lumefantrine [Ligand Id: 9969] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL38827 (Benflumelol, Benflumetol, CPG-56695, Dl-benflumelol, GNF-PF-1971, Lumefantrine, Lumefantrinum) |
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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 | 5.09 | pIC50 | 8128.31 | nM | IC50 | Eur J Med Chem (2011) 46: 618-630 [PMID:21185626] |
| ChEMBL | Inhibitory concentration against IKr potassium channel | B | 5.09 | pIC50 | 8100 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 4771-4777 [PMID:15324906] |
| ChEMBL | Inhibition of human ERG by fluorescence polarization assay | B | 6.42 | pIC50 | 377 | nM | IC50 | J Med Chem (2017) 60: 6036-6044 [PMID:28653845] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 3D7 by [3H]hypoxanthine incorporation assay | F | 5.77 | pIC50 | 1689 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 3131-3134 [PMID:19364853] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum harboring wild type pfcrt-76 and wild type pfmdr-1-86 gene after 18 hrs by [3H]hypoxanthine incorporation assay | F | 6.76 | pIC50 | 173 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 5069-5073 [PMID:19770282] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum harboring wild type pfmdr-1-86 gene after 18 hrs by [3H]hypoxanthine incorporation assay | F | 6.91 | pIC50 | 124 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 5069-5073 [PMID:19770282] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum harboring mutant pfcrt-76 and wild type pfmdr-1-86 gene after 18 hrs by [3H]hypoxanthine incorporation assay | F | 7 | pIC50 | 99 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 5069-5073 [PMID:19770282] |
| ChEMBL | Antiplasmodial activity against multidrug-sensitive Plasmodium falciparum 3D7 after 18 hrs by [3H]hypoxanthine incorporation assay | F | 7.02 | pIC50 | 96 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 5069-5073 [PMID:19770282] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum harboring wild type and mutant pfcrt-76 gene after 18 hrs by [3H]hypoxanthine incorporation assay | F | 7.17 | pIC50 | 67 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 5069-5073 [PMID:19770282] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum harboring wild type pfcrt-76 and mutant pfmdr-1-86 gene after 18 hrs by [3H]hypoxanthine incorporation assay | F | 7.2 | pIC50 | 63 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 5069-5073 [PMID:19770282] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum harboring wild type and mutant pfmdr-1-86 gene after 18 hrs by [3H]hypoxanthine incorporation assay | F | 7.24 | pIC50 | 57 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 5069-5073 [PMID:19770282] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum | F | 7.25 | pIC50 | 56 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3302-3307 [PMID:20516285] |
| ChEMBL | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2mef infected in human erythrocytes assessed as inhibition of [3H]hypoxanthine incorporation after 48 hrs by beta liquid scintillation counting method | F | 7.25 | pIC50 | 56 | nM | IC50 | Bioorg Med Chem (2011) 19: 7519-7525 [PMID:22055713] |
| ChEMBL | Antiplasmodial activity against multidrug-resistant Plasmodium falciparum VS/1 by [3H]hypoxanthine incorporation assay | F | 7.28 | pIC50 | 53 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 3131-3134 [PMID:19364853] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum clinical isolate after 18 hrs by [3H]hypoxanthine incorporation assay | F | 7.3 | pIC50 | 50 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 5069-5073 [PMID:19770282] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum harboring mutant pfcrt-76 gene after 18 hrs by [3H]hypoxanthine incorporation assay | F | 7.37 | pIC50 | 43 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 5069-5073 [PMID:19770282] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum harboring mutant pfmdr-1-86 gene after 18 hrs by [3H]hypoxanthine incorporation assay | F | 7.37 | pIC50 | 43 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 5069-5073 [PMID:19770282] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum harboring mutant pfcrt-76 and mutant pfmdr-1-86 gene after 18 hrs by [3H]hypoxanthine incorporation assay | F | 7.51 | pIC50 | 31 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 5069-5073 [PMID:19770282] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum Dd2 in erythrocytes | F | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 543-545 [PMID:11844668] |
| ChEMBL | Inhibition against Plasmodium falciparum Dd2 in erythrocytes in semiautomated micro dilution assay | F | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2159-2161 [PMID:12798326] |
| ChEMBL | Anti-malarial activity against Plasmodium falciparum Dd2 | F | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1539-1541 [PMID:12699750] |
| ChEMBL | Inhibitory activity against Plasmodium falciparum Dd2 in erythrocytes by semiautomated micro dilution | F | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 361-363 [PMID:12565929] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum 3D7 in erythrocytes | F | 7.54 | pIC50 | 29 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 543-545 [PMID:11844668] |
| ChEMBL | Antiplasmodial activity against multidrug-resistant Plasmodium falciparum VS/1 after 18 hrs by [3H]hypoxanthine incorporation assay | F | 7.62 | pIC50 | 24 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 5069-5073 [PMID:19770282] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum harboring K1 allele group of msp1, 3D7 allele group of msp2 gene and 94 bp of 7A11, 196bp of C4M79 and 336bp of C4M69 locus measured on day 23 by [3H]hypoxanthine incorporation assay | F | 7.82 | pIC50 | 15.2 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 2283-2284 [PMID:18411319] |
