atovaquone [Ligand Id: 9695] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1450 (Wellvone, 566C, Mepron, Atovaquone, 566C80)
  • Dihydroorotate dehydrogenase in Plasmodium falciparum [ChEMBL: CHEMBL3486] [UniProtKB: Q54A96]
  • dihydroorotate dehydrogenase (quinone)/Dihydroorotate dehydrogenase in Human [ChEMBL: CHEMBL1966] [GtoPdb: 2604] [UniProtKB: Q02127]
  • dihydroorotate dehydrogenase (quinone)/Dihydroorotate dehydrogenase in Rat [ChEMBL: CHEMBL2383] [GtoPdb: 2604] [UniProtKB: Q63707]
  • Dihydroorotate dehydrogenase in Saccharomyces cerevisiae S288c [ChEMBL: CHEMBL5621] [UniProtKB: P28272]
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  • Plasmodium falciparum (isolate K1 / Thailand) in Plasmodium falciparum K1 [ChEMBL: CHEMBL612856]
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  • Plasmodium falciparum cytochrome b in Plasmodium falciparum TM90C2A [GtoPdb: 3087]
  • Plasmodium falciparum cytochrome b in Plasmodium falciparum K1 [GtoPdb: 3087]
  • Plasmodium falciparum cytochrome b in Plasmodium falciparum NF54 [GtoPdb: 3087]
  • Plasmodium falciparum cytochrome b in Plasmodium falciparum 7G8 [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
Dihydroorotate dehydrogenase in Plasmodium falciparum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3486] [UniProtKB: Q54A96]
ChEMBL Inhibition of plasmodium falciparum DHODH assessed as inhibition of [14C]bicarbonate incorporation into pyrimidine nucleotide by HPLC analysis B 4.57 pKi 27000 nM Ki J. Med. Chem. (2013) 56: 3148-3167 [PMID:23452331]
ChEMBL Inhibition of Plasmodium falciparum DHOD B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 972-975 [PMID:19097788]
dihydroorotate dehydrogenase (quinone)/Dihydroorotate dehydrogenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1966] [GtoPdb: 2604] [UniProtKB: Q02127]
ChEMBL Competitive inhibition of human purified recombinant DHODH in presence of cofactor ubiquinone B 5.57 pKi 2.7 uM Kic J. Med. Chem. (2013) 56: 3148-3167 [PMID:23452331]
ChEMBL Inhibition of human purified recombinant DHODH B 4.84 pIC50 14500 nM IC50 J. Med. Chem. (2013) 56: 3148-3167 [PMID:23452331]
dihydroorotate dehydrogenase (quinone)/Dihydroorotate dehydrogenase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2383] [GtoPdb: 2604] [UniProtKB: Q63707]
ChEMBL Competitive inhibition of rat purified recombinant DHODH in presence of cofactor ubiquinone B 7.22 pKi 60 nM Kic J. Med. Chem. (2013) 56: 3148-3167 [PMID:23452331]
ChEMBL Inhibition of rat purified recombinant DHODH B 6.15 pIC50 700 nM IC50 J. Med. Chem. (2013) 56: 3148-3167 [PMID:23452331]
Dihydroorotate dehydrogenase in Saccharomyces cerevisiae S288c (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5621] [UniProtKB: P28272]
ChEMBL Inhibition of Saccharomyces cerevisiae DHOD B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 972-975 [PMID:19097788]
Plasmodium berghei (target type: ORGANISM) [ChEMBL: CHEMBL612653]
ChEMBL Antimalarial activity against sporozoite stage of Plasmodium berghei yoelii infected in human HepG2 cells F 7.66 pIC50 22 nM IC50 J. Med. Chem. (2016) 59: 264-281 [PMID:26640981]
ChEMBL Antimalarial activity against liver stages of Plasmodium berghei assessed as inhibition of cytochrome bc1 complex F 7.71 pIC50 19.7 nM IC50 J. Med. Chem. (2012) 55: 995-1012 [PMID:22122518]
ChEMBL Antiplasmodial activity against liver-stage of Plasmodium berghei expressing firefly luciferase infected in human Huh-7 cells after 48 hrs by bioluminescence assay F 8.74 pIC50 1.8 nM IC50 Eur. J. Med. Chem. (2015) 101: 266-273 [PMID:26142491]
ChEMBL Antimalarial activity against GFP-fused Plasmodium berghei ANKA liver stage infected in HuH7 cells pretreated for 1 hr followed by parasite infection after 48 hrs by luciferase reporter gene assay F 9 pIC50 1 nM IC50 J Med Chem (2017) 60: 1432-1448 [PMID:28094524]
