primaquine [Ligand Id: 9952] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL506 (Primaquine)
  • Chloroquine resistance transporter in Plasmodium falciparum [ChEMBL: CHEMBL1795182] [UniProtKB: Q9N623]
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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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  • SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Chloroquine resistance transporter in Plasmodium falciparum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795182] [UniProtKB: Q9N623]
ChEMBL Inhibition of chloroquine-resistant Plasmodium falciparum Dd2 CRT expressed in Xenopus laevis oocytes plasma membrane assessed as reduction of [3H]-chloroquine transportation after 1 to 2 hrs B 4.17 pIC50 68000 nM IC50 ACS Med. Chem. Lett. (2014) 5: 576-581 [PMID:24900883]
CYP1A2/Cytochrome P450 1A2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3356] [GtoPdb: 1319] [UniProtKB: P05177]
ChEMBL DRUGMATRIX: CYP450, 1A2 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) B 6.74 pIC50 182.4 nM IC50 DrugMatrix in vitro pharmacology data
Monoamine oxidase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1951] [GtoPdb: 2489] [UniProtKB: P21397]
ChEMBL Inhibition of human recombinant MAOA assessed as conversion of kynuramine to 4-hydroxyquinoline preincubated for 15 mins by fluorimetric assay B 4.12 pIC50 75700 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 1701-1704 [PMID:22264472]
Monoamine oxidase B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2039] [GtoPdb: 2490] [UniProtKB: P27338]
ChEMBL Inhibition of human recombinant MAOB assessed as conversion of kynuramine to 4-hydroxyquinoline preincubated for 15 mins by fluorimetric assay B 4.02 pIC50 94500 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 1701-1704 [PMID:22264472]
Plasmodium berghei (target type: ORGANISM) [ChEMBL: CHEMBL612653]
ChEMBL Antimalarial activity against liver stages of Plasmodium berghei F 4.89 pIC50 13000 nM IC50 J. Med. Chem. (2012) 55: 995-1012 [PMID:22122518]
ChEMBL Antiplasmodial activity against liver stage Plasmodium berghei infected in Huh7 cells assessed as inhibition of parasite infection incubated for 1 hr prior to infection measured at 24 hrs by luciferase reporter gene assay F 5.02 pIC50 9500 nM IC50 Bioorg. Med. Chem. (2016) 24: 1786-1792 [PMID:26968650]
ChEMBL Antiplasmodial activity against liver-stage of Plasmodium berghei expressing firefly luciferase infected in human Huh-7 cells after 48 hrs by bioluminescence assay F 5.07 pIC50 8428 nM IC50 Eur. J. Med. Chem. (2015) 101: 266-273 [PMID:26142491]
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 5.1 pIC50 8000 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 610-613 [PMID:23290049]
ChEMBL Antiplasmodial activity against liver stage of Plasmodium berghei expressing GFP infected in human Huh7 cells by luminescence assay F 5.12 pIC50 7500 nM IC50 J. Nat. Prod. (2013) 76: 1064-1070 [PMID:23806111]
ChEMBL Antiplasmodial activity against liver sporozoite stage of Plasmodium berghei expressing luciferase and GFP infected in human HuH7 cells assessed as inhibition of parasite development incubated for 1 hr prior to parasite infection measured after 48 hrs by Alamar blue assay F 5.12 pIC50 7500 nM IC50 Eur. J. Med. Chem. (2013) 69: 872-880 [PMID:24125849]
ChEMBL Antimalarial activity against liver stage of Plasmodium berghei infected in human Huh7 cells after 48 hrs by luciferase assay F 5.12 pIC50 7500 nM IC50 ACS Med. Chem. Lett. (2014) 5: 108-112 [PMID:24900781]
ChEMBL Antiplasmodial activity against liver stage of Plasmodium berghei sporozoites expressing firefly luciferase infected in human Huh7 cells assessed as inhibition of parasite development treated 1 hr prior to infection followed by compound replenisment at 24 hrs post-infection measured 48 hrs after infection by bioluminescence analysis F 5.12 pIC50 7500 nM IC50 MedChemComm (2012) 3: 1170-1172
ChEMBL Antimalarial activity against Plasmodium berghei infected in human HuH7 cells assessed as inhibition of liver cell infection F 5.12 pIC50 7500 nM IC50 Bioorg. Med. Chem. (2015) 23: 5098-5119 [PMID:25593097]
ChEMBL Antiplasmodial activity against liver stage of Plasmodium berghei infected in human HuH7 cells assessed as parasite growth inhibition incubated for 1 hr prior to parasite infection measured after 48 hrs F 5.12 pIC50 7500 nM IC50 J. Med. Chem. (2013) 56: 7679-7690 [PMID:24020770]
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 5.12 pIC50 7500 nM IC50 J. Med. Chem. (2013) 56: 556-567 [PMID:23273038]
