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

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ChEMBL ligand: CHEMBL76 (Chloroquine, Chlorochine, NSC-187208, Aralen)
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  • beta-secretase 1/Beta-secretase 1 in Human [ChEMBL: CHEMBL4822] [GtoPdb: 2330] [UniProtKB: P56817]
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  • Histidine-rich protein in Plasmodium falciparum [ChEMBL: CHEMBL1923] [UniProtKB: P05227]
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  • Plasmodium falciparum (isolate FcB1 / Columbia) in Plasmodium falciparum FcB1/Columbia [ChEMBL: CHEMBL612608]
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  • Plasmodium falciparum (isolate K1 / Thailand) in Plasmodium falciparum K1 [ChEMBL: CHEMBL612856]
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  • MRGPRX1 in Human [GtoPdb: 156] [UniProtKB: Q96LB2]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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]
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 F 6.15 pIC50 700 nM IC50 Eur. J. Med. Chem. (2010) 45: 616-622 [PMID:19926173]
ChEMBL Antiplasmodial activity against chloroquinone-resistant Plasmodium falciparum W2 F 6.15 pIC50 700 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 396-401 [PMID:17981462]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 infected in human A+ erythrocytes assessed as inhibition of parasite proliferation after 48 hrs F 6.15 pIC50 700 nM IC50 Bioorg. Med. Chem. (2010) 18: 6012-6023 [PMID:20638854]
ChEMBL Antimalarial activity as reduced parasitaemia after 48 hrs against chloroquine, pyrimethamine and proguanil-resistant Plasmodium falciparum W2 infected in type A+ human erythrocytes by flow cytometry F 6.15 pIC50 700 nM IC50 Bioorg. Med. Chem. (2009) 17: 4313-4322 [PMID:19482476]
ChEMBL Antiplasmodial activity against multidrug-resistant Plasmodium falciparum W2 infected human erythrocytes after 48 hrs by flow cytometry F 6.15 pIC50 700 nM IC50 Eur. J. Med. Chem. (2010) 45: 864-869 [PMID:19914747]
ChEMBL Antimalarial activity against Plasmodium falciparum Dd2 infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation preincubated for 24 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by scintillation counting method F 6.16 pIC50 690 nM IC50 J Med Chem (2017) 60: 5889-5908 [PMID:28635296]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 infected in human RBCs after 72 hrs by parasite lactate dehydrogenase assay F 6.17 pIC50 681 nM IC50 J. Med. Chem. (2012) 55: 10387-10404 [PMID:23145816]
ChEMBL Antimalarial activity against Plasmodium falciparum IMT K14 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter F 6.18 pIC50 665 nM IC50 Antimicrob. Agents Chemother. (2010) 54: 3537-3544 [PMID:20547801]
ChEMBL Antiplasmodial activity against chloroquine-susceptible Plasmodium falciparum K14 infected in human erythrocytes assessed as inhibition of [3H]hypoxanthine uptake after 48 hrs F 6.19 pIC50 648.6 nM IC50 J. Med. Chem. (2010) 53: 3214-3226 [PMID:20329733]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum FCR3 F 6.19 pIC50 645 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 6434-6438 [PMID:17949976]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 assessed as inhibition of parasite LDH activity after 72 hrs by spectrophotometry F 6.2 pIC50 632 nM IC50 Eur. J. Med. Chem. (2011) 46: 1757-1767 [PMID:21396743]
ChEMBL Antimicrobial activity against chloroquine-sensitive Plasmodium falciparum W2 by ELISA F 6.2 pIC50 630.6 nM IC50 Antimicrob. Agents Chemother. (2010) 54: 1200-1206 [PMID:20065051]
ChEMBL Antimalarial activity against chloroquine-resistant/mefloquine-sensitive Plasmodium falciparum W2 by malaria SYBR green 1-based fluorescence (MSF) assay F 6.2 pIC50 630 nM IC50 Bioorg. Med. Chem. Lett. (2015) 25: 327-332 [PMID:25488841]
ChEMBL Antimalarial activity against multidrug-resistant Plasmodium falciparum TM93-C1088 infected in human O positive red blood cells assessed as inhibition of [3H]-hypoxanthine uptake after 48 hrs F 6.21 pIC50 620 nM IC50 J. Nat. Prod. (2011) 74: 74-78 [PMID:21155593]
ChEMBL Antimalarial activity against Plasmodium falciparum W2 F 6.21 pIC50 616.94 nM IC50 J. Med. Chem. (2008) 51: 2261-2266 [PMID:18330976]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum FcM29 by [3H]hypoxanthine uptake F 6.22 pIC50 600 nM IC50 J. Nat. Prod. (2008) 71: 1189-1192 [PMID:18512987]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum indochina W2 assessed as [3H]-hypoxanthine incorporation by liquid scintillation counting analysis F 6.23 pIC50 595 nM IC50 Bioorg. Med. Chem. (2015) 23: 2176-2186 [PMID:25801154]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 infected in human red blood cells after 48 hrs by SYBR test F 6.23 pIC50 590 nM IC50 Bioorg. Med. Chem. Lett. (2016) 26: 1881-1884 [PMID:26988303]
ChEMBL In vitro inhibitory activity against Plasmodium falciparum NF54-R in blood F 6.24 pIC50 570 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 2773-2776 [PMID:15125930]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 infected in human erythrocytes measured after 72 hrs by malstat reagent based LDH release assay F 6.24 pIC50 570 nM IC50 ACS Med Chem Lett (2018) 9: 980-985 [PMID:30344903]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 infected in human A+ erythrocytes assessed as inhibition of [3H]hypoxanthine uptake after 48 hrs by scintillation counting F 6.25 pIC50 563 nM IC50 Bioorg. Med. Chem. (2010) 18: 8085-8091 [PMID:20934349]
