Page last updated: 2024-12-06

doxofylline

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

Description

Doxofylline is a synthetic theophylline derivative with bronchodilator properties. It is used to treat asthma and chronic obstructive pulmonary disease (COPD). Doxofylline has a longer duration of action than theophylline, and it is less likely to cause side effects such as nausea, vomiting, and insomnia. It is thought to work by relaxing the muscles in the airways, making it easier to breathe. Doxofylline is typically taken by mouth, and it is available in both immediate-release and extended-release formulations. The synthesis of doxofylline involves a multi-step process that starts with theophylline. The molecule is then modified to create the desired bronchodilator activity. Research on doxofylline continues to explore its potential therapeutic benefits and investigate its mechanism of action. It is studied to understand its efficacy in treating different respiratory conditions and to assess its safety and tolerability in various patient populations.'

doxofylline : An oxopurine that is a derivative of xanthine, methylated at N-1 and N-3 and carrying a 1,3-dioxolan-2-ylmethyl group at N-7, used in the treatment of asthma. [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]

Cross-References

ID SourceID
PubMed CID50942
CHEMBL ID1527608
CHEBI ID94714
SCHEMBL ID37963
MeSH IDM0094833

Synonyms (101)

Synonym
AC-3492
AB00828111-06
do-309
abc-1213
maxivent
ventax
doxofylline
abc-12/3
ansimar
7-(1,3-dioxolan-2-ylmethyl)-1,3-dimethyl-3,7-dihydro-1h-purine-2,6-dione
maxivent (tn)
doxofylline (usan/inn)
69975-86-6
D03898
NCGC00159330-02
brn 0561195
1h-purine-2,6-dione, 3,7-dihydro-7-(1,3-dioxolan-2-ylmethyl)-1,3-dimethyl-
doxophylline
theophylline, 7-(1,3-dioxolan-2-ylmethyl)-
doxofyllinum [inn-latin]
einecs 274-239-6
abc 12/3
dioxyfilline
doxofylline [usan:inn]
1h-purine-2,6-dione, 7-(1,3-dioxolan-2-ylmethyl)-3,7-dihydro-1,3-dimethyl-
7-(1,3-dioxolon-2-ylmethyl)-1,2,3,6-tetrahydro-1,3-dimethyl-2,6-purindion
2-(7'-theophyllinemethyl)-1,3-dioxolane
7-(1,3-dioxolan-2-ylmethyl)theophylline
2-(7'-teofillinmetil)-1,3-diossolano [italian]
doxofilina [inn-spanish]
smr000543614
MLS001214637
HMS2090E04
L001990
STK735429
A836720
7-(1,3-dioxolan-2-ylmethyl)-1,3-dimethyl-purine-2,6-dione
nsc-759645
CHEMBL1527608
synasma
2-(7'-teofillinmetil)-1,3-diossolano
unii-mpm23gmo7z
doxofilina
mpm23gmo7z ,
nsc 759645
5-26-14-00120 (beilstein handbook reference)
doxofyllinum
dtxsid7022968 ,
cas-69975-86-6
tox21_111577
dtxcid002968
HMS2877P10
BBL012263
nsc759645
pharmakon1600-01502358
S4164
AKOS005535592
7-((1,3-dioxolan-2-yl)methyl)-1,3-dimethyl-1h-purine-2,6(3h,7h)-dione
FT-0630792
doxofylline [mart.]
doxofylline [mi]
doxofylline [usan]
doxofylline [who-dd]
doxofylline [inn]
CCG-213050
SCHEMBL37963
tox21_111577_1
NCGC00159330-03
tox21 111577
CS-8019
HY-B0004
D4302
7-(1,3-dioxolan-2-ylmethyl)-1,3-dimethyl-1h-purine-2,6-dione
7-(1,3-dioxolan-2-ylmethyl)-1,3-dimethylxanthine
AB00828111_07
AB00828111_08
mfcd00865218
DB09273
7-(1,3-dioxolan-2-ylmethyl)-3,7-dihydro-1,3-dimethyl-1h-purine-2,6-dione
SR-01000789760-2
sr-01000789760
SR-01000789760-3
7-[(1,3-dioxolan-2-yl)methyl]-1,3-dimethyl-2,3,6,7-tetrahydro-1h-purine-2,6-dione
doxofylline, united states pharmacopeia (usp) reference standard
CHEBI:94714
HMS3652H03
doxofylline, >=98% (hplc)
HMS3714M21
NCGC00159330-04
SW199176-2
DS-7424
Q425887
doxofylline,(s)
BCP12155
NCGC00159330-10
HMS3885B09
D90272
7-((1,3-dioxolan-2-yl)methyl)-1,3-dimethyl-3,7-dihydro-1h-purine-2,6-dione
BD164389
7uh ,
SY053230

