chloroquine [Ligand Id: 5535] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL76 (Chloroquine, Chlorochine, NSC-187208, Aralen)
  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
  • This target only has 1 pki data point
1 CHEMBL76_lig_chart_1 Alpha-2a adrenergic receptor Human
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  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
  • This target only has 1 pki data point
2 CHEMBL76_lig_chart_2 Alpha-2b adrenergic receptor Human
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  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
  • This target only has 1 pki data point
3 CHEMBL76_lig_chart_3 Alpha-2c adrenergic receptor Human
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  • Beta amyloid A4 protein in Human [ChEMBL: CHEMBL2487] [UniProtKB: P05067]
  • This target only has 0 pki data point
4 CHEMBL76_lig_chart_4 Beta amyloid A4 protein Human
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  • beta-secretase 1/Beta-secretase 1 in Human [ChEMBL: CHEMBL4822] [GtoPdb: 2330] [UniProtKB: P56817]
  • This target only has 0 pki data point
5 CHEMBL76_lig_chart_5 Beta-secretase 1 Human
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  • Dihydrofolate reductase in Bovine [ChEMBL: CHEMBL1075051] [UniProtKB: P00376]
  • This target only has 0 pki data point
6 CHEMBL76_lig_chart_6 Dihydrofolate reductase Bovine
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  • Falcipain 2 in Plasmodium falciparum [ChEMBL: CHEMBL1697672] [UniProtKB: Q9NAW2]
  • This target only has 0 pki data point
7 CHEMBL76_lig_chart_7 Falcipain 2 Plasmodium falciparum
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  • Kv11.1/HERG in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
  • This target only has 1 pki data point
8 CHEMBL76_lig_chart_8 HERG Human
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  • Histidine-rich protein in Plasmodium falciparum [ChEMBL: CHEMBL1923] [UniProtKB: P05227]
  • This target only has 0 pki data point
9 CHEMBL76_lig_chart_9 Histidine-rich protein Plasmodium falciparum
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  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
  • This target only has 1 pki data point
10 CHEMBL76_lig_chart_10 Muscarinic acetylcholine receptor M1 Human
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
  • This target only has 1 pki data point
11 CHEMBL76_lig_chart_11 Muscarinic acetylcholine receptor M2 Human
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  • M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
  • This target only has 1 pki data point
12 CHEMBL76_lig_chart_12 Muscarinic acetylcholine receptor M3 Human
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  • M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
  • This target only has 1 pki data point
13 CHEMBL76_lig_chart_13 Muscarinic acetylcholine receptor M4 Human
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  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
  • This target only has 1 pki data point
14 CHEMBL76_lig_chart_14 Muscarinic acetylcholine receptor M5 Human
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  • Plasmodium berghei [ChEMBL: CHEMBL612653]
  • This target only has 0 pki data point
15 CHEMBL76_lig_chart_15 Plasmodium berghei Plasmodium berghei
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  • Plasmodium falciparum [ChEMBL: CHEMBL364]
  • This target only has 0 pki data point
16 CHEMBL76_lig_chart_16 Plasmodium falciparum Plasmodium falciparum
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  • Plasmodium falciparum 3D7 [ChEMBL: CHEMBL2366922]
