1.3 nM EC50 Eur J Med Chem (2019) 181: 111353-111353 [PMID:31525705]
ChEMBL Antimalarial activity against Plasmodium falciparum TM93-C1088 assessed as suppression of parasitemia after 72 hrs by SYBR Green I-based fluorescence method F 9 pEC50 1 nM EC50 J Med Chem (2014) 57: 3818-3834 [PMID:24720377]
ChEMBL Antimicrobial activity against clinical isolates of Plasmodium falciparum F 9 pEC50 1 nM EC50 J Med Chem (2013) 56: 7741-7749 [PMID:23927720]
ChEMBL Antiparasitic activity against Plasmodium falciparum F 9.24 pEC50 0.58 nM EC50 Eur J Med Chem (2019) 181: 111353-111353 [PMID:31525705]
Plasmodium falciparum D6 (target type: ORGANISM) [ChEMBL: CHEMBL2367107]
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 MRA-285 infected in human red blood cells assessed as suppression of parasitemia after 72 hrs by SYBR Green I-based fluorescence method F 8.66 pEC50 2.2 nM EC50 J Med Chem (2014) 57: 3818-3834 [PMID:24720377]
Plasmodium falciparum cytochrome b in Plasmodium falciparum TM90C2B [GtoPdb: 3087]
GtoPdb Parasite growth inhibition assay - 8.55 pIC50 2.84 nM IC50 Sci Transl Med (2013) 5: 177ra37 [PMID:23515079]
GtoPdb Parasite growth inhibition assay - 8.77 pIC50 1.7 nM IC50 Sci Transl Med (2013) 5: 177ra37 [PMID:23515079]
Plasmodium falciparum cytochrome b in Plasmodium berghei [GtoPdb: 3087]
GtoPdb Parasite liver stage assay - 8.99 pEC50 1.02 nM EC50 Sci Transl Med (2013) 5: 177ra37 [PMID:23515079]
Plasmodium falciparum cytochrome b in Plasmodium cynomolgi [GtoPdb: 3087]
GtoPdb Parasite liver stage assay - 7 pIC50 ~100 nM IC50 Sci Transl Med (2013) 5: 177ra37 [PMID:23515079]
Plasmodium falciparum cytochrome b in Plasmodium falciparum NF54 [GtoPdb: 3087]
GtoPdb Parasite late stage (IV–V) gametocyte assay - 7.14 pIC50 71.9 nM IC50 Sci Transl Med (2013) 5: 177ra37 [PMID:23515079]
Plasmodium falciparum cytochrome b in Plasmodium falciparum Dd2 [GtoPdb: 3087]
GtoPdb Parasite growth inhibition assay - 8.6 pIC50 2.5 nM IC50 Sci Transl Med (2013) 5: 177ra37 [PMID:23515079]
Plasmodium falciparum cytochrome b in Plasmodium falciparum D6 [GtoPdb: 3087]
GtoPdb Parasite growth inhibition assay - 8.51 pIC50 3.06 nM IC50 Sci Transl Med (2013) 5: 177ra37 [PMID:23515079]
GtoPdb Parasite growth inhibition assay - 8.66 pIC50 2.2 nM IC50 Sci Transl Med (2013) 5: 177ra37 [PMID:23515079]

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]