ChEMBL Antiplasmodial activity against liver stage Plasmodium berghei infected in human HuH7 cells co-expressing GFP-Luccon treated for 1 hr prior to infection followed by 24 hrs after compound washout measured after 48 hrs post-infection by Alamar Blue assay F 9.42 pIC50 0.38 nM IC50 J. Med. Chem. (2013) 56: 4811-4815 [PMID:23701465]
ChEMBL HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells F 9.52 pIC50 0.3 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2012) 109: 8511-8516 [PMID:22586124]
ChEMBL Gametocytocidal activity against GFP-fused Plasmodium berghei liver stage gametocytes infected in human HepG2-A16-CD81-EGFP cells after 48 hrs by luciferase reporter gene assay F 9.59 pIC50 0.26 nM IC50 J Med Chem (2017) 60: 6036-6044 [PMID:28653845]
ChEMBL Antimalarial activity against exo-erythrocytic form of Plasmodium berghei infected in human HepG2 cells after 48 hrs F 9.8 pIC50 0.16 nM IC50 Eur. J. Med. Chem. (2014) 82: 204-213 [PMID:24904967]
ChEMBL Antiplasmodial activity against exo-erythrocytic stage of GFP-Luc-fused Plasmodium berghei ANKA infected in human HepG2 cells after 48 hrs by bioluminescence assay F 10.85 pIC50 0.01 nM IC50 Eur J Med Chem (2018) 158: 801-813 [PMID:30245402]
ChEMBL Antimicrobial activity against Plasmodium berghei sporozoites infected in 12 hrs compound pretreated human HepG2 cells assessed as reduction in viability of exoerythrocytic forms measured after 48 hrs of incubation by luciferase bioluminescence assay F 9.3 pEC50 0.5 nM EC50 J. Med. Chem. (2014) 57: 2773-2788 [PMID:24641010]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 gametocytes (stage 4 & 5) F 4.3 pIC50 50400 nM IC50 Antimicrob. Agents Chemother. (2007) 51: 1463-1472 [PMID:17242150]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 gametocytes (stage 2 & 3) F 4.62 pIC50 24000 nM IC50 Antimicrob. Agents Chemother. (2007) 51: 1463-1472 [PMID:17242150]
ChEMBL Antimalarial activity against atoquinone-resistant Plasmodium falciparum TM90C2B containing cytochrome-b Y268S mutant F 4.92 pIC50 12000 nM IC50 J. Med. Chem. (2012) 55: 1844-1857 [PMID:22364417]
ChEMBL Antimalarial activity against atoquinone-resistant Plasmodium falciparum TM90C2B F 4.92 pIC50 12000 nM IC50 J. Med. Chem. (2012) 55: 1831-1843 [PMID:22364416]
ChEMBL Antiplasmodial activity against multidrug-resistant Plasmodium falciparum TM90C2B by SYBR Green 1-based fluorescence assay F 4.92 pIC50 12000 nM IC50 Antimicrob. Agents Chemother. (2010) 54: 3597-3604 [PMID:20547797]
ChEMBL Antimalarial activity against schizont stage of atovaquone-resistant Plasmodium falciparum Tm90C2b infected in erythrocytes assessed as inhibition of [3H]hypoxanthine incorporation after 48 hrs by scintillation counting analysis F 5 pIC50 >10000 nM IC50 MedChemComm (2011) 2: 430-435
ChEMBL Antimalarial activity against Plasmodium falciparum DD2 expressing Saccharomyces cerevisiae DHOD by [3H]hypoxanthine uptake F 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 972-975 [PMID:19097788]
ChEMBL Antimalarial activity against drug resistant Plasmodium falciparum TM90C2B infected in human erythrocytes assessed as growth inhibition after 48 hrs by SYBR Green 1 staining-based fluorescence assay F 5 pIC50 9908 nM IC50 MedChemComm (2015) 6: 1252-1259
ChEMBL Antiplasmodial activity against Plasmodium falciparum SB1 after 72 hrs by SYBR I method F 5.7 pIC50 >2000 nM IC50 J. Med. Chem. (2014) 57: 5702-5713 [PMID:24914738]
ChEMBL Antiplasmodial activity against Plasmodium falciparum SB1-A6 harboring mutations conferring drug-resistance by SYBR-green based assay F 5.7 pIC50 >2000 nM IC50 J. Med. Chem. (2014) 57: 6642-6652 [PMID:25007124]