  • This target only has 0 pki data point
17 CHEMBL76_lig_chart_17 Plasmodium falciparum 3D7 Plasmodium falciparum 3D7
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  • Plasmodium falciparum D6 [ChEMBL: CHEMBL2367107]
  • This target only has 0 pki data point
18 CHEMBL76_lig_chart_18 Plasmodium falciparum D6 Plasmodium falciparum D6
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  • Plasmodium falciparum (isolate FcB1 / Columbia) in Plasmodium falciparum FcB1/Columbia [ChEMBL: CHEMBL612608]
  • This target only has 0 pki data point
19 CHEMBL76_lig_chart_19 Plasmodium falciparum (isolate FcB1 / Columbia) Plasmodium falciparum FcB1/Columbia
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  • Plasmodium falciparum (isolate K1 / Thailand) in Plasmodium falciparum K1 [ChEMBL: CHEMBL612856]
  • This target only has 0 pki data point
20 CHEMBL76_lig_chart_20 Plasmodium falciparum (isolate K1 / Thailand) Plasmodium falciparum K1
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  • Plasmodium falciparum NF54 [ChEMBL: CHEMBL2367131]
  • This target only has 0 pki data point
21 CHEMBL76_lig_chart_21 Plasmodium falciparum NF54 Plasmodium falciparum NF54
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  • Plasmodium knowlesi [ChEMBL: CHEMBL613011]
  • This target only has 0 pki data point
22 CHEMBL76_lig_chart_22 Plasmodium knowlesi Plasmodium knowlesi
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  • Plasmodium malariae [ChEMBL: CHEMBL613257]
  • This target only has 0 pki data point
23 CHEMBL76_lig_chart_23 Plasmodium malariae Plasmodium malariae
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  • Plasmodium vivax [ChEMBL: CHEMBL613013]
  • This target only has 0 pki data point
24 CHEMBL76_lig_chart_24 Plasmodium vivax Plasmodium vivax
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  • Plasmodium yoelii [ChEMBL: CHEMBL612889]
  • This target only has 0 pki data point
25 CHEMBL76_lig_chart_25 Plasmodium yoelii Plasmodium yoelii
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  • Prion protein in Human [ChEMBL: CHEMBL4869] [UniProtKB: P04156]
  • This target only has 0 pki data point
26 CHEMBL76_lig_chart_26 Prion protein Human
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  • Quinone reductase 2 in Human [ChEMBL: CHEMBL3959] [UniProtKB: P16083]
  • This target only has 0 pki data point
27 CHEMBL76_lig_chart_27 Quinone reductase 2 Human
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  • Riboflavin-binding protein in Chicken [ChEMBL: CHEMBL1944489] [UniProtKB: P02752]
  • This target only has 0 pki data point
28 CHEMBL76_lig_chart_28 Riboflavin-binding protein Chicken
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  • σ2/Sigma intracellular receptor 2 in Human [ChEMBL: CHEMBL4105907] [GtoPdb: 2553] [UniProtKB: Q5BJF2]
  • This target only has 1 pki data point
29 CHEMBL76_lig_chart_29 Sigma intracellular receptor 2 Human
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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
  • This target only has 1 pki data point
30 CHEMBL76_lig_chart_30 Sigma opioid receptor Human
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  • MRGPRX1 in Human [GtoPdb: 156] [UniProtKB: Q96LB2]
  • This target only has 0 pki data point
31 CHEMBL76_lig_chart_31 MRGPRX1 Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL Activity of compound against Alpha-2A (ADRA2A) adrenergic receptor by displacement of [3H]-rauwolscine B 5.36 pKi 4365.16 nM Ki A SARS-CoV-2 protein interaction map reveals targets for drug repurposing
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
