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

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ChEMBL ligand: CHEMBL361497 (Arsumax, Artesunate, NSC-712571)
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  • Plasmodium falciparum (isolate K1 / Thailand) in Plasmodium falciparum K1 [ChEMBL: CHEMBL612856]
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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 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 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 chloroquine-resistant Plasmodium falciparum Dd2 F 7.51 pIC50 31.2 nM IC50 Eur. J. Med. Chem. (2013) 66: 314-323 [PMID:23811093]
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 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 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 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 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-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 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 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 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 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/mefloquine-resistant Plasmodium falciparum SKF58 F 8 pIC50 10 nM IC50 Eur. J. Med. Chem. (2015) 94: 56-62 [PMID:25747499]
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-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 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 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 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 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 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
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 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 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 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 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 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 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 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 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 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 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 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 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 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
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 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 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 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 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-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 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 multidrug-resistant Plasmodium falciparum K1 F 8.52 pIC50 3 nM IC50 J Med Chem (2018) 61: 4213-4227 [PMID:29665687]
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 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 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 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 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 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 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 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
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 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 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 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 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 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]
ChEMBL Antiplasmodial activity against drug-sensitive Plasmodium falciparum 3D7 ring stage forms assessed as inhibition of parasite growth after 72 hrs by DAPI staining-based confocal microscopic analysis F 8.68 pIC50 2.1 nM IC50 J Nat Prod (2019) 82: 1019-1023 [PMID:30865443]
ChEMBL Antimalarial activity against multidrug-resistant Plasmodium falciparum clinical isolates infected assessed as reduction in parasite growth after 35 to 56 hrs by nucleic acid staining based flow cytometry F 8.68 pIC50 2.1 nM IC50 J Med Chem (2019) 62: 2485-2498 [PMID:30715882]
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as inhibition of [3H]hypoxanthine incorporation F 8.7 pIC50 2 nM IC50 Antimicrob. Agents Chemother. (2011) 55: 961-966 [PMID:21135175]
