ChEMBL ligand: CHEMBL506 (Primaquine)
Chloroquine resistance transporter in Plasmodium falciparum [ChEMBL: CHEMBL1795182] [UniProtKB: Q9N623] There should be some charts here, you may need to enable JavaScript!
CYP1A2/Cytochrome P450 1A2 in Human [ChEMBL: CHEMBL3356] [GtoPdb: 1319] [UniProtKB: P05177] There should be some charts here, you may need to enable JavaScript!
Monoamine oxidase A in Human [ChEMBL: CHEMBL1951] [GtoPdb: 2489] [UniProtKB: P21397] There should be some charts here, you may need to enable JavaScript!
Monoamine oxidase B in Human [ChEMBL: CHEMBL2039] [GtoPdb: 2490] [UniProtKB: P27338] There should be some charts here, you may need to enable JavaScript!
Plasmodium berghei [ChEMBL: CHEMBL612653] There should be some charts here, you may need to enable JavaScript!
Plasmodium falciparum [ChEMBL: CHEMBL364] There should be some charts here, you may need to enable JavaScript!
Plasmodium falciparum 3D7 [ChEMBL: CHEMBL2366922] There should be some charts here, you may need to enable JavaScript!
Plasmodium falciparum (isolate FcB1 / Columbia) in Plasmodium falciparum FcB1/Columbia [ChEMBL: CHEMBL612608] There should be some charts here, you may need to enable JavaScript!
Plasmodium falciparum (isolate K1 / Thailand) in Plasmodium falciparum K1 [ChEMBL: CHEMBL612856] There should be some charts here, you may need to enable JavaScript!
Plasmodium falciparum NF54 [ChEMBL: CHEMBL2367131] There should be some charts here, you may need to enable JavaScript!
Plasmodium yoelii [ChEMBL: CHEMBL612889] There should be some charts here, you may need to enable JavaScript!
Plasmodium yoelii yoelii [ChEMBL: CHEMBL612328] There should be some charts here, you may need to enable JavaScript!
Quinone reductase 2 in Human [ChEMBL: CHEMBL3959] [UniProtKB: P16083] There should be some charts here, you may need to enable JavaScript!
SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] There should be some charts here, you may need to enable JavaScript!

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]