ChEMBL Activity of compound against Alpha 2B (ADRA2B) adrenergic receptor by displacement of [3H]-rauwolscine B 4.5 pKi 31622.78 nM Ki A SARS-CoV-2 protein interaction map reveals targets for drug repurposing
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
ChEMBL Activity of compound against Alpha 2C (ADRA2C) adrenergic receptor by displacement of [3H]-rauwolscine B 5 pKi 10000 nM Ki A SARS-CoV-2 protein interaction map reveals targets for drug repurposing
Beta amyloid A4 protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2487] [UniProtKB: P05067]
ChEMBL Modulation of human wild-type APP695 expressed in SH-SY5Y cells assessed as inhibition of amyloid beta (1 to 42 residues) production measured after 24 hrs by ELISA B 4.89 pIC50 12800 nM IC50 Bioorg Med Chem (2018) 26: 2151-2164 [PMID:29559198]
ChEMBL Modulation of human wild-type APP695 expressed in SH-SY5Y cells assessed as inhibition of amyloid beta (1 to 40 residues) production measured after 24 hrs B 5.15 pIC50 7000 nM IC50 Bioorg Med Chem (2018) 26: 2151-2164 [PMID:29559198]
beta-secretase 1/Beta-secretase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4822] [GtoPdb: 2330] [UniProtKB: P56817]
ChEMBL Inhibition of BACE1 in human SH-SY5Y cells harboring wild type APP695 assessed as reduction in amyloid beta (1 to 42) level after 24 hrs by ELISA method B 4.9 pIC50 12700 nM IC50 Eur J Med Chem (2018) 159: 104-125 [PMID:30268822]
ChEMBL Inhibition of BACE1 in human SH-SY5Y cells harboring wild type APP695 assessed as reduction in amyloid beta (1 to 40) level after 24 hrs by ELISA method B 5.15 pIC50 7000 nM IC50 Eur J Med Chem (2018) 159: 104-125 [PMID:30268822]
Dihydrofolate reductase in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075051] [UniProtKB: P00376]
ChEMBL Inhibition of bovine liver DHFR B 7.52 pIC50 30.1 nM IC50 Bioorg Med Chem (2017) 25: 5396-5406 [PMID:28789907]
ChEMBL Inhibition of bovine liver DHFR pre-incubated 2 mins before dihydrofolic acid substrate addition and measured over 10 mins in presence of NADPH B 7.52 pIC50 30.1 nM IC50 Bioorg Med Chem (2017) 25: 4064-4075 [PMID:28634040]
Falcipain 2 in Plasmodium falciparum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1697672] [UniProtKB: Q9NAW2]
ChEMBL Inhibition of falcipain-2 in chloroquine resistant Plasmodium falciparum RKL9 schizont stage infected in human erythrocytes assessed as reduction in bacterial growth after 24 hrs by Giemsa staining based assay B 6.7 pIC50 200 nM IC50 Bioorg Med Chem Lett (2018) 28: 1566-1569 [PMID:29602682]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG expressed in CHO cells B 5.12 pKi 7500 nM Ki ACS Med. Chem. Lett. (2013) 4: 1037-1041 [PMID:24900603]
ChEMBL Inhibition of human ERG B 5.6 pIC50 2511.89 nM IC50 Eur. J. Med. Chem. (2011) 46: 618-630 [PMID:21185626]
ChEMBL Inhibitory concentration against IKr potassium channel B 5.6 pIC50 2500 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 4771-4777 [PMID:15324906]
ChEMBL Inhibition of human cloned ERG B 5.6 pIC50 2500 nM IC50 J. Med. Chem. (2009) 52: 1408-1415 [PMID:19222165]
ChEMBL Inhibition of human ERG expressed in HEK293 cells assessed as reduction in tail current at membrane potential of +20 mV B 5.6 pIC50 2500 nM IC50 Bioorg. Med. Chem. Lett. (2015) 25: 1390-1393 [PMID:25746816]
Histidine-rich protein in Plasmodium falciparum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1923] [UniProtKB: P05227]
ChEMBL Inhibition of 1-monooleoyl glycerol (MOG) induced beta-hematin formation F 4.12 pIC50 76500 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 3783-3787 [PMID:14552779]
ChEMBL Inhibition of beta-hematin formation in Plasmodium falciparum F 4.12 pIC50 75000 nM IC50 Bioorg. Med. Chem. Lett. (2001) 11: 2075-2077 [PMID:11514142]