ChEMBL Antiplasmodial activity against liver stage Plasmodium berghei infected in human HuH7 cells co-expressing GFP-Luccon treated for 1 hr prior to infection followed by 24 hrs after compound washout measured after 48 hrs post-infection by Alamar Blue assay F 5.12 pIC50 7500 nM IC50 J. Med. Chem. (2013) 56: 4811-4815 [PMID:23701465]
ChEMBL Antiplasmodial activity against liver stage of Plasmodium berghei ANKA infected in human HepG2 cells F 5.12 pIC50 7500 nM IC50 J. Nat. Prod. (2013) 76: 1064-1070 [PMID:23806111]
ChEMBL Antiplasmodial activity against liver-stage GFP expressing Plasmodium berghei sporozoites infected in human HuH7 cells assessed as inhibition of parasite schizonts development after 48 hrs by FACS analysis F 5.7 pIC50 2000 nM IC50 J. Med. Chem. (2009) 52: 7800-7807 [PMID:19799426]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 F 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 6101-6106 [PMID:17900897]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 gametocytes after 48 hrs by microscopy F 5.02 pIC50 9650 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 4666-4669 [PMID:18653332]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 after 48 hrs by [3H]hypoxanthine uptake F 5.11 pIC50 7700 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 4666-4669 [PMID:18653332]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum FcM29 after 48 hrs by [3H]hypoxanthine uptake F 5.14 pIC50 7250 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 4666-4669 [PMID:18653332]
ChEMBL Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum F32 after 48 hrs by [3H]hypoxanthine uptake F 5.17 pIC50 6830 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 4666-4669 [PMID:18653332]
ChEMBL Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum F32 after 48 hrs F 5.17 pIC50 6830 nM IC50 Eur. J. Med. Chem. (2010) 45: 2854-2859 [PMID:20362359]
ChEMBL Antimalarial activity against asexual stage of Plasmodium falciparum 3D7 after 72 hrs by image-based HTS assay F 5.22 pIC50 6090 nM IC50 J. Med. Chem. (2013) 56: 7727-7740 [PMID:23927763]
ChEMBL Antimalarial activity against early (1 to 3) gametocytic stage of Plasmodium falciparum after 72 hrs by image-based HTS assay F 5.23 pIC50 5860 nM IC50 J. Med. Chem. (2013) 56: 7727-7740 [PMID:23927763]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 gametocytes (stage 2 & 3) F 5.34 pIC50 4580 nM IC50 Antimicrob. Agents Chemother. (2007) 51: 1463-1472 [PMID:17242150]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 F 5.48 pIC50 3340 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 485-488 [PMID:18077165]
ChEMBL Antiplasmodial activity against chloroquine-resistant blood stage Plasmodium falciparum W2 after 48 hrs by FACS analysis F 5.48 pIC50 3300 nM IC50 J. Med. Chem. (2009) 52: 7800-7807 [PMID:19799426]
ChEMBL Antimalarial activity against chloroquine-resistant erythrocyte stage of Plasmodium falciparum W2 after 48 hrs F 5.48 pIC50 3300 nM IC50 ACS Med. Chem. Lett. (2014) 5: 108-112 [PMID:24900781]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 F 5.48 pIC50 3300 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 4150-4153 [PMID:18539459]
ChEMBL Antimalarial activity against Plasmodium falciparum KT3 gametocytes F 5.68 pIC50 2100 nM IC50 J. Med. Chem. (2012) 55: 10328-10344 [PMID:23075290]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 infected in human red blood cells after 48 hrs by SYBR test F 5.72 pIC50 1890 nM IC50 Bioorg. Med. Chem. Lett. (2016) 26: 1881-1884 [PMID:26988303]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 gametocytes (stage 4 & 5) F 5.81 pIC50 1540 nM IC50 Antimicrob. Agents Chemother. (2007) 51: 1463-1472 [PMID:17242150]
ChEMBL Antimalarial activity against multidrug-resistant Plasmodium falciparum W2 by SYBR green-based assay F 5.83 pIC50 1470 nM IC50 Bioorg. Med. Chem. Lett. (2015) 25: 1100-1103 [PMID:25650255]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 asexual gametocytes F 5.88 pIC50 1320 nM IC50 Antimicrob. Agents Chemother. (2007) 51: 1463-1472 [PMID:17242150]
ChEMBL Antimalarial activity against Plasmodium falciparum KT1 gametocytes F 6.1 pIC50 800 nM IC50 J. Med. Chem. (2012) 55: 10328-10344 [PMID:23075290]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 by [3H]hypoxanthine incorporation assay F 6.49 pIC50 326 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 3131-3134 [PMID:19364853]
