Page last updated: 2024-12-05

amodiaquine hydrochloride

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth

Cross-References

ID SourceID
PubMed CID64646
CHEMBL ID1357648
MeSH IDM0496322
PubMed CID16051921
CHEMBL ID1630
SCHEMBL ID12094969
MeSH IDM0496322

Synonyms (75)

Synonym
PRESTWICK_677
amodiaquin dihydrochloride dihydrate
cas-6398-98-7
NCGC00017063-01
6398-98-7
D02466
amodiaquine hydrochloride (usp)
camoquin hydrochloride (tn)
4-[(7-chloroquinolin-4-yl)amino]-2-(diethylaminomethyl)phenol dihydrate dihydrochloride
HMS1568N20
A834604
4-[(7-chloranylquinolin-4-yl)amino]-2-(diethylaminomethyl)phenol dihydrate dihydrochloride
4-[(7-chloro-4-quinolinyl)amino]-2-(diethylaminomethyl)phenol dihydrate dihydrochloride
tox21_110765
dtxcid1025568
dtxsid3045568 ,
S4589
amodiaquine dihydrochloride dihydrate
NCGC00017063-02
cam-aq 1
phenol, 4-((7-chloro-4-quinolinyl)amino)-2-((diethylamino)methyl)-, dihydrochloride, dihydrate
4-((7-chloro-4-quinolyl)amino)-alpha-(diethylamino)-o-cresol dihydrochloride dihydrate
nsc 755863
unii-k6pw2s574l
k6pw2s574l ,
o-cresol, 4-((7-chloro-4-quinolyl)amino)-alpha-(diethylamino)-, dihydrochloride, dihydrate
sn 10751
amodiaquine hydrochloride [usp]
amodiaquin dihydrochlorid-2-wasser
NCGC00017063-03
4-[(7-chloro-4-quinolyl)amino]-alpha-(diethylamino)-o-cresol dihydrochloride dihydrate
amodiaquine hydrochloride [usp-rs]
amodiaquine hydrochloride [orange book]
amodiaquine dihydrochloride dihydrate [mi]
amodiaquine hydrochloride [vandf]
amodiaquine hydrochloride dihydrate [who-dd]
amodiaquine hydrochloride [usp monograph]
amodiaquine hydrochloride [who-dd]
amodiaquine hydrochloride [mart.]
amodiaquine hydrochloride [who-ip]
amodiaquini hydrochloridum [who-ip latin]
AKOS016339633
CCG-220309
KS-5250
KS-1326
CS-4895
amodiaquini hydrochloridum
CHEMBL1357648
amodiaquine (dihydrochloride dihydrate)
HY-B1322
mfcd09260307
4-(7-chloro-4-quinolinylamino)-2-(diethylaminomethyl)phenol dihydrochloride dihydrate
4-[(7-chloroquinolin-4-yl)amino]-2-(diethylaminomethyl)phenol;dihydrate;dihydrochloride
FT-0740309
Z1552192759
s4589 amodiaquin (dihydrochlori
Q27122169
A16405
D95328
6398-98-7 (hcl hydrate)
amodiaquin hcl hydrate
amodiaquindihydrochloridedihydrate
amodiaquine hydrochloride
TCMDC-123932 ,
CHEMBL1630
amodiaquine hcl
AKOS016339644
SCHEMBL12094969
1702335-79-2
4-((7-chloroquinolin-4-yl)amino)-2-((diethylamino)methyl)phenol xhydrochloride
4-((7-chloroquinolin-4-yl)amino)-2-((diethylamino)methyl)phenol hydrochloride
118490-14-5
amodiaquin (dihydrochloride)
[5-[(7-chloroquinolin-1-ium-4-yl)amino]-2-hydroxyphenyl]methyl-diethylazanium;dichloride;dihydrate
4-[(7-chloroquinolin-4-yl)amino]-2-(diethylaminomethyl)phenol;hydrochloride

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" Pharmacokinetic (PK) data informing the optimum dosing of these drug regimens is limited, especially in children."( Pharmacokinetics of artemether-lumefantrine and artesunate-amodiaquine in children in Kampala, Uganda.
Annerberg, A; Aweeka, F; Clark, TD; Dorsey, G; Drysdale, T; German, P; Kalyango, JN; Kamya, MR; Lindegardh, N; McGee, B; Mwesigwa, J; Parikh, S; Rosenthal, PJ, 2010
)
0.36

Compound-Compound Interactions

ExcerptReferenceRelevance
" Competitive uptake of radiolabeled chloroquine and dihydroartemisinin in combination with other antimalarials was observed."( Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
Adagu, IS; Fivelman, QL; Warhurst, DC, 2007
)
0.34
"The hepatic organic anion transporting polypeptides (OATPs) influence the pharmacokinetics of several drug classes and are involved in many clinical drug-drug interactions."( Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
Artursson, P; Haglund, U; Karlgren, M; Kimoto, E; Lai, Y; Norinder, U; Vildhede, A; Wisniewski, JR, 2012
)
0.38

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
" This result correlated well with an in vivo pharmacokinetics study, which showed low bioavailability of 6c in rats."( Tetrazole-based deoxyamodiaquines: synthesis, ADME/PK profiling and pharmacological evaluation as potential antimalarial agents.
Barteau, S; Chibale, K; Gut, J; Heudi, O; Kameni-Tcheudji, J; Mugumbate, GC; Njoroge, M; Rosenthal, PJ; Streckfuss, J; Tukulula, M, 2013
)
0.39

Dosage Studied

ExcerptRelevanceReference
" Depending on the intended indication and dosing regimen, PPL can delay or stop development of a compound in the drug discovery process."( Evaluation of a published in silico model and construction of a novel Bayesian model for predicting phospholipidosis inducing potential.
Gehlhaar, D; Greene, N; Johnson, TO; Pelletier, DJ; Tilloy-Ellul, A,
)
0.13
" The nonlinear clearance of DEAQ and the wide variability in kinetic parameters have safety implications for weight-based dosing of higher-body-weight children with AQ."( Effect of concomitant artesunate administration and cytochrome P4502C8 polymorphisms on the pharmacokinetics of amodiaquine in Ghanaian children with uncomplicated malaria.
Adjei, GO; Alifrangis, M; Goka, BQ; Hoegberg, LC; Kristensen, K; Kurtzhals, JA; Rodrigues, OP, 2008
)
0.35
" Pharmacokinetic (PK) data informing the optimum dosing of these drug regimens is limited, especially in children."( Pharmacokinetics of artemether-lumefantrine and artesunate-amodiaquine in children in Kampala, Uganda.
Annerberg, A; Aweeka, F; Clark, TD; Dorsey, G; Drysdale, T; German, P; Kalyango, JN; Kamya, MR; Lindegardh, N; McGee, B; Mwesigwa, J; Parikh, S; Rosenthal, PJ, 2010
)
0.36
" We determined the association between amodiaquine dosage by body weight and mild adverse events (AEs) and investigated whether alternative age-based regimens could improve dosing accuracy and tolerability, using data from two trials of IPTc in Senegal, one in which AQ dose was determined by age and the other in which it was determined by weight category."( Amodiaquine dosage and tolerability for intermittent preventive treatment to prevent malaria in children.
Ba, EH; Cairns, M; Cames, C; Cisse, B; Gaye, O; Greenwood, BM; Milligan, PJ; Simondon, K; Sokhna, C; Trape, JF, 2010
)
0.36
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
anticoronaviral agentAny antiviral agent which inhibits the activity of coronaviruses.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (1)

ClassDescription
hydrochlorideA salt formally resulting from the reaction of hydrochloric acid with an organic base.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (24)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency1.25890.004023.8416100.0000AID485290
TDP1 proteinHomo sapiens (human)Potency12.76220.000811.382244.6684AID686978; AID686979
AR proteinHomo sapiens (human)Potency10.20960.000221.22318,912.5098AID743035
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency5.01190.00137.762544.6684AID914; AID915
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency3.98110.035520.977089.1251AID504332
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency7.94330.00207.533739.8107AID891
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency11.35880.000323.4451159.6830AID743065; AID743067
gemininHomo sapiens (human)Potency5.70070.004611.374133.4983AID624297
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency15.47190.005612.367736.1254AID624032
lethal factor (plasmid)Bacillus anthracis str. A2012Potency10.00000.020010.786931.6228AID912
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency12.58930.316212.765731.6228AID881
Cellular tumor antigen p53Homo sapiens (human)Potency14.29990.002319.595674.0614AID651631
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency12.58930.00638.235039.8107AID881
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cytochrome P450 1A2Homo sapiens (human)IC50 (µMol)15.00000.00011.774010.0000AID346854; AID419167
Histidine-rich protein PFHRP-IIPlasmodium falciparum (malaria parasite P. falciparum)IC50 (µMol)395,083.50000.07651.12552.9000AID274221; AID278900
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)64.00000.00011.753610.0000AID346855; AID346856; AID419164; AID419165
Cytochrome P450 2C8Homo sapiens (human)IC50 (µMol)2.70000.00081.88487.9000AID346852; AID419169
Cytochrome P450 2D6Homo sapiens (human)IC50 (µMol)6.10000.00002.015110.0000AID346850; AID419168
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)62.00000.00002.800510.0000AID346853; AID419170
Cytochrome P450 2C19Homo sapiens (human)IC50 (µMol)85.00000.00002.398310.0000AID346851; AID419171
Histamine N-methyltransferaseHomo sapiens (human)Ki0.01900.01900.01900.0190AID672049
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)2.40000.00091.901410.0000AID346849
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
HeparanaseHomo sapiens (human)Kd52.60000.24000.24000.2400AID738328
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Histamine N-methyltransferaseHomo sapiens (human)Activity0.01000.01000.01000.0100AID387771
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (224)