ChEMBL Inhibition of 1-monooleoyl glycerol induced beta-hematin formation F 4.22 pIC50 60000 nM IC50 Bioorg. Med. Chem. Lett. (2006) 16: 31-35 [PMID:16263280]
ChEMBL Inhibition of lipid-induced beta-hematin formation F 4.33 pIC50 46300 nM IC50 J. Med. Chem. (2006) 49: 4707-4714 [PMID:16854077]
ChEMBL Inhibition of beta-hematin formation F 4.42 pIC50 38000 nM IC50 J. Med. Chem. (2002) 45: 4975-4983 [PMID:12408708]
ChEMBL Inhibition of beta-hematin formation after 16 hrs F 4.81 pIC50 15400 nM IC50 Antimicrob. Agents Chemother. (2007) 51: 2842-2847 [PMID:17562796]
ChEMBL Inhibition of hematin polymerization F 4.82 pIC50 15000 nM IC50 J. Med. Chem. (1999) 42: 4630-4639 [PMID:10579825]
ChEMBL Inhibition of beta-hematin polymerization B 6.4 pIC50 400 nM IC50 J. Med. Chem. (2007) 50: 394-398 [PMID:17228883]
ChEMBL Inhibitory activity against beta-hematin formation F 7.12 pIC50 76.5 nM IC50 J. Med. Chem. (2003) 46: 542-557 [PMID:12570376]
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
ChEMBL Activity of compound against Muscarinic acetylcholine receptor M1 (CHRM1) by displacement of 3H-QNB B 5.04 pKi 9120.11 nM Ki A SARS-CoV-2 protein interaction map reveals targets for drug repurposing
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL Activity of compound against Muscarinic acetylcholine receptor M2 (CHRM2) by displacement of 3H-QNB B 5.33 pKi 4677.35 nM Ki A SARS-CoV-2 protein interaction map reveals targets for drug repurposing
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
ChEMBL Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB B 5.48 pKi 3311.31 nM Ki A SARS-CoV-2 protein interaction map reveals targets for drug repurposing
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
ChEMBL Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNB B 5.24 pKi 5754.4 nM Ki A SARS-CoV-2 protein interaction map reveals targets for drug repurposing
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
ChEMBL Activity of compound against Muscarinic acetylcholine receptor M5 (CHRM5) by displacement of 3H-QNB B 4.66 pKi 21877.62 nM Ki A SARS-CoV-2 protein interaction map reveals targets for drug repurposing
Plasmodium berghei (target type: ORGANISM) [ChEMBL: CHEMBL612653]
ChEMBL Antiplasmodial activity against Plasmodium berghei liver stage form transfected in human Huh-7 cells assessed as cell viability after 48 hrs by luciferase reporter gene assay F 4.8 pIC50 15900 nM IC50 J. Med. Chem. (2013) 56: 556-567 [PMID:23273038]
ChEMBL Antiplasmodial activity against liver stage of Plasmodium berghei expressing GFP-Luc infected in HuH7 cells incubated at 1 hr prior to infection followed by compound replenisment at 24 hrs post-infection measured after 48 hrs by Alamar blue assay F 4.82 pIC50 >15000 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 610-613 [PMID:23290049]
ChEMBL Antimalarial activity against exo-erythrocytic form of Plasmodium berghei infected in human HepG2 cells after 48 hrs F 5 pIC50 >10000 nM IC50 Eur. J. Med. Chem. (2014) 82: 204-213 [PMID:24904967]
ChEMBL Antimalarial activity against sporozoite stage of Plasmodium berghei yoelii infected in human HepG2 cells F 5.05 pIC50 9000 nM IC50 J. Med. Chem. (2016) 59: 264-281 [PMID:26640981]
ChEMBL Antimalarial activity against schizonts of chloroquine-sensitive Plasmodium berghei ANKA 2.34 after 16 hrs F 7.22 pIC50 60 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 7048-7051 [PMID:23084276]
