atovaquone [Ligand Id: 9695] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1450 (566C, 566C80, 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 |
|---|---|---|---|---|---|---|---|---|
| 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 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 | 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 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 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 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 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 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 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 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 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 | 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 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 | 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 | 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 | 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 | 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 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 | 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 | 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 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 | 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 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 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 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 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 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 | |