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]
  • 0
1 CHEMBL1450_lig_chart_1 Dihydroorotate dehydrogenase Plasmodium falciparumHumanRatSaccharomyces cerevisiae S288c
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  • Dihydroorotate dehydrogenase (quinone), mitochondrial in Schistosoma mansoni [ChEMBL: CHEMBL4523950] [UniProtKB: G4VFD7]
  • This target only has 0 pki data point
  • 0
2 CHEMBL1450_lig_chart_2 Dihydroorotate dehydrogenase (quinone), mitochondrial Schistosoma mansoni
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  • Plasmodium berghei [ChEMBL: CHEMBL612653]
  • This target only has 0 pki data point
  • 0
3 CHEMBL1450_lig_chart_3 Plasmodium berghei Plasmodium berghei
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  • Plasmodium falciparum [ChEMBL: CHEMBL364]
  • This target only has 0 pki data point
  • 0
4 CHEMBL1450_lig_chart_4 Plasmodium falciparum Plasmodium falciparum
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  • Plasmodium falciparum 3D7 [ChEMBL: CHEMBL2366922]
  • This target only has 0 pki data point
  • 0
5 CHEMBL1450_lig_chart_5 Plasmodium falciparum 3D7 Plasmodium falciparum 3D7
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  • Plasmodium falciparum D6 [ChEMBL: CHEMBL2367107]
  • This target only has 0 pki data point
  • 0
6 CHEMBL1450_lig_chart_6 Plasmodium falciparum D6 Plasmodium falciparum D6
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  • Plasmodium falciparum (isolate K1 / Thailand) in Plasmodium falciparum K1 [ChEMBL: CHEMBL612856]
  • This target only has 0 pki data point
  • 0
7 CHEMBL1450_lig_chart_7 Plasmodium falciparum (isolate K1 / Thailand) Plasmodium falciparum K1
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  • Plasmodium falciparum NF54 [ChEMBL: CHEMBL2367131]
  • This target only has 0 pki data point
  • 0
8 CHEMBL1450_lig_chart_8 Plasmodium falciparum NF54 Plasmodium falciparum NF54
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  • Plasmodium yoelii [ChEMBL: CHEMBL612889]
  • This target only has 0 pki data point
  • 0
9 CHEMBL1450_lig_chart_9 Plasmodium yoelii Plasmodium yoelii
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  • Plasmodium yoelii yoelii [ChEMBL: CHEMBL612328]
  • This target only has 0 pki data point
  • 0
10 CHEMBL1450_lig_chart_10 Plasmodium yoelii yoelii Plasmodium yoelii yoelii
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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]
  • This target only has 0 pki data point
  • 0
11 CHEMBL1450_lig_chart_11 Plasmodium falciparum cytochrome b Plasmodium falciparum TM90C2APlasmodium falciparum K1Plasmodium falciparum NF54Plasmodium falciparum 7G8Plasmodium falciparum D6
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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]
ChEMBL Inhibition of human DHODH B 5.59 pIC50 2600 nM IC50 Eur J Med Chem (2019) 183: 111681-111681 [PMID:31557612]
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]
Dihydroorotate dehydrogenase (quinone), mitochondrial in Schistosoma mansoni (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523950] [UniProtKB: G4VFD7]
ChEMBL Inhibition of Schistosoma mansoni DHODH using DHO as substrate measured at 4 secs interval for 60 secs by DCIP reduction based indirect assay B 6.36 pIC50 432 nM IC50 Eur J Med Chem (2019) 167: 357-366 [PMID:30776695]
ChEMBL Inhibition of Schistosoma mansoni DHODH B 6.37 pIC50 430 nM IC50 Eur J Med Chem (2019) 183: 111681-111681 [PMID:31557612]
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 Antimalarial activity against luciferase-expressing Plasmodium berghei ANKA 676m1cl1 sporozoites infected in human HepG2A16 cells measured after 45 hrs by luciferase-luciferin based reporter assay F 8.19 pIC50 6.5 nM IC50 J Med Chem (2019) 62: 3475-3502 [PMID:30852885]
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 luciferase expressing Plasmodium berghei sporozoites infected in human HuH7 cells assessed as reduction in parasite load preincubated for 1 hr followed by parasite infection and measured after 46 hrs by bioluminescence assay F 9.15 pIC50 0.7 nM IC50 J Med Chem (2020) 63: 1750-1762 [PMID:32011136]
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 Antiplasmodial activity against exoerythrocytic-stage of Plasmodium berghei ANKA infected in human HepG2 cells expressing CD81 pretreated with cells for 18 hrs followed by parasite infection and measured after 48 hrs by brightglo-luminescence assay F 8.55 pEC50 2.8 nM EC50 ACS Med Chem Lett (2019) 10: 137-141 [PMID:30655961]
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 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 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 Antimalarial activity against Plasmodium falciparum TM90C2B incubated for 48 hrs by [3H]-hypoxanthine incorporation assay F 4.94 pIC50 11500 nM IC50 ACS Med Chem Lett (2020) 11: 49-55 [PMID:31938463]
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 atovaquone-resistant Plasmodium falciparum TM90C2B F 5 pIC50 >10000 nM IC50 J Med Chem (2016) 59: 5587-5603 [PMID:26791529]