Processvia Protein(s)Taxonomy
lipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
phospholipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
apoptotic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell population proliferationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of macrophage derived foam cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell migrationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
prostate gland developmentPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
regulation of epithelial cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of chemokine productionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of peroxisome proliferator activated receptor signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of keratinocyte differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell cyclePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of growthPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
hepoxilin biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
endocannabinoid signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cannabinoid biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxin A4 biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid oxidationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxygenase pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycle G2/M phase transitionCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
ER overload responseCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
mitophagyCellular tumor antigen p53Homo sapiens (human)
in utero embryonic developmentCellular tumor antigen p53Homo sapiens (human)
somitogenesisCellular tumor antigen p53Homo sapiens (human)
release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
hematopoietic progenitor cell differentiationCellular tumor antigen p53Homo sapiens (human)
T cell proliferation involved in immune responseCellular tumor antigen p53Homo sapiens (human)
B cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
T cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
response to ischemiaCellular tumor antigen p53Homo sapiens (human)
nucleotide-excision repairCellular tumor antigen p53Homo sapiens (human)
double-strand break repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
protein import into nucleusCellular tumor antigen p53Homo sapiens (human)
autophagyCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorCellular tumor antigen p53Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
Ras protein signal transductionCellular tumor antigen p53Homo sapiens (human)
gastrulationCellular tumor antigen p53Homo sapiens (human)
neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
protein localizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA replicationCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
determination of adult lifespanCellular tumor antigen p53Homo sapiens (human)
mRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
rRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
response to salt stressCellular tumor antigen p53Homo sapiens (human)
response to inorganic substanceCellular tumor antigen p53Homo sapiens (human)
response to X-rayCellular tumor antigen p53Homo sapiens (human)
response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
positive regulation of gene expressionCellular tumor antigen p53Homo sapiens (human)
cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
viral processCellular tumor antigen p53Homo sapiens (human)
glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
cerebellum developmentCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell growthCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCellular tumor antigen p53Homo sapiens (human)
negative regulation of telomere maintenance via telomeraseCellular tumor antigen p53Homo sapiens (human)
T cell differentiation in thymusCellular tumor antigen p53Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of tissue remodelingCellular tumor antigen p53Homo sapiens (human)
cellular response to UVCellular tumor antigen p53Homo sapiens (human)
multicellular organism growthCellular tumor antigen p53Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilityCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
entrainment of circadian clock by photoperiodCellular tumor antigen p53Homo sapiens (human)
mitochondrial DNA repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
transcription initiation-coupled chromatin remodelingCellular tumor antigen p53Homo sapiens (human)
negative regulation of proteolysisCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assemblyCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
response to antibioticCellular tumor antigen p53Homo sapiens (human)
fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
circadian behaviorCellular tumor antigen p53Homo sapiens (human)
bone marrow developmentCellular tumor antigen p53Homo sapiens (human)
embryonic organ developmentCellular tumor antigen p53Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationCellular tumor antigen p53Homo sapiens (human)
protein stabilizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of helicase activityCellular tumor antigen p53Homo sapiens (human)
protein tetramerizationCellular tumor antigen p53Homo sapiens (human)
chromosome organizationCellular tumor antigen p53Homo sapiens (human)
neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
hematopoietic stem cell differentiationCellular tumor antigen p53Homo sapiens (human)
negative regulation of glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
type II interferon-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
cardiac septum morphogenesisCellular tumor antigen p53Homo sapiens (human)
positive regulation of programmed necrotic cell deathCellular tumor antigen p53Homo sapiens (human)
protein-containing complex assemblyCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressCellular tumor antigen p53Homo sapiens (human)
thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
necroptotic processCellular tumor antigen p53Homo sapiens (human)
cellular response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
cellular response to xenobiotic stimulusCellular tumor antigen p53Homo sapiens (human)
cellular response to ionizing radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to UV-CCellular tumor antigen p53Homo sapiens (human)
stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
cellular response to actinomycin DCellular tumor antigen p53Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
cellular senescenceCellular tumor antigen p53Homo sapiens (human)
replicative senescenceCellular tumor antigen p53Homo sapiens (human)
oxidative stress-induced premature senescenceCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
oligodendrocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of execution phase of apoptosisCellular tumor antigen p53Homo sapiens (human)
negative regulation of mitophagyCellular tumor antigen p53Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of G1 to G0 transitionCellular tumor antigen p53Homo sapiens (human)
negative regulation of miRNA processingCellular tumor antigen p53Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
negative regulation of pentose-phosphate shuntCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
regulation of fibroblast apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
positive regulation of cellular senescenceCellular tumor antigen p53Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
steroid catabolic processCytochrome P450 1A2Homo sapiens (human)
porphyrin-containing compound metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 1A2Homo sapiens (human)
cholesterol metabolic processCytochrome P450 1A2Homo sapiens (human)
estrogen metabolic processCytochrome P450 1A2Homo sapiens (human)
toxin biosynthetic processCytochrome P450 1A2Homo sapiens (human)
post-embryonic developmentCytochrome P450 1A2Homo sapiens (human)
alkaloid metabolic processCytochrome P450 1A2Homo sapiens (human)
regulation of gene expressionCytochrome P450 1A2Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 1A2Homo sapiens (human)
dibenzo-p-dioxin metabolic processCytochrome P450 1A2Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
lung developmentCytochrome P450 1A2Homo sapiens (human)
methylationCytochrome P450 1A2Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 1A2Homo sapiens (human)
retinol metabolic processCytochrome P450 1A2Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 1A2Homo sapiens (human)
cellular respirationCytochrome P450 1A2Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 1A2Homo sapiens (human)
hydrogen peroxide biosynthetic processCytochrome P450 1A2Homo sapiens (human)
oxidative demethylationCytochrome P450 1A2Homo sapiens (human)
cellular response to cadmium ionCytochrome P450 1A2Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
lipid hydroxylationCytochrome P450 2C8Homo sapiens (human)
organic acid metabolic processCytochrome P450 2C8Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C8Homo sapiens (human)
steroid metabolic processCytochrome P450 2C8Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C8Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C8Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C8Homo sapiens (human)
retinol metabolic processCytochrome P450 2C8Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 2C8Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C8Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C8Homo sapiens (human)
oxidative demethylationCytochrome P450 2C8Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C8Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2D6Homo sapiens (human)
steroid metabolic processCytochrome P450 2D6Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2D6Homo sapiens (human)
estrogen metabolic processCytochrome P450 2D6Homo sapiens (human)
coumarin metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
alkaloid catabolic processCytochrome P450 2D6Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2D6Homo sapiens (human)
isoquinoline alkaloid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2D6Homo sapiens (human)
retinol metabolic processCytochrome P450 2D6Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2D6Homo sapiens (human)
negative regulation of bindingCytochrome P450 2D6Homo sapiens (human)
oxidative demethylationCytochrome P450 2D6Homo sapiens (human)
negative regulation of cellular organofluorine metabolic processCytochrome P450 2D6Homo sapiens (human)
arachidonic acid metabolic processCytochrome P450 2D6Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C9 Homo sapiens (human)
steroid metabolic processCytochrome P450 2C9 Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2C9 Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C9 Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C9 Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
urea metabolic processCytochrome P450 2C9 Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 2C9 Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
amide metabolic processCytochrome P450 2C9 Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
oxidative demethylationCytochrome P450 2C9 Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid metabolic processCytochrome P450 2C19Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C19Homo sapiens (human)
steroid metabolic processCytochrome P450 2C19Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C19Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C19Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C19Homo sapiens (human)
histamine metabolic processHistamine N-methyltransferaseHomo sapiens (human)
histamine catabolic processHistamine N-methyltransferaseHomo sapiens (human)
histidine catabolic processHistamine N-methyltransferaseHomo sapiens (human)
respiratory gaseous exchange by respiratory systemHistamine N-methyltransferaseHomo sapiens (human)
methylationHistamine N-methyltransferaseHomo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
proteoglycan metabolic processHeparanaseHomo sapiens (human)
cell-matrix adhesionHeparanaseHomo sapiens (human)
response to organic substanceHeparanaseHomo sapiens (human)
positive regulation of vascular endothelial growth factor productionHeparanaseHomo sapiens (human)
positive regulation of blood coagulationHeparanaseHomo sapiens (human)
heparan sulfate proteoglycan catabolic processHeparanaseHomo sapiens (human)
heparin metabolic processHeparanaseHomo sapiens (human)
positive regulation of osteoblast proliferationHeparanaseHomo sapiens (human)
regulation of hair follicle developmentHeparanaseHomo sapiens (human)
positive regulation of hair follicle developmentHeparanaseHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionHeparanaseHomo sapiens (human)
establishment of endothelial barrierHeparanaseHomo sapiens (human)
vascular wound healingHeparanaseHomo sapiens (human)
protein transmembrane transportHeparanaseHomo sapiens (human)
angiogenesis involved in wound healingHeparanaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (84)

Processvia Protein(s)Taxonomy
iron ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
calcium ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
protein bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 13S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 8(S)-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 15-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 9S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
transcription cis-regulatory region bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
core promoter sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
TFIID-class transcription factor complex bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
protease bindingCellular tumor antigen p53Homo sapiens (human)
p53 bindingCellular tumor antigen p53Homo sapiens (human)
DNA bindingCellular tumor antigen p53Homo sapiens (human)
chromatin bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activityCellular tumor antigen p53Homo sapiens (human)
mRNA 3'-UTR bindingCellular tumor antigen p53Homo sapiens (human)
copper ion bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingCellular tumor antigen p53Homo sapiens (human)
zinc ion bindingCellular tumor antigen p53Homo sapiens (human)
enzyme bindingCellular tumor antigen p53Homo sapiens (human)
receptor tyrosine kinase bindingCellular tumor antigen p53Homo sapiens (human)
ubiquitin protein ligase bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase regulator activityCellular tumor antigen p53Homo sapiens (human)
ATP-dependent DNA/DNA annealing activityCellular tumor antigen p53Homo sapiens (human)
identical protein bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase bindingCellular tumor antigen p53Homo sapiens (human)
protein heterodimerization activityCellular tumor antigen p53Homo sapiens (human)
protein-folding chaperone bindingCellular tumor antigen p53Homo sapiens (human)
protein phosphatase 2A bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCellular tumor antigen p53Homo sapiens (human)
14-3-3 protein bindingCellular tumor antigen p53Homo sapiens (human)
MDM2/MDM4 family protein bindingCellular tumor antigen p53Homo sapiens (human)
disordered domain specific bindingCellular tumor antigen p53Homo sapiens (human)
general transcription initiation factor bindingCellular tumor antigen p53Homo sapiens (human)
molecular function activator activityCellular tumor antigen p53Homo sapiens (human)
promoter-specific chromatin bindingCellular tumor antigen p53Homo sapiens (human)
monooxygenase activityCytochrome P450 1A2Homo sapiens (human)
iron ion bindingCytochrome P450 1A2Homo sapiens (human)
protein bindingCytochrome P450 1A2Homo sapiens (human)
electron transfer activityCytochrome P450 1A2Homo sapiens (human)
oxidoreductase activityCytochrome P450 1A2Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 1A2Homo sapiens (human)
enzyme bindingCytochrome P450 1A2Homo sapiens (human)
heme bindingCytochrome P450 1A2Homo sapiens (human)
demethylase activityCytochrome P450 1A2Homo sapiens (human)
caffeine oxidase activityCytochrome P450 1A2Homo sapiens (human)
aromatase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
hydroperoxy icosatetraenoate dehydratase activityCytochrome P450 1A2Homo sapiens (human)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
monooxygenase activityCytochrome P450 2C8Homo sapiens (human)
iron ion bindingCytochrome P450 2C8Homo sapiens (human)
protein bindingCytochrome P450 2C8Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C8Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 2C8Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C8Homo sapiens (human)
aromatase activityCytochrome P450 2C8Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 2C8Homo sapiens (human)
heme bindingCytochrome P450 2C8Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C8Homo sapiens (human)
monooxygenase activityCytochrome P450 2D6Homo sapiens (human)
iron ion bindingCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activityCytochrome P450 2D6Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2D6Homo sapiens (human)
heme bindingCytochrome P450 2D6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2D6Homo sapiens (human)
monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
iron ion bindingCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C9 Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
aromatase activityCytochrome P450 2C9 Homo sapiens (human)
heme bindingCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C9 Homo sapiens (human)
monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
iron ion bindingCytochrome P450 2C19Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxygen bindingCytochrome P450 2C19Homo sapiens (human)
enzyme bindingCytochrome P450 2C19Homo sapiens (human)
heme bindingCytochrome P450 2C19Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C19Homo sapiens (human)
aromatase activityCytochrome P450 2C19Homo sapiens (human)
long-chain fatty acid omega-1 hydroxylase activityCytochrome P450 2C19Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C19Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C19Homo sapiens (human)
histamine N-methyltransferase activityHistamine N-methyltransferaseHomo sapiens (human)
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
beta-glucuronidase activityHeparanaseHomo sapiens (human)
protein bindingHeparanaseHomo sapiens (human)
heparanase activityHeparanaseHomo sapiens (human)
syndecan bindingHeparanaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (39)

