artesunate [Ligand Id: 9956] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL361497 (.alpha.-artesunic acid, Artesunate, Artesunate amivas, Artesunatum, Artesunic acid, Dihydroqinghaosu hemisuccinate, LJPC-0118, NSC-712571, Plasmotrin, Qinghaozhi, Saphnate, Zysunate)
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum NF54 by LDH release assay F 5.28 pIC50 <5202 nM IC50 Eur J Med Chem (2018) 148: 39-53 [PMID:29454189]
ChEMBL Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum NF54 by lactate dehydrogenase assay F 5.28 pIC50 <5200 nM IC50 J Nat Prod (2018) 81: 41-48 [PMID:29309141]
ChEMBL Antimicrobial activity against Plasmodium falciparum F 5.52 pIC50 3000 nM IC50 Bioorg Med Chem (2010) 18: 2225-2231 [PMID:20185316]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 infected in erythrocytes after 48 hrs by [3H]hypoxanthine incorporation assay F 5.62 pIC50 2400 nM IC50 J Med Chem (2009) 52: 7954-7957 [PMID:19908867]
ChEMBL Gametocytocidal antimalarial activity against chloroquine-sensitive Plasmodium falciparum NF54 late gametocyte stage after 72 hrs by alamar blue assay F 5.64 pIC50 2300 nM IC50 J Nat Prod (2013) 76: 388-393 [PMID:23286240]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 infected in erythrocytes after 96 hrs by [3H]hypoxanthine incorporation assay F 5.68 pIC50 2100 nM IC50 J Med Chem (2009) 52: 7954-7957 [PMID:19908867]
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in erythrocytes after 96 hrs by [3H]hypoxanthine incorporation assay F 5.7 pIC50 2000 nM IC50 J Med Chem (2009) 52: 7954-7957 [PMID:19908867]
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in erythrocytes after 48 hrs by [3H]hypoxanthine incorporation assay F 5.77 pIC50 1700 nM IC50 J Med Chem (2009) 52: 7954-7957 [PMID:19908867]
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 in presence of ascorbic acid F 6.15 pIC50 700 nM IC50 Eur J Med Chem (2015) 95: 16-28 [PMID:25791675]
ChEMBL Antimalarial activity against Plasmodium falciparum NF54 late gametocytes transfected with luciferase gene incubated for 48 hrs by luciferase reporter gene assay F 6.59 pIC50 259 nM IC50 ACS Med Chem Lett (2020) 11: 49-55 [PMID:31938463]
ChEMBL Antiplasmodial activity against Plasmodium falciparum NF54 after 48 hrs by lactate dehydrogenase assay F 6.71 pIC50 194 nM IC50 J Med Chem (2018) 61: 9371-9385 [PMID:30256636]
ChEMBL Antimalarial activity against Plasmodium falciparum NF54 infected in human erythrocytes preincubated for 48 hrs followed by [3H]-hypoxanthine addition and measured after 24 hrs by liquid scintillation counting F 6.71 pIC50 194 nM IC50 J Med Chem (2018) 61: 9371-9385 [PMID:30256636]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 gametocytes (stage 4 & 5) F 6.97 pIC50 108 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 7.14 pIC50 72 nM IC50 Antimicrob Agents Chemother (2007) 51: 1463-1472 [PMID:17242150]
ChEMBL Antimalarial activity against Plasmodium falciparum NF54 early gametocytes transfected with luciferase gene incubated for 48 hrs by luciferase reporter gene assay F 7.2 pIC50 63 nM IC50 ACS Med Chem Lett (2020) 11: 49-55 [PMID:31938463]
ChEMBL Antiplasmodial activity chloroquine-resistant Plasmodium falciparum Dd2 by lactate dehydrogenase assay F 7.34 pIC50 46 nM IC50 Bioorg Med Chem Lett (2014) 24: 1214-1217 [PMID:24468411]
ChEMBL Gametocytocidal activity against transgenic Plasmodium falciparum NF54-pfs16-GFP late stage gametocytes after 72 hrs by mitotracker red CM-H2XRos dye based confocal imaging assay F 7.36 pIC50 44 nM IC50 J Med Chem (2014) 57: 7971-7976 [PMID:25195945]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 F 7.51 pIC50 31.2 nM IC50 Eur J Med Chem (2013) 66: 314-323 [PMID:23811093]
ChEMBL Antiplasmodial activity against chloroquine-resistant asexual erythrocytic stage of Plasmodium falciparum Dd2 assessed as parasite growth inhibition by lactate dehydrogenase assay F 7.51 pIC50 31.2 nM IC50 J Med Chem (2014) 57: 435-448 [PMID:24354322]
ChEMBL Antimalarial activity against Plasmodium falciparum D10 clone M2 assessed as inhibition of [3H]hypoxanthine incorporation F 7.56 pIC50 27.7 nM IC50 Antimicrob Agents Chemother (2010) 54: 3842-3852 [PMID:20566762]
