artesunate [Ligand Id: 9956] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL361497 (.alpha.-artesunic acid, Arsumax, Artesunate, 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 | 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 | 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 | 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 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 | 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 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 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 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 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 | 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 | 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 | 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 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 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 | 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 | 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 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 | 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 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 | 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 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 | 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 [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 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 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 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 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 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 | 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 | 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 | 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 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 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 | 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 | 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 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 (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 multidrug-resistant Plasmodium falciparum K1 | F | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2018) 61: 4213-4227 [PMID:29665687] |
| 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 | 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 | 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 | 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 | 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 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 | 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 | 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 | 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 | 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 | 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 | 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 Plasmodium falciparum TM90C2b harbouring Pf-crt, Pf-mdrl,Pfd-hfr, Pf-cytbQ0 mutated loci assessed as inhibition of parasite growth incubated for 48 hrs by [3H]hypoxanthine incorporation assay based liquid scintillation counting method | F | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2021) 64: 12582-12602 [PMID:34437804] |
| 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 3D7 by SyBR Green method | F | 8.7 | pIC50 | 2 | nM | IC50 | Eur J Med Chem (2020) 188: 111983-111983 [PMID:31911292] |
| 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 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 | 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 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 | 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 [PMID:31803400] |
| 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 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 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 synchronous ring stage of Plasmodium falciparum Dd2 assessed as parasite growth inhibition incubated for 72 hrs by Griffith assay based fluorescence analysis | F | 8.89 | pIC50 | 1.3 | nM | IC50 | Eur J Med Chem (2021) 221: 113518-113518 [PMID:34058708] |
| 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 | 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 fluorescence assay | F | 9 | pIC50 | 1 | nM | IC50 | J Nat Prod (2018) 81: 1079-1083 [PMID:29533611] |
| 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 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 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 | 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 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 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 synchronous ring stage of Plasmodium falciparum 3D7 assessed as parasite growth inhibition incubated for 72 hrs by Griffith assay based fluorescence analysis | F | 9.05 | pIC50 | 0.9 | nM | IC50 | Eur J Med Chem (2021) 221: 113518-113518 [PMID:34058708] |
| 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 chloroquine-sensitive Plasmodium falciparum 3D7 infected in human erythrocytes assessed as inhibition of parasite growth incubated for 72 hrs by DAPI staining based fluorescence analysis | F | 9.17 | pIC50 | 0.67 | |||