ChEMBL Antiplasmodial activity against multidrug-resistant Plasmodium falciparum VS/1 by [3H]hypoxanthine incorporation assay F 6.49 pIC50 326 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 3131-3134 [PMID:19364853]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 gametocytes assessed as suppression of parasitemia after 4 hrs by Giemsa staining F 8.05 pIC50 8.9 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 4393-4398 [PMID:19667291]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 assessed as suppression of parasitemia after 4 hrs by Giemsa staining F 8.15 pIC50 7.14 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 4393-4398 [PMID:19667291]
ChEMBL Antiplasmodial activity against Plasmodium falciparum F32 assessed as suppression of parasitemia after 4 hrs by Giemsa staining F 8.21 pIC50 6.17 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 4393-4398 [PMID:19667291]
Plasmodium falciparum 3D7 (target type: ORGANISM) [ChEMBL: CHEMBL2366922]
ChEMBL Antimicrobial activity against chloroquine-sensitive Plasmodium falciparum 3D7 F 6.34 pIC50 460 nM IC50 Eur. J. Med. Chem. (2015) 90: 280-295 [PMID:25461328]
Plasmodium falciparum (isolate FcB1 / Columbia) in Plasmodium falciparum FcB1/Columbia (target type: ORGANISM) [ChEMBL: CHEMBL612608]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum FcB1 after 48 hrs by [3H]hypoxanthine uptake F 5.16 pIC50 6870 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 4666-4669 [PMID:18653332]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum FcB1/Columbia after 48 hrs F 5.16 pIC50 6870 nM IC50 Eur. J. Med. Chem. (2010) 45: 2854-2859 [PMID:20362359]
ChEMBL Antiplasmodial activity against Plasmodium falciparum FcB1/Columbia assessed as suppression of parasitemia after 4 hrs by Giemsa staining F 8.05 pIC50 8.9 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 4393-4398 [PMID:19667291]
Plasmodium falciparum (isolate K1 / Thailand) in Plasmodium falciparum K1 (target type: ORGANISM) [ChEMBL: CHEMBL612856]
ChEMBL Antimalarial activity against Plasmodium falciparum K1 assessed as inhibition of [3H] hypoxanthine uptake by liquid scintillation counting F 6.19 pIC50 643 nM IC50 ACS Med. Chem. Lett. (2013) 4: 128-131 [PMID:24900574]
ChEMBL Antimicrobial activity against chloroquine-resistant Plasmodium falciparum K1 F 6.34 pIC50 460 nM IC50 Eur. J. Med. Chem. (2015) 90: 280-295 [PMID:25461328]
Plasmodium falciparum NF54 (target type: ORGANISM) [ChEMBL: CHEMBL2367131]
ChEMBL Antiplasmodial activity against blood stage of chloroquine-sensitive Plasmodium falciparum NF54 by parasite lactate dehydrogenase assay F 6.05 pIC50 892 nM IC50 Eur. J. Med. Chem. (2015) 101: 266-273 [PMID:26142491]
Plasmodium yoelii (target type: ORGANISM) [ChEMBL: CHEMBL612889]
ChEMBL Antiplasmodial activity against liver stage of Plasmodium yoelii 17X NL sporozoites infected in human HepG2 cells expressing CD81 after 48 hrs by DAPI staining-based immunofluorescence analysis F 5.94 pIC50 1160 nM IC50 Eur. J. Med. Chem. (2015) 95: 16-28 [PMID:25791675]
ChEMBL Antimalarial activity against sporozoite stage of Plasmodium yoelii assessed as invasion of human HepG2 cells expressing CD81 incubated for 2 hrs prior to inoculation measured after 1 hr by immunofluorescence assay in presence of penicillin/streptomycin F 6 pIC50 <1000 nM IC50 J. Med. Chem. (2013) 56: 7761-7771 [PMID:23927658]
ChEMBL Antimalarial activity against liver stages of Plasmodium yoelii 265 BY infected in Swiss mouse after 48 hrs by fluorescence microscopy F 7.12 pIC50 75 nM IC50 J. Med. Chem. (2012) 55: 995-1012 [PMID:22122518]
Plasmodium yoelii yoelii (target type: ORGANISM) [ChEMBL: CHEMBL612328]
ChEMBL Antimalarial activity against Plasmodium yoelii 265 sporozoites in primary mice (Mus musculus) hepatocytes after 48 hrs F 6.19 pIC50 640 nM IC50 Bioorg. Med. Chem. (2008) 16: 6186-6192 [PMID:18456502]
ChEMBL Antimicrobial activity against Plasmodium yoelii 265 liver infected in mammalian hepatocytes after 48 hrs F 7.12 pIC50 75.7 nM IC50 Antimicrob. Agents Chemother. (2008) 52: 1215-1220 [PMID:18212104]
ChEMBL Antimalarial activity against liver stages of Plasmodium yoelii yoelii F 7.12 pIC50 75.7 nM IC50 J. Med. Chem. (2012) 55: 995-1012 [PMID:22122518]
Quinone reductase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3959] [UniProtKB: P16083]
ChEMBL Inhibition of human recombinant NQO2 B 5.12 pIC50 7500 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 7331-7336 [PMID:21074425]
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) B 8.08 pKi 8.4 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) B 7.8 pIC50 16 nM IC50 DrugMatrix in vitro pharmacology data

ChEMBL data shown on this page come from version 25:

A.P. Bento, A. Gaulton, A. Hersey, et al. (2014). The ChEMBL bioactivity database: an update. Nucl. Acids Res. Database Issue. 42 D1083-D1090. [PMID:24214965]