ChEMBL Antimalarial activity against Plasmodium falciparum D10 clone 1 assessed as inhibition of [3H]hypoxanthine incorporation F 7.58 pIC50 26.6 nM IC50 Antimicrob Agents Chemother (2010) 54: 3842-3852 [PMID:20566762]
ChEMBL Antimalarial activity against Plasmodium falciparum D10 clone M1 assessed as inhibition of [3H]hypoxanthine incorporation F 7.58 pIC50 26.5 nM IC50 Antimicrob Agents Chemother (2010) 54: 3842-3852 [PMID:20566762]
ChEMBL Antimalarial activity against Plasmodium falciparum D10 harboring pfATP6 263E mutant assessed as inhibition of [3H]hypoxanthine incorporation F 7.58 pIC50 26.2 nM IC50 Antimicrob Agents Chemother (2010) 54: 3842-3852 [PMID:20566762]
ChEMBL Antimalarial activity against Plasmodium falciparum D10 clone M1 harboring pfATP6 L263 mutant assessed as inhibition of [3H]hypoxanthine incorporation F 7.58 pIC50 26.2 nM IC50 Antimicrob Agents Chemother (2010) 54: 3842-3852 [PMID:20566762]
ChEMBL Antimalarial activity against Plasmodium falciparum D10 clone M3 assessed as inhibition of [3H]hypoxanthine incorporation F 7.61 pIC50 24.3 nM IC50 Antimicrob Agents Chemother (2010) 54: 3842-3852 [PMID:20566762]
ChEMBL Antiplasmodial activity against chloroquine-sensitive asexual erythrocytic stage of Plasmodium falciparum NF54 assessed as parasite growth inhibition by parasite lactate dehydrogenase assay F 7.62 pIC50 24.2 nM IC50 Bioorg Med Chem (2015) 23: 4163-4171 [PMID:26174655]
ChEMBL Antimalarial activity against Plasmodium falciparum D10 clone 1 harboring pfATP6 L263 mutant assessed as inhibition of [3H]hypoxanthine incorporation F 7.63 pIC50 23.6 nM IC50 Antimicrob Agents Chemother (2010) 54: 3842-3852 [PMID:20566762]
ChEMBL Antimalarial activity against Plasmodium falciparum D10 harboring pfATP6 L263 mutant assessed as inhibition of [3H]hypoxanthine incorporation F 7.63 pIC50 23.6 nM IC50 Antimicrob Agents Chemother (2010) 54: 3842-3852 [PMID:20566762]
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 7.64 pIC50 22.8 nM IC50 ACS Med Chem Lett (2020) 11: 49-55 [PMID:31938463]
ChEMBL Antimalarial activity against Plasmodium falciparum 7G8 clone M4 assessed as inhibition of [3H]hypoxanthine incorporation F 7.67 pIC50 21.3 nM IC50 Antimicrob Agents Chemother (2010) 54: 3842-3852 [PMID:20566762]
ChEMBL Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum NF54 by LDH assay F 7.7 pIC50 20 nM IC50 Medchemcomm (2013) 4: 724-730
ChEMBL Gametocytocidal activity against synchronous stage 1 to 3 of transgenic Plasmodium falciparum NF54 gametocyte harboring pfs16 promoter assessed as parasite viability after 72 hrs by luciferase reporter gene assay F 7.72 pIC50 19 nM IC50 J Med Chem (2013) 56: 6200-6215 [PMID:23837878]
ChEMBL OSM: Inhibition of Plasmodium falciparum 3D7 growth using a SYBR green I fluorescence based assay. GSK Tres Cantos. F 7.72 pIC50 19 nM IC50 Open Source Malaria Deposition 1. http://malaria.ourexperiment.org
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum NF54 F 7.73 pIC50 18.43 nM IC50 Eur J Med Chem (2021) 213: 113193-113193 [PMID:33508479]
ChEMBL Antimalarial activity against chloroquine-resistant asexual intraerythrocytic stage of Plasmodium falciparum Dd2 assessed as inhibition of parasite growth by lactate dehydrogenase assay F 7.76 pIC50 17.4 nM IC50 Eur J Med Chem (2015) 101: 52-62 [PMID:26114811]
ChEMBL Antiplasmodial activity against Plasmodium falciparum assessed as inhibition of [3H]hypoxanthine incorporation F 7.77 pIC50 17 nM IC50 Med Chem Res (2011) 20: 321-332
ChEMBL Antimalarial activity against Plasmodium falciparum D10 clone 2 assessed as inhibition of [3H]hypoxanthine incorporation F 7.77 pIC50 16.8 nM IC50 Antimicrob Agents Chemother (2010) 54: 3842-3852 [PMID:20566762]
ChEMBL Antimalarial activity against Plasmodium falciparum 7G8 clone M1 assessed as inhibition of [3H]hypoxanthine incorporation F 7.8 pIC50 16 nM IC50 Antimicrob Agents Chemother (2010) 54: 3842-3852 [PMID:20566762]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 by LDH release assay F 7.82 pIC50 15 nM IC50 Eur J Med Chem (2018) 148: 39-53 [PMID:29454189]
ChEMBL Antimalarial activity against Plasmodium falciparum 7G8 harboring pfATP6 263E mutant assessed as inhibition of [3H]hypoxanthine incorporation F 7.83 pIC50 14.9 nM IC50 Antimicrob Agents Chemother (2010) 54: 3842-3852 [PMID:20566762]