Processvia Protein(s)Taxonomy
nucleusPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytosolPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytoskeletonPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
plasma membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
adherens junctionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
focal adhesionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
extracellular exosomePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
nuclear bodyCellular tumor antigen p53Homo sapiens (human)
nucleusCellular tumor antigen p53Homo sapiens (human)
nucleoplasmCellular tumor antigen p53Homo sapiens (human)
replication forkCellular tumor antigen p53Homo sapiens (human)
nucleolusCellular tumor antigen p53Homo sapiens (human)
cytoplasmCellular tumor antigen p53Homo sapiens (human)
mitochondrionCellular tumor antigen p53Homo sapiens (human)
mitochondrial matrixCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulumCellular tumor antigen p53Homo sapiens (human)
centrosomeCellular tumor antigen p53Homo sapiens (human)
cytosolCellular tumor antigen p53Homo sapiens (human)
nuclear matrixCellular tumor antigen p53Homo sapiens (human)
PML bodyCellular tumor antigen p53Homo sapiens (human)
transcription repressor complexCellular tumor antigen p53Homo sapiens (human)
site of double-strand breakCellular tumor antigen p53Homo sapiens (human)
germ cell nucleusCellular tumor antigen p53Homo sapiens (human)
chromatinCellular tumor antigen p53Homo sapiens (human)
transcription regulator complexCellular tumor antigen p53Homo sapiens (human)
protein-containing complexCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C8Homo sapiens (human)
plasma membraneCytochrome P450 2C8Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C8Homo sapiens (human)
cytoplasmCytochrome P450 2C8Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C8Homo sapiens (human)
mitochondrionCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulumCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2D6Homo sapiens (human)
cytoplasmCytochrome P450 2D6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2D6Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C9 Homo sapiens (human)
plasma membraneCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
cytoplasmCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C19Homo sapiens (human)
plasma membraneCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C19Homo sapiens (human)
cytoplasmCytochrome P450 2C19Homo sapiens (human)
cytosolHistamine N-methyltransferaseHomo sapiens (human)
nucleoplasmHistamine N-methyltransferaseHomo sapiens (human)
cytoplasmHistamine N-methyltransferaseHomo sapiens (human)
centrosomeHistamine N-methyltransferaseHomo sapiens (human)
cytosolHistamine N-methyltransferaseHomo sapiens (human)
extracellular exosomeHistamine N-methyltransferaseHomo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
extracellular regionHeparanaseHomo sapiens (human)
nucleusHeparanaseHomo sapiens (human)
nucleoplasmHeparanaseHomo sapiens (human)
lysosomeHeparanaseHomo sapiens (human)
lysosomal membraneHeparanaseHomo sapiens (human)
specific granule lumenHeparanaseHomo sapiens (human)
lysosomal lumenHeparanaseHomo sapiens (human)
intracellular membrane-bounded organelleHeparanaseHomo sapiens (human)
membrane raftHeparanaseHomo sapiens (human)
extracellular spaceHeparanaseHomo sapiens (human)
extracellular matrixHeparanaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (380)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID511262Toxicity in children with malaria over 2 years of age assessed as incidence of vomiting at >=15 mg/kg/day, perorally co-treated with 500 mg sulfalene/25 mg pyrimethamine2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Amodiaquine dosage and tolerability for intermittent preventive treatment to prevent malaria in children.
AID449708ST_JUDE: Plasmodium falciparum K1 EC50 (uM) as measured by SYBR green dye2010Nature, May-20, Volume: 465, Issue:7296
Chemical genetics of Plasmodium falciparum.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID673344Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 assessed as [3H]hypoxanthine incorporation after 24 hrs by scintillation counting2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Benzoheterocyclic amodiaquine analogues with potent antiplasmodial activity: synthesis and pharmacological evaluation.
AID449717ST_JUDE: Cytotoxicity using luciferase to measure ATP as an indicator of the viability of human epithelial embryonic kidney cells (HEK293)2010Nature, May-20, Volume: 465, Issue:7296
Chemical genetics of Plasmodium falciparum.
AID704275Antimalarial activity against Plasmodium berghei NK-65 infected in ICR mouse assessed as host survival at 30 mg/kg, po administered at 72, 96 and 120 hrs post infection measured on day 23 post infection by Thompson test2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
Lead optimization of 3-carboxyl-4(1H)-quinolones to deliver orally bioavailable antimalarials.
AID366981Antimalarial activity after 24 hrs against chloroquine-resistant Plasmodium falciparum K1/Thailand by [3H]hypoxanthine uptake2008European journal of medicinal chemistry, Oct, Volume: 43, Issue:10
Synthesis and antimalarial activity of carbamate and amide derivatives of 4-anilinoquinoline.
AID449711ST_JUDE: Cytotoxicity against Plasmodium falciparum V1/S2010Nature, May-20, Volume: 465, Issue:7296
Chemical genetics of Plasmodium falciparum.
AID738327Binding affinity to recombinant heparanase catalytic stie (unknown origin) expressed in Escherichia coli BL21 (DE3) by NMR analysis2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
Hit identification of novel heparanase inhibitors by structure- and ligand-based approaches.
AID346858Antimalarial activity against chloroquine-sensitive Plasmodium falciparum HB3 in human erythrocytes after 48 hrs by [3H]hypoxanthine uptake2009Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5
Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID319198Antimalarial activity against Plasmodium falciparum HB32008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Two-step synthesis of achiral dispiro-1,2,4,5-tetraoxanes with outstanding antimalarial activity, low toxicity, and high-stability profiles.
AID129429Number of mice surviving at 60 days postinfection when administered as a single dose of 160 mg/kg (sc) 72-h post infection1987Journal of medicinal chemistry, May, Volume: 30, Issue:5
Synthesis and antimalarial effects of 4-[(7-chloro-4-quinolinyl)amino]-2-[(diethylamino)methyl] -6-alkylphenols and their N omega-oxides.
AID434599Antimalarial activity against Plasmodium falciparum THAI2009European journal of medicinal chemistry, Aug, Volume: 44, Issue:8
Recent developments in the design and synthesis of hybrid molecules based on aminoquinoline ring and their antiplasmodial evaluation.
AID511271Toxicity in children with malaria assessed as febrile incidence at 15-17 mg/kg/day, perorally and co-treated with sulfadoxine and pyrimethamine during intermittent preventive treatment to prevent malaria in children regimen2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Amodiaquine dosage and tolerability for intermittent preventive treatment to prevent malaria in children.
AID105841Cytotoxicity upon MRC-5 cells (diploid embryonic lung cell line) at 6.3 uM concentration2001Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17
Synthesis and in vitro and in vivo antimalarial activity of new 4-anilinoquinolines.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID323684Reduction of [3H]dihydroartemisinin uptake in chloroquine-sensitive Plasmodium falciparum 3D7 infected erythrocytes after 90 min2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID319197Antimalarial activity against Plasmodium falciparum V1/S2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Two-step synthesis of achiral dispiro-1,2,4,5-tetraoxanes with outstanding antimalarial activity, low toxicity, and high-stability profiles.
AID511268Toxicity in children with malaria assessed as febrile incidence at <15 mg/kg/day, perorally and co-treated with sulfadoxine and pyrimethamine during intermittent preventive treatment to prevent malaria in children regimen2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Amodiaquine dosage and tolerability for intermittent preventive treatment to prevent malaria in children.
AID671998Binding affinity to human serum albumin assessed as Stern-Volmer association constant at pH 7.4 and 310K by spectrofluorimetry2012European journal of medicinal chemistry, Aug, Volume: 54Investigation of the interaction between amodiaquine and human serum albumin by fluorescence spectroscopy and molecular modeling.
AID738328Binding affinity to recombinant heparanase catalytic stie (unknown origin) expressed in Escherichia coli BL21 (DE3) by surface plasmon resonance assay2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
Hit identification of novel heparanase inhibitors by structure- and ligand-based approaches.
AID511257Toxicity in children with malaria under 2 years of age assessed as incidence of vomiting administered with 250 mg sulfalene/12.5 mg pyrimethamine on first day followed by compound treatment at <=15 mg/kg/day, perorally2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Amodiaquine dosage and tolerability for intermittent preventive treatment to prevent malaria in children.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID588208Literature-mined public compounds from Lowe et al phospholipidosis modelling dataset2010Molecular pharmaceutics, Oct-04, Volume: 7, Issue:5
Predicting phospholipidosis using machine learning.
AID772516Antimalarial activity against mature gametocytic stage of Plasmodium falciparum assessed as inhibition of mature gamete exflagellation at 10 uM incubated for 24 hrs prior to exflagellation induction at 21 degC measured after 20 mins by microscopic analysi2013Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
Using genetic methods to define the targets of compounds with antimalarial activity.
AID774661Antimalarial activity against late (4 to 5) gametocytic stage of Plasmodium falciparum after 72 hrs by image-based HTS assay2013Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
Approaches to protozoan drug discovery: phenotypic screening.
AID497994Half life in Ugandan children patient with uncomplicated malaria assessed as desethylamodiaquine level at 10 mg/kg, perorally qd on first 2 days and then 5 mg/kg, perorally on third day co-administered with artesunate at 4 mg/kg, perorallybid for 3 days2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Pharmacokinetics of artemether-lumefantrine and artesunate-amodiaquine in children in Kampala, Uganda.
AID558825Antimicrobial activity against Plasmodium falciparum 3D7 by DAPI growth inhibition assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Colorimetric high-throughput screen for detection of heme crystallization inhibitors.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID594543Antiplasmodial activity against Plasmodium berghei ANKA infected in C57BL/6 mouse assessed as reduction in parasitemia at 1 mg, ip daily for 5 days measured after 72 hrs relative to control2011European journal of medicinal chemistry, May, Volume: 46, Issue:5
Amodiaquine analogues containing NO-donor substructures: synthesis and their preliminary evaluation as potential tools in the treatment of cerebral malaria.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID449705NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
AID519975Antimalarial activity against early trophozoite-stage Plasmodium falciparum 3D7 infected in erythrocyte assessed as reduction in parasite hemoglobin content at 5 times IC50 after 8 hrs in presence of 40 uM protease inhibitor ALLN2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Differential effects of quinoline antimalarials on endocytosis in Plasmodium falciparum.
AID586608Antimalarial 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 serum2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Ex vivo activity of histone deacetylase inhibitors against multidrug-resistant clinical isolates of Plasmodium falciparum and P. vivax.
AID553833Tmax in children with uncomplicated malaria assessed as desethylamodiaquine at 10 mg/kg, po administered as single dose2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Effect of concomitant artesunate administration and cytochrome P4502C8 polymorphisms on the pharmacokinetics of amodiaquine in Ghanaian children with uncomplicated malaria.
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
AID1121064Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in human erythrocytes after 96 hrs by luciferase based delayed death assay2012MedChemComm, Dec, Volume: 3, Issue:12
A furoxan-amodiaquine hybrid as a potential therapeutic for three parasitic diseases().
AID346855Inhibition of human recombinant CYP3A4 using phenyl-piperazinyl-methyl-benzyl-resofurin as substrate2009Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5
Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century.
AID555958Antimalarial activity against chloroquine-resistant Plasmodium vivax infected in human assessed as clearance of peripheral parasitemia at total dose of 30 mg/kg administered as three daily doses measured 48 hrs post dose2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
In vivo and in vitro efficacy of amodiaquine monotherapy for treatment of infection by chloroquine-resistant Plasmodium vivax.
AID497979Cmax in Ugandan children patient with uncomplicated malaria assessed as desethylamodiaquine level at 10 mg/kg, perorally qd on first 2 days and then 5 mg/kg, perorally on third day co-administered with artesunate at 4 mg/kg, perorally bid for 3 days2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Pharmacokinetics of artemether-lumefantrine and artesunate-amodiaquine in children in Kampala, Uganda.
AID366982Selectivity index, ratio of IC50 for human MRC5 cells to IC50 for chloroquine-resistant Plasmodium falciparum FcB1R/Colombia2008European journal of medicinal chemistry, Oct, Volume: 43, Issue:10
Synthesis and antimalarial activity of carbamate and amide derivatives of 4-anilinoquinoline.
AID519193Antimicrobial activity against Plasmodium vivax at the ring stage by microscopy2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Determinants of in vitro drug susceptibility testing of Plasmodium vivax.
AID419163Metabolic stability in human liver microsomes assessed as intrinsic clearance per gram of liver2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
AID419112Antimalarial activity as reduced parasitaemia against Plasmodium berghei ANKA infected CD1 mice (Mus musculus) perorally dosed daily over 4 days2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
AID704274Antimalarial activity against Plasmodium berghei NK-65 infected in ICR mouse assessed as host survival at 30 mg/kg, po administered at 72, 96 and 120 hrs post infection measured on day 17 post infection by Thompson test2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
Lead optimization of 3-carboxyl-4(1H)-quinolones to deliver orally bioavailable antimalarials.
AID157852Antimalarial activity against Plasmodium falciparum T9-961994Journal of medicinal chemistry, Apr-29, Volume: 37, Issue:9
The effect of fluorine substitution on the metabolism and antimalarial activity of amodiaquine.
AID585012Antimalarial activity against Plasmodium ovale ring stage infected in red blood cells in presence of AB+ human serum by drug susceptibility assay2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
In vivo and in vitro efficacy of chloroquine against Plasmodium malariae and P. ovale in Papua, Indonesia.
AID105681Cytotoxicity upon MPMs (mouse peritoneal macrophages) at 2 uM concentration; NT=No toxicity2001Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17
Synthesis and in vitro and in vivo antimalarial activity of new 4-anilinoquinolines.
AID418857Antimalarial activity against chloroquine-sensitive Plasmodium falciparum K12009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
AID323672Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D72007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID346853Inhibition of human recombinant CYP2C92009Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5
Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century.
AID449703NOVARTIS: Inhibition of Plasmodium falciparum 3D7 (drug-susceptible) proliferation in erythrocyte-based infection assay 2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
AID478788Antimalarial activity against chloroquine and pyrimethamine-resistant Plasmodium falciparum K1 infected in human erythrocytes after 72 hrs by spectrophotometry based Malstat method2010Journal of natural products, May-28, Volume: 73, Issue:5
Isomeric tropane alkaloids from the aerial parts of Schizanthus tricolor.
AID140549Change in mean survival time of trophozoite-induced Plasmodium berghei infection after 20 mg/kg subcutaneous dose1987Journal of medicinal chemistry, May, Volume: 30, Issue:5
Synthesis and antimalarial effects of 4-[(7-chloro-4-quinolinyl)amino]-2-[(diethylamino)methyl] -6-alkylphenols and their N omega-oxides.
AID636371Antimalarial activity against chloroquine-resistant Plasmodium falciparum VS/1 infected in human A positive erythrocytes assessed as inhibition of [G-3H]-hypoxanthine uptake after 24 hrs by liquid scintillation counting2012Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
Febrifugine analogue compounds: synthesis and antimalarial evaluation.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID419165Inhibition of human CYP3A4 using PPR substrate2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
AID496819Antimicrobial activity against Plasmodium falciparum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID419113Antimalarial activity as reduced parasitaemia against Plasmodium yoelii 17X infected CD1 mice (Mus musculus) perorally dosed daily for 4 days2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
AID123289Lethal dose that killed mice in 48 hr1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Synthesis of some novel amodiaquine analogues as potential antimalarial and antifilarial compounds.
AID515780Intrinsic solubility of the compound in water2010Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19
QSAR-based solubility model for drug-like compounds.
AID519197Antimicrobial activity against Plasmodium vivax trophozoites measured within 30 hrs by microscopy2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Determinants of in vitro drug susceptibility testing of Plasmodium vivax.
AID555959Toxicity in patient infected with chloroquine-resistant Plasmodium vivax assessed as occurrence of anemia at total dose of 30 mg/kg administered as three daily doses measured 7 days post dose2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
In vivo and in vitro efficacy of amodiaquine monotherapy for treatment of infection by chloroquine-resistant Plasmodium vivax.
AID274221Inhibition of beta-hematin formation by BHIA assay2006Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
Synthesis of N1-arylidene-N2-quinolyl- and N2-acrydinylhydrazones as potent antimalarial agents active against CQ-resistant P. falciparum strains.
AID101680Antifilarial activity against Litomosoides carinii infections in the Jird at dose 100 mg/kg administered orally1983Journal of medicinal chemistry, Sep, Volume: 26, Issue:9
Synthesis and antifilarial activity of N-[4-[[4-alkoxy-3-[(dialkylamino)methyl]phenyl]amino]- 2-pyrimidinyl]-N'-phenylguanidines.
AID382474Antimalarial activity against chloroquine-resistant Plasmodium falciparum Thai after 24 hrs by semiautomated micro dilution assay2008European journal of medicinal chemistry, Feb, Volume: 43, Issue:2
Synthesis and antimalarial activity of new analogues of amodiaquine.
AID414510Vacuolar accumulation ratio in pH 5.2 digestive vacuole2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
AID497981AUC (0-infinity) in Ugandan children patient with uncomplicated malaria at 10 mg/kg, perorally qd on first 2 days and then 5 mg/kg, perorally on third day co-administered with artesunate at 4 mg/kg, perorally bid for 3 days2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Pharmacokinetics of artemether-lumefantrine and artesunate-amodiaquine in children in Kampala, Uganda.
AID765175Antiplasmodial activity chloroquine-resistant Plasmodium falciparum W2 using YOYO-1 staining after 48 hrs by FACS analysis2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Tetrazole-based deoxyamodiaquines: synthesis, ADME/PK profiling and pharmacological evaluation as potential antimalarial agents.
AID323677Antimalarial activity against chloroquine-resistant Plasmodium falciparum 34-1/E2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID418858Antimalarial activity against chloroquine-sensitive Plasmodium falciparum PH32009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
AID774658Antimalarial activity against asexual stage of Plasmodium falciparum 3D7 after 72 hrs by image-based HTS assay2013Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
Approaches to protozoan drug discovery: phenotypic screening.
AID419172Toxicity against Wistar rat hepatocytes after 6 hrs by trypan blue exclusion method2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
AID636366Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in human A positive erythrocytes assessed as inhibition of [G-3H]-hypoxanthine uptake after 24 hrs by liquid scintillation counting2012Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
Febrifugine analogue compounds: synthesis and antimalarial evaluation.
AID671996Binding affinity to human serum albumin assessed as Stern-Volmer association constant at pH 7.4 and 291K by spectrofluorimetry2012European journal of medicinal chemistry, Aug, Volume: 54Investigation of the interaction between amodiaquine and human serum albumin by fluorescence spectroscopy and molecular modeling.
AID419167Inhibition of human CYP1A22009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
AID439585Antimalarial activity against chloroquine-susceptible Plasmodium falciparum 3D7 assessed as inhibition of parasite growth after 48 hrs by [3H]hypoxanthine reuptake assay2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
A new series of amodiaquine analogues modified in the basic side chain with in vitro antileishmanial and antiplasmodial activity.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID419173Therapeutic index, ratio of IC50 for Wistar rat hepatocytes to IC50 for Plasmodium falciparum HB32009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
AID105670Cytotoxicity upon MPMs (mouse peritoneal macrophages) at 12.5 uM concentration; Toxic Compound2001Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17
Synthesis and in vitro and in vivo antimalarial activity of new 4-anilinoquinolines.
AID105843Cytotoxicity upon MRC-5 cells (diploid embryonic lung cell line) at 8 uM concentration2001Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17
Synthesis and in vitro and in vivo antimalarial activity of new 4-anilinoquinolines.
AID576576Antimalarial activity against Plasmodium vivax infected in human erythrocytes assessed as growth inhibition by microscopic analysis using giemsa staining2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro activity of pyronaridine against multidrug-resistant Plasmodium falciparum and Plasmodium vivax.
AID346861Antimalarial activity as reduced parasitaemia against Plasmodium yoelii 17X infected CD1 mice (Mus musculus) after 4 days2009Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5
Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century.
AID672050Inhibition of Plasmodium falciparum phosphoethanolamine methyltransferase using phospethanolamine as substrate by radiochemical assay in presence of S-adenosylmethionine2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Crystal structure of phosphoethanolamine methyltransferase from Plasmodium falciparum in complex with amodiaquine.
AID434598Antimalarial activity against chloroquine-resistant Plasmodium falciparum FcB12009European journal of medicinal chemistry, Aug, Volume: 44, Issue:8
Recent developments in the design and synthesis of hybrid molecules based on aminoquinoline ring and their antiplasmodial evaluation.
AID678715Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID553832Cmax in children with uncomplicated malaria assessed as desethylamodiaquine at 10 mg/kg, po administered as single dose2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Effect of concomitant artesunate administration and cytochrome P4502C8 polymorphisms on the pharmacokinetics of amodiaquine in Ghanaian children with uncomplicated malaria.
AID519195Antimicrobial activity against Plasmodium vivax trophozoites measured after 30 hrs by microscopy2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Determinants of in vitro drug susceptibility testing of Plasmodium vivax.
AID129940Change in mean survival time for control (average 6.2 days) versus treated mice (Mus musculus) 72 hrs after 20 mg/kg subcutaneous dose1986Journal of medicinal chemistry, Jun, Volume: 29, Issue:6
Synthesis, antimalarial activity, and quantitative structure-activity relationships of tebuquine and a series of related 5-[(7-chloro-4-quinolinyl)amino]-3-[(alkylamino)methyl] [1,1'-biphenyl]-2-ols and N omega-oxides.
AID366980Antimalarial activity after 24 hrs against chloroquine-resistant Plasmodium falciparum FcB1R/Colombia by [3H]hypoxanthine uptake2008European journal of medicinal chemistry, Oct, Volume: 43, Issue:10
Synthesis and antimalarial activity of carbamate and amide derivatives of 4-anilinoquinoline.
AID699540Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID419162Metabolic stability in monkey liver microsomes assessed as intrinsic clearance per gram of liver2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
AID323683Reduction of [3H]dihydroartemisinin uptake in chloroquine-resistant Plasmodium falciparum K1 infected erythrocytes after 90 min2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID710074Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 infected in human RBCs after 72 hrs by parasite lactate dehydrogenase assay2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Mimicking the intramolecular hydrogen bond: synthesis, biological evaluation, and molecular modeling of benzoxazines and quinazolines as potential antimalarial agents.
AID672048Inhibition of Haemonchus contortus phosphoethanolamine methyltransferase1-mediated conversion of phosphoethanolamine to phosphomonomethylethanolamine by radiochemical assay in presence of S-adenosylmethionine2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Crystal structure of phosphoethanolamine methyltransferase from Plasmodium falciparum in complex with amodiaquine.
AID449721ST_JUDE: Cytotoxicity against Plasmodium falciparum SB-A62010Nature, May-20, Volume: 465, Issue:7296
Chemical genetics of Plasmodium falciparum.
AID330911Binding affinity to human serum albumin on sepharose column by affinity chromatography2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Selective plasma protein binding of antimalarial drugs to alpha1-acid glycoprotein.
AID419171Inhibition of human CYP2C192009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
AID754524Inhibition of hemozoin formation in 9.7 M acetate buffer at pH 4.8 at 60 degC after 2 hrs by microtiter-based high-throughput assay2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Quinoline drug-heme interactions and implications for antimalarial cytostatic versus cytocidal activities.
AID576575Antimalarial activity against Plasmodium falciparum infected in human erythrocytes assessed as growth inhibition by microscopic analysis using giemsa staining2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro activity of pyronaridine against multidrug-resistant Plasmodium falciparum and Plasmodium vivax.
AID636365Antimalarial activity against Plasmodium falciparum PH3 infected in human A positive erythrocytes assessed as inhibition of [G-3H]-hypoxanthine uptake after 24 hrs by liquid scintillation counting2012Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
Febrifugine analogue compounds: synthesis and antimalarial evaluation.
AID346862Antimalarial activity as ED100 in peripheral blood against Plasmodium yoelii 17X infected CD1 mice (Mus musculus) after 4 days2009Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5
Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century.
AID346864Binding affinity to heme in DMSO assessed as equilibrium constant by UV-visible spectrophotometry2009Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5
Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century.
AID553836AUC in children with uncomplicated malaria assessed as desethylamodiaquine at 10 mg/kg, po administered as single dose2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Effect of concomitant artesunate administration and cytochrome P4502C8 polymorphisms on the pharmacokinetics of amodiaquine in Ghanaian children with uncomplicated malaria.
AID346849Inhibition of human cloned ERG2009Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5
Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century.
AID330907Displacement of quinaldine red from human AAG by fluorescence method2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Selective plasma protein binding of antimalarial drugs to alpha1-acid glycoprotein.
AID671997Binding affinity to human serum albumin assessed as Stern-Volmer association constant at pH 7.4 and 301K by spectrofluorimetry2012European journal of medicinal chemistry, Aug, Volume: 54Investigation of the interaction between amodiaquine and human serum albumin by fluorescence spectroscopy and molecular modeling.
AID678717Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID671994Binding affinity to human serum albumin assessed as modified Stern-Volmer association constant at pH 7.4 and 291K by spectrofluorimetry in presence of ibuprofen2012European journal of medicinal chemistry, Aug, Volume: 54Investigation of the interaction between amodiaquine and human serum albumin by fluorescence spectroscopy and molecular modeling.
AID671989Binding affinity to human serum albumin assessed as modified Stern-Volmer association constant at pH 7.4 and 310K by spectrofluorimetry2012European journal of medicinal chemistry, Aug, Volume: 54Investigation of the interaction between amodiaquine and human serum albumin by fluorescence spectroscopy and molecular modeling.
AID157864In vitro inhibitory activity against chloroquine-resistant Plasmodium falciparum K11999Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15
New 4-aminoquinoline Mannich base antimalarials. 1. Effect of an alkyl substituent in the 5'-position of the 4'-hydroxyanilino side chain.
AID672047Inhibition of Haemonchus contortus phosphoethanolamine methyltransferase2 conversion of phosphomonomethylethanolamine to phosphodimethylethanolamine by radiochemical assay in presence of S-adenosylmethionine2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Crystal structure of phosphoethanolamine methyltransferase from Plasmodium falciparum in complex with amodiaquine.
AID519196Antimicrobial activity against Plasmodium vivax at the ring stage measured after 30 hrs by microscopy2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Determinants of in vitro drug susceptibility testing of Plasmodium vivax.
AID346851Inhibition of human recombinant CYP2C192009Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5
Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century.
AID101681Antifilarial activity against Litomosoides carinii infections in the Jird at dose 100 mg/kg administered subcutaneously1983Journal of medicinal chemistry, Sep, Volume: 26, Issue:9
Synthesis and antifilarial activity of N-[4-[[4-alkoxy-3-[(dialkylamino)methyl]phenyl]amino]- 2-pyrimidinyl]-N'-phenylguanidines.
AID754533Inhibition of hemozoin formation by microtiter plate-based high-throughput assay2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Quinoline drug-heme interactions and implications for antimalarial cytostatic versus cytocidal activities.
AID419111Antimalarial activity against chloroquine-resistant Plasmodium falciparum J1642009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
