atovaquone [Ligand Id: 9695] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1450 (566C, 566C80, Atovacuona, Atovaquone, Mepron, NSC-759582, Wellvone) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| ABCG2/ATP-binding cassette sub-family G member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0] | ||||||||
| ChEMBL | Inhibition of ABCG2 (unknown origin) expressed in human HEK293 cells membrane vesicles assessed inhibition of BCRP- mediated transport of 3[H]-E1S for 1 to 5 mins using [3H]-estrone sulfate as substrate by rapid filtration technique | B | 6.64 | pIC50 | 230 | nM | IC50 | Eur J Med Chem (2022) 237: 114346-114346 [PMID:35483322] |
| 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 recombinant human DHODH expressed in baculovirus infected insect cells using dihydroorotate as substrate and decylubiquinone as co-substrate by 2,6-dichlorophenol-indophenol-coupled spectrophotometric analysis | B | 4.84 | pIC50 | 14500 | nM | IC50 | J Med Chem (2020) 63: 7633-7652 [PMID:32496056] |
| 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 Plasmodium berghei | F | 7.71 | pIC50 | 19.7 | nM | IC50 | Eur J Med Chem (2021) 210: 113084-113084 [PMID:33333397] |
| 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 gene assay | F | 8.19 | pIC50 | 6.5 | nM | IC50 | J Med Chem (2020) 63: 6179-6202 [PMID:32390431] |
| 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 | Antimalarial activity against luciferase expressing liver stage Plasmodium berghei ANKA infected in human Huh-7 cells assessed as reduction in parasite load measured after 44 hrs post infection by Bright-glo reagent based luciferase reporter assay | F | 8 | pEC50 | 10 | nM | EC50 | Bioorg Med Chem Lett (2023) 92: 129410-129410 [PMID:37478957] |
| 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 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 atovaquone-resistant Plasmodium falciparum TM90C2B | F | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2016) 59: 5587-5603 [PMID:26791529] |
| 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 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 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 multidrug resistant Plasmodium falciparum Tm90-C2B infected in human erythrocytes measured after after 72 hrs by SYBR green dye based fluorescence assay | F | 5.08 | pIC50 | 8256 | nM | IC50 | J Med Chem (2020) 63: 6179-6202 [PMID:32390431] |
| 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 asexual blood stage of multidrug-resistant Plasmodium falciparum TM90C2B infected in human erythrocytes assessed as reduction in parasite growth incubated for 72 hrs by SYBR green 1 staining based assay | F | 5.08 | pIC50 | 8256 | nM | IC50 | J Med Chem (2021) 64: 8739-8754 [PMID:34111350] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum Tm90-C2B infected in human Erythrocyte measured after 72 hrs by SYBR green fluorescence dye based microplate reader analysis | F | 5.29 | pIC50 | 5090 | nM | IC50 | Eur J Med Chem (2018) 146: 1-14 [PMID:29360043] |
| 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 | 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 | 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 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 | 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 | 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 | 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 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 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 | 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 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 | Antimalarial activity against artemisinin-sensitive Plasmodium falciparum F32-TEM by SYBR green dye based fluorescence assay | F | 8.68 | pIC50 | 2.1 | nM | IC50 | Bioorg Med Chem Lett (2021) 39: 127884-127884 [PMID:33636304] |
| 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 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 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 | 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 Plasmodium falciparum NF54 by SYBR Green-based method | F | 8.85 | pIC50 | 1.4 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 952-955 [PMID:25599834] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum NF54 by SYBR-green based assay | F | 8.85 | pIC50 | 1.4 | nM | IC50 | J Med Chem (2014) 57: 6642-6652 [PMID:25007124] |