| ChEMBL | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 infected in human type A-positive red blood cells assessed as growth inhibition after 72 hrs by spectrophotometrically | F | 7.92 | pIC50 | 12 | nM | IC50 | Bioorg Med Chem (2014) 22: 5757-5765 [PMID:25311562] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum D6 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter | F | 8.1 | pIC50 | 8 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 2248-2252 [PMID:19307369] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum 3D7 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter | F | 8.1 | pIC50 | 8 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 2248-2252 [PMID:19307369] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum W2 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter | F | 8.1 | pIC50 | 8 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 2248-2252 [PMID:19307369] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum FCM29 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter | F | 8.1 | pIC50 | 8 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 2248-2252 [PMID:19307369] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum FCR3 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter | F | 8.1 | pIC50 | 8 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 2248-2252 [PMID:19307369] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum PA assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter | F | 8.1 | pIC50 | 8 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 2248-2252 [PMID:19307369] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum HB3 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter | F | 8.1 | pIC50 | 8 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 2248-2252 [PMID:19307369] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum 106/1 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter | F | 8.1 | pIC50 | 8 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 2248-2252 [PMID:19307369] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT Bres assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter | F | 8.1 | pIC50 | 8 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 2248-2252 [PMID:19307369] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT Guy assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter | F | 8.1 | pIC50 | 8 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 2248-2252 [PMID:19307369] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT A4 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter | F | 8.1 | pIC50 | 8 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 2248-2252 [PMID:19307369] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT 31 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter | F | 8.1 | pIC50 | 8 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 2248-2252 [PMID:19307369] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT 8425 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter | F | 8.1 | pIC50 | 8 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 2248-2252 [PMID:19307369] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT 9881 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter | F | 8.1 | pIC50 | 8 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 2248-2252 [PMID:19307369] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT 10336 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter | F | 8.1 | pIC50 | 8 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 2248-2252 [PMID:19307369] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT 10500 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter | F | 8.1 | pIC50 | 8 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 2248-2252 [PMID:19307369] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT 16332 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter | F | 8.1 | pIC50 | 8 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 2248-2252 [PMID:19307369] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT K14 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter | F | 8.1 | pIC50 | 8 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 2248-2252 [PMID:19307369] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT K2 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter | F | 8.1 | pIC50 | 8 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 2248-2252 [PMID:19307369] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT K4 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter | F | 8.1 | pIC50 | 8 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 2248-2252 [PMID:19307369] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT L1 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter | F | 8.1 | pIC50 | 8 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 2248-2252 [PMID:19307369] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum IMT Vol assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter | F | 8.1 | pIC50 | 8 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 2248-2252 [PMID:19307369] |
| ChEMBL | Antimalarial activity against drug-resistant Plasmodium falciparum Dd2 harboring V259L mutant infected in human erythrocytes after 72 hrs by SYBR green 1-based fluorescence assay | F | 8.19 | pIC50 | 6.5 | nM | IC50 | J Med Chem (2019) 62: 3475-3502 [PMID:30852885] |