ChEMBL Antiplasmodial activity against Plasmodium falciparum Dd2 asexual blood stages after 3 days by HRP2 detection based ELISA method F 8.7 pIC50 2 nM IC50 J. Med. Chem. (2014) 57: 7971-7976 [PMID:25195945]
ChEMBL Antispasmodial activity against multidrug-resistant asexual blood stages of Plasmodium falciparum Dd2 after 72 hrs by HRP2-based ELISA F 8.7 pIC50 2 nM IC50 J Med Chem (2017) 60: 6036-6044 [PMID:28653845]
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum PA infected in erythrocytes after 48 hrs by [3H]hypoxanthine incorporation assay F 8.7 pIC50 2 nM IC50 J. Med. Chem. (2009) 52: 7954-7957 [PMID:19908867]
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum FCM29 infected in erythrocytes after 48 hrs by [3H]hypoxanthine incorporation assay F 8.72 pIC50 1.9 nM IC50 J. Med. Chem. (2009) 52: 7954-7957 [PMID:19908867]
ChEMBL Antispasmodial activity against chloroquine-sensitive asexual blood stages of Plasmodium falciparum 3D7 after 72 hrs by HRP2-based ELISA F 8.72 pIC50 1.9 nM IC50 J Med Chem (2017) 60: 6036-6044 [PMID:28653845]
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum IMT K2 infected in erythrocytes after 48 hrs by [3H]hypoxanthine incorporation assay F 8.74 pIC50 1.8 nM IC50 J. Med. Chem. (2009) 52: 7954-7957 [PMID:19908867]
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum IMTL1 infected in erythrocytes after 48 hrs by [3H]hypoxanthine incorporation assay F 8.77 pIC50 1.7 nM IC50 J. Med. Chem. (2009) 52: 7954-7957 [PMID:19908867]
ChEMBL Antimalarial activity against synchronized ring stage Plasmodium falciparum 3D7 transfected with nano-luciferase assessed as parasite growth inhibition after 48 hrs by Nano-Glo luciferase assay F 8.79 pIC50 1.64 nM IC50 MedChemComm (2019) 10: 1599-1605
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum FcM29 F 8.8 pIC50 1.6 nM IC50 Antimicrob. Agents Chemother. (2007) 51: 1463-1472 [PMID:17242150]
ChEMBL Antimalarial activity against Plasmodium falciparum 3D7 after 72 hrs by DAPI staining-based confocal imaging analysis F 8.8 pIC50 1.6 nM IC50 J Med Chem (2019) 62: 622-640 [PMID:30537832]
ChEMBL Antimalarial activity against Plasmodium falciparum K1 incubated for 48 hrs by [3H]-hypoxanthine incorporation assay F 8.85 pIC50 1.4 nM IC50 ACS Med Chem Lett (2020) 11: 49-55 [PMID:31938463]
ChEMBL Antiparasitic activity against Plasmodium falciparum Dd2 assessed as growth inhibition after 72 hrs by DAPI staining-based confocal image analysis F 8.89 pIC50 1.3 nM IC50 Eur. J. Med. Chem. (2016) 110: 43-64 [PMID:26807544]
ChEMBL Antimalarial activity against trophozoites stage of Plasmodium falciparum assessed as parasites growth inhibition using giemsa staining after 24 to 56 hrs by microscopic analysis in presence of 10% human serum F 8.92 pIC50 1.19 nM IC50 Antimicrob. Agents Chemother. (2011) 55: 961-966 [PMID:21135175]
ChEMBL Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 measured after 72 hrs by DAPI staining based high throughput screening assay F 9 pIC50 1 nM IC50 Bioorg Med Chem Lett (2017) 27: 2602-2607 [PMID:28400231]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 after 72 hrs by DAPI staining based fluorescence assay F 9 pIC50 1 nM IC50 J Nat Prod (2018) 81: 1079-1083 [PMID:29533611]
ChEMBL Antiplasmodial activity against drug-sensitive Plasmodium falciparum 3D7 ring stage infected in human erythrocytes after 72 hrs by DAPI staining based method F 9 pIC50 1 nM IC50 J Nat Prod (2018) 81: 1588-1597 [PMID:29969262]
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 after 72 hrs by DAPI staining based confocal microplate imaging method F 9 pIC50 1 nM IC50 J Nat Prod (2017) 80: 3211-3217 [PMID:29236492]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 after 72 hrs by DAPI staining based confocal microplate imaging method F 9 pIC50 1 nM IC50 J Nat Prod (2017) 80: 3211-3217 [PMID:29236492]
ChEMBL Antimalarial activity against Plasmodium falciparum Dd2 after 72 hrs by DAPI staining-based fluorescence microscopic analysis F 9 pIC50 1 nM IC50 Bioorg Med Chem Lett (2017) 27: 4091-4095 [PMID:28774427]
ChEMBL Antimalarial activity against Plasmodium falciparum Dd2 after 72 hrs by DAPI staining-based confocal imaging analysis F 9 pIC50 1 nM IC50 J Med Chem (2019) 62: 622-640 [PMID:30537832]
ChEMBL Antimalarial activity against Plasmodium falciparum assessed as parasites growth inhibition using giemsa staining after 24 to 56 hrs by microscopic analysis in presence of 10% human serum F 9.04 pIC50 0.92 nM IC50 Antimicrob. Agents Chemother. (2011) 55: 961-966 [PMID:21135175]