ChEMBL Antimalarial activity after 48 hrs against atovaquone-resistant Plasmodium falciparum FCR3 by [3H]hypoxanthine uptake F 5.72 pIC50 1890 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 3476-3480 [PMID:19467600]
ChEMBL Antimalarial activity against Plasmodium falciparum FCR3-A infected erythrocytes as [3H]hypoxanthine incorporation F 5.87 pIC50 1360 nM IC50 J. Med. Chem. (2008) 51: 2845-2852 [PMID:18396855]
ChEMBL Antimicrobial activity against Plasmodium falciparum F 6 pIC50 1000 nM IC50 Bioorg. Med. Chem. (2010) 18: 2225-2231 [PMID:20185316]
ChEMBL Antimicrobial activity against Plasmodium falciparum harboring Y268S mutant Cytb gene, 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 F 6.41 pIC50 390 nM IC50 Antimicrob. Agents Chemother. (2008) 52: 2283-2284 [PMID:18411319]
ChEMBL Antimalarial activity against schizont stage of atovaquone-resistant Plasmodium falciparum Tm90C2b infected in erythrocytes assessed as inhibition of [3H]hypoxanthine incorporation after 96 hrs by scintillation counting analysis F 6.41 pIC50 388 nM IC50 MedChemComm (2011) 2: 430-435
ChEMBL Antimalarial activity against Plasmodium falciparum TM90C2B infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation preincubated for 24 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by scintillation counting method F 7.46 pIC50 >35 nM IC50 J Med Chem (2017) 60: 5889-5908 [PMID:28635296]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 asexual gametocytes F 8.34 pIC50 4.6 nM IC50 Antimicrob. Agents Chemother. (2007) 51: 1463-1472 [PMID:17242150]
ChEMBL Antimalarial activity against liver stages of Plasmodium falciparum NF54 infected in human HepG2-A16 cells expressing CD81 assessed as growth inhibition of hepatic parasite after 5 days by fluorescence microscopy F 8.4 pIC50 3.95 nM IC50 J. Med. Chem. (2012) 55: 995-1012 [PMID:22122518]
ChEMBL Antimalarial activity against schizont stage of chloroquine-resistant Plasmodium falciparum W2 infected in erythrocytes assessed as inhibition of [3H]hypoxanthine incorporation after 48 hrs by scintillation counting analysis F 8.41 pIC50 3.9 nM IC50 MedChemComm (2011) 2: 430-435
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 infected in RBC by flow cytometry analysis F 8.52 pIC50 3 nM IC50 Eur. J. Med. Chem. (2013) 59: 48-53 [PMID:23202850]
ChEMBL Antimalarial activity against Plasmodium falciparum T9-96 infected Rhesus positive human erythrocytes by [3H]hypoxanthine uptake F 8.52 pIC50 3 nM IC50 J. Med. Chem. (2008) 51: 2845-2852 [PMID:18396855]
ChEMBL Antimalarial activity against Plasmodium falciparum IMT Vol assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter F 8.62 pIC50 2.4 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 8.62 pIC50 2.4 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 8.62 pIC50 2.4 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 8.62 pIC50 2.4 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2248-2252 [PMID:19307369]
ChEMBL Antimalarial activity against Plasmodium falciparum D6 assessed as incorporation of [3H]hypoxanthine after 48 hrs by scintillation counter F 8.62 pIC50 2.4 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 8.62 pIC50 2.4 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 8.62 pIC50 2.4 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 8.62 pIC50 2.4 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 8.62 pIC50 2.4 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 8.62 pIC50 2.4 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 8.62 pIC50 2.4 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 8.62 pIC50 2.4 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 8.62 pIC50 2.4 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 8.62 pIC50 2.4 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 8.62 pIC50 2.4 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 8.62 pIC50 2.4 