Research Excerpts

Overview

Doxofylline is an effective bronchodilator for relieving airway obstruction in patients with asthma or chronic obstructive pulmonary disease (COPD) It has been used as a treatment for respiratory diseases for more than 30 years. Its influence on antibiotics remains poorly understood.

ExcerptReferenceRelevance
"Doxofylline is a newer generation xanthine with both bronchodilating and anti-inflammatory activities, but its influence on antibiotics remains poorly understood."( Doxofylline Protects Gram-Negative Pathogens against Antibiotic-Mediated Killing.
Chen, H; Li, J; Liu, Y; Shen, W; Xu, M; Yang, N; Yang, Y; Zhang, H; Zheng, Y, 2021
)
2.79
"Doxofylline is a newer generation xanthine with both bronchodilating and anti-inflammatory activities and for this reason it has been called "novofylline"."( The effect of doxofylline in asthma and COPD.
Cazzola, M; Matera, MG, 2020
)
1.64
"Doxofylline is an effective bronchodilator for relieving airway obstruction in patients with asthma or chronic obstructive pulmonary disease (COPD), and displays a better safety profile with respect to theophylline. "( Impact of doxofylline in COPD: A pairwise meta-analysis.
Calzetta, L; Cazzola, M; Matera, MG; Page, C; Rogliani, P, 2018
)
2.33
"Doxofylline is a xanthine drug that has been used as a treatment for respiratory diseases for more than 30 years. "( Doxofylline, a novofylline inhibits lung inflammation induced by lipopolysacharide in the mouse.
Man, F; Page, CP; Riffo-Vasquez, Y, 2014
)
3.29
"Doxofylline is a xanthine molecule that appears to be both bronchodilator and anti-inflammatory with an improved therapeutic window over conventional xanthines such as theophylline and the evidence supporting the effects of doxofylline in the treatment of lung diseases is discussed."( Doxofylline: a "novofylline".
Page, CP, 2010
)
2.52
"Doxofylline is a xanthine molecule having both bronchodilator and anti-inflammatory activity with an improved therapeutic window over conventional xanthines such as theophylline."( The mechanism of action of doxofylline is unrelated to HDAC inhibition, PDE inhibition or adenosine receptor antagonism.
Allegra, L; Jolas, T; Page, CP; van Mastbergen, J, 2012
)
1.4
"Doxofylline is a new xanthine derivative with significant bronchodilatatory activity. "( Doxofylline in rat brain in relation to locomotor activity.
Cravanzola, C; Franzone, JS; Grosa, G; Reboani, MC,
)
3.02
"Doxofylline (ANSIMAR) is a new adenosine-nonblocking anti-asthmatic drug with potent bronchodilator activity that does not display the typical extrapulmonary side effects of theophylline--a potent adenosine antagonist. "( Doxofylline, an adenosine-nonblocking xanthine, does not induce cardiostimulant effects.
Cirillo, R; Franzone, JS; Grossi, E, 1989
)
3.16
"Doxofylline is a new antibronchospastic drug, recently introduced in therapy, with pharmacological properties like theophylline, a potent adenosine receptor antagonist. "( Doxofylline and theophylline are xanthines with partly different mechanisms of action in animals.
Barone, D; Cirillo, R; Franzone, JS, 1988
)
3.16

Effects

ExcerptReferenceRelevance
"Doxofylline also has a very low affinity for adenosine receptors inhibiting cAMP-phosphodiesterase as does theophylline."( Doxofylline differs from methylxanthines in its movement of cytosolic calcium.
Cirillo, R; Franzone, JS; Reboani, MC, 1991
)
2.45
"Doxofylline also has a very low affinity for adenosine receptors inhibiting cAMP-phosphodiesterase as does theophylline."( Doxofylline differs from methylxanthines in its movement of cytosolic calcium.
Cirillo, R; Franzone, JS; Reboani, MC, 1991
)
2.45

Toxicity

The comparative study showed that doxofylline was more effective as evidenced by improvement in PFT as well as clinical symptoms. Theophylline reduced incidence of adverse effects and emergency bronchodilator use.