| ChEMBL | Antimalarial activity against drug-sensitive Plasmodium falciparum NF54 by SYBR green-based assay | F | 8.85 | pIC50 | 1.4 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 1100-1103 [PMID:25650255] |
| 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 | Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum NF54 after 72 hrs by SYBR I method | F | 8.87 | pIC50 | 1.36 | nM | IC50 | J Med Chem (2014) 57: 5702-5713 [PMID:24914738] |
| 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 | nM | IC50 | Eur J Med Chem (2015) 95: 16-28 [PMID:25791675] |
| 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 | Antimalarial activity against Plasmodium falciparum TM91C235 | F | 8.92 | pIC50 | 1.2 | nM | IC50 | Eur J Med Chem (2021) 210: 113084-113084 [PMID:33333397] |
| 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 | 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 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 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 Plasmodium falciparum W2 | F | 9 | pIC50 | 1 | nM | IC50 | Eur J Med Chem (2021) 210: 113084-113084 [PMID:33333397] |
| 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 | 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 | Antiplasmodial activity against chloroquine/pyrimethamine/proguanil-resistant Plasmodium falciparum K1 infected in human erythrocytes after 72 hrs by SYBR Green 1 dye based fluorescence spectrophotometric method | F | 9 | pIC50 | 1 | nM | IC50 | Eur J Med Chem (2017) 125: 68-86 [PMID:27654395] |
| 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 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 | Antiplasmodial activity against asexual Plasmodium falciparum 3D7 infected in human erythrocytes assessed as reduction in parasitemia measured after 72 hrs by LDH assay | F | 9.02 | pIC50 | 0.96 | nM | IC50 | J Nat Prod (2021) 84: 126-135 [PMID:33369420] |
| 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 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 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 | Antimalarial activity against Plasmodium falciparum K1 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 | 9.15 | pIC50 | 0.7 | nM | IC50 | J Med Chem (2017) 60: 5889-5908 [PMID:28635296] |
| 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 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 | 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 | 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 | Antiplasmodial activity against Plasmodium falciparum Dd2 infected in human Erythrocyte measured after 72 hrs by SYBR green fluorescence dye based microplate reader analysis | F | 9.3 | pIC50 | 0.5 | nM | IC50 | Eur J Med Chem (2018) 146: 1-14 [PMID:29360043] |
| 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 D6 | F | 9.47 | pIC50 | 0.34 | nM | IC50 | Eur J Med Chem (2021) 210: 113084-113084 [PMID:33333397] |
| 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 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 D6 infected in human Erythrocyte measured after 72 hrs by SYBR green fluorescence dye based microplate reader analysis | F | 9.52 | pIC50 | 0.3 | nM | IC50 | Eur J Med Chem (2018) 146: 1-14 [PMID:29360043] |
| ChEMBL | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 measured after 48 hrs by SYBR green1 dye based fluorescence assay | F | 9.52 | pIC50 | 0.3 | nM | IC50 | ACS Med Chem Lett (2018) 9: 1205-1210 [PMID:30613327] |
| 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 3D7 asexual forms incubated for 72 hrs by luminescence method | F | 9.57 | pIC50 | 0.27 | nM | IC50 | Eur J Med Chem (2020) 188: 111983-111983 [PMID:31911292] |
| 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 Plasmodium falciparum clinical isolates measured after 72 hrs by SYBR green dye based fluorescence assay | F | 9.57 | pIC50 | 0.27 | nM | IC50 | J Med Chem (2020) 63: 6179-6202 [PMID:32390431] |
| ChEMBL | Antimalarial activity against multidrug resistant Plasmodium falciparum 7G8 infected in human erythrocytes measured after after 72 hrs by SYBR green dye based fluorescence assay | F | 9.7 | pIC50 | 0.2 | nM | IC50 | J Med Chem (2020) 63: 6179-6202 [PMID:32390431] |
| ChEMBL | Antimalarial activity against multidrug-resistant Plasmodium falciparum 7G8 infected in human erythrocytes by SYBR green 1-based fluorescence assay | F | 9.7 | pIC50 | 0.2 | nM | IC50 | J Med Chem (2019) 62: 3475-3502 [PMID:30852885] |
| ChEMBL | Antiplasmodial activity against asexual blood stage of multidrug-resistant Plasmodium falciparum 7G8 infected in human erythrocytes assessed as reduction in parasite growth incubated for 72 hrs by SYBR green 1 staining based assay | F | 9.7 | pIC50 | 0.2 | nM | IC50 | J Med Chem (2021) 64: 8739-8754 [PMID:34111350] |