ChEMBL Antimicrobial activity against Plasmodium berghei sporozoites infected in 12 hrs compound pretreated human HepG2 cells assessed as reduction in viability of exoerythrocytic forms measured after 48 hrs of incubation by luciferase bioluminescence assay F 5 pEC50 >10000 nM EC50 J. Med. Chem. (2014) 57: 2773-2788 [PMID:24641010]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Inhibition of hematin polymerization in Plasmodium falciparum F 4.1 pIC50 80000 nM IC50 J. Med. Chem. (1998) 41: 4360-4364 [PMID:9784111]
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 4.22 pIC50 60000 nM IC50 J. Med. Chem. (2013) 56: 6200-6215 [PMID:23837878]
ChEMBL Inhibition of hydrogen peroxide-mediated haem detoxification in Plasmodium falciparum F 4.43 pIC50 37000 nM IC50 Bioorg. Med. Chem. Lett. (2001) 11: 2075-2077 [PMID:11514142]
ChEMBL Antimalarial activity after 72 hrs against chloroquine-sensitive Plasmodium falciparum D6 infected in erythrocytes by LDH assay F 4.53 pIC50 29700 nM IC50 Bioorg. Med. Chem. (2009) 17: 741-751 [PMID:19084416]
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in erythrocytes after 96 hrs by [3H]hypoxanthine incorporation assay F 4.68 pIC50 21000 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 4.72 pIC50 19000 nM IC50 J. Med. Chem. (2009) 52: 7954-7957 [PMID:19908867]
ChEMBL Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum NF54 by lactate dehydrogenase assay F 4.79 pIC50 16300 nM IC50 J Nat Prod (2018) 81: 41-48 [PMID:29309141]
ChEMBL Antimalarial activity against Plasmodium falciparum 3D7 infected in human O positive erythrocytes assessed as reduction of parasite growth after 24 to 44 hrs by Giemsa staining F 4.82 pIC50 15000 nM IC50 Eur. J. Med. Chem. (2013) 67: 158-165 [PMID:23851117]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum K14 infected in human red blood cells after 48 hrs by [3H]hypoxanthine incorporation assay F 4.96 pIC50 11000 nM IC50 Eur. J. Med. Chem. (2014) 87: 364-371 [PMID:25282260]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 gametocytes (stage 4 & 5) F 4.97 pIC50 10700 nM IC50 Antimicrob. Agents Chemother. (2007) 51: 1463-1472 [PMID:17242150]
ChEMBL Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by 1536-well format based SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay F 5.26 pIC50 5500 nM IC50 Eur. J. Med. Chem. (2013) 60: 497-502 [PMID:23354072]
ChEMBL In vitro inhibitory activity against Plasmodium falciparum F 5.52 pIC50 3000 nM IC50 Bioorg. Med. Chem. Lett. (2001) 11: 1851-1854 [PMID:11459645]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by 1536-well format based SYBR green assay F 5.7 pIC50 2000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
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 5.74 pIC50 1828 nM IC50 Eur J Med Chem (2017) 140: 595-603 [PMID:28988153]
ChEMBL Displacement of chloroquine from Fe(3+) FPIX-loaded membrane F 5.75 pIC50 1760 nM IC50 J. Med. Chem. (2002) 45: 4975-4983 [PMID:12408708]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by 1536-well format based SYBR green assay F 5.8 pIC50 1600 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by 1536-well format based SYBR green assay F 5.8 pIC50 1600 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antimalarial activity against Plasmodium falciparum infected in human O+ erythrocytes after 48 hrs by HRP2-ELISA method F 5.99 pIC50 1030 nM IC50 Bioorg. Med. Chem. (2010) 18: 5626-5633 [PMID:20621497]
ChEMBL Antimalarial activity against Plasmodium falciparum V1/S infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation preincubated for 24 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by scintillation counting method F 6 pIC50 >1000 nM IC50 J Med Chem (2017) 60: 5889-5908 [PMID:28635296]
ChEMBL Antimalarial activity against chloroquine and pyrimethamine-resistant Plasmodium falciparum W2 assessed as inhibition of parasite growth F 6 pIC50 >1000 nM IC50 J. Med. Chem. (2015) 58: 4573-4580 [PMID:25906200]