ExcerptReferenceRelevance
" Each patient was followed up fortnightly for the assessment of efficacy parameters using a pulmonary function test (PFT), clinical symptoms and emergency drug use, and safety was assessed by recording adverse drug reactions."( Comparative study of the efficacy and safety of theophylline and doxofylline in patients with bronchial asthma and chronic obstructive pulmonary disease.
Kumar, R; Lal, D; Manocha, S; Ray, A; Vijayan, VK, 2015
)
0.65
"The comparative study showed that doxofylline was more effective as evidenced by improvement in PFT as well as clinical symptoms, and reduced incidence of adverse effects and emergency bronchodilator use."( Comparative study of the efficacy and safety of theophylline and doxofylline in patients with bronchial asthma and chronic obstructive pulmonary disease.
Kumar, R; Lal, D; Manocha, S; Ray, A; Vijayan, VK, 2015
)
0.93
" In addition, we assessed the risk of adverse events by normalising data on safety as a function of person-weeks."( Efficacy and safety profile of xanthines in COPD: a network meta-analysis.
Barnes, PJ; Calzetta, L; Cazzola, M; Criner, GJ; Gabriella Matera, M; Martinez, FJ; Papi, A, 2018
)
0.48
" Short-term efficacy, pulmonary ventilation function, patient quality of life, peripheral blood TNF-alpha and PGDF-B levels, and adverse drug reactions were observed."( Effects of Doxofylline Combined with Ceftazidime on Clinical Efficacy, Drug Safety, and Prognosis in Patients with Chronic Obstructive Pulmonary Disease Complicated with Infection.
Wang, Y, 2021
)
1.01
" During the treatment, the remission time of typical respiratory manifestations was recorded, and the adverse reactions were observed."( Efficacy and safety of combined doxofylline and salbutamol in treatment of acute exacerbation of chronic obstructive pulmonary disease.
Bao, H; Du, X; Zhao, D, 2021
)
0.9
" In addition, the adverse reaction rate had no significant difference between two groups (p>0."( Efficacy and safety of combined doxofylline and salbutamol in treatment of acute exacerbation of chronic obstructive pulmonary disease.
Bao, H; Du, X; Zhao, D, 2021
)
0.9

Pharmacokinetics

ExcerptReferenceRelevance
" The developed assay method was applied to a pharmacokinetic study in human volunteers following oral administration of DFL tablet."( Development and validation of a sensitive LC-MS/MS method with electrospray ionization for quantitation of doxofylline in human serum: application to a clinical pharmacokinetic study.
Mullangi, R; Narasu, ML; Shankar, BP; Sreenivas, N, 2008
)
0.56
"The prepared immediate release and controlled release pastilles were subjected to in vivo pharmacokinetic studies in rats."( Evaluation of in vivo behavior of controlled and pulsatile release pastilles using pharmacokinetic and γ-scintigraphic techniques.
Chakraborty, S; Mishra, B; Shukla, D, 2012
)
0.38
"The in vivo pharmacokinetic study of controlled release pastille formulation showed significant decrease in C(max) with increase in t(max), which indicates that the effect of dosage form would last for longer duration."( Evaluation of in vivo behavior of controlled and pulsatile release pastilles using pharmacokinetic and γ-scintigraphic techniques.
Chakraborty, S; Mishra, B; Shukla, D, 2012
)
0.38
" The method was validated as per ICH guidelines and successfully applied to a pharmacokinetic study of doxofylline in rats."( Development of a validated LC-MS/MS method for determination of doxofylline on rat dried blood spots and urine: application to pharmacokinetics.
Agwane, SB; Naidu, ChG; Prasad, KG; Rao, RN; Saida, S, 2013
)
0.84