| ChEMBL | Antimalarial activity against multidrug-resistant Plasmodium falciparum Dd2 infected in human erythrocytes by SYBR green 1-based fluorescence assay | F | 10 | pIC50 | 0.1 | nM | IC50 | J Med Chem (2019) 62: 3475-3502 [PMID:30852885] |
| ChEMBL | Antiplasmodial activity against asexual blood stage of multidrug-resistant Plasmodium falciparum Dd2 infected in human erythrocytes assessed as reduction in parasite growth incubated for 72 hrs by SYBR green 1 staining based assay | F | 10 | pIC50 | 0.1 | nM | IC50 | J Med Chem (2021) 64: 8739-8754 [PMID:34111350] |
| ChEMBL | Antiplasmodial activity against asexual stage of chloroquine-sensitive Plasmodium falciparum D6 infected in human erythrocytes assessed as reduction in parasite growth incubated for 72 hrs by SYBR green 1 staining based assay | F | 10 | pIC50 | 0.1 | nM | IC50 | J Med Chem (2021) 64: 8739-8754 [PMID:34111350] |
| ChEMBL | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 infected in human erythrocytes by SYBR green 1-based fluorescence assay | F | 10 | pIC50 | 0.1 | nM | IC50 | J Med Chem (2019) 62: 3475-3502 [PMID:30852885] |
| ChEMBL | Antimalarial activity against multidrug resistant Plasmodium falciparum D6 infected in human erythrocytes measured after after 72 hrs by SYBR green dye based fluorescence assay | F | 10 | pIC50 | 0.1 | nM | IC50 | J Med Chem (2020) 63: 6179-6202 [PMID:32390431] |
| ChEMBL | Antimalarial activity against multidrug resistant Plasmodium falciparum Dd2 infected in human erythrocytes measured after after 72 hrs by SYBR green dye based fluorescence assay | F | 10 | pIC50 | 0.1 | nM | IC50 | J Med Chem (2020) 63: 6179-6202 [PMID:32390431] |
| 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 Plasmodium falciparum TM90-C2B | F | 4.74 | pEC50 | 18400 | nM | EC50 | J Med Chem (2016) 59: 6943-6960 [PMID:27291102] |
| ChEMBL | Antimalarial activity against chloroquine, pyrimethamine, mefloquine and atovaquone- resistant Plasmodium falciparum TM90-C2B infected in human erythrocytes assessed as reduction in parasite growth incubated for 48 hrs followed by addition of [3H]-hypoxanthine and measured after 24 hrs by Topcount liquid scintillation counting method | F | 4.74 | pEC50 | 18197.01 | nM | EC50 | J Med Chem (2021) 64: 6581-6595 [PMID:33979164] |
| 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 asexual stage mefloquine-resistant Plasmodium falciparum W2 mef assessed as reduction in parasitemia incubated for 72 hrs by LDH assay | F | 7.19 | pEC50 | 64 | nM | EC50 | J Med Chem (2023) 66: 3540-3565 [PMID:36812492] |
| ChEMBL | Antimalarial activity against asexual stage multidrug-resistant Plasmodium falciparum Dd2 assessed as reduction in parasitemia incubated for 72 hrs by LDH assay | F | 7.46 | pEC50 | 35 | nM | EC50 | J Med Chem (2023) 66: 3540-3565 [PMID:36812492] |
| ChEMBL | Antimalarial activity against asexual stage multidrug-resistant Plasmodium falciparum 3D7 assessed as reduction in parasitemia incubated for 72 hrs by LDH assay | F | 7.64 | pEC50 | 23 | nM | EC50 | J Med Chem (2023) 66: 3540-3565 [PMID:36812492] |
| 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/pyrimethamine-resistant Plasmodium falciparum K1 infected in O-positive erythrocytes assessed as reduction in parasitemia after 72 hrs by spectrofluorometry | F | 7.82 | pEC50 | 15 | nM | EC50 | J Med Chem (2012) 55: 4205-4219 [PMID:22435599] |
| ChEMBL | Antimalarial activity against asexual stage multidrug-resistant Plasmodium falciparum CAM3 RS39T assessed as reduction in parasitemia incubated for 72 hrs by LDH assay | F | 7.92 | pEC50 | 12 | nM | EC50 | J Med Chem (2023) 66: 3540-3565 [PMID:36812492] |
| ChEMBL | Antimalarial activity against asexual stage mefloquine-resistant Plasmodium falciparum K1 Mef assessed as reduction in parasitemia incubated for 72 hrs by LDH assay | F | 7.96 | pEC50 | 11 | nM | EC50 | J Med Chem (2023) 66: 3540-3565 [PMID:36812492] |
| ChEMBL | Antimalarial activity against asexual stage Rev-resistant Plasmodium falciparum CAM3 assessed as reduction in parasitemia incubated for 72 hrs by LDH assay | F | 8.03 | pEC50 | 9.4 | nM | EC50 | J Med Chem (2023) 66: 3540-3565 [PMID:36812492] |
| ChEMBL | Antimalarial activity against asexual stage multidrug-resistant Plasmodium falciparum Dd2 ATV harboring cytochrome B M13313 mutant assessed as reduction in parasitemia incubated for 72 hrs by LDH assay | F | 8.3 | pEC50 | 5 | nM | EC50 | J Med Chem (2023) 66: 3540-3565 [PMID:36812492] |