ChEMBL Antimalarial activity against Plasmodium falciparum 7G8 clone M1 harboring pfATP6 L263 mutant assessed as inhibition of [3H]hypoxanthine incorporation F 7.83 pIC50 14.9 nM IC50 Antimicrob Agents Chemother (2010) 54: 3842-3852 [PMID:20566762]
ChEMBL Antiplasmodial activity against chloroquine-resistant synchronized trophozoite stage of Plasmodium falciparum Dd2 after 48 hrs by NBT dye based LDH assay F 7.84 pIC50 14.3 nM IC50 J Med Chem (2017) 60: 10245-10256 [PMID:29185748]
ChEMBL Antimalarial activity against Plasmodium falciparum 7G8 clone 1 assessed as inhibition of [3H]hypoxanthine incorporation F 7.85 pIC50 14.2 nM IC50 Antimicrob Agents Chemother (2010) 54: 3842-3852 [PMID:20566762]
ChEMBL Antimalarial activity against Plasmodium falciparum 7G8 harboring pfATP6 L263 mutant assessed as inhibition of [3H]hypoxanthine incorporation F 7.87 pIC50 13.5 nM IC50 Antimicrob Agents Chemother (2010) 54: 3842-3852 [PMID:20566762]
ChEMBL Antimalarial activity against Plasmodium falciparum 7G8 clone 1 harboring pfATP6 L263 mutant assessed as inhibition of [3H]hypoxanthine incorporation F 7.87 pIC50 13.5 nM IC50 Antimicrob Agents Chemother (2010) 54: 3842-3852 [PMID:20566762]
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 7.88 pIC50 13.3 nM IC50 ACS Med Chem Lett (2020) 11: 49-55 [PMID:31938463]
ChEMBL Antimalarial activity against Plasmodium falciparum 7G8 clone M2 assessed as inhibition of [3H]hypoxanthine incorporation F 7.88 pIC50 13.3 nM IC50 Antimicrob Agents Chemother (2010) 54: 3842-3852 [PMID:20566762]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 incubated for 48 hrs by parasite lactate dehydrogenase assay F 7.89 pIC50 13 nM IC50 ACS Med Chem Lett (2019) 10: 714-719 [PMID:31097988]
ChEMBL Antimalarial activity against chloroquine-sensitive asexual intraerythrocytic stage of Plasmodium falciparum NF54 assessed as inhibition of parasite growth by lactate dehydrogenase assay F 7.9 pIC50 12.6 nM IC50 Eur J Med Chem (2015) 101: 52-62 [PMID:26114811]
ChEMBL Antimalarial activity against Plasmodium falciparum 7G8 clone M3 assessed as inhibition of [3H]hypoxanthine incorporation F 7.91 pIC50 12.4 nM IC50 Antimicrob Agents Chemother (2010) 54: 3842-3852 [PMID:20566762]
ChEMBL Antimalarial activity against Plasmodium falciparum 7G8 clone 2 assessed as inhibition of [3H]hypoxanthine incorporation F 7.92 pIC50 12.1 nM IC50 Antimicrob Agents Chemother (2010) 54: 3842-3852 [PMID:20566762]
ChEMBL Antigametocytocidal activity against Plasmodium falciparum NF54-pfs16-GPF late (4 to 6) gametocyte assessed as viability after 72 hrs by MitoTracker Red CM-H2XRos/micro-plate confocal imaging system F 7.92 pIC50 12 nM IC50 Bioorg Med Chem Lett (2015) 25: 327-332 [PMID:25488841]
ChEMBL Antiplasmodial activity against chloroquine-resistant asexual erythrocytic stage of Plasmodium falciparum Dd2 assessed as [3H]-hypoxanthine incorporation by lactate dehydrogenase assay F 7.96 pIC50 11 nM IC50 Eur J Med Chem (2015) 92: 91-102 [PMID:25544689]
ChEMBL Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum NF54 incubated for 48 hrs by parasite lactate dehydrogenase assay F 8 pIC50 10 nM IC50 ACS Med Chem Lett (2019) 10: 714-719 [PMID:31097988]
ChEMBL Antiplasmodial activity against chloroquine/mefloquine-resistant Plasmodium falciparum SKF58 F 8 pIC50 10 nM IC50 Eur J Med Chem (2015) 94: 56-62 [PMID:25747499]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 F 8 pIC50 10 nM IC50 Medchemcomm (2014) 5: 842-852 [PMID:25089179]
ChEMBL Antiplasmodial activity against chloroquine-sensitive asexual blood stage of Plasmodium falciparum NF54 by LDH assay F 8.01 pIC50 9.8 nM IC50 Eur J Med Chem (2019) 180: 121-133 [PMID:31301563]
ChEMBL Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum NF54 by LDH assay F 8.03 pIC50 9.3 nM IC50 Bioorg Med Chem Lett (2017) 27: 658-661 [PMID:28012840]
ChEMBL Antimalarial activity against Plasmodium falciparum 3D7 infected in human erythrocytes assessed as parasite growth inhibition after 72 hrs by SYBR Green I assay F 8.05 pIC50 9 nM IC50 Bioorg Med Chem (2015) 23: 5452-5458 [PMID:26260339]
ChEMBL Antimalarial activity against CQ-sensitive Plasmodium falciparum 3D7 infected in erythrocytes by SYBR Green dye based fluorescence assay F 8.05 pIC50 9 nM IC50 Eur J Med Chem (2021) 209: 112941-112941 [PMID:33158577]