AID555960Toxicity in patient infected with chloroquine-resistant Plasmodium vivax assessed as occurrence of anemia at total dose of 30 mg/kg administered as three daily doses measured 24 days post dose2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
In vivo and in vitro efficacy of amodiaquine monotherapy for treatment of infection by chloroquine-resistant Plasmodium vivax.
AID748926Antiplasmodial activity against drug-sensitive Plasmodium falciparum 3D72013Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
Recent advances in malaria drug discovery.
AID404304Effect on human MRP2-mediated estradiol-17-beta-glucuronide transport in Sf9 cells inverted membrane vesicles relative to control2008Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2).
AID497980Half life in Ugandan children patient with uncomplicated malaria at 10 mg/kg, perorally qd on first 2 days and then 5 mg/kg, perorally on third day co-administered with artesunate at 4 mg/kg, perorally bid for 3 days2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Pharmacokinetics of artemether-lumefantrine and artesunate-amodiaquine in children in Kampala, Uganda.
AID346856Inhibition of human recombinant CYP3A4 using N-N,diethyl-formamide as substrate2009Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5
Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century.
AID105676Cytotoxicity upon MPMs (mouse peritoneal macrophages) at 6.3 uM concentration; Toxic Compound2001Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17
Synthesis and in vitro and in vivo antimalarial activity of new 4-anilinoquinolines.
AID576571Antimalarial activity against Plasmodium falciparum at the ring stage infected in human erythrocytes assessed as growth inhibition by microscopic analysis using giemsa staining2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro activity of pyronaridine against multidrug-resistant Plasmodium falciparum and Plasmodium vivax.
AID497977AUC (0-infinity) in Ugandan children patient with uncomplicated malaria assessed as desethylamodiaquine level at 10 mg/kg, perorally qd on first 2 days and then 5 mg/kg, perorally on third day co-administered with artesunate at 4 mg/kg, perorally bid for 2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Pharmacokinetics of artemether-lumefantrine and artesunate-amodiaquine in children in Kampala, Uganda.
AID671992Apparent binding affinity to human serum albumin at pH 7.4 and 310K by spectrofluorimetrysis2012European journal of medicinal chemistry, Aug, Volume: 54Investigation of the interaction between amodiaquine and human serum albumin by fluorescence spectroscopy and molecular modeling.
AID671993Binding affinity to human serum albumin assessed as modified Stern-Volmer association constant at pH 7.4 and 291K by spectrofluorimetry in presence of warfarin2012European journal of medicinal chemistry, Aug, Volume: 54Investigation of the interaction between amodiaquine and human serum albumin by fluorescence spectroscopy and molecular modeling.
AID366979Antimalarial activity against chloroquine-sensitive Plasmodium falciparum THAI/Thailand as [3H]hypoxanthine uptake after 24 hrs by semi-automated micro dilution2008European journal of medicinal chemistry, Oct, Volume: 43, Issue:10
Synthesis and antimalarial activity of carbamate and amide derivatives of 4-anilinoquinoline.
AID754530Inhibition of hemozoin formation in 8 M acetate buffer at pH 5 after 18 hrs by microtiter plate-based high-throughput assay2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Quinoline drug-heme interactions and implications for antimalarial cytostatic versus cytocidal activities.
AID101688Antifilarial activity against Litomosoides carinii infections in the Jird at dose 25 mg/kg administered subcutaneously1983Journal of medicinal chemistry, Sep, Volume: 26, Issue:9
Synthesis and antifilarial activity of N-[4-[[4-alkoxy-3-[(dialkylamino)methyl]phenyl]amino]- 2-pyrimidinyl]-N'-phenylguanidines.
AID387771Inhibition of histamine N-methyl-transferase2008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Design, synthesis, and docking studies of novel benzopyrone derivatives as H(1)-antihistaminic agents.
AID519194Antimicrobial activity against Plasmodium vivax at the trophozoites by microscopy treated during ring stage2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Determinants of in vitro drug susceptibility testing of Plasmodium vivax.
AID346854Inhibition of human recombinant CYP1A22009Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5
Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century.
AID511258Toxicity in children with malaria under 2 years of age assessed as incidence of fever administered with 250 mg sulfalene/12.5 mg pyrimethamine on first day followed by compound treatment at <=15 mg/kg/day, perorally2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Amodiaquine dosage and tolerability for intermittent preventive treatment to prevent malaria in children.
AID678721Metabolic stability in human liver microsomes assessed as GSH adduct formation at 100 uM after 90 mins by HPLC-MS analysis2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID511261Toxicity in children with malaria under 2 years of age assessed as incidence of headache administered with 250 mg sulfalene/12.5 mg pyrimethamine on first day followed by compound treatment at <=15 mg/kg/day, perorally2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Amodiaquine dosage and tolerability for intermittent preventive treatment to prevent malaria in children.
AID382476Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 after 24 hrs by semiautomated micro dilution assay2008European journal of medicinal chemistry, Feb, Volume: 43, Issue:2
Synthesis and antimalarial activity of new analogues of amodiaquine.
AID555962Antimalarial activity against chloroquine-resistant Plasmodium vivax by Giemsa staining2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
In vivo and in vitro efficacy of amodiaquine monotherapy for treatment of infection by chloroquine-resistant Plasmodium vivax.
AID449720ST_JUDE: Cytotoxicity against Plasmodium falciparum W22010Nature, May-20, Volume: 465, Issue:7296
Chemical genetics of Plasmodium falciparum.
AID140551Change in mean survival time of trophozoite-induced Plasmodium berghei infection after 40 mg/kg subcutaneous dose1987Journal of medicinal chemistry, May, Volume: 30, Issue:5
Synthesis and antimalarial effects of 4-[(7-chloro-4-quinolinyl)amino]-2-[(diethylamino)methyl] -6-alkylphenols and their N omega-oxides.
AID419179Toxicity in po dosed mouse assessed as drug level causing no observed adverse effects administered as single dose2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
AID754531Inhibition of hemozoin formation in 0.5 M acetate buffer at pH 4.8 after 12 hrs by tube-based high-throughput assay2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Quinoline drug-heme interactions and implications for antimalarial cytostatic versus cytocidal activities.
AID754536Inhibition of hemozoin formation in 0.5 M acetate buffer at pH 4.8 after 24 hrs by microtiter plate-based high-throughput assay2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Quinoline drug-heme interactions and implications for antimalarial cytostatic versus cytocidal activities.
AID43622Time taken for In vitro anti-filarial activity to immobilize breinlia booliati (Microfilaria)1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Synthesis of some novel amodiaquine analogues as potential antimalarial and antifilarial compounds.
AID511263Toxicity in children with malaria over 2 years of age assessed as incidence of fever at >=15 mg/kg/day, perorally co-treated with 500 mg sulfalene/25 mg pyrimethamine2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Amodiaquine dosage and tolerability for intermittent preventive treatment to prevent malaria in children.
AID774663Antimalarial activity against early (1 to 3) gametocytic stage of Plasmodium falciparum after 72 hrs by image-based HTS assay2013Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
Approaches to protozoan drug discovery: phenotypic screening.
AID449722ST_JUDE: Cytotoxicity against Plasmodium falciparum D10 transfected with yeast DHOD2010Nature, May-20, Volume: 465, Issue:7296
Chemical genetics of Plasmodium falciparum.
AID678712Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID586607Antimalarial activity against ring stage of Plasmodium vivax assessed as parasites growth inhibition using giemsa staining after 24 to 56 hrs by microscopic analysis in presence of 20% human serum2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Ex vivo activity of histone deacetylase inhibitors against multidrug-resistant clinical isolates of Plasmodium falciparum and P. vivax.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID511276Toxicity in children with malaria assessed as incidence of vomiting at >19 mg/kg/day, perorally and cotreated with Sulfadoxine and pyrimethamine during intermittent preventive treatment to prevent malaria in children regimen2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Amodiaquine dosage and tolerability for intermittent preventive treatment to prevent malaria in children.
AID511273Toxicity in children with malaria assessed as incidence of vomiting at 17-19 mg/kg/day, perorally and cotreated with Sulfadoxine and pyrimethamine during intermittent preventive treatment to prevent malaria in children regimen2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Amodiaquine dosage and tolerability for intermittent preventive treatment to prevent malaria in children.
AID586612Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as inhibition of [3H]hypoxanthine incorporation2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Ex vivo activity of histone deacetylase inhibitors against multidrug-resistant clinical isolates of Plasmodium falciparum and P. vivax.
AID414511Lipid accumulation ratio in pH 5.2 digestive vacuole2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
AID346859Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 in human erythrocytes after 48 hrs by [3H]hypoxanthine uptake2009Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5
Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century.
AID323674Antimalarial activity against chloroquine-resistant Plasmodium falciparum K12007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID129937Change in mean survival time for control (average 6.2 days) versus treated mice (Mus musculus) 72 hrs after 10 mg/kg subcutaneous dose1986Journal of medicinal chemistry, Jun, Volume: 29, Issue:6
Synthesis, antimalarial activity, and quantitative structure-activity relationships of tebuquine and a series of related 5-[(7-chloro-4-quinolinyl)amino]-3-[(alkylamino)methyl] [1,1'-biphenyl]-2-ols and N omega-oxides.
AID555957Antimalarial activity against chloroquine-resistant Plasmodium vivax infected in human assessed as clearance of peripheral parasitemia at total dose of 30 mg/kg administered as three daily doses measured within 24 hrs post dose2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
In vivo and in vitro efficacy of amodiaquine monotherapy for treatment of infection by chloroquine-resistant Plasmodium vivax.
AID158706In vitro inhibition of chloroquine-resistant Plasmodium falciparum K11997Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4
Synthesis, antimalarial activity, and molecular modeling of tebuquine analogues.
AID323670Antimalarial activity against chloroquine-sensitive Plasmodium falciparum FC272007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID1140209Binding affinity to haematin assessed as inhibition of beta-haematin formation after 5 to 6 hrs by pyridine-ferrichrome-based method2014Bioorganic & medicinal chemistry, May-01, Volume: 22, Issue:9
Synthesis, β-haematin inhibition, and in vitro antimalarial testing of isocryptolepine analogues: SAR study of indolo[3,2-c]quinolines with various substituents at C2, C6, and N11.
AID157865In vitro inhibitory activity against chloroquine-sensitive Plasmodium falciparum HB31999Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15
New 4-aminoquinoline Mannich base antimalarials. 1. Effect of an alkyl substituent in the 5'-position of the 4'-hydroxyanilino side chain.
AID323685Reduction of [3H]dihydroartemisinin uptake in chloroquine-resistant Plasmodium falciparum RSA11 infected erythrocytes after 90 min2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID636370Antimalarial activity against Plasmodium falciparum TM4 infected in human A positive erythrocytes assessed as inhibition of [G-3H]-hypoxanthine uptake after 24 hrs by liquid scintillation counting2012Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
Febrifugine analogue compounds: synthesis and antimalarial evaluation.
AID419182Toxicity in po dosed mouse assessed as induction of hematological toxicity at drug dose above no observed adverse effects level2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
AID101687Antifilarial activity against Litomosoides carinii infections in the Jird at dose 25 mg/kg administered orally1983Journal of medicinal chemistry, Sep, Volume: 26, Issue:9
Synthesis and antifilarial activity of N-[4-[[4-alkoxy-3-[(dialkylamino)methyl]phenyl]amino]- 2-pyrimidinyl]-N'-phenylguanidines.
AID497997AUC in Gabonian malarial children aged 6 months to 10 years assessed as desethylamodiaquine level at 30 mg/kg measured on third day post dose2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Pharmacokinetics of artemether-lumefantrine and artesunate-amodiaquine in children in Kampala, Uganda.
AID585009Antimalarial activity against Plasmodium malariae trophozoite stage infected in red blood cells in presence of AB+ human serum by drug susceptibility assay2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
In vivo and in vitro efficacy of chloroquine against Plasmodium malariae and P. ovale in Papua, Indonesia.
AID135296Antimalarial activity, administered as a single subcutaneous dose of 640 mg/kg, 72 hrs post infection measured as number of mice (Mus musculus) surviving at 60 days post infection1986Journal of medicinal chemistry, Jun, Volume: 29, Issue:6
Synthesis, antimalarial activity, and quantitative structure-activity relationships of tebuquine and a series of related 5-[(7-chloro-4-quinolinyl)amino]-3-[(alkylamino)methyl] [1,1'-biphenyl]-2-ols and N omega-oxides.
AID135291Antimalarial activity as 60-day survivors in Plasmodium berghei infected mice (Mus musculus) after single 160mg/kg subcutaneous dose 72 hr post infection1986Journal of medicinal chemistry, Jun, Volume: 29, Issue:6
Synthesis, antimalarial activity, and quantitative structure-activity relationships of tebuquine and a series of related 5-[(7-chloro-4-quinolinyl)amino]-3-[(alkylamino)methyl] [1,1'-biphenyl]-2-ols and N omega-oxides.
AID129432Number of mice surviving at 60 days postinfection when administered as a single dose of 320 mg/kg (sc) 72-h post infection1987Journal of medicinal chemistry, May, Volume: 30, Issue:5
Synthesis and antimalarial effects of 4-[(7-chloro-4-quinolinyl)amino]-2-[(diethylamino)methyl] -6-alkylphenols and their N omega-oxides.
AID418855Antimalarial activity against chloroquine-resistant Plasmodium falciparum TM62009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID511274Toxicity in children with malaria assessed as febrile incidence at 17-19 mg/kg/day, perorally and cotreated with Sulfadoxine and pyrimethamine during intermittent preventive treatment to prevent malaria in children regimen2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Amodiaquine dosage and tolerability for intermittent preventive treatment to prevent malaria in children.
AID511266Toxicity in children with malaria over 2 years of age assessed as incidence of headache at >=15 mg/kg/day, perorally co-treated with 500 mg sulfalene/25 mg pyrimethamine2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Amodiaquine dosage and tolerability for intermittent preventive treatment to prevent malaria in children.
AID710075Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D10 infected in human RBCs after 72 hrs by parasite lactate dehydrogenase assay2012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Mimicking the intramolecular hydrogen bond: synthesis, biological evaluation, and molecular modeling of benzoxazines and quinazolines as potential antimalarial agents.