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 8.62 pIC50 2.4 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 8.62 pIC50 2.4 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 8.62 pIC50 2.4 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 8.62 pIC50 2.4 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 8.62 pIC50 2.4 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 8.62 pIC50 2.4 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2248-2252 [PMID:19307369]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR I method F 8.63 pIC50 2.32 nM IC50 J. Med. Chem. (2014) 57: 5702-5713 [PMID:24914738]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 harboring mutations conferring drug-resistance by SYBR-green based assay F 8.64 pIC50 2.3 nM IC50 J. Med. Chem. (2014) 57: 6642-6652 [PMID:25007124]
ChEMBL Antiplasmodial activity against Plasmodium falciparum Dd2 harboring mutations conferring drug-resistance by SYBR-green based assay F 8.7 pIC50 2 nM IC50 J. Med. Chem. (2014) 57: 6642-6652 [PMID:25007124]
ChEMBL Antimalarial activity against schizont stage of chloroquine-resistant Plasmodium falciparum W2 infected in erythrocytes assessed as inhibition of [3H]hypoxanthine incorporation after 96 hrs by scintillation counting analysis F 8.7 pIC50 2 nM IC50 MedChemComm (2011) 2: 430-435
ChEMBL Antimalarial activity against Plasmodium falciparum Dd2 infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation preincubated for 24 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by scintillation counting method F 8.7 pIC50 2 nM IC50 J Med Chem (2017) 60: 5889-5908 [PMID:28635296]
ChEMBL Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR I method F 8.7 pIC50 2 nM IC50 J. Med. Chem. (2014) 57: 5702-5713 [PMID:24914738]
ChEMBL Antimalarial activity against Plasmodium falciparum DD2 by [3H]hypoxanthine uptake F 8.7 pIC50 2 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 972-975 [PMID:19097788]
ChEMBL Antimalarial activity against chloroquine-resistant/mefloquine-sensitive Plasmodium falciparum W2 ring stage forms infected in human erythrocytes assessed as reduction in parasite growth after 48 hrs by parasite LDH release assay F 8.91 pIC50 1.22 nM IC50 Eur J Med Chem (2018) 145: 191-205 [PMID:29324340]
ChEMBL Antimalarial activity after 48 hrs against chloroquine-resistant Plasmodium falciparum W2 by [3H]hypoxanthine uptake F 8.92 pIC50 1.2 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 3476-3480 [PMID:19467600]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 harboring mutations conferring drug-resistance by SYBR-green based assay F 8.92 pIC50 1.2 nM IC50 J. Med. Chem. (2014) 57: 6642-6652 [PMID:25007124]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR I method F 8.94 pIC50 1.16 nM IC50 J. Med. Chem. (2014) 57: 5702-5713 [PMID:24914738]
ChEMBL Inhibitory activity against Plasmodium falciparum Dd2 in erythrocytes F 9 pIC50 1 nM IC50 Bioorg. Med. Chem. Lett. (2001) 11: 423-424 [PMID:11212126]
ChEMBL OSM: Inhibition of Plasmodium falciparum 3D7 growth using a SYBR green I fluorescence based assay. GSK Tres Cantos. F 9 pIC50 1 nM IC50 Open Source Malaria Deposition 1. http://malaria.ourexperiment.org
ChEMBL Antimalarial activity against ring stage Plasmodium falciparum 3D7 infected in human erythrocytes after 48 hrs by flow cytometry F 9 pIC50 1 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 1299-1307 [PMID:22243961]
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation preincubated for 24 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by scintillation counting method F 9 pIC50 1 nM IC50 J Med Chem (2017) 60: 5889-5908 [PMID:28635296]