Compound-Compound Interactions

ExcerptReferenceRelevance
"BACKGROUND The aim of this study was to investigate the effects of doxofylline combined with ceftazidime on clinical efficacy, drug safety, and prognosis in patients with COPD complicated with infection."( Effects of Doxofylline Combined with Ceftazidime on Clinical Efficacy, Drug Safety, and Prognosis in Patients with Chronic Obstructive Pulmonary Disease Complicated with Infection.
Wang, Y, 2021
)
1.25

Bioavailability

ExcerptReferenceRelevance
" The relative bioavailability of the sustained-release pellets was studied in six beagle dogs after oral administration in a fast state using a commercially available immediate release tablet as a reference."( Preparation and bioavailability of sustained-release doxofylline pellets in beagle dogs.
He, HB; Huang, HF; Lu, Y; Tang, X, 2008
)
0.6
"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

Dosage Studied

Doxofylline decreased airway responsiveness at the dosage which dose not affect the heart rate and respiratory rate compared with theophylline. The aim of the study was to design a multilayered dosage form of doxofyllines.

ExcerptRelevanceReference
" These results suggest that doxofylline decreased airway responsiveness at the dosage which dose not affect the heart rate and respiratory rate compared with theophylline."( [Effects of theophylline and doxofylline on airway responsiveness in beagles].
Adachi, M; Horikoshi, S; Idaira, K; Imai, T; Okamoto, M; Sugeta, A, 1997
)
0.88
" Dosage recommended for children> 6 yrs of age is 6 mg/Kg/dose BID."( Doxofylline: The next generation methylxanthine.
Kabra, SK; Lodha, R; Sankar, J, 2008
)
1.79
"The present work was undertaken with an objective to design a multilayered dosage form of doxofylline, using pastillation technology, for the chronotherapeutic management of nocturnal asthma."( In vitro and in vivo evaluation of multilayered pastilles for chronotherapeutic management of nocturnal asthma.
Chakraborty, S; Mishra, B; Shukla, D, 2012
)
0.6
"The present work opens a new alternative to the conventional tablet or capsule dosage form for the development of both immediate-release and modified-release drug delivery systems."( In vitro and in vivo evaluation of multilayered pastilles for chronotherapeutic management of nocturnal asthma.
Chakraborty, S; Mishra, B; Shukla, D, 2012
)
0.38
"The in vivo pharmacokinetic study of controlled release pastille formulation showed significant decrease in C(max) with increase in t(max), which indicates that the effect of dosage form would last for longer duration."( Evaluation of in vivo behavior of controlled and pulsatile release pastilles using pharmacokinetic and γ-scintigraphic techniques.
Chakraborty, S; Mishra, B; Shukla, D, 2012
)
0.38
"This study opens a new alternative to the conventional tablet or capsule dosage form for the development of both immediate and modified release drug delivery systems."( Evaluation of in vivo behavior of controlled and pulsatile release pastilles using pharmacokinetic and γ-scintigraphic techniques.
Chakraborty, S; Mishra, B; Shukla, D, 2012
)
0.38
" The TNJ protective effects were concentration-dependent, indicating a dose-response correlation, that can be attributed to a powerful antioxidant and/or free radical scavenger ability of TNJ."( Antimutagenic and antirecombinagenic activities of noni fruit juice in somatic cells of Drosophila melanogaster.
Cunha, KS; De Andrade, HH; De Andrade, LR; Dihl, RR; Franchi, LP; Guimarães, NN; Lehmann, M,
)
0.13
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
bronchodilator agentAn agent that causes an increase in the expansion of a bronchus or bronchial tubes.
antitussiveAn agent that suppresses cough. Antitussives have a central or a peripheral action on the cough reflex, or a combination of both. Compare with expectorants, which are considered to increase the volume of secretions in the respiratory tract, so facilitating their removal by ciliary action and coughing, and mucolytics, which decrease the viscosity of mucus, facilitating its removal by ciliary action and expectoration.
anti-asthmatic drugA drug used to treat asthma.
[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
oxopurine
[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 (5)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency13.33320.001022.650876.6163AID1224839
chromobox protein homolog 1Homo sapiens (human)Potency100.00000.006026.168889.1251AID540317
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency12.58930.010323.856763.0957AID2662
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency22.38720.050127.073689.1251AID588590
Cellular tumor antigen p53Homo sapiens (human)Potency0.29850.002319.595674.0614AID651631
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (124)

Processvia Protein(s)Taxonomy
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (34)