ChEMBL Antimicrobial activity against Plasmodium falciparum F 6 pIC50 1000 nM IC50 Bioorg. Med. Chem. (2010) 18: 2225-2231 [PMID:20185316]
ChEMBL Antimalarial activity against chloroquine and pyrimethamine-resistant Plasmodium falciparum V1/S assessed as inhibition of parasite growth F 6 pIC50 >1000 nM IC50 J. Med. Chem. (2015) 58: 4573-4580 [PMID:25906200]
ChEMBL Antimalarial activity against chloroquine, pyrimethamine, and mefloquine-resistant Plasmodium falciparum Dd2 infected in human O positive red blood cells assessed as inhibition of [3H]-hypoxanthine uptake after 48 hrs F 6.01 pIC50 980 nM IC50 J. Nat. Prod. (2011) 74: 74-78 [PMID:21155593]
ChEMBL Inhibition of chloroquine uptake from intact parasites F 6.02 pIC50 950 nM IC50 J. Med. Chem. (2002) 45: 4975-4983 [PMID:12408708]
ChEMBL In vitro inhibitory activity against multidrug-resistant Plasmodium falciparum W2 Indochina F 6.05 pIC50 900 nM IC50 J. Med. Chem. (2002) 45: 3195-3209 [PMID:12109904]
ChEMBL Antiplasmodial activity against chloroquine-susceptible Plasmodium falciparum FCM29 infected in human erythrocytes assessed as inhibition of [3H]hypoxanthine uptake after 48 hrs F 6.06 pIC50 879 nM IC50 J. Med. Chem. (2010) 53: 3214-3226 [PMID:20329733]
ChEMBL Antimalarial activity against chloroquine, pyrimethamine and cycloguanil-resistant Plasmodium falciparum VS1 after 24 hrs F 6.07 pIC50 860 nM IC50 Bioorg. Med. Chem. (2007) 15: 5551-5562 [PMID:17548196]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 asynchronous cultures infected in human erythrocytes measured after 72 hrs by SYBR Green1 dye based fluorescence assay F 6.08 pIC50 830 nM IC50 MedChemComm (2018) 9: 1232-1238
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 by pLDH assay F 6.09 pIC50 810 nM IC50 J. Med. Chem. (2006) 49: 7088-7094 [PMID:17125261]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 infected in human erythrocytes assessed as inhibition of parasite growth after 24 hrs by [3H]hypoxanthine incorporation assay F 6.11 pIC50 780 nM IC50 Eur. J. Med. Chem. (2013) 62: 168-176 [PMID:23353738]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 after 48 to 72 hrs by SYBR green-1 assay F 6.12 pIC50 750 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 6167-6171 [PMID:24080459]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 infected in human RBC assessed as parasite growth inhibition measured as LDH activity after 72 hrs by plate reader analysis F 6.14 pIC50 720 nM IC50 Eur. J. Med. Chem. (2015) 98: 160-169 [PMID:26005918]
ChEMBL Antimicrobial activity against Plasmodium falciparum W2 after 72 hrs by LDH activity assay F 6.14 pIC50 720 nM IC50 MedChemComm (2013) 4: 1042-1048
ChEMBL Antiplasmodial activity against Plasmodium falciparum Dd2 assessed as inhibition of [3H]hypoxanthine incorporation incubated for 24 hrs prior to [3H]hypoxanthine addition measured after 24 hrs by beta scintillation counting F 6.15 pIC50 710 nM IC50 ACS Med. Chem. Lett. (2012) 3: 373-377 [PMID:24900481]
ChEMBL Antiplasmodial activity against drug resistant Plasmodium falciparum Dd2 ring stage cells assessed as reduction parasitemia by Malstat assay F 6.15 pIC50 710 nM IC50 Bioorg. Med. Chem. (2012) 20: 5277-5289 [PMID:22858300]
ChEMBL Antimalarial activity against chloroquine, pyrimethamine, proguanil-resistant Plasmodium falciparum infected in human erythrocytes after 48 hrs by flow cytometry F 6.15 pIC50 700 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 5962-5964 [PMID:19748781]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 infected in human erythrocyte after 48 hrs by flow cytometry