ChEMBL Antimalarial activity against Plasmodium falciparum NF54 infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation preincubated for 24 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by scintillation counting method F 9 pIC50 1 nM IC50 J Med Chem (2017) 60: 5889-5908 [PMID:28635296]
ChEMBL Antimalarial activity against Plasmodium falciparum T9/94 infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation preincubated for 24 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by scintillation counting method F 9 pIC50 1 nM IC50 J Med Chem (2017) 60: 5889-5908 [PMID:28635296]
ChEMBL Antimalarial activity against Plasmodium falciparum TM90C2A infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation preincubated for 24 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by scintillation counting method F 9 pIC50 1 nM IC50 J Med Chem (2017) 60: 5889-5908 [PMID:28635296]
ChEMBL Antimalarial activity against Plasmodium falciparum V1/S infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation preincubated for 24 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by scintillation counting method F 9 pIC50 1 nM IC50 J Med Chem (2017) 60: 5889-5908 [PMID:28635296]
ChEMBL Antimalarial activity against NITD609-resistant Plasmodium falciparum Dd2 Clone2 bearing P-type ATPase4 T418N and P990R mutations after 72 hrs by SYBR green based fluorescence assay F 9.1 pIC50 0.8 nM IC50 Science (2010) 329: 1175-1180 [PMID:20813948]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 by SYBR Green 1-based fluorescence assay F 9.1 pIC50 0.8 nM IC50 Antimicrob. Agents Chemother. (2010) 54: 3597-3604 [PMID:20547797]
ChEMBL Antimalarial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green based fluorescence assay F 9.1 pIC50 0.8 nM IC50 Science (2010) 329: 1175-1180 [PMID:20813948]
ChEMBL Antimalarial activity against Plasmodium falciparum Nigerian assessed as [3H]hypoxanthine uptake after 48 hrs by liquid scintillation counting F 9.12 pIC50 0.75 nM IC50 Eur. J. Med. Chem. (2009) 44: 4778-4782 [PMID:19747753]
ChEMBL Growth inhibition of Plasmodium falciparum ring stage in infected erythrocytes by DAPI growth assay F 9.18 pIC50 0.66 nM IC50 Antimicrob. Agents Chemother. (2007) 51: 716-723 [PMID:17116676]
ChEMBL Growth inhibition of Plasmodium falciparum ring stage in infected erythrocytes by DAPI growth assay F 9.2 pIC50 0.63 nM IC50 Antimicrob. Agents Chemother. (2007) 51: 716-723 [PMID:17116676]
ChEMBL Growth inhibition of Plasmodium falciparum as reduced [3H]hypoxanthine incorporation F 9.21 pIC50 0.61 nM IC50 Antimicrob. Agents Chemother. (2007) 51: 716-723 [PMID:17116676]
ChEMBL Antimalarial activity against NITD609-resistant Plasmodium falciparum Dd2 Clone1 bearing P-type ATPase4 I398F and P990R mutations after 72 hrs by SYBR green based fluorescence assay F 9.22 pIC50 0.6 nM IC50 Science (2010) 329: 1175-1180 [PMID:20813948]
ChEMBL Antimalarial activity against NITD609-resistant Plasmodium falciparum Dd2 Clone3 bearing P-type ATPase4 D1247Y mutations after 72 hrs by SYBR green based fluorescence assay F 9.22 pIC50 0.6 nM IC50 Science (2010) 329: 1175-1180 [PMID:20813948]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 infected in human erythrocytes assessed as reduction in parasitemia after 48 hrs by flow cytometry analysis F 9.3 pIC50 0.5 nM IC50 ACS Med. Chem. Lett. (2012) 3: 1029-1033 [PMID:24936235]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 infected in RBCs by firefly luciferase reporter gene assay F 9.39 pIC50 0.41 nM IC50 Antimicrob. Agents Chemother. (2010) 54: 3597-3604 [PMID:20547797]
ChEMBL Antimalarial activity against drug resistant Plasmodium falciparum W2 infected in human erythrocytes assessed as growth inhibition after 48 hrs by SYBR Green 1 staining-based fluorescence assay F 9.52 pIC50 0.3 nM IC50 MedChemComm (2015) 6: 1252-1259