Processvia Protein(s)Taxonomy
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (19)

Processvia Protein(s)Taxonomy
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (79)

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.
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.
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.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
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.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1874852Cmax in Gottingen minipig at 5 mg/kg, iv measured upto 24 hrs by HPLC-MS method2022ACS medicinal chemistry letters, Aug-11, Volume: 13, Issue:8
An Unexpected Deuterium-Induced Metabolic Switch in Doxophylline.
AID1874875Antifibrotic activity against Pseudomonas aeruginosa-induced pulmonary fibrosis C57BL/6 mouse model assessed as effect on poly(ADP-ribose) polymerase level at 80 mg/kg, os qd pretreated with compound for 1 hr followed by Pseudomonas aeruginosa instillatio2022ACS medicinal chemistry letters, Aug-11, Volume: 13, Issue:8
An Unexpected Deuterium-Induced Metabolic Switch in Doxophylline.
AID1874868Antifibrotic activity against BLM-induced lung injury C57BL/6 mouse model assessed as reduction in collagen thickness at 80 mg/kg, po qd pretreated with compound for 1 hr followed by BLM treatment and measured on day 21 by Masson trichrome staining based 2022ACS medicinal chemistry letters, Aug-11, Volume: 13, Issue:8
An Unexpected Deuterium-Induced Metabolic Switch in Doxophylline.
AID1874874Antifibrotic activity against Pseudomonas aeruginosa-induced pulmonary fibrosis C57BL/6 mouse model assessed as effect on nitrotyrosine expression at 80 mg/kg, os qd pretreated with compound for 1 hr followed by Pseudomonas aeruginosa instillation and mea2022ACS medicinal chemistry letters, Aug-11, Volume: 13, Issue:8
An Unexpected Deuterium-Induced Metabolic Switch in Doxophylline.
AID1874847Half life in CD1 mouse at 80 mg/kg, po measured upto 24 hrs by HPLC-MS method2022ACS medicinal chemistry letters, Aug-11, Volume: 13, Issue:8
An Unexpected Deuterium-Induced Metabolic Switch in Doxophylline.
AID1874851Half life in Gottingen minipig at 5 mg/kg, iv measured upto 24 hrs by HPLC-MS method2022ACS medicinal chemistry letters, Aug-11, Volume: 13, Issue:8
An Unexpected Deuterium-Induced Metabolic Switch in Doxophylline.
AID1874871Antifibrotic activity against Pseudomonas aeruginosa-induced pulmonary fibrosis C57BL/6 mouse model assessed as reduction in MPO level at 80 mg/kg, os qd pretreated with compound for 1 hr followed by Pseudomonas aeruginosa instillation and measured after 2022ACS medicinal chemistry letters, Aug-11, Volume: 13, Issue:8
An Unexpected Deuterium-Induced Metabolic Switch in Doxophylline.
AID1874843Half life in CD1 mouse at 20 mg/kg, iv measured upto 24 hrs by HPLC-MS method2022ACS medicinal chemistry letters, Aug-11, Volume: 13, Issue:8
An Unexpected Deuterium-Induced Metabolic Switch in Doxophylline.
AID1874849AUC (0 to t) in CD1 mouse at 80 mg/kg, po measured upto 24 hrs by HPLC-MS method2022ACS medicinal chemistry letters, Aug-11, Volume: 13, Issue:8
An Unexpected Deuterium-Induced Metabolic Switch in Doxophylline.
AID1874854Clearance in Gottingen minipig at 5 mg/kg, iv measured upto 24 hrs by HPLC-MS method2022ACS medicinal chemistry letters, Aug-11, Volume: 13, Issue:8
An Unexpected Deuterium-Induced Metabolic Switch in Doxophylline.
AID1874848Cmax in CD1 mouse at 80 mg/kg, po measured upto 24 hrs by HPLC-MS method2022ACS medicinal chemistry letters, Aug-11, Volume: 13, Issue:8
An Unexpected Deuterium-Induced Metabolic Switch in Doxophylline.
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.
AID1874850Apparent oral clearance in CD1 mouse at 80 mg/kg measured upto 24 hrs by HPLC-MS method2022ACS medicinal chemistry letters, Aug-11, Volume: 13, Issue:8
An Unexpected Deuterium-Induced Metabolic Switch in Doxophylline.
AID1874856Cmax in Gottingen minipig at 20 mg/kg, po measured upto 24 hrs by HPLC-MS method2022ACS medicinal chemistry letters, Aug-11, Volume: 13, Issue:8
An Unexpected Deuterium-Induced Metabolic Switch in Doxophylline.
AID1874870Antifibrotic activity against Pseudomonas aeruginosa-induced pulmonary fibrosis C57BL/6 mouse model assessed as reduction in accumulation of immune cells bronchoalveolar lavage at 80 mg/kg, os qd pretreated with compound for 1 hr followed by Pseudomonas a2022ACS medicinal chemistry letters, Aug-11, Volume: 13, Issue:8
An Unexpected Deuterium-Induced Metabolic Switch in Doxophylline.
AID1874877Antifibrotic activity against Pseudomonas aeruginosa-induced pulmonary fibrosis C57BL/6 mouse model assessed as decrease in lung inflammation at 80 mg/kg, os qd pretreated with compound for 1 hr followed by Pseudomonas aeruginosa instillation and measured2022ACS medicinal chemistry letters, Aug-11, Volume: 13, Issue:8