ChEMBL Antimalarial activity against multidrug resistant Plasmodium falciparum K1 infected in human erythrocytes assessed as inhibition of parasite proliferation after 96 hrs by SYBR Green I fluorescence based assay F 8.05 pIC50 8.97 nM IC50 Bioorg Med Chem Lett (2016) 26: 3006-3009 [PMID:27210430]
ChEMBL Antiplasmodial activity against asexual erythrocytic stage of chloroquine-resistant Plasmodium falciparum Dd2 assessed as parasite growth inhibition after 48 hrs by lactate dehydrogenase assay F 8.09 pIC50 8.1 nM IC50 Eur J Med Chem (2014) 76: 470-481 [PMID:24602791]
ChEMBL Antiplasmodial activity against chloroquine-sensitive asexual erythrocyte stage form Plasmodium falciparum NF54 measured after 48 hrs by pLDH assay F 8.1 pIC50 8 nM IC50 Eur J Med Chem (2016) 122: 635-646 [PMID:27448920]
ChEMBL Antimicrobial activity against Plasmodium falciparum at ring stage F 8.1 pIC50 8 nM IC50 Antimicrob Agents Chemother (2008) 52: 2435-2441 [PMID:18443130]
ChEMBL Gametocytocidal activity against synchronous stage 4 to 5 of transgenic Plasmodium falciparum NF54 gametocyte harboring pfs16 promoter assessed as parasite viability after 72 hrs by MitoTracker Red CMXRos-based assay F 8.1 pIC50 8 nM IC50 J Med Chem (2013) 56: 6200-6215 [PMID:23837878]
ChEMBL Gametocytocidal activity against transgenic GFP-fused Plasmodium falciparum NF54 late stage gametocytes after 72 hrs by Mitotracker Red CMH2XRos staining based imaging method F 8.1 pIC50 8 nM IC50 Eur J Med Chem (2018) 158: 801-813 [PMID:30245402]
ChEMBL Antimalarial activity against chloroquine-sensitive asexual Plasmodium falciparum NF54 infected in human erythrocytes assessed as inhibition of parasite proliferation after 96 hrs by SYBR Green I fluorescence based assay F 8.1 pIC50 7.88 nM IC50 Bioorg Med Chem Lett (2016) 26: 3006-3009 [PMID:27210430]
ChEMBL Antiplasmodial activity against chloroquine-resistant synchronized trophozoite stage of Plasmodium falciparum 7G8 after 48 hrs by NBT dye based LDH assay F 8.11 pIC50 7.7 nM IC50 J Med Chem (2017) 60: 10245-10256 [PMID:29185748]
ChEMBL Antiplasmodial activity against chloroquine-resistant asexual erythrocyte stage form Plasmodium falciparum Dd2 measured after 48 hrs by pLDH assay F 8.12 pIC50 7.5 nM IC50 Eur J Med Chem (2016) 122: 635-646 [PMID:27448920]
ChEMBL Antiplasmodium activity against chloroquine-sensitive Plasmodium falciparum NF54 asexual blood stage forms infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation incubated for 48 hrs by liquid scintillation counting method F 8.15 pIC50 7 nM IC50 Medchemcomm (2019) 10: 450-455 [PMID:31015908]
ChEMBL Antimalarial activity against multidrug resistant Plasmodium falciparum W2 infected in human erythrocytes assessed as inhibition of parasite proliferation after 96 hrs by SYBR Green I fluorescence based assay F 8.17 pIC50 6.77 nM IC50 Bioorg Med Chem Lett (2016) 26: 3006-3009 [PMID:27210430]
ChEMBL Antiplasmodial activity against chloroquine-sensitive asexual erythrocytic stage of Plasmodium falciparum D10 assessed as parasite growth inhibition by lactate dehydrogenase assay F 8.2 pIC50 6.3 nM IC50 J Med Chem (2014) 57: 435-448 [PMID:24354322]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 asexual gametocytes F 8.22 pIC50 6 nM IC50 Antimicrob Agents Chemother (2007) 51: 1463-1472 [PMID:17242150]
ChEMBL Antimalarial activity against Plasmodium falciparum Dd2 harbouring Pf-crt, Pf-mdrl,Pf-dhfr, Pf-dhps mutated loci assessed as inhibition of parasite growth incubated for 48 hrs by [3H]hypoxanthine incorporation assay based liquid scintillation counting method F 8.22 pIC50 6 nM IC50 J Med Chem (2021) 64: 12582-12602 [PMID:34437804]
ChEMBL Antimalarial activity against Plasmodium falciparum NF54 assessed as inhibition of parasite growth incubated for 48 hrs by [3H]hypoxanthine incorporation assay based liquid scintillation counting method F 8.22 pIC50 6 nM IC50 J Med Chem (2021) 64: 12582-12602 [PMID:34437804]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 assessed as inhibition of parasite proliferation after 96 hrs by SYBR Green I-based fluorescence method F 8.24 pIC50 5.71 nM IC50 Eur J Med Chem (2015) 90: 33-44 [PMID:25461309]
ChEMBL Antiplasmodial activity against chloroquine-sensitive synchronized trophozoite stage of Plasmodium falciparum NF54 after 48 hrs by NBT dye based LDH assay F 8.25 pIC50 5.6 nM IC50 J Med Chem (2017) 60: 10245-10256 [PMID:29185748]