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 after 72 hrs by DAPI staining based fluorescence assay F 9.05 pIC50 0.9 nM IC50 J Nat Prod (2018) 81: 1079-1083 [PMID:29533611]
ChEMBL Antimalarial activity against Plasmodium falciparum 3D7 after 72 hrs by DAPI staining-based fluorescence microscopic analysis F 9.05 pIC50 0.9 nM IC50 Bioorg Med Chem Lett (2017) 27: 4091-4095 [PMID:28774427]
ChEMBL Antiparasitic activity against chloroquine/quinine/pyrimethamine/sulfadoxine/NITD609-resistant Plasmodium falciparum Dd2 clone 2 assessed as growth inhibition after 72 hrs by DAPI staining-based confocal image analysis F 9.05 pIC50 0.9 nM IC50 Eur. J. Med. Chem. (2016) 110: 43-64 [PMID:26807544]
ChEMBL Antimalarial activity against ring stage of Plasmodium falciparum assessed as parasites growth inhibition using giemsa staining after 24 to 56 hrs by microscopic analysis in presence of 10% human serum F 9.06 pIC50 0.88 nM IC50 Antimicrob. Agents Chemother. (2011) 55: 961-966 [PMID:21135175]
ChEMBL Antimalarial activity against Plasmodium falciparum infected in human erythrocytes assessed as growth inhibition by microscopic analysis using giemsa staining F 9.17 pIC50 0.68 nM IC50 Antimicrob. Agents Chemother. (2010) 54: 5146-5150 [PMID:20876370]
ChEMBL Antiplasmodial activity against 4-aminoquinoline/antifolates-resistant Plasmodium falciparum Dd2 ring stage infected in human erythrocytes after 72 hrs by DAPI staining based method F 9.17 pIC50 0.67 nM IC50 J Nat Prod (2018) 81: 1588-1597 [PMID:29969262]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 measured after 72 hrs by DAPI staining based high throughput screening assay F 9.17 pIC50 0.67 nM IC50 Bioorg Med Chem Lett (2017) 27: 2602-2607 [PMID:28400231]
ChEMBL Antiplasmodial activity against chloroquine and pyrimethamine resistant Plasmodium falciparum K1 assessed as reduction in [3H]-hypoxanthine incorporation incubated for 48 hrs by liquid scintillation counting method F 9.3 pIC50 0.5 nM IC50 Eur J Med Chem (2017) 140: 595-603 [PMID:28988153]
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in human RBC after 72 hrs by DAPI staining based confocal microscopic method F 9.32 pIC50 0.48 nM IC50 J Nat Prod (2017) 80: 114-125 [PMID:28001067]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 assessed as inhibition of parasite growth after 72 hrs by DAPI staining-based confocal microscopic analysis F 9.35 pIC50 0.44 nM IC50 J. Nat. Prod. (2015) 78: 2932-2939 [PMID:26651537]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 infected in human RBC after 72 hrs by DAPI staining based confocal microscopic method F 9.36 pIC50 0.44 nM IC50 J Nat Prod (2017) 80: 114-125 [PMID:28001067]
ChEMBL Antiplasmodial activity against asexual form of Plasmodium falciparum NF54 assessed as reduction in female gametocytes activation preincubated for 48 hrs followed by gametocytes activation and measured after 24 hrs by fluorescence based automated inverted microscopic analysis F 5 pEC50 >10000 nM EC50 J Med Chem (2019) 62: 9217-9235 [PMID:31566384]
ChEMBL Antiplasmodial activity against asexual form of Plasmodium falciparum NF54 assessed as reduction in male gametocytes activation preincubated for 48 hrs followed by gametocytes activation and measured after 24 hrs by fluorescence based automated inverted microscopic analysis F 5 pEC50 >10000 nM EC50 J Med Chem (2019) 62: 9217-9235 [PMID:31566384]
ChEMBL Antiplasmodial activity against asexual form of Plasmodium falciparum NF54 assessed as reduction in female gametocytes activation preincubated for 48 hrs followed by gametocytes activation and measured after 24 hrs by fluorescence based automated inverted microscopic analysis F 5 pEC50 >10000 nM EC50 J Med Chem (2019) 62: 9217-9235 [PMID:31566384]
ChEMBL Antiplasmodial activity against asexual form of Plasmodium falciparum NF54 assessed as reduction in male gametocytes activation preincubated for 48 hrs followed by gametocytes activation and measured after 24 hrs by fluorescence based automated inverted microscopic analysis F 5 pEC50 >10000 nM EC50 J Med Chem (2019) 62: 9217-9235 [PMID:31566384]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7A erythrocytic stage assessed as reduction in [3H]hypoxanthine incorporation preincubated for 24 hrs followed by [3H]hypoxanthine addition and measured after 24 hrs by microbeta scintillation counting method F 7.52 pEC50 30 nM EC50