AID419115Binding affinity to heme assessed as binding constant for stepwise binding of 2 equivalent of drug to 1 molecule of heme in presence of 40% DMSO by UV-visible spectroscopy2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
AID346850Inhibition of human recombinant CYP2D62009Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5
Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century.
AID497983Cmax in Ugandan children patient with uncomplicated malaria at 10 mg/kg, perorally qd on first 2 days and then 5 mg/kg, perorally on third day co-administered with artesunate at 4 mg/kg, perorally bid for 3 days2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Pharmacokinetics of artemether-lumefantrine and artesunate-amodiaquine in children in Kampala, Uganda.
AID317958Relative IC50 against Plasmodium falciparum K1 and 3D72008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
Antimalarial dual drugs based on potent inhibitors of glutathione reductase from Plasmodium falciparum.
AID765177Antiplasmodial activity chloroquine-sensitive Plasmodium falciparum 3D7 infected in human A+ erythrocytes assessed as reduction of [3H]hypoxanthine incorporation after 24 hrs by scintillation counting2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Tetrazole-based deoxyamodiaquines: synthesis, ADME/PK profiling and pharmacological evaluation as potential antimalarial agents.
AID419183Distribution coefficient, log D at pH 7.42009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
AID754535Inhibition of hemozoin formation in 0.5 M acetate buffer at pH 4.8 after 12 hrs by microtiter plate-based high-throughput assay in presence of trophozoite lysate2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Quinoline drug-heme interactions and implications for antimalarial cytostatic versus cytocidal activities.
AID346860Antimalarial activity as reduced parasitaemia against Plasmodium berghei ANKA infected CD1 mice (Mus musculus) after 4 days2009Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5
Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century.
AID159618In vivo inhibition of Plasmodium falciparum infected male Swiss albino mice (Mus musculus) by oral dose1999Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15
New 4-aminoquinoline Mannich base antimalarials. 1. Effect of an alkyl substituent in the 5'-position of the 4'-hydroxyanilino side chain.
AID673343Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum W2 infected in human erythrocytes after 48 hrs by Geimsa staining2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Benzoheterocyclic amodiaquine analogues with potent antiplasmodial activity: synthesis and pharmacological evaluation.
AID511278Toxicity in children with malaria assessed as incidence of rashes at >19 mg/kg/day, perorally and co-treated with sulfadoxine and pyrimethamine during intermittent preventive treatment to prevent malaria in children regimen2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Amodiaquine dosage and tolerability for intermittent preventive treatment to prevent malaria in children.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID230695Ratio of activity of quinine versus compound against Plasmodium berghei in mice1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Synthesis of some novel amodiaquine analogues as potential antimalarial and antifilarial compounds.
AID497982AUC (0-8 hrs) in Ugandan children patient with uncomplicated malaria at 10 mg/kg, perorally qd on first 2 days and then 5 mg/kg, perorally on third day co-administered with artesunate at 4 mg/kg, perorally bid for 3 days2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Pharmacokinetics of artemether-lumefantrine and artesunate-amodiaquine in children in Kampala, Uganda.
AID449714ST_JUDE: Cytotoxicity using Alamar Blue to measure viability of Leishmania major2010Nature, May-20, Volume: 465, Issue:7296
Chemical genetics of Plasmodium falciparum.
AID419114Antimalarial activity as minimal concentration for parasite elimination at day 23 against Plasmodium yoelii 17X peroral inoculated CD1 mice (Mus musculus) dosed 1 hrs post infection then daily for 4 days2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID319196Antimalarial activity against Plasmodium falciparum GC032008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Two-step synthesis of achiral dispiro-1,2,4,5-tetraoxanes with outstanding antimalarial activity, low toxicity, and high-stability profiles.
AID237426Partition coefficient (logP)2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Antileishmanial pyrazolopyridine derivatives: synthesis and structure-activity relationship analysis.
AID129435Number of mice surviving at 60 days postinfection when administered as a single dose of 640 mg/kg (sc) 72-h post infection1987Journal of medicinal chemistry, May, Volume: 30, Issue:5
Synthesis and antimalarial effects of 4-[(7-chloro-4-quinolinyl)amino]-2-[(diethylamino)methyl] -6-alkylphenols and their N omega-oxides.
AID366983Cytotoxicity against human MRC5 cells after 7 days by MTT assay2008European journal of medicinal chemistry, Oct, Volume: 43, Issue:10
Synthesis and antimalarial activity of carbamate and amide derivatives of 4-anilinoquinoline.
AID152136In vitro antimalarial activity against Plasmodium falciparum HB2003Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
Isoquine and related amodiaquine analogues: a new generation of improved 4-aminoquinoline antimalarials.
AID449704NOVARTIS: Inhibition of Plasmodium falciparum W2 (drug-resistant) proliferation in erythrocyte-based infection assay2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
AID540236Phospholipidosis-positive literature compound observed in human
AID576572Antimalarial activity against Plasmodium falciparum trophozoites infected in human erythrocytes assessed as growth inhibition by microscopic analysis using giemsa staining2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro activity of pyronaridine against multidrug-resistant Plasmodium falciparum and Plasmodium vivax.
AID419110Antimalarial activity against chloroquine-resistant Plasmodium falciparum V1/S2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
AID129942Difference in mean survival time in mice (Mus musculus) (control = 6.2 days) after single 40mg/kg subcutaneous dose 72hr post infection1986Journal of medicinal chemistry, Jun, Volume: 29, Issue:6
Synthesis, antimalarial activity, and quantitative structure-activity relationships of tebuquine and a series of related 5-[(7-chloro-4-quinolinyl)amino]-3-[(alkylamino)methyl] [1,1'-biphenyl]-2-ols and N omega-oxides.
AID594533Vasodilatory activity in pre-contracted Wistar rat aortic rings2011European journal of medicinal chemistry, May, Volume: 46, Issue:5
Amodiaquine analogues containing NO-donor substructures: synthesis and their preliminary evaluation as potential tools in the treatment of cerebral malaria.
AID449713ST_JUDE: Cytotoxicity using luciferase to measure ATP as an indicator of the viability of Trypanosoma brucei2010Nature, May-20, Volume: 465, Issue:7296
Chemical genetics of Plasmodium falciparum.
AID419181Toxicity in po dosed mouse assessed as induction of hepatotoxicity at drug dose above no observed adverse effects level2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
AID236591pKa was determined2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Antileishmanial pyrazolopyridine derivatives: synthesis and structure-activity relationship analysis.
AID419160Metabolic stability in rat liver microsomes assessed as intrinsic clearance per gram of liver2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
AID449716ST_JUDE: Cytotoxicity using luciferase to measure ATP as an indicator of the viability of human epithelial hepatocellular carcinoma cells (HepG2)2010Nature, May-20, Volume: 465, Issue:7296
Chemical genetics of Plasmodium falciparum.
AID497978AUC (0-120 hrs) in Ugandan children patient with uncomplicated malaria assessed as desethylamodiaquine level at 10 mg/kg, perorally qd on first 2 days and then 5 mg/kg, perorally on third day co-administered with artesunate at 4 mg/kg, perorally bid for 32010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Pharmacokinetics of artemether-lumefantrine and artesunate-amodiaquine in children in Kampala, Uganda.
AID330908Binding affinity to human serum albumin by circular dichroism and UV/VIS spectroscopic method2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Selective plasma protein binding of antimalarial drugs to alpha1-acid glycoprotein.
AID317956Antiparasitic activity against chloroquine-sensitive Plasmodium falciparum 3D72008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
Antimalarial dual drugs based on potent inhibitors of glutathione reductase from Plasmodium falciparum.
AID418853In vivo antimalarial activity against Plasmodium yoelii NS peroral dosage2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
AID323671Antimalarial activity against chloroquine-sensitive Plasmodium falciparum T9962007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID317957Antiparasitic activity against chloroquine-resistant Plasmodium falciparum K12008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
Antimalarial dual drugs based on potent inhibitors of glutathione reductase from Plasmodium falciparum.
AID699539Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID558824Inhibition of heme crystallization by hemichrome inhibition of beta-hematin assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Colorimetric high-throughput screen for detection of heme crystallization inhibitors.
AID738326Binding affinity to recombinant heparanase catalytic stie (unknown origin) expressed in Escherichia coli BL21 (DE3) by saturation transfer difference analysis2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
Hit identification of novel heparanase inhibitors by structure- and ligand-based approaches.
AID158707In vitro inhibition of chloroquine-sensitive Plasmodium falciparum HB31997Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4
Synthesis, antimalarial activity, and molecular modeling of tebuquine analogues.
AID152137Inhibitory activity against chloroquine-resistant Plasmodium falciparum K12001Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17
Synthesis and in vitro and in vivo antimalarial activity of new 4-anilinoquinolines.
AID105832Cytotoxicity upon MRC-5 cells (diploid embryonic lung cell line) at 12.5 uM concentration2001Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17
Synthesis and in vitro and in vivo antimalarial activity of new 4-anilinoquinolines.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID152139In vitro antimalarial activity against chloroquine-resistant Plasmodium falciparum K12003Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
Isoquine and related amodiaquine analogues: a new generation of improved 4-aminoquinoline antimalarials.
AID247877Tested for growth inhibitory activity against Leishmania amazonensis promastigotes2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
Antileishmanial pyrazolopyridine derivatives: synthesis and structure-activity relationship analysis.
AID511269Toxicity in children with malaria assessed as incidence of rashes at <15 mg/kg/day, perorally and co-treated with sulfadoxine and pyrimethamine during intermittent preventive treatment to prevent malaria in children regimen2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Amodiaquine dosage and tolerability for intermittent preventive treatment to prevent malaria in children.
AID511259Toxicity in children with malaria under 2 years of age assessed as incidence of rashes administered with 250 mg sulfalene/12.5 mg pyrimethamine on first day followed by compound treatment at <=15 mg/kg/day, perorally2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Amodiaquine dosage and tolerability for intermittent preventive treatment to prevent malaria in children.
AID434584Antimalarial activity against chloroquine-resistant Plasmodium falciparum K12009European journal of medicinal chemistry, Aug, Volume: 44, Issue:8
Recent developments in the design and synthesis of hybrid molecules based on aminoquinoline ring and their antiplasmodial evaluation.
AID228277Cellular accumulation ratio (CAR) for chloroquine sensitive HB3 strain of Plasmodium falciparum1997Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4
Synthesis, antimalarial activity, and molecular modeling of tebuquine analogues.
AID235112Resistance factor by IC50(K1)/IC50(HB3)1999Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15
New 4-aminoquinoline Mannich base antimalarials. 1. Effect of an alkyl substituent in the 5'-position of the 4'-hydroxyanilino side chain.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID323676Antimalarial activity against chloroquine-resistant Plasmodium falciparum 7G8-mdr7G82007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID382479Inhibition of haem polymerization after 24 hrs2008European journal of medicinal chemistry, Feb, Volume: 43, Issue:2
Synthesis and antimalarial activity of new analogues of amodiaquine.
AID636367Antimalarial activity against Plasmodium falciparum Dd2 infected in human A positive erythrocytes assessed as inhibition of [G-3H]-hypoxanthine uptake after 24 hrs by liquid scintillation counting2012Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
Febrifugine analogue compounds: synthesis and antimalarial evaluation.
AID382483Antimalarial activity as increased MST in Plasmodium berghei ANKA 65 infected Swiss CD1 at 10 mg/kg initial oral followed by intraperitoneal dose after 4 days2008European journal of medicinal chemistry, Feb, Volume: 43, Issue:2
Synthesis and antimalarial activity of new analogues of amodiaquine.
AID511275Toxicity in children with malaria assessed as incidence of rashes at 17-19 mg/kg/day, perorally and cotreated with Sulfadoxine and pyrimethamine during intermittent preventive treatment to prevent malaria in children regimen2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Amodiaquine dosage and tolerability for intermittent preventive treatment to prevent malaria in children.
AID671988Binding affinity to human serum albumin assessed as modified Stern-Volmer association constant at pH 7.4 and 301K by spectrofluorimetry2012European journal of medicinal chemistry, Aug, Volume: 54Investigation of the interaction between amodiaquine and human serum albumin by fluorescence spectroscopy and molecular modeling.
AID511277Toxicity in children with malaria assessed as febrile incidence at >19 mg/kg/day, perorally and co-treated with sulfadoxine and pyrimethamine during intermittent preventive treatment to prevent malaria in children regimen2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Amodiaquine dosage and tolerability for intermittent preventive treatment to prevent malaria in children.
AID519979Antimalarial activity against Plasmodium falciparum 3D7 infected in erythrocyte assessed as increase in vesicle content after 8 hrs by immunofluorescence microscopy2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Differential effects of quinoline antimalarials on endocytosis in Plasmodium falciparum.
AID585010Antimalarial activity against Plasmodium malariae ring stage infected in red blood cells in presence of AB+ human serum by drug susceptibility assay2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
In vivo and in vitro efficacy of chloroquine against Plasmodium malariae and P. ovale in Papua, Indonesia.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID497998AUC in Nigerian human adult malaria patient assessed as desethylamodiaquine level at 25 mg/kg measured on third day post dose2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Pharmacokinetics of artemether-lumefantrine and artesunate-amodiaquine in children in Kampala, Uganda.
AID519190Antimicrobial activity against Plasmodium vivax trophozoites by microscopy2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Determinants of in vitro drug susceptibility testing of Plasmodium vivax.
AID382475Antimalarial activity against chloroquine-resistant Plasmodium falciparum FcB1R after 24 hrs by semiautomated micro dilution assay2008European journal of medicinal chemistry, Feb, Volume: 43, Issue:2