ChEMBL Antimalarial activity against Plasmodium falciparum TM90C2B infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation preincubated for 24 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by scintillation counting method F 6.25 pIC50 561 nM IC50 J Med Chem (2017) 60: 5889-5908 [PMID:28635296]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 asexual gametocytes F 6.25 pIC50 560 nM IC50 Antimicrob. Agents Chemother. (2007) 51: 1463-1472 [PMID:17242150]
ChEMBL Antimalarial activity against Plasmodium falciparum W2 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter F 6.25 pIC50 556 nM IC50 Antimicrob. Agents Chemother. (2010) 54: 3537-3544 [PMID:20547801]
ChEMBL Antimalarial activity against chloroquine/sulfadoxine-resistant Plasmodium falciparum W2 infected in human A+ erythrocytes assessed as reduction in parasite growth after 72 hrs by HRP2 detection based ELISA F 6.26 pIC50 550 nM IC50 Bioorg. Med. Chem. (2016) 24: 4492-4498 [PMID:27485600]
ChEMBL Antimalarial activity against Plasmodium falciparum K1 infected in human erythrocytes after 72 hrs by lactate dehydrogenase assay F 6.27 pIC50 540 nM IC50 J Nat Prod (2017) 80: 3120-3127 [PMID:29182338]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 after 24 hrs by [G-3H]-hypoxanthine incorporation assay F 6.27 pIC50 540 nM IC50 Eur J Med Chem (2017) 139: 22-47 [PMID:28800458]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum PFB Brazil by [3H]hypoxanthine uptake F 6.27 pIC50 540 nM IC50 J. Nat. Prod. (2001) 64: 12-16 [PMID:11170658]
ChEMBL Growth inhibition of chloroquine-resistant Plasmodium falciparum KI F 6.27 pIC50 540 nM IC50 Bioorg. Med. Chem. Lett. (2001) 11: 2075-2077 [PMID:11514142]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 F 6.27 pIC50 540 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 6434-6438 [PMID:17949976]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum D10 F 6.27 pIC50 540 nM IC50 Eur. J. Med. Chem. (2010) 45: 3245-3264 [PMID:20466465]
ChEMBL Antimalarial activity against Plasmodium falciparum IMT Bres assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter F 6.27 pIC50 538 nM IC50 Antimicrob. Agents Chemother. (2010) 54: 3537-3544 [PMID:20547801]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 by LDH assay F 6.28 pIC50 530 nM IC50 MedChemComm (2013) 4: 724-730
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 infected in human erythrocytes assessed as inhibition of [3H]hypoxanthine uptake after 48 hrs F 6.28 pIC50 527 nM IC50 J. Med. Chem. (2010) 53: 3214-3226 [PMID:20329733]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 assessed as growth inhibition after 18 hrs by [3H]-hypoxanthine uptake assay F 6.28 pIC50 525 nM IC50 J. Med. Chem. (2015) 58: 3411-3431 [PMID:25654185]
ChEMBL Antimalarial activity against Plasmodium falciparum IMT A4 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter F 6.28 pIC50 525 nM IC50 Antimicrob. Agents Chemother. (2010) 54: 3537-3544 [PMID:20547801]
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum IMT K2 infected in erythrocytes after 48 hrs by [3H]hypoxanthine incorporation assay F 6.28 pIC50 523 nM IC50 J. Med. Chem. (2009) 52: 7954-7957 [PMID:19908867]
ChEMBL Antimalarial activity against Plasmodium falciparum IMT K2 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter F 6.28 pIC50 523 nM IC50 Antimicrob. Agents Chemother. (2010) 54: 3537-3544 [PMID:20547801]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Bre1 assessed as inhibition of [3H]hypoxanthine incorporation F 6.28 pIC50 520 nM IC50 Bioorg. Med. Chem. (2009) 17: 8032-8039 [PMID:19879150]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum Bre1 by hypoxanthine uptake F 6.28 pIC50 520 nM IC50 Bioorg. Med. Chem. (2007) 15: 3278-3289 [PMID:17339112]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 F 6.28 pIC50 520 nM IC50 J Nat Prod (2017) 80: 134-140 [PMID:28055207]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 infected in human type A-positive red blood cells assessed as parasite lactate dehydrogenase activity after 72 hrs by spectrophotometric analysis F 6.28 pIC50 520 nM IC50 J. Med. Chem. (2011) 54: 8526-8540 [PMID:22054038]
ChEMBL Antiparasitic activity against chloroquine-resistant Plasmodium falciparum K1 F 6.28 pIC50 519.3 nM IC50 J. Med. Chem. (2008) 51: 1260-1277 [PMID:18260613]
ChEMBL Antimalarial activity against schizont stage of chloroquine-resistant Plasmodium falciparum W2 infected in erythrocytes assessed as inhibition of [3H]hypoxanthine incorporation after 48 hrs by scintillation counting analysis F 6.28 pIC50 519 nM IC50 MedChemComm (2011) 2: 430-435
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum FCM29 infected in erythrocytes after 48 hrs by [3H]hypoxanthine incorporation assay F 6.29 pIC50 508 nM IC50 J. Med. Chem. (2009) 52: 7954-7957 [PMID:19908867]
ChEMBL Antimalarial activity against Plasmodium falciparum FCM29 assessed as inhibition of [3H] incorporation after 48 hrs by scintillation counter F 6.29 pIC50 508 nM