ChEMBL Antiplasmodial activity chloroquine-sensitive Plasmodium falciparum 3D7 infected in human A+ erythrocytes assessed as inhibition of [3H]-hypoxanthine incorporation after 24 hrs by scintillation counting F 8.28 pIC50 5.3 nM IC50 Eur J Med Chem (2012) 52: 82-97 [PMID:22459876]
ChEMBL Antiplasmodial activity against Plasmodium falciparum NF54 F 8.28 pIC50 <5.2 nM IC50 Eur J Med Chem (2021) 219: 113408-113408 [PMID:33989911]
ChEMBL Antiplasmodial activity against chloroquine-resistant asexual erythrocytic stage of Plasmodium falciparum Dd2 assessed as parasite growth inhibition by parasite lactate dehydrogenase assay F 8.28 pIC50 <5.2 nM IC50 Bioorg Med Chem (2015) 23: 4163-4171 [PMID:26174655]
ChEMBL Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum NF54 asexual erythrocyte stages by parasite lactate dehydrogenase assay F 8.28 pIC50 5.2 nM IC50 Bioorg Med Chem Lett (2014) 24: 5207-5211 [PMID:25316314]
ChEMBL Antiplasmodial activity against asexual erythrocytic stage of chloroquine-sensitive Plasmodium falciparum NF54 assessed as parasite growth inhibition after 48 hrs by lactate dehydrogenase assay F 8.28 pIC50 <5.2 nM IC50 Eur J Med Chem (2014) 76: 470-481 [PMID:24602791]
ChEMBL Antimalarial activity against ring-stage chloroquine-susceptible Plasmodium falciparum 3D7 preincubated for 6 hrs followed by compound wash and measured after 66 hrs by Giemsa-staining based light microscopic analysis F 8.29 pIC50 5.1 nM IC50 Eur J Med Chem (2019) 163: 404-412 [PMID:30530192]
ChEMBL Antiplasmodial activity against chloroquine-sensitive asexual erythrocytic stage of Plasmodium falciparum NF54 assessed as [3H]-hypoxanthine incorporation by lactate dehydrogenase assay F 8.3 pIC50 5 nM IC50 Eur J Med Chem (2015) 92: 91-102 [PMID:25544689]
ChEMBL Antiplasmodial activity chloroquine-sensitive Plasmodium falciparum NF54 by lactate dehydrogenase assay F 8.3 pIC50 5 nM IC50 Bioorg Med Chem Lett (2014) 24: 1214-1217 [PMID:24468411]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 infected in human erythrocytes assessed as [3H]hypoxanthine incorporation after 48 hrs by betaplate liquid scintillation counting analysis F 8.31 pIC50 4.9 nM IC50 Medchemcomm (2011) 2: 661-665
ChEMBL Antimalarial activity against ring-stage multidrug-resistant Plasmodium falciparum Dd2 preincubated for 6 hrs followed by compound wash and measured after 66 hrs by Giemsa-staining based light microscopic analysis F 8.34 pIC50 4.6 nM IC50 Eur J Med Chem (2019) 163: 404-412 [PMID:30530192]
ChEMBL Antiplasmodial activity against blood stage of chloroquine-sensitive Plasmodium falciparum NF54 by parasite lactate dehydrogenase assay F 8.36 pIC50 4.4 nM IC50 Eur J Med Chem (2015) 101: 266-273 [PMID:26142491]
ChEMBL Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 F 8.38 pIC50 4.2 nM IC50 Eur J Med Chem (2015) 94: 56-62 [PMID:25747499]
ChEMBL Antimalarial activity against Plasmodium falciparum NF54 within 48 hrs F 8.38 pIC50 4.2 nM IC50 Antimicrob Agents Chemother (2007) 51: 667-672 [PMID:17145800]
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum NF54 infected in mouse at 30 mg/kg, po F 8.38 pIC50 4.2 nM IC50 J Med Chem (2013) 56: 2547-2555 [PMID:23489135]
ChEMBL Antiplasmodial activity against chloroquine/mefloquine-resistant Plasmodium falciparum SRIV35 F 8.39 pIC50 4.1 nM IC50 Eur J Med Chem (2015) 94: 56-62 [PMID:25747499]
ChEMBL Antimalarial activity against Plasmodium falciparum Cam3.1 harbouring Pf-crt, Pf-mdrl,Pf-dhfr, Pf-dhps, pf-kelch13 mutated loci assessed as inhibition of parasite growth incubated for 48 hrs by [3H]hypoxanthine incorporation assay based liquid scintillation counting method F 8.4 pIC50 4 nM IC50 J Med Chem (2021) 64: 12582-12602 [PMID:34437804]
ChEMBL Antimalarial activity against drug-sensitive Plasmodium falciparum NF54 F 8.4 pIC50 4 nM IC50 J Med Chem (2014) 57: 2789-2798 [PMID:24568587]
ChEMBL Antimalarial activity against Plasmodium falciparum NF54 infected in human erythrocytes assessed as reduction in [3H]hypoxanthine incorporation preincubated for 48 hrs followed by [3H]hypoxanthine addition measured after 24 hrs by liquid scintillation counting F 8.4 pIC50 4 nM IC50 Medchemcomm (2017) 8: 1152-1157 [PMID:30108825]