An Unexpected Deuterium-Induced Metabolic Switch in Doxophylline.
AID1874846Clearance in CD1 mouse at 20 mg/kg, iv measured upto 24 hrs by HPLC-MS method2022ACS medicinal chemistry letters, Aug-11, Volume: 13, Issue:8
An Unexpected Deuterium-Induced Metabolic Switch in Doxophylline.
AID1874855Half life in Gottingen minipig at 20 mg/kg, po measured upto 24 hrs by HPLC-MS method2022ACS medicinal chemistry letters, Aug-11, Volume: 13, Issue:8
An Unexpected Deuterium-Induced Metabolic Switch in Doxophylline.
AID1874866Antifibrotic activity against BLM-induced lung injury C57BL/6 mouse model assessed as decrease in MPO level at 80 mg/kg, po qd pretreated with compound for 1 hr followed by BLM treatment and measured on day 21 by colorimetric assay2022ACS medicinal chemistry letters, Aug-11, Volume: 13, Issue:8
An Unexpected Deuterium-Induced Metabolic Switch in Doxophylline.
AID1874869Antifibrotic activity against BLM-induced lung injury C57BL/6 mouse model assessed as reduction in collagen thickness at 80 mg/kg, po qd pretreated with compound for 1 hr followed by BLM treatment and measured on day 21 by picrosirius red staining method2022ACS medicinal chemistry letters, Aug-11, Volume: 13, Issue:8
An Unexpected Deuterium-Induced Metabolic Switch in Doxophylline.
AID1874872Antifibrotic activity against Pseudomonas aeruginosa-induced pulmonary fibrosis C57BL/6 mouse model assessed as reduction in inflammatory interstitial infiltrate at 80 mg/kg, os qd pretreated with compound for 1 hr followed by Pseudomonas aeruginosa insti2022ACS medicinal chemistry letters, Aug-11, Volume: 13, Issue:8
An Unexpected Deuterium-Induced Metabolic Switch in Doxophylline.
AID1874865Antifibrotic activity against BLM-induced lung injury C57BL/6 mouse model assessed as reduction in lung wet/dry ratio by measuring liquid accumulation at 80 mg/kg, po qd pretreated with compound for 1 hr followed by BLM treatment and measured on day 212022ACS medicinal chemistry letters, Aug-11, Volume: 13, Issue:8
An Unexpected Deuterium-Induced Metabolic Switch in Doxophylline.
AID1874873Antifibrotic activity against Pseudomonas aeruginosa-induced pulmonary fibrosis C57BL/6 mouse model assessed as effect on collagen deposition at 80 mg/kg, os qd pretreated with compound for 1 hr followed by Pseudomonas aeruginosa instillation and measured2022ACS medicinal chemistry letters, Aug-11, Volume: 13, Issue:8
An Unexpected Deuterium-Induced Metabolic Switch in Doxophylline.
AID1874867Antifibrotic activity against BLM-induced lung injury C57BL/6 mouse model assessed as decrease in inflammatory interstitial infiltrate at 80 mg/kg, po qd pretreated with compound for 1 hr followed by BLM treatment and measured on day 21 by H and E stainin2022ACS medicinal chemistry letters, Aug-11, Volume: 13, Issue:8
An Unexpected Deuterium-Induced Metabolic Switch in Doxophylline.
AID1874845AUC (0 to t) in CD1 mouse at 20 mg/kg, iv measured upto 24 hrs by HPLC-MS method2022ACS medicinal chemistry letters, Aug-11, Volume: 13, Issue:8
An Unexpected Deuterium-Induced Metabolic Switch in Doxophylline.
AID1874864Antifibrotic activity against BLM-induced lung injury C57BL/6 mouse model assessed as reduction in accumulation of immune cells bronchoalveolar lavage at 80 mg/kg, po qd pretreated with compound for 1 hr followed by BLM treatment and measured on day 21 by2022ACS medicinal chemistry letters, Aug-11, Volume: 13, Issue:8
An Unexpected Deuterium-Induced Metabolic Switch in Doxophylline.
AID1874858Apparent oral clearance in Gottingen minipig at 20 mg/kg measured upto 24 hrs by HPLC-MS method2022ACS medicinal chemistry letters, Aug-11, Volume: 13, Issue:8
An Unexpected Deuterium-Induced Metabolic Switch in Doxophylline.
AID1874844Cmax in CD1 mouse at 20 mg/kg, iv measured upto 24 hrs by HPLC-MS method2022ACS medicinal chemistry letters, Aug-11, Volume: 13, Issue:8
An Unexpected Deuterium-Induced Metabolic Switch in Doxophylline.
AID1874876Inhibition of Pseudomonas aeruginosa-induced apoptosis in C57BL/6 mouse at 80 mg/kg, os qd pretreated with compound for 1 hr followed by Pseudomonas aeruginosa instillation and measured after 7 days by TUNEL assay2022ACS medicinal chemistry letters, Aug-11, Volume: 13, Issue:8
An Unexpected Deuterium-Induced Metabolic Switch in Doxophylline.
AID1874853AUC (0 to t) in Gottingen minipig at 5 mg/kg, iv measured upto 24 hrs by HPLC-MS method2022ACS medicinal chemistry letters, Aug-11, Volume: 13, Issue:8
An Unexpected Deuterium-Induced Metabolic Switch in Doxophylline.
AID1874857AUC (0 to t) in Gottingen minipig at 20 mg/kg, po measured upto 24 hrs by HPLC-MS method2022ACS medicinal chemistry letters, Aug-11, Volume: 13, Issue:8
An Unexpected Deuterium-Induced Metabolic Switch in Doxophylline.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (94)