| ChEMBL | Antimalarial activity against asexual stage multidrug-resistant Plasmodium falciparum PNG 1776 assessed as reduction in parasitemia incubated for 72 hrs by LDH assay | F | 8.31 | pEC50 | 4.9 | nM | EC50 | J Med Chem (2023) 66: 3540-3565 [PMID:36812492] |
| ChEMBL | Antimalarial activity against asexual stage multidrug-resistant Plasmodium falciparum K1 assessed as reduction in parasitemia incubated for 72 hrs by LDH assay | F | 8.44 | pEC50 | 3.6 | nM | EC50 | J Med Chem (2023) 66: 3540-3565 [PMID:36812492] |
| 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 chloroquine and pyrimethamine resistant Plasmodium falciparum W2 infected in human erythrocytes assessed as reduction in parasite growth incubated for 48 hrs followed by addition of [3H]-hypoxanthine and measured after 24 hrs by Topcount liquid scintillation counting method | F | 8.85 | pEC50 | 1.41 | nM | EC50 | J Med Chem (2021) 64: 6581-6595 [PMID:33979164] |
| 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 Plasmodium falciparum W2 | F | 8.86 | pEC50 | 1.39 | nM | EC50 | J Med Chem (2016) 59: 6943-6960 [PMID:27291102] |
| ChEMBL | Antiplasmodial activity against asexual blood stage Plasmodium falciparum 3D7 infected in human RBC assessed as parasite growth inhibition incubated for 72 hrs by SYBR Green dye based fluorescence assay | F | 8.89 | pEC50 | 1.3 | nM | EC50 | J Med Chem (2021) 64: 2739-2761 [PMID:33620219] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 3D7 infected in human RBC assessed as parasite growth inhibition incubated for 48 hrs by 3H-hypoxanthine incorporation assay | F | 9 | pEC50 | 1 | nM | EC50 | J Med Chem (2021) 64: 2739-2761 [PMID:33620219] |
| ChEMBL | Antiplasmodial activity against multidrug-resistant Plasmodium falciparum K1 infected in human erythrocytes assessed as reduction in parasite growth incubated for 72 hrs by SYBR green I fluorescence based assay | F | 9 | pEC50 | 1 | nM | EC50 | Eur J Med Chem (2021) 224: 113722-113722 [PMID:34364164] |
| 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-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] |
| 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] |
| 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 yoelii (target type: ORGANISM) [ChEMBL: CHEMBL612889] | ||||||||
| ChEMBL | Antimalarial activity against sporozoite stage of Plasmodium yoelii assessed as invasion of human HepG2 cells expressing CD81 incubated for 2 hrs prior to inoculation measured after 1 hr by immunofluorescence assay in presence of penicillin/streptomycin | F | 6 | pIC50 | <1000 | nM | IC50 | J Med Chem (2013) 56: 7761-7771 [PMID:23927658] |
| ChEMBL | Antiplasmodial activity against liver stage of Plasmodium yoelii 17X NL sporozoites infected in human HepG2 cells expressing CD81 after 48 hrs by DAPI staining-based immunofluorescence analysis | F | 8.05 | pIC50 | 9 | nM | IC50 | Eur J Med Chem (2015) 95: 16-28 [PMID:25791675] |
| Plasmodium yoelii yoelii (target type: ORGANISM) [ChEMBL: CHEMBL612328] | ||||||||
| ChEMBL | Antimicrobial activity against Plasmodium yoelii 265 liver infected in mammalian hepatocytes after 48 hrs | F | 7.24 | pIC50 | 57 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 1215-1220 [PMID:18212104] |
| Plasmodium falciparum cytochrome b in Plasmodium falciparum TM90C2A [GtoPdb: 3087] | ||||||||
| GtoPdb | Parasite growth inhibition assay | - | 9.3 | pIC50 | 0.5 | nM | IC50 | PLoS Med (2012) 9: e1001169 [PMID:22363211] |
| Plasmodium falciparum cytochrome b in Plasmodium falciparum K1 [GtoPdb: 3087] | ||||||||
| GtoPdb | Parasite growth inhibition assay | - | 8.96 | pIC50 | 1.1 | nM | IC50 | PLoS Med (2012) 9: e1001169 [PMID:22363211] |
| Plasmodium falciparum cytochrome b in Plasmodium falciparum NF54 [GtoPdb: 3087] | ||||||||
| GtoPdb | Parasite growth inhibition assay | - | 9.22 | pIC50 | 0.6 | nM | IC50 | PLoS Med (2012) 9: e1001169 [PMID:22363211] |
| Plasmodium falciparum cytochrome b in Plasmodium falciparum 7G8 [GtoPdb: 3087] | ||||||||
| GtoPdb | Parasite growth inhibition assay | - | 9.52 | pIC50 | 0.3 | nM | IC50 | PLoS Med (2012) 9: e1001169 [PMID:22363211] |
| Plasmodium falciparum cytochrome b in Plasmodium falciparum D6 [GtoPdb: 3087] | ||||||||
| GtoPdb | Parasite growth inhibition assay | - | 10 | pIC50 | 0.1 | nM | IC50 | PLoS Med (2012) 9: e1001169 [PMID:22363211] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