ChEMBL Antimalarial activity against drug-sensitive Plasmodium falciparum NF54 F 8.4 pIC50 4 nM IC50 J Med Chem (2018) 61: 4213-4227 [PMID:29665687]
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as inhibition of parasite proliferation after 96 hrs by SYBR Green I-based fluorescence method F 8.4 pIC50 4 nM IC50 Eur J Med Chem (2015) 90: 33-44 [PMID:25461309]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum NF54 F 8.4 pIC50 4 nM IC50 J Med Chem (2011) 54: 7713-7719 [PMID:21966980]
ChEMBL Antiplasmodial activity against chloroquine-sensitive asexual blood stage of Plasmodium falciparum NF54 infected in human RBC assessed as reduction in [3H]hypoxanthine incorporation preincubated for 48 hrs followed by [3H]hypoxanthine addition measured after 24 hrs by liquid scintillation counting method F 8.4 pIC50 4 nM IC50 J Med Chem (2019) 62: 1022-1035 [PMID:30562027]
ChEMBL Antiplasmodial activity against multidrug-sensitive Plasmodium falciparum NF54 by [3H]-hypoxanthine incorporation assay F 8.4 pIC50 4 nM IC50 J Med Chem (2015) 58: 7572-7579 [PMID:26322748]
ChEMBL Antiplasmodial activity against multidrug-sensitive Plasmodium falciparum NF54 infected in human erythrocytes assessed as reduction in [3H]hypoxanthine incorporation preincubated for 48 hrs followed by [3H]hypoxanthine addition and measured after 24 hrs by liquid scintillation counting method F 8.4 pIC50 4 nM IC50 J Med Chem (2016) 59: 9890-9905 [PMID:27748596]
ChEMBL Antiplasmodial activity against multidrug resistant Plasmodium falciparum K1 infected in human erythrocytes after 48 hrs by [3H]-hypoxanthine incorporation assay F 8.4 pIC50 4 nM IC50 J Med Chem (2015) 58: 8713-8722 [PMID:26502160]
ChEMBL Antiplasmodial activity against drug-sensitive blood stage Plasmodium falciparum 3D7 by SYBR green 1 staining based fluorescence assay F 8.4 pIC50 4 nM IC50 J Nat Prod (2018) 81: 188-202 [PMID:29297684]
ChEMBL Antimalarial activity against Plasmodium falciparum K1 harbouring Pf-crt, Pf-mdrl,Pf-dhfr, Pf-dhps mutated loci assessed as inhibition of parasite growth incubated for 48 hrs by [3H]hypoxanthine incorporation assay based liquid scintillation counting method F 8.4 pIC50 4 nM IC50 J Med Chem (2021) 64: 12582-12602 [PMID:34437804]
ChEMBL Antiplasmodial activity against chloroquine sensitive Plasmodium falciparum NF54 infected in human RBC after 48 hrs by [3H]hypoxanthine incorporation assay F 8.4 pIC50 4 nM IC50 Medchemcomm (2015) 6: 2023-2028
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum Nigerian infected in human blood after 48 hrs by [3H]-hypoxanthine incorporation assay F 8.42 pIC50 3.8 nM IC50 Bioorg Med Chem Lett (2019) 29: 2203-2207 [PMID:31255483]
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum IMT10500 infected in erythrocytes after 48 hrs by [3H]hypoxanthine incorporation assay F 8.42 pIC50 3.8 nM IC50 J Med Chem (2009) 52: 7954-7957 [PMID:19908867]
ChEMBL Antimalarial activity against late stage gametocyte stage of Plasmodium falciparum NF54 after 72 hrs F 8.42 pIC50 3.8 nM IC50 Eur J Med Chem (2014) 82: 204-213 [PMID:24904967]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 F 8.46 pIC50 3.5 nM IC50 Eur J Med Chem (2015) 94: 56-62 [PMID:25747499]
ChEMBL Antimalarial activity against late (4 to 5) gametocytic stage of Plasmodium falciparum after 72 hrs by image-based HTS assay F 8.46 pIC50 3.43 nM IC50 J Med Chem (2013) 56: 7727-7740 [PMID:23927763]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 F 8.47 pIC50 3.4 nM IC50 J Med Chem (2013) 56: 2547-2555 [PMID:23489135]
ChEMBL Antiplasmodial activity against erythrocytic stage of chloroquine-sensitive Plasmodium falciparum 3D7 assessed as inhibition of parasite growth incubated for 3 days by HRP2-ELISA assay F 8.48 pIC50 3.3 nM IC50 Eur J Med Chem (2022) 244: 114774-114774 [PMID:36306538]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 infected in RBCs by firefly luciferase reporter gene assay F 8.48 pIC50 3.3 nM IC50 Antimicrob Agents Chemother (2010) 54: 3597-3604 [PMID:20547797]
ChEMBL Antiplasmodial activity against drug-resistant Plasmodium falciparum Dd2 ring stage forms assessed as inhibition of parasite growth after 72 hrs by DAPI staining-based confocal microscopic analysis F 8.48 pIC50 3.3 nM IC50 J Nat Prod (2019) 82: 1019-1023 [PMID:30865443]