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 infected in human erythrocytes F 9.55 pIC50 0.28 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 2976-2979 [PMID:22414614]
ChEMBL Antimalarial activity against Plasmodium falciparum 3D7A infected erythrocytes by [3H]hypoxanthine uptake F 9.57 pIC50 0.27 nM IC50 J. Med. Chem. (2008) 51: 2845-2852 [PMID:18396855]
ChEMBL Antimalarial activity against multi-drug-resistant Plasmodium falciparum TM90-C2B infected in human type A+ erythrocytes assessed as growth inhibition after 72 hrs by SYBR Green I assay F 4.74 pEC50 18400 nM EC50 J. Med. Chem. (2014) 57: 8860-8879 [PMID:25148516]
ChEMBL Antimalarial activity against mefloquine/chloroquine/atovaquone/pyrimethamine-resistant Plasmodium falciparum TM90-C2B infected in human type A-positive erythrocytes after 48 hrs by [3H]-hypoxanthine incorporation assay F 4.74 pEC50 18000 nM EC50 J Med Chem (2018) 61: 1450-1473 [PMID:29215279]
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 5.11 pEC50 7700 nM EC50 J. Med. Chem. (2014) 57: 3818-3834 [PMID:24720377]
ChEMBL Antimalarial activity against multidrug-resistant Plasmodium falciparum TM90-C2B infected in O-positive erythrocytes assessed as reduction in parasitemia after 72 hrs by spectrofluorometry F 5.82 pEC50 >1500 nM EC50 J. Med. Chem. (2012) 55: 4205-4219 [PMID:22435599]
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D10 expressing yeast DHODH infected in O-positive erythrocytes assessed as reduction in parasitemia after 72 hrs by spectrofluorometry F 5.82 pEC50 >1500 nM EC50 J. Med. Chem. (2012) 55: 4205-4219 [PMID:22435599]
ChEMBL Antimalarial activity against chloroquine, mefloquine, pyrimethamine and atovaquone-resistant Plasmodium falciparum TM90-C2B infected in human A positive erythrocytes after 72 hrs by SYBR Green I assay F 6.77 pEC50 >170 nM EC50 J. Med. Chem. (2011) 54: 4399-4426 [PMID:21630666]
ChEMBL Antimalarial activity against chloroquine-, mefloquine-, pyrimethamine-,atovaquone-resistant ring stage Plasmodium falciparum TM90-C2B infected in human A positive erythrocytes after 72 hrs by SYBR green 1-based fluorescence assay F 6.77 pEC50 >170 nM EC50 J. Med. Chem. (2011) 54: 8321-8327 [PMID:22111907]
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D10 infected in O-positive erythrocytes assessed as reduction in parasitemia after 72 hrs by spectrofluorometry F 7.8 pEC50 16 nM EC50 J. Med. Chem. (2012) 55: 4205-4219 [PMID:22435599]
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D10 expressing yeast DHODH infected in O-positive erythrocytes assessed as reduction in parasitemia after 72 hrs by spectrofluorometry in presence of PG F 8.7 pEC50 2 nM EC50 J. Med. Chem. (2012) 55: 4205-4219 [PMID:22435599]
ChEMBL Antimalarial activity against Plasmodium falciparum 3D7 infected in human A positive erythrocytes by [3H]hypoxanthine uptake assay in presence of serum in medium F 8.82 pEC50 1.5 nM EC50 J. Med. Chem. (2011) 54: 3935-3949 [PMID:21517059]
ChEMBL Antimalarial activity against pyrimethamine/chloroquine-resistant Plasmodium falciparum W2 infected in human type A-positive erythrocytes after 48 hrs by [3H]-hypoxanthine incorporation assay F 8.85 pEC50 1.4 nM EC50 J Med Chem (2018) 61: 1450-1473 [PMID:29215279]
ChEMBL Antimalarial activity against multi-drug-resistant Plasmodium falciparum W2 infected in human type A+ erythrocytes assessed as growth inhibition after 72 hrs by SYBR Green I assay F 8.85 pEC50 1.4 nM EC50 J. Med. Chem. (2014) 57: 8860-8879 [PMID:25148516]
ChEMBL Antimalarial activity against chloroquine and pyrimethamine-resistant Plasmodium falciparum W2 infected in human A+ erythrocytes after 72 hrs by SYBR Green I assay F 9.27 pEC50 0.54 nM EC50 J. Med. Chem. (2010) 53: 7076-7094 [PMID:20828199]