ChEMBL Antimalarial activity against atovaquone-resistant Plasmodium falciparum TM90C2B F 5 pIC50 >10000 nM IC50 J Med Chem (2016) 59: 5587-5603 [PMID:26791529]
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 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 Antimalarial activity against chloroquine-resistant Plasmodium falciparum TM90C2B harboring Y268S mutant measured after 48 hrs by SYBR green1 dye based fluorescence assay F 5 pIC50 9908 nM IC50 ACS Med Chem Lett (2018) 9: 1205-1210 [PMID:30613327]
ChEMBL Antimalarial activity against atovaquone-resistant Plasmodium falciparum Tm90-C2B infected in human erythrocytes by SYBR green 1-based fluorescence assay F 5.08 pIC50 8256 nM IC50 J Med Chem (2019) 62: 3475-3502 [PMID:30852885]
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 Antimalarial activity against trophozoite stage of Plasmodium falciparum 3D7 infected-erythrocytes assessed as reduction in Leu efflux after 4 hrs by UPLC method F 6 pIC50 >1000 nM IC50 Bioorg Med Chem Lett (2016) 26: 4846-4850 [PMID:27544402]
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 drug-resistant Plasmodium falciparum Dd2 harboring M133I mutant infected in human erythrocytes after 72 hrs by SYBR green 1-based fluorescence assay F 8.16 pIC50 6.9 nM IC50 J Med Chem (2019) 62: 3475-3502 [PMID:30852885]
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 drug-resistant Plasmodium falciparum Dd2 harboring V259L mutant infected in human erythrocytes after 72 hrs by SYBR green 1-based fluorescence assay F 8.39 pIC50 4.1 nM IC50 J Med Chem (2019) 62: 3475-3502 [PMID:30852885]
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 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 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 asexual stage of Plasmodium falciparum 3D7 infected in erythrocytes assessed as reduction in parasite growth incubated for 48 hrs under hypoxic condition by Hoechst 33342 staining based flow cytometry F 8.55 pIC50 2.8 nM IC50 ACS Med Chem Lett (2020) 11: 49-55 [PMID:31938463]
ChEMBL Antimalarial activity against asexual stage of Plasmodium falciparum Dd2 infected in erythrocytes assessed as reduction in parasite growth incubated for 48 hrs under hypoxic condition by Hoechst 33342 staining based flow cytometry F 8.6 pIC50 2.5 nM IC50 ACS Med Chem Lett (2020) 11: 49-55 [PMID:31938463]
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 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 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 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 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 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 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 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 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 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 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 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 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 8.72 pIC50 1.9 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 8.85 pIC50 1.4 nM IC50 J Med Chem (2019) 62: 3475-3502 [PMID:30852885]
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 Antiplasmodial activity against chloroquine/proguanil/pyrimethamine-resistant synchronized stage of Plasmodium falciparum K1 after 72 hrs by SYBR green1 staining based spectrophotometric method F 9 pIC50 1 nM IC50 ACS Med Chem Lett (2019) 10: 34-39 [PMID:30655943]
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 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 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 chloroquine/mefloquine-sensitive Plasmodium falciparum 3D7 infected-erythrocytes assessed as parasite growth inhibition after 48 to 54 hrs by SYBR green 1-based replication method F 9.22 pIC50 0.6 nM IC50 Bioorg Med Chem Lett (2016) 26: 4846-4850 [PMID:27544402]
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 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 Plasmodium falciparum K1 incubated for 48 hrs by [3H]-hypoxanthine incorporation assay F 9.3 pIC50 0.5 nM IC50 ACS Med Chem Lett (2020) 11: 49-55 [PMID:31938463]
ChEMBL Antimalarial activity against Plasmodium falciparum 3D7 infected in human erythrocytes after 72 hrs by SYBR green 1-based fluorescence assay F 9.3 pIC50 0.5 nM IC50 J Med Chem (2019) 62: 3475-3502 [PMID:30852885]
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 Plasmodium falciparum 3D7 F 9.4 pIC50 0.4 nM IC50 J Med Chem (2016) 59: 5587-5603 [PMID:26791529]
ChEMBL Antimalarial activity against Plasmodium falciparum NF54 incubated for 48 hrs by [3H]-hypoxanthine incorporation assay F 9.4 pIC50 0.4 nM IC50 ACS Med Chem Lett (2020) 11: 49-55 [PMID:31938463]
ChEMBL Antimalarial activity against Plasmodium falciparum 3D7 F 9.4 pIC50 0.4 nM IC50 J Med Chem (2016) 59: 5587-5603 [PMID:26791529]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 measured after 48 hrs by SYBR green1 dye based fluorescence assay F 9.52