ChEMBL Antimalarial activity against asexual stage of Plasmodium falciparum K1 assessed as reduction in parasite growth incubated for 96 hrs by SYBR Green I dye-based fluorescence assay F 8.49 pIC50 3.26 nM IC50 ACS Med Chem Lett (2020) 11: 49-55 [PMID:31938463]
ChEMBL Antimalarial activity against Plasmodium falciparum NF54 incubated for 48 hrs by [3H]-hypoxanthine incorporation assay F 8.49 pIC50 3.2 nM IC50 ACS Med Chem Lett (2020) 11: 49-55 [PMID:31938463]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 F 8.49 pIC50 3.2 nM IC50 Antimicrob Agents Chemother (2008) 52: 1291-1296 [PMID:18268087]
ChEMBL Gametocytocidal activity against transgenic GFP-fused Plasmodium falciparum NF54 early stage gametocytes after 72 hrs by Mitotracker Red CMH2XRos staining based confocal microscopic method F 8.52 pIC50 3 nM IC50 J Med Chem (2017) 60: 6036-6044 [PMID:28653845]
ChEMBL Antimalarial activity against Plasmodium falciparum 7G8 harbouring Pf-crt, Pf-mdrl,Pf-dhfr, Pf-dhps mutated loci assessed as inhibition of parasite growth incubated for 48 hrs by [3H]hypoxanthine incorporation assay based liquid scintillation counting method F 8.52 pIC50 3 nM IC50 J Med Chem (2021) 64: 12582-12602 [PMID:34437804]
ChEMBL Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum K1 F 8.52 pIC50 3 nM IC50 J Med Chem (2011) 54: 7713-7719 [PMID:21966980]
ChEMBL Gametocytocidal activity against transgenic GFP-fused Plasmodium falciparum NF54 ring stage gametocytes after 72 hrs by Mitotracker Red CMH2XRos staining based confocal microscopic method F 8.52 pIC50 3 nM IC50 J Med Chem (2017) 60: 6036-6044 [PMID:28653845]
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum IMTVo1 infected in erythrocytes after 48 hrs by [3H]hypoxanthine incorporation assay F 8.52 pIC50 3 nM IC50 J Med Chem (2009) 52: 7954-7957 [PMID:19908867]
ChEMBL Antiplasmodial activity against multidrug-resistant Plasmodium falciparum K1 infected in erythrocytes assessed as reduction in [3H]hypoxanthine incorporation preincubated for 48 hrs followed by [3H]hypoxanthine addition and measured after 24 hrs by liquid scintillation counting method F 8.52 pIC50 3 nM IC50 J Med Chem (2016) 59: 9890-9905 [PMID:27748596]
ChEMBL Antiplasmodial activity against drug sensitive Plasmodium falciparum NF54 infected in human erythrocytes after 48 hrs by [3H]-hypoxanthine incorporation assay F 8.52 pIC50 3 nM IC50 J Med Chem (2015) 58: 8713-8722 [PMID:26502160]
ChEMBL Antiplasmodial activity against chloroquine/cycloguanil/pyrimethamine-resistant blood stage Plasmodium falciparum K1 by SYBR green 1 staining based fluorescence assay F 8.52 pIC50 3 nM IC50 J Nat Prod (2018) 81: 188-202 [PMID:29297684]
ChEMBL Antiplasmodial activity against multidrug-resistant Plasmodium falciparum K1 by [3H]-hypoxanthine incorporation assay F 8.52 pIC50 3 nM IC50 J Med Chem (2015) 58: 7572-7579 [PMID:26322748]
ChEMBL Antimalarial activity against multidrug-resistant Plasmodium falciparum K1 F 8.52 pIC50 3 nM IC50 J Med Chem (2018) 61: 4213-4227 [PMID:29665687]
ChEMBL Antiplasmodial activity against chloroquine-resistant asexual blood stage of Plasmodium falciparum K1 infected in human RBC assessed as reduction in [3H]hypoxanthine incorporation preincubated for 48 hrs followed by [3H]hypoxanthine addition measured after 24 hrs by liquid scintillation counting method F 8.52 pIC50 3 nM IC50 J Med Chem (2019) 62: 1022-1035 [PMID:30562027]
ChEMBL Antigametocytocidal activity against Plasmodium falciparum NF54-pfs16-GPF early (1 to 3) gametocyte assessed as viability after 72 hrs by MitoTracker Red CM-H2XRos/micro-plate confocal imaging system F 8.52 pIC50 3 nM IC50 Bioorg Med Chem Lett (2015) 25: 327-332 [PMID:25488841]
ChEMBL Gametocytocidal activity against transgenic GFP-fused Plasmodium falciparum NF54 early stage gametocytes after 72 hrs by Mitotracker Red CMH2XRos staining based imaging method F 8.52 pIC50 3 nM IC50 Eur J Med Chem (2018) 158: 801-813 [PMID:30245402]
ChEMBL Antimalarial activity against multidrug-resistant Plasmodium falciparum K1 F 8.52 pIC50 3 nM IC50 J Med Chem (2014) 57: 2789-2798 [PMID:24568587]
ChEMBL Antimalarial activity against Plasmodium falciparum K1 infected in human erythrocytes preincubated for 48 hrs followed by [3H]-hypoxanthine addition and measured after 24 hrs by liquid scintillation counting F 8.52 pIC50 3 nM IC50 J Med Chem (2018) 61: 9371-9385 [PMID:30256636]