ChEMBL Antimalarial activity against chloroquine and pyrimethamine-resistant Plasmodium falciparum W2 infected in human A positive erythrocytes after 72 hrs by SYBR Green I assay F 9.28 pEC50 0.53 nM EC50 J. Med. Chem. (2011) 54: 4399-4426 [PMID:21630666]
ChEMBL Antimalarial activity against chloroquine-, pyrimethamine-resistant ring stage Plasmodium falciparum W2 infected in human A positive erythrocytes after 72 hrs by SYBR green 1-based fluorescence assay F 9.28 pEC50 0.53 nM EC50 J. Med. Chem. (2011) 54: 8321-8327 [PMID:22111907]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 infected in human erythrocyte assessed as growth inhibition by SYBR Green-1 assay F 9.72 pEC50 0.19 nM EC50 Eur. J. Med. Chem. (2015) 102: 320-333 [PMID:26295174]
Plasmodium falciparum 3D7 (target type: ORGANISM) [ChEMBL: CHEMBL2366922]
ChEMBL Antimalarial activity against schizont stage of chloroquine-susceptible Plasmodium falciparum 3D7 infected in erythrocytes assessed as inhibition of [3H]hypoxanthine incorporation after 48 hrs by scintillation counting analysis F 8.64 pIC50 2.3 nM IC50 MedChemComm (2011) 2: 430-435
ChEMBL Antimalarial activity against schizont stage of chloroquine-susceptible Plasmodium falciparum 3D7 infected in erythrocytes assessed as inhibition of [3H]hypoxanthine incorporation after 96 hrs by scintillation counting analysis F 8.72 pIC50 1.9 nM IC50 MedChemComm (2011) 2: 430-435
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 cultured in human erythrocytes incubated for 48 hrs by [3H]-hypoxanthine incorporation assay F 9 pIC50 1 nM IC50 J. Med. Chem. (2015) 58: 5344-5354 [PMID:26067904]
ChEMBL Antimalarial activity against Plasmodium falciparum 3D7 infected in erythrocytes incubated for 48 hrs by [3H]hypoxanthine incorporation assay F 9 pIC50 1 nM IC50 J. Med. Chem. (2015) 58: 6448-6455 [PMID:26222445]
ChEMBL Antimalarial activity against Plasmodium falciparum 3D7 infected in erythrocytes incubated for 72 hrs by [3H]hypoxanthine incorporation assay F 9.52 pIC50 0.3 nM IC50 J. Med. Chem. (2015) 58: 6448-6455 [PMID:26222445]
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in human erythrocyte assessed as growth inhibition by SYBR Green-1 assay F 9.46 pEC50 0.35 nM EC50 Eur. J. Med. Chem. (2015) 102: 320-333 [PMID:26295174]
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 10 pEC50 0.1 nM EC50 J. Med. Chem. (2014) 57: 3818-3834 [PMID:24720377]
Plasmodium falciparum (isolate K1 / Thailand) in Plasmodium falciparum K1 (target type: ORGANISM) [ChEMBL: CHEMBL612856]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 after 48 hrs using Hema 3 staining by microscopic analysis F 7.75 pIC50 17.7 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 4512-4515 [PMID:21723121]
ChEMBL Antiplasmodial activity against multidrug-resistant Plasmodium falciparum K1 by SYBR Green-based method F 8.64 pIC50 2.3 nM IC50 Bioorg. Med. Chem. Lett. (2015) 25: 952-955 [PMID:25599834]
ChEMBL Antiplasmodial activity against Plasmodium falciparum K1 by SYBR-green based assay F 8.64 pIC50 2.3 nM IC50 J. Med. Chem. (2014) 57: 6642-6652 [PMID:25007124]
ChEMBL Antimalarial activity against multidrug-resistant Plasmodium falciparum K1 by SYBR green-based assay F 8.64 pIC50 2.3 nM IC50 Bioorg. Med. Chem. Lett. (2015) 25: 1100-1103 [PMID:25650255]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 after 72 hrs by SYBR I method F 8.65 pIC50 2.26 nM IC50 J. Med. Chem. (2014) 57: 5702-5713 [PMID:24914738]
ChEMBL Antiplasmodial activity against Plasmodium falciparum K1 infected in human erythrocytes after 72 hrs by SYBR Green I fluorescence assay F 8.82 pIC50 1.5 nM IC50 Bioorg. Med. Chem. (2013) 21: 7155-7164 [PMID:24080103]
ChEMBL Antiplasmodial activity against multi-drug resistant Plasmodium falciparum K1 infected in human erythrocytes assessed as parasite growth inhibition after 72 hrs by SYBR Green I dye-based fluorescence assay F 8.89 pIC50 1.3