| ChEMBL | Antimalarial activity against multidrug-resistant Plasmodium falciparum Dd2 infected in human erythrocytes by SYBR green 1-based fluorescence assay | F | 8.24 | pIC50 | 5.7 | nM | IC50 | J Med Chem (2019) 62: 3475-3502 [PMID:30852885] |
| ChEMBL | Antimalarial activity against drug-resistant Plasmodium falciparum 3D7 harboring A82T/V259L double mutant infected in human erythrocytes after 72 hrs by SYBR green 1-based fluorescence assay | F | 8.35 | pIC50 | 4.5 | nM | IC50 | J Med Chem (2019) 62: 3475-3502 [PMID:30852885] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum clinical isolates measured after 72 hrs by SYBR green dye based fluorescence assay | F | 8.38 | pIC50 | 4.2 | nM | IC50 | J Med Chem (2020) 63: 6179-6202 [PMID:32390431] |
| ChEMBL | Antimalarial activity against drug-resistant Plasmodium falciparum Dd2 harboring M133I mutant infected in human erythrocytes after 72 hrs by SYBR green 1-based fluorescence assay | F | 8.44 | pIC50 | 3.6 | nM | IC50 | J Med Chem (2019) 62: 3475-3502 [PMID:30852885] |
| ChEMBL | Antimalarial activity against drug-resistant Plasmodium falciparum Dd2 harboring M133I/A138T double mutant infected in human erythrocytes after 72 hrs by SYBR green 1-based fluorescence assay | F | 8.44 | pIC50 | 3.6 | nM | IC50 | J Med Chem (2019) 62: 3475-3502 [PMID:30852885] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum 3D7A asexual forms assessed as inhibition of [G-3H]hypoxanthine uptake incubated for 24 hrs followed by [G-3H]hypoxanthine addition and measured after 18 hrs by liquid scintillation spectrometry | F | 8.49 | pIC50 | 3.2 | nM | IC50 | Eur J Med Chem (2020) 188: 111983-111983 [PMID:31911292] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum 3D7 infected in human erythrocytes after 72 hrs by SYBR green 1-based fluorescence assay | F | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2019) 62: 3475-3502 [PMID:30852885] |
| ChEMBL | Antimicrobial activity against chloroquine-sensitive Plasmodium falciparum D6 by ELISA | F | 8.74 | pIC50 | 1.82 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 1200-1206 [PMID:20065051] |
| ChEMBL | Antimicrobial activity against chloroquine-resistant Plasmodium falciparum HB3 by ELISA | F | 8.85 | pIC50 | 1.41 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 1200-1206 [PMID:20065051] |
| ChEMBL | Antimicrobial activity against Plasmodium falciparum by ELISA | F | 9.29 | pIC50 | 0.51 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 1200-1206 [PMID:20065051] |
| ChEMBL | Antimicrobial activity against chloroquine-sensitive Plasmodium falciparum W2 by ELISA | F | 9.35 | pIC50 | 0.45 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 1200-1206 [PMID:20065051] |
| ChEMBL | Antimicrobial activity against Plasmodium falciparum harboring mdr1 N86Y/D1246Y/Y184F mutant gene by ELISA | F | 9.72 | pIC50 | 0.19 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 1200-1206 [PMID:20065051] |
| ChEMBL | NOVARTIS: Inhibition of Plasmodium falciparum 3D7 (drug-susceptible) proliferation in erythrocyte-based infection assay | F | 6.11 | pEC50 | 777 | nM | EC50 | Proc Natl Acad Sci U S A (2008) 105: 9059-9064 [PMID:18579783] |
| ChEMBL | NOVARTIS: Inhibition of Plasmodium falciparum W2 (drug-resistant) proliferation in erythrocyte-based infection assay | F | 6.29 | pEC50 | 518 | nM | EC50 | Proc Natl Acad Sci U S A (2008) 105: 9059-9064 [PMID:18579783] |
| ChEMBL | Antiplasmodial activity against multidrug-resistant Plasmodium falciparum W2 infected in human erythrocytes | F | 9.35 | pEC50 | 0.45 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 2829-2843 [PMID:23587422] |
| Plasmodium falciparum 3D7 (target type: ORGANISM) [ChEMBL: CHEMBL2366922] | ||||||||
| ChEMBL | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in human type A-positive red blood cells assessed as growth inhibition after 72 hrs by spectrophotometrically | F | 7.92 | pIC50 | 12 | nM | IC50 | Bioorg Med Chem (2014) 22: 5757-5765 [PMID:25311562] |
| Plasmodium falciparum (isolate K1 / Thailand) in Plasmodium falciparum K1 (target type: ORGANISM) [ChEMBL: CHEMBL612856] | ||||||||
| ChEMBL | Antimicrobial activity against chloroquine-resistant Plasmodium falciparum K1 by ELISA | F | 9.51 | pIC50 | 0.31 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 1200-1206 [PMID:20065051] |
| Plasmodium vivax (target type: ORGANISM) [ChEMBL: CHEMBL613013] | ||||||||
| ChEMBL | Antimicrobial activity against Plasmodium vivax at the ring stage measured after 30 hrs by microscopy | F | 7.42 | pIC50 | 37.6 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 1040-1045 [PMID:18180357] |
| ChEMBL | Antimicrobial activity against Plasmodium vivax trophozoites measured after 30 hrs by microscopy | F | 7.48 | pIC50 | 32.9 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 1040-1045 [PMID:18180357] |
| ChEMBL | Antimicrobial activity against Plasmodium vivax at the ring stage measured within 30 hrs by microscopy | F | 7.61 | pIC50 | 24.8 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 1040-1045 [PMID:18180357] |
| ChEMBL | Antimalarial activity against chloroquine-resistant Plasmodium vivax by Giemsa staining | F | 7.8 | pIC50 | 16 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 1094-1099 [PMID:19104023] |
| ChEMBL | Antimicrobial activity against Plasmodium vivax trophozoites measured within 30 hrs by microscopy | F | 7.84 | pIC50 | 14.6 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 1040-1045 [PMID:18180357] |
ChEMBL data shown on this page come from version 33:
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]