ChEMBL Antiplasmodial activity against Plasmodium falciparum K1 after 48 hrs by lactate dehydrogenase assay F 8.52 pIC50 3 nM IC50 J Med Chem (2018) 61: 9371-9385 [PMID:30256636]
ChEMBL Antimalarial activity against asexual stage of Plasmodium falciparum NF54 assessed as reduction in parasite growth incubated for 96 hrs by SYBR Green I dye-based fluorescence assay F 8.52 pIC50 3 nM IC50 ACS Med Chem Lett (2020) 11: 49-55 [PMID:31938463]
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum FC27 infected in human RBC assessed as reduction in parasite growth after 35 to 56 hrs by nucleic acid staining based flow cytometry F 8.54 pIC50 2.9 nM IC50 J Med Chem (2019) 62: 2485-2498 [PMID:30715882]
ChEMBL Antiplasmodium activity against multidrug resistant Plasmodium falciparum K1 asexual blood stage forms infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation incubated for 48 hrs by liquid scintillation counting method F 8.54 pIC50 2.9 nM IC50 Medchemcomm (2019) 10: 450-455 [PMID:31015908]
ChEMBL Antiplasmodial activity chloroquine-resistant Plasmodium falciparum K1 infected in human A+ erythrocytes assessed as inhibition of [3H]-hypoxanthine incorporation after 24 hrs by scintillation counting F 8.55 pIC50 2.8 nM IC50 Eur J Med Chem (2012) 52: 82-97 [PMID:22459876]
ChEMBL Antimalarial activity against Plasmodium falciparum TM90C2B incubated for 48 hrs by [3H]-hypoxanthine incorporation assay F 8.57 pIC50 2.7 nM IC50 ACS Med Chem Lett (2020) 11: 49-55 [PMID:31938463]
ChEMBL Antiplasmodial activity against chloroquine sensitive Plasmodium falciparum NF54 assessed as reduction in [3H]-hypoxanthine incorporation incubated for 48 hrs by liquid scintillation counting method F 8.59 pIC50 2.6 nM IC50 Eur J Med Chem (2017) 140: 595-603 [PMID:28988153]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 by [3H]hypoxanthine incorporation assay F 8.59 pIC50 2.6 nM IC50 Bioorg Med Chem Lett (2017) 27: 658-661 [PMID:28012840]
ChEMBL Antimalarial activity against Plasmodium falciparum FCR-3/Gambia F 8.6 pIC50 2.5 nM IC50 Medchemcomm (2014) 5: 842-852 [PMID:25089179]
ChEMBL Antimicrobial activity against Plasmodium falciparum NF54 F 8.6 pIC50 2.5 nM IC50 ACS Med Chem Lett (2011) 2: 316-319 [PMID:21666827]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 assessed as inhibition of parasite growth after 48 hrs by [3H]hypoxanthine reuptake assay F 8.61 pIC50 2.46 nM IC50 Eur J Med Chem (2009) 44: 5071-5079 [PMID:19811859]
ChEMBL Antimalarial activity against drug sensitive Plasmodium falciparum NF54 F 8.62 pIC50 2.4 nM IC50 Eur J Med Chem (2021) 210: 113084-113084 [PMID:33333397]
ChEMBL Antimalarial activity against drug resistant Plasmodium falciparum K1 F 8.62 pIC50 2.4 nM IC50 Eur J Med Chem (2021) 210: 113084-113084 [PMID:33333397]
ChEMBL Antimalarial activity against asexual stage of Plasmodium falciparum W2 assessed as reduction in parasite growth incubated for 96 hrs by SYBR Green I dye-based fluorescence assay F 8.62 pIC50 2.4 nM IC50 ACS Med Chem Lett (2020) 11: 49-55 [PMID:31938463]
ChEMBL Antimalarial activity against drug resistant Plasmodium falciparum W2 F 8.62 pIC50 2.4 nM IC50 Eur J Med Chem (2021) 210: 113084-113084 [PMID:33333397]
ChEMBL Antiplasmodial activity against chloroquine resistant Plasmodium falciparum by HRP2 ELISA analysis F 8.63 pIC50 2.34 nM IC50 Eur J Med Chem (2021) 219: 113408-113408 [PMID:33989911]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum FcB1 F 8.64 pIC50 2.3 nM IC50 Antimicrob Agents Chemother (2007) 51: 1463-1472 [PMID:17242150]
ChEMBL Antiparasitic activity against chloroquine-sensitive Plasmodium falciparum by [3H]hypoxanthine incorporation F 8.64 pIC50 2.3 nM IC50 J Med Chem (2008) 51: 1260-1277 [PMID:18260613]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 infected in human RBC assessed as reduction in parasite growth after 35 to 56 hrs by nucleic acid staining based flow cytometry F 8.64 pIC50 2.3 nM IC50 J Med Chem (2019) 62: 2485-2498 [PMID:30715882]
ChEMBL Antimalarial activity against asexual stage of Plasmodium falciparum 3D7 after 72 hrs by image-based HTS assay F 8.66 pIC50 2.2 nM IC50 J Med Chem (2013) 56: 7727-7740 [PMID:23927763]