TimeframeStudies, This Drug (%)All Drugs %
pre-199011 (11.70)18.7374
1990's12 (12.77)18.2507
2000's14 (14.89)29.6817
2010's38 (40.43)24.3611
2020's19 (20.21)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 89.74

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index89.74 (24.57)
Research Supply Index4.86 (2.92)
Research Growth Index4.93 (4.65)
Search Engine Demand Index158.19 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (89.74)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials22 (20.75%)5.53%
Reviews13 (12.26%)6.00%
Case Studies1 (0.94%)4.05%
Observational1 (0.94%)0.25%
Other69 (65.09%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (4)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Efficacy Of Doxophylline As A Sparing Treatment For Inhaled Corticosteroids In Mexican Children With Asthma [NCT03879590]Phase 360 participants (Anticipated)Interventional2019-05-31Not yet recruiting
A Randomized, Open Labeled Comparative Study to Assess the Efficacy and Safety of Controller Medications as Add on to Inhaled Steroid and Long Acting β2 Agonist in Treatment of Moderate to Severe Persistent Bronchial Asthma [NCT01055041]50 participants (Actual)Interventional2008-12-31Completed
Effect of Doxofylline on Bronchial Obstruction, in add-on to Maximal Inhalation Therapy, in Clinically Stable COPD Patients. [NCT04238221]Phase 478 participants (Anticipated)Interventional2020-09-01Not yet recruiting
Efficacy and Safety Study of Acetylcysteine/Doxofylline 1200/400 mg Effervescent Tablet in the Treatment of Moderate-Severe Chronic Obstructive Pulmonary Disease (COPD) [NCT03388853]Phase 468 participants (Actual)Interventional2018-02-20Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]