Synthesis and antimalarial activity of new analogues of amodiaquine.
AID553835Terminal half life in children with uncomplicated malaria assessed as desethylamodiaquine at 10 mg/kg, po administered as single dose2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Effect of concomitant artesunate administration and cytochrome P4502C8 polymorphisms on the pharmacokinetics of amodiaquine in Ghanaian children with uncomplicated malaria.
AID319194Antimalarial activity against Plasmodium falciparum DD22008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Two-step synthesis of achiral dispiro-1,2,4,5-tetraoxanes with outstanding antimalarial activity, low toxicity, and high-stability profiles.
AID558823Inhibition of heme crystallization by cell-free heme crystallization screen assay2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Colorimetric high-throughput screen for detection of heme crystallization inhibitors.
AID511272Toxicity in children with malaria assessed as incidence of rashes at 15-17 mg/kg/day, perorally and co-treated with sulfadoxine and pyrimethamine during intermittent preventive treatment to prevent malaria in children regimen2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Amodiaquine dosage and tolerability for intermittent preventive treatment to prevent malaria in children.
AID366988Toxicity in Plasmodium berghei ANKA 65 infected Swiss CD1 mice (Mus musculus)2008European journal of medicinal chemistry, Oct, Volume: 43, Issue:10
Synthesis and antimalarial activity of carbamate and amide derivatives of 4-anilinoquinoline.
AID319200Antimalarial activity against Plasmodium falciparum TM42008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Two-step synthesis of achiral dispiro-1,2,4,5-tetraoxanes with outstanding antimalarial activity, low toxicity, and high-stability profiles.
AID419159Metabolic stability in mouse liver microsomes assessed as intrinsic clearance per gram of liver2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
AID497975AUC (0-infinity) in healthy human adult at 600 mg administered as single dose2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Pharmacokinetics of artemether-lumefantrine and artesunate-amodiaquine in children in Kampala, Uganda.
AID636369Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 infected in human A positive erythrocytes assessed as inhibition of [G-3H]-hypoxanthine uptake after 24 hrs by liquid scintillation counting2012Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
Febrifugine analogue compounds: synthesis and antimalarial evaluation.
AID366984Antimalarial activity as reduced parasitaemia in Plasmodium berghei ANKA 65 infected Swiss CD1 mice (Mus musculus) at 10 mg/kg/day peroral dose then intraperitoneal dose for 4 days2008European journal of medicinal chemistry, Oct, Volume: 43, Issue:10
Synthesis and antimalarial activity of carbamate and amide derivatives of 4-anilinoquinoline.
AID586606Antimalarial activity against trophozoites stage of Plasmodium vivax assessed as parasites growth inhibition using giemsa staining after 24 to 56 hrs by microscopic analysis in presence of 20% human serum2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Ex vivo activity of histone deacetylase inhibitors against multidrug-resistant clinical isolates of Plasmodium falciparum and P. vivax.
AID754525Inhibition of hemozoin formation in 1 M acetate buffer at pH 4.8 after 4.17 hrs by microtiter-based high-throughput assay in presence of 0.012 mg/mL Tween 202013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Quinoline drug-heme interactions and implications for antimalarial cytostatic versus cytocidal activities.
AID562110Antiplasmodial activity against multidrug-resistant Plasmodium falciparum VS/1 by [3H]hypoxanthine incorporation assay2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
In vitro chemosensitization of Plasmodium falciparum to antimalarials by verapamil and probenecid.
AID586610Antimalarial activity against Plasmodium vivax assessed as parasites growth inhibition using giemsa staining after 24 to 56 hrs by microscopic analysis in presence of 20% human serum2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Ex vivo activity of histone deacetylase inhibitors against multidrug-resistant clinical isolates of Plasmodium falciparum and P. vivax.
AID393144Antitubercular activity against Mycobacterium tuberculosis H37Rv after 5 days by microplate alamar blue assay2009Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4
Synthesis and in vitro antitubercular activity of a series of quinoline derivatives.
AID105674Cytotoxicity upon MPMs (mouse peritoneal macrophages) at 32 uM concentration; Toxic Compound.2001Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17
Synthesis and in vitro and in vivo antimalarial activity of new 4-anilinoquinolines.
AID319199Antimalarial activity against Plasmodium falciparum PH32008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Two-step synthesis of achiral dispiro-1,2,4,5-tetraoxanes with outstanding antimalarial activity, low toxicity, and high-stability profiles.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID105685Cytotoxicity upon MPMs (mouse peritoneal macrophages) at 3.1 uM concentration; NT= No toxicity.2001Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17
Synthesis and in vitro and in vivo antimalarial activity of new 4-anilinoquinolines.
AID553834Primary phase half life in children with uncomplicated malaria assessed as desethylamodiaquine at 10 mg/kg, po administered as single dose2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Effect of concomitant artesunate administration and cytochrome P4502C8 polymorphisms on the pharmacokinetics of amodiaquine in Ghanaian children with uncomplicated malaria.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID519974Antimalarial activity against early trophozoite-stage Plasmodium falciparum 3D7 infected in erythrocyte assessed as reduction in parasite hemoglobin content at 5 times IC50 after 8 hrs2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Differential effects of quinoline antimalarials on endocytosis in Plasmodium falciparum.
AID382478Cytotoxicity against human MCR5 cells after 7 days by MTT assay2008European journal of medicinal chemistry, Feb, Volume: 43, Issue:2
Synthesis and antimalarial activity of new analogues of amodiaquine.
AID497996AUC (0-infinity) in healthy human adult assessed as desethylamodiaquine level at 600 mg administered as single dose2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Pharmacokinetics of artemether-lumefantrine and artesunate-amodiaquine in children in Kampala, Uganda.
AID319195Antimalarial activity against Plasmodium falciparum K12008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Two-step synthesis of achiral dispiro-1,2,4,5-tetraoxanes with outstanding antimalarial activity, low toxicity, and high-stability profiles.
AID157851Antimalarial activity against Plasmodium falciparum K11994Journal of medicinal chemistry, Apr-29, Volume: 37, Issue:9
The effect of fluorine substitution on the metabolism and antimalarial activity of amodiaquine.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID419116Binding affinity to heme assessed as binding constant for stepwise binding of 2 molecules of heme to 1 equivalent of drug in presence of 40% DMSO by UV-visible spectroscopy2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
AID419170Inhibition of human CYP2C92009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
AID419117Inhibition of beta-hematin formation as molar equivalent relative to hemin causing blockade in BHIA2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
AID765176Antiplasmodial activity chloroquine-resistant Plasmodium falciparum K1 infected in human A+ erythrocytes assessed as reduction of [3H]hypoxanthine incorporation after 24 hrs by scintillation counting2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Tetrazole-based deoxyamodiaquines: synthesis, ADME/PK profiling and pharmacological evaluation as potential antimalarial agents.
AID485979Inhibition of CETP in rabbit serum at 10 uM after 1 hr by fluorescent cholesteryl esters transfer assay2010European journal of medicinal chemistry, Apr, Volume: 45, Issue:4
Discovery of new cholesteryl ester transfer protein inhibitors via ligand-based pharmacophore modeling and QSAR analysis followed by synthetic exploration.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID323682Reduction of [3H]dihydroartemisinin uptake in chloroquine-sensitive Plasmodium falciparum FC27 infected erythrocytes after 90 min2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID419180Toxicity in po dosed mouse assessed as drug level causing no observed adverse effects administered as once daily for 4 days2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
AID672049Inhibition of histamine N-methyltransferase by radiochemical assay2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Crystal structure of phosphoethanolamine methyltransferase from Plasmodium falciparum in complex with amodiaquine.
AID754532Inhibition of hemozoin formation in acetonitrile trophozoite extract by microtiter plate-based high-throughput assay2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Quinoline drug-heme interactions and implications for antimalarial cytostatic versus cytocidal activities.
AID419161Metabolic stability in dog liver microsomes assessed as intrinsic clearance per gram of liver2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
AID775955Inhibition of NP-40-induced beta-haematin formation after 5 to 6 hrs hrs by UV-vis spectroscopic analysis2013European journal of medicinal chemistry, Nov, Volume: 69In vitro antimalarial activity, β-haematin inhibition and structure-activity relationships in a series of quinoline triazoles.
AID519977Antimalarial activity against schizont-stage Plasmodium falciparum 3D7 infected in erythrocyte assessed as inhibition of horseradish peroxidase(HRP) uptake after 10 hrs by colorimetric peroxidase assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Differential effects of quinoline antimalarials on endocytosis in Plasmodium falciparum.
AID382480Antimalarial activity in Plasmodium berghei ANKA 65 infected Swiss CD1 mice (Mus musculus) as reduced parasitaemia at 10 mg/kg initial oral dose and further intraperitoneal dose after 4 days2008European journal of medicinal chemistry, Feb, Volume: 43, Issue:2
Synthesis and antimalarial activity of new analogues of amodiaquine.
AID105835Cytotoxicity upon MRC-5 cells (diploid embryonic lung cell line) at 25 uM concentration2001Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17
Synthesis and in vitro and in vivo antimalarial activity of new 4-anilinoquinolines.
AID671987Binding affinity to human serum albumin assessed as modified Stern-Volmer association constant at pH 7.4 and 291K by spectrofluorimetry2012European journal of medicinal chemistry, Aug, Volume: 54Investigation of the interaction between amodiaquine and human serum albumin by fluorescence spectroscopy and molecular modeling.
AID449718ST_JUDE: Cytotoxicity using luciferase to measure ATP as an indicator of the viability of human Burkitt''s lymphoma lymphoblast cells (Raji)2010Nature, May-20, Volume: 465, Issue:7296
Chemical genetics of Plasmodium falciparum.
AID439583Antileishmanial activity against Leishmania donovani MHOM/ET/ 67/HU3 amastigote infected in CD1 mouse peritoneal exudate macrophages assessed as parasite growth inhibition after 5 days by Giemsa staining2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
A new series of amodiaquine analogues modified in the basic side chain with in vitro antileishmanial and antiplasmodial activity.
AID449706NOVARTIS: Inhibition Frequency Index (IFI) - the number of HTS assays where a compound showed > 50% inhibition/induction, expressed as a percentage of the number of assays in which the compound was tested.2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
AID754527Inhibition of hemozoin formation in 12.9 M acetate buffer at pH 4.5 at 60 degC after 1 hr by microtiter-based high-throughput assay2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Quinoline drug-heme interactions and implications for antimalarial cytostatic versus cytocidal activities.
AID710073Resistant index, ratio of IC50 for chloroquine-resistant Plasmodium falciparum W2 to IC50 for chloroquine-sensitive Plasmodium falciparum D102012Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
Mimicking the intramolecular hydrogen bond: synthesis, biological evaluation, and molecular modeling of benzoxazines and quinazolines as potential antimalarial agents.
AID151990Inhibitory activity against chloroquine-resistant Plasmodium falciparum FcB1R2001Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17
Synthesis and in vitro and in vivo antimalarial activity of new 4-anilinoquinolines.
AID519198Antimicrobial activity against Plasmodium vivax at the ring stage measured within 30 hrs by microscopy2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Determinants of in vitro drug susceptibility testing of Plasmodium vivax.
AID323675Antimalarial activity against chloroquine-resistant Plasmodium falciparum RSA112007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID586613Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 assessed as inhibition of [3H]hypoxanthine incorporation2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Ex vivo activity of histone deacetylase inhibitors against multidrug-resistant clinical isolates of Plasmodium falciparum and P. vivax.
AID418859Antimalarial activity against chloroquine-resistant Plasmodium falciparum TM42009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
AID576577Antimalarial activity against Plasmodium vivax with >50% parasites at ring stage infected in human erythrocytes assessed as growth inhibition after 30 to 50 hrs by microscopic analysis using giemsa staining2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro activity of pyronaridine against multidrug-resistant Plasmodium falciparum and Plasmodium vivax.
AID135297Antimalarial activity, administered as a single subcutaneous dose of 80 mg/kg, 72 hrs post infection measured as number of mice (Mus musculus) surviving at 60 days post infection1986Journal of medicinal chemistry, Jun, Volume: 29, Issue:6
Synthesis, antimalarial activity, and quantitative structure-activity relationships of tebuquine and a series of related 5-[(7-chloro-4-quinolinyl)amino]-3-[(alkylamino)methyl] [1,1'-biphenyl]-2-ols and N omega-oxides.
AID159617In vivo inhibition of Plasmodium falciparum infected male Swiss albino mice (Mus musculus) by intraperitoneal dose1999Journal of medicinal chemistry, Jul-29, Volume: 42, Issue:15
New 4-aminoquinoline Mannich base antimalarials. 1. Effect of an alkyl substituent in the 5'-position of the 4'-hydroxyanilino side chain.
AID419169Inhibition of human CYP2C82009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID135293Antimalarial activity as 60-day survivors in infected mice (Mus musculus) after single 320mg/kg subcutaneous dose 72 hr post infection1986Journal of medicinal chemistry, Jun, Volume: 29, Issue:6
Synthesis, antimalarial activity, and quantitative structure-activity relationships of tebuquine and a series of related 5-[(7-chloro-4-quinolinyl)amino]-3-[(alkylamino)methyl] [1,1'-biphenyl]-2-ols and N omega-oxides.
AID419178Toxicity in po dosed mouse assessed as maximal nonlethal dose administered as single dose2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
AID105839Cytotoxicity upon MRC-5 cells (diploid embryonic lung cell line) at 32 uM concentration2001Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17
Synthesis and in vitro and in vivo antimalarial activity of new 4-anilinoquinolines.
AID699541Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID439587Cytotoxicity against human KB cells after 72 hrs by Alamar blue assay2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
A new series of amodiaquine analogues modified in the basic side chain with in vitro antileishmanial and antiplasmodial activity.
AID586611Antimalarial 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 serum2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Ex vivo activity of histone deacetylase inhibitors against multidrug-resistant clinical isolates of Plasmodium falciparum and P. vivax.
AID576573Antimalarial activity against Plasmodium vivax at the ring stage infected in human erythrocytes assessed as growth inhibition by microscopic analysis using giemsa staining2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro activity of pyronaridine against multidrug-resistant Plasmodium falciparum and Plasmodium vivax.
AID678722Covalent binding affinity to human liver microsomes assessed per mg of protein at 10 uM after 60 mins presence of NADPH2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID449707ST_JUDE: Plasmodium falciparum 3D7 EC50 (uM) as measured by SYBR green dye2010Nature, May-20, Volume: 465, Issue:7296
Chemical genetics of Plasmodium falciparum.
AID671990Apparent binding affinity to human serum albumin at pH 7.4 and 291K by spectrofluorimetry2012European journal of medicinal chemistry, Aug, Volume: 54Investigation of the interaction between amodiaquine and human serum albumin by fluorescence spectroscopy and molecular modeling.
AID317959Cytotoxicity against human KB cells by alamar blue assay2008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
Antimalarial dual drugs based on potent inhibitors of glutathione reductase from Plasmodium falciparum.
AID346852Inhibition of human recombinant CYP2C82009Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5
Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century.
AID418860Antimalarial activity against chloroquine-sensitive Plasmodium falciparum Dd22009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
AID754534Inhibition of hemozoin formation in parasite digestive vacuole extract by microtiter plate-based high-throughput assay2013Journal of medicinal chemistry, Jul-11, Volume: 56, Issue:13
Quinoline drug-heme interactions and implications for antimalarial cytostatic versus cytocidal activities.
AID678714Inhibition of human CYP2C19 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 3-butyryl-7-methoxycoumarin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID317969Antiparasitic activity against chloroquine-sensitive Plasmodium falciparum by [3H]hypoxanthine incorporation2008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
Antimalarial dual drugs based on potent inhibitors of glutathione reductase from Plasmodium falciparum.
AID594532Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 assessed as inhibition of parasite LDH activity after 72 hrs by spectrophotometry2011European journal of medicinal chemistry, May, Volume: 46, Issue:5
Amodiaquine analogues containing NO-donor substructures: synthesis and their preliminary evaluation as potential tools in the treatment of cerebral malaria.
AID477933Inhibition of beta-hematin formation assessed as drug-hematin ratio for 50% inhibition after 60 mins by colorimetric analysis2010Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8
Antimalarial versus cytotoxic properties of dual drugs derived from 4-aminoquinolines and Mannich bases: interaction with DNA.
AID636368Antimalarial activity against chloroquine-resistant Plasmodium falciparum TM6 infected in human A positive erythrocytes assessed as inhibition of [G-3H]-hypoxanthine uptake after 24 hrs by liquid scintillation counting2012Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
Febrifugine analogue compounds: synthesis and antimalarial evaluation.
AID671991Apparent binding affinity to human serum albumin at pH 7.4 and 301K by spectrofluorimetry2012European journal of medicinal chemistry, Aug, Volume: 54Investigation of the interaction between amodiaquine and human serum albumin by fluorescence spectroscopy and molecular modeling.
AID625294Drug Induced Liver Injury Prediction System (DILIps) validation dataset; compound DILI positive/negative as observed in O'Brien data2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID511270Toxicity in children with malaria assessed as incidence of vomiting at 15-17 mg/kg/day, perorally and cotreated with Sulfadoxine and pyrimethamine during intermittent preventive treatment to prevent malaria in children regimen2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Amodiaquine dosage and tolerability for intermittent preventive treatment to prevent malaria in children.
AID366985Antimalarial activity as increased mean survival time in Plasmodium berghei ANKA 65 infected Swiss CD1 mice (Mus musculus) at 10 mg/kg peroral dose day 1 with intraperitoneal dose over 4 days2008European journal of medicinal chemistry, Oct, Volume: 43, Issue:10
Synthesis and antimalarial activity of carbamate and amide derivatives of 4-anilinoquinoline.
AID152329In vitro antimalarial activity against Plasmodium yoelii NS in peter 4-day assay2003Journal of medicinal chemistry, Nov-06, Volume: 46, Issue:23
Isoquine and related amodiaquine analogues: a new generation of improved 4-aminoquinoline antimalarials.
AID511260Toxicity in children with malaria under 2 years of age assessed as incidence of itching administered with 250 mg sulfalene/12.5 mg pyrimethamine on first day followed by compound treatment at <=15 mg/kg/day, perorally2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Amodiaquine dosage and tolerability for intermittent preventive treatment to prevent malaria in children.
AID1121063Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in human erythrocytes after 96 hrs by SYBR Green I staining2012MedChemComm, Dec, Volume: 3, Issue:12
A furoxan-amodiaquine hybrid as a potential therapeutic for three parasitic diseases().
AID449709ST_JUDE: Cytotoxicity against Plasmodium falciparum 3D72010Nature, May-20, Volume: 465, Issue:7296
Chemical genetics of Plasmodium falciparum.
AID449712ST_JUDE: Growth inhibition of to Toxoplasma gondii, in human U-2OS cells, as measured by luciferase.2010Nature, May-20, Volume: 465, Issue:7296
Chemical genetics of Plasmodium falciparum.
AID594531Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum D10 assessed as inhibition of parasite LDH activity after 72 hrs by spectrophotometry2011European journal of medicinal chemistry, May, Volume: 46, Issue:5
Amodiaquine analogues containing NO-donor substructures: synthesis and their preliminary evaluation as potential tools in the treatment of cerebral malaria.
AID43623Time taken for In vitro anti-filarial activity to immobilize breinlia booliati (adult worms)1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Synthesis of some novel amodiaquine analogues as potential antimalarial and antifilarial compounds.
AID449715ST_JUDE: Cytotoxicity using luciferase to measure ATP as an indicator of the viability of human foreskin fibroblast cells (BJ)2010Nature, May-20, Volume: 465, Issue:7296
Chemical genetics of Plasmodium falciparum.
AID678716Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID449719ST_JUDE: Cytotoxicity against Plasmodium falciparum Dd22010Nature, May-20, Volume: 465, Issue:7296
Chemical genetics of Plasmodium falciparum.
AID129437Number of mice surviving at 60 days postinfection when administered as a single dose of 80 mg/kg (sc) 72-h post infection1987Journal of medicinal chemistry, May, Volume: 30, Issue:5
Synthesis and antimalarial effects of 4-[(7-chloro-4-quinolinyl)amino]-2-[(diethylamino)methyl] -6-alkylphenols and their N omega-oxides.
AID419164Inhibition of human CYP3A4 using DEF substrate2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
AID576574Antimalarial activity against Plasmodium vivax trophozoites infected in human erythrocytes assessed as growth inhibition by microscopic analysis using giemsa staining2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro activity of pyronaridine against multidrug-resistant Plasmodium falciparum and Plasmodium vivax.
AID511264Toxicity in children with malaria over 2 years of age assessed as incidence of rashes at >=15 mg/kg/day, perorally co-treated with 500 mg sulfalene/25 mg pyrimethamine2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Amodiaquine dosage and tolerability for intermittent preventive treatment to prevent malaria in children.
AID152140Inhibitory activity against chloroquine-resistant Plasmodium falciparum THAI2001Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17
Synthesis and in vitro and in vivo antimalarial activity of new 4-anilinoquinolines.
AID519976Antimalarial activity against early trophozoite-stage Plasmodium falciparum 3D7 infected in erythrocyte assessed as reduction in parasite hemoglobin content at 5 times IC50 after 8 hrs in presence of 40 uM protease inhibitor E642008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Differential effects of quinoline antimalarials on endocytosis in Plasmodium falciparum.
AID555963Toxicity in human infected with chloroquine-Resistant Plasmodium vivax assessed as occurrence of nausea at total dose of 30 mg/kg administered as three daily doses2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
In vivo and in vitro efficacy of amodiaquine monotherapy for treatment of infection by chloroquine-resistant Plasmodium vivax.
AID382477Selectivity index, ratio of CC50 for human MRC5 cells to IC50 for Plasmodium falciparum K12008European journal of medicinal chemistry, Feb, Volume: 43, Issue:2
Synthesis and antimalarial activity of new analogues of amodiaquine.
AID115750Minimum effective dose which on 5th day reduced the mean infection level to one-fiftieth of the control1981Journal of medicinal chemistry, Dec, Volume: 24, Issue:12
Synthesis of some novel amodiaquine analogues as potential antimalarial and antifilarial compounds.
AID105837Cytotoxicity upon MRC-5 cells (diploid embryonic lung cell line) at 3.1 uM concentration2001Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17
Synthesis and in vitro and in vivo antimalarial activity of new 4-anilinoquinolines.
AID594534Vasodilatory activity in pre-contracted Wistar rat aortic rings in presence of 1 uM ODQ2011European journal of medicinal chemistry, May, Volume: 46, Issue:5
Amodiaquine analogues containing NO-donor substructures: synthesis and their preliminary evaluation as potential tools in the treatment of cerebral malaria.
AID586609Antimalarial 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 serum2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Ex vivo activity of histone deacetylase inhibitors against multidrug-resistant clinical isolates of Plasmodium falciparum and P. vivax.
AID511267Toxicity in children with malaria assessed as incidence of vomiting at <15 mg/kg/day, perorally and co-treated with sulfadoxine and pyrimethamine during intermittent preventive treatment to prevent malaria in children regimen2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Amodiaquine dosage and tolerability for intermittent preventive treatment to prevent malaria in children.
AID555956Toxicity in patient infected with chloroquine-resistant Plasmodium vivax assessed as occurrence of vomiting at total dose of 30 mg/kg administered as three daily doses measured 30 minutes post dose2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
In vivo and in vitro efficacy of amodiaquine monotherapy for treatment of infection by chloroquine-resistant Plasmodium vivax.
AID678713Inhibition of human CYP2C9 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-methoxy-4-trifluoromethylcoumarin-3-acetic acid as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID105829Cytotoxicity upon MRC-5 cells (diploid embryonic lung cell line) at 1 uM concentration2001Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17
Synthesis and in vitro and in vivo antimalarial activity of new 4-anilinoquinolines.
AID511265Toxicity in children with malaria over 2 years of age assessed as incidence of itching at >=15 mg/kg/day, perorally co-treated with 500 mg sulfalene/25 mg pyrimethamine2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Amodiaquine dosage and tolerability for intermittent preventive treatment to prevent malaria in children.
AID555961Antimalarial activity against chloroquine-Resistant Plasmodium vivax infected in human assessed as parasite recurrence rate at total dose of 30 mg/kg administered as three daily doses measured on day 28 post dose2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
In vivo and in vitro efficacy of amodiaquine monotherapy for treatment of infection by chloroquine-resistant Plasmodium vivax.
AID671995Induction of conformational changes in human serum albumin assessed as decrease in absorbance at pH 7.4 and 291K by UV-Vis absorption spectrophotometric analysis2012European journal of medicinal chemistry, Aug, Volume: 54Investigation of the interaction between amodiaquine and human serum albumin by fluorescence spectroscopy and molecular modeling.
AID323673Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 106/12007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
AID449710ST_JUDE: Cytotoxicity against Plasmodium falciparum K12010Nature, May-20, Volume: 465, Issue:7296
Chemical genetics of Plasmodium falciparum.
AID414512Partition coefficient, log P of the compound2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
AID278900Inhibition of Tween 20-induced beta-hematin formation by colorimetric assay2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Simple colorimetric inhibition assay of heme crystallization for high-throughput screening of antimalarial compounds.
AID346857Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 in human erythrocytes after 48 hrs by [3H]hypoxanthine uptake2009Journal of medicinal chemistry, Mar-12, Volume: 52, Issue:5
Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century.
AID419168Inhibition of human CYP2D62009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
AID519192Antimicrobial activity against Plasmodium falciparum trophozoites by microscopy treated during ring stage2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Determinants of in vitro drug susceptibility testing of Plasmodium vivax.
AID26114pKa value of compound was evaluated1994Journal of medicinal chemistry, Apr-29, Volume: 37, Issue:9
The effect of fluorine substitution on the metabolism and antimalarial activity of amodiaquine.
AID519191Antimicrobial activity against Plasmodium falciparum at the ring stage by microscopy2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Determinants of in vitro drug susceptibility testing of Plasmodium vivax.
AID439586Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 assessed as inhibition of parasite growth after 48 hrs by [3H]hypoxanthine reuptake assay2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
A new series of amodiaquine analogues modified in the basic side chain with in vitro antileishmanial and antiplasmodial activity.
AID418856Antimalarial activity against chloroquine-sensitive Plasmodium falciparum HB32009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
AID1159588Biochemical screen of P. falciparum CDPK42016PloS one, , Volume: 11, Issue:3
Biochemical Screening of Five Protein Kinases from Plasmodium falciparum against 14,000 Cell-Active Compounds.
AID1159586Biochemical screen of P. falciparum PK62016PloS one, , Volume: 11, Issue:3
Biochemical Screening of Five Protein Kinases from Plasmodium falciparum against 14,000 Cell-Active Compounds.
AID1159585Biochemical screen of P. falciparum CDPK12016PloS one, , Volume: 11, Issue:3
Biochemical Screening of Five Protein Kinases from Plasmodium falciparum against 14,000 Cell-Active Compounds.
AID1159587Biochemical screen of P. falciparum PK72016PloS one, , Volume: 11, Issue:3
Biochemical Screening of Five Protein Kinases from Plasmodium falciparum against 14,000 Cell-Active Compounds.
AID1159589Biochemical screen of P. falciparum MAPK22016PloS one, , Volume: 11, Issue:3
Biochemical Screening of Five Protein Kinases from Plasmodium falciparum against 14,000 Cell-Active Compounds.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (73)

TimeframeStudies, This Drug (%)All Drugs %
pre-19904 (5.48)18.7374
1990's3 (4.11)18.2507
2000's26 (35.62)29.6817
2010's37 (50.68)24.3611
2020's3 (4.11)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Trials2 (2.94%)5.53%
Reviews0 (0.00%)6.00%
Reviews5 (7.35%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Observational0 (0.00%)0.25%
Other7 (100.00%)84.16%
Other61 (89.71%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]