Page last updated: 2024-12-06

doxantrazole

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

Description

doxantrazole: structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID40119
CHEMBL ID22336
SCHEMBL ID5494067
MeSH IDM0055425

Synonyms (35)

Synonym
HMS1673H18
10,10-dioxo-3-(1h-tetrazol-5-yl)thioxanthen-9-one
3-(1h-tetraazol-5-yl)-9h-thioxanthen-9-one 10,10-dioxide
NCI60_002690
mls003115914 ,
nsc311586
nsc-311586
51762-95-9
doxantrazole
doxantrol
OPREA1_710946
OPREA1_382578
3-(5-tetrazolyl)thioxanthone-10,10-dioxide
nsc 311586
3-(1h-tetrazol-5-yl)-9h-thioxanthen-9-one 10,10-dioxide
einecs 257-397-0
CHEMBL22336
AKOS000520902
smr000111703
10,10-dioxo-3-(2h-tetrazol-5-yl)thioxanthen-9-one
bdbm50414228
u5q9uw0hch ,
unii-u5q9uw0hch
bw-59c
3-(5-tetrazolyl)thioxanthen-9-one 10,10-dioxide
3-(5tetrazolyl)thioxanthone-10,10-dioxide
VIDCTSLIEZMQRF-UHFFFAOYSA-N
3-(5-tetrazolyl) thioxanthone-10,10-dioxide
SCHEMBL5494067
DTXSID70199692
91x ,
3-(1h-tetrazol-5-yl)-10lambda~6~-thioxanthene-9,10,10-trione
3-(5-tetrazolyl) thioxanthone 10,10-dioxide
BRD-K78868812-001-06-7
Q27290721

Research Excerpts

Treatment

ExcerptReferenceRelevance
"Pretreatment with doxantrazole and GSK143 (0.03-10 μM) concentration dependently blocked substance P and trinitrophenyl induced β-hexosaminidase release."( Inhibition of spleen tyrosine kinase as treatment of postoperative ileus.
Boeckxstaens, GE; Cailotto, C; de Jonge, WJ; Di Giovangiulio, M; Farro, G; Gomez-Pinilla, PJ; Lee, K; Lugo, D; Matteoli, G; Nemethova, A; Ramirez-Molina, C; Skynner, MJ; van Bree, SH; van de Bovenkamp, FS, 2013
)
0.71

Bioavailability

ExcerptReferenceRelevance
" In vitro availability was determined from absorption rate constants and absorption profiles obtained using the Sartorius absorption and solubility simulators."( Correlation of bioavailability in man with simulated absorption data for three doxantrazole preparations.
Bye, A; Jones, H, 1979
)
0.49

Dosage Studied

ExcerptRelevanceReference
" Both substance P and histamine produced sigmoid dose-response curves for the following parameters: 1 min and 5 min planimetrically measured areas of erythema, and mean diameter of weal."( Vascular responses of human skin to injection of substance P and mechanism of action.
Coutts, AA; Eady, RA; Greaves, MW; Jorizzo, JL, 1983
)
0.27
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
USP1 protein, partialHomo sapiens (human)Potency39.81070.031637.5844354.8130AID743255
[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)
Serine/threonine-protein kinase Chk1Homo sapiens (human)Ki0.50120.00050.23480.6590AID419415
[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)
G-protein coupled receptor 35Homo sapiens (human)EC50 (µMol)3.40000.00202.50079.8000AID1354835
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (35)

Processvia Protein(s)Taxonomy
DNA damage checkpoint signalingSerine/threonine-protein kinase Chk1Homo sapiens (human)
G2/M transition of mitotic cell cycleSerine/threonine-protein kinase Chk1Homo sapiens (human)
inner cell mass cell proliferationSerine/threonine-protein kinase Chk1Homo sapiens (human)
DNA replicationSerine/threonine-protein kinase Chk1Homo sapiens (human)
DNA repairSerine/threonine-protein kinase Chk1Homo sapiens (human)
chromatin remodelingSerine/threonine-protein kinase Chk1Homo sapiens (human)
protein phosphorylationSerine/threonine-protein kinase Chk1Homo sapiens (human)
apoptotic processSerine/threonine-protein kinase Chk1Homo sapiens (human)
DNA damage responseSerine/threonine-protein kinase Chk1Homo sapiens (human)
nucleus organizationSerine/threonine-protein kinase Chk1Homo sapiens (human)
mitotic G2 DNA damage checkpoint signalingSerine/threonine-protein kinase Chk1Homo sapiens (human)
regulation of double-strand break repair via homologous recombinationSerine/threonine-protein kinase Chk1Homo sapiens (human)
peptidyl-threonine phosphorylationSerine/threonine-protein kinase Chk1Homo sapiens (human)
regulation of cell population proliferationSerine/threonine-protein kinase Chk1Homo sapiens (human)
signal transduction in response to DNA damageSerine/threonine-protein kinase Chk1Homo sapiens (human)
mitotic G2/M transition checkpointSerine/threonine-protein kinase Chk1Homo sapiens (human)
positive regulation of cell cycleSerine/threonine-protein kinase Chk1Homo sapiens (human)
negative regulation of gene expression, epigeneticSerine/threonine-protein kinase Chk1Homo sapiens (human)
negative regulation of mitotic nuclear divisionSerine/threonine-protein kinase Chk1Homo sapiens (human)
regulation of mitotic centrosome separationSerine/threonine-protein kinase Chk1Homo sapiens (human)
negative regulation of G0 to G1 transitionSerine/threonine-protein kinase Chk1Homo sapiens (human)
cellular response to mechanical stimulusSerine/threonine-protein kinase Chk1Homo sapiens (human)
cellular response to caffeineSerine/threonine-protein kinase Chk1Homo sapiens (human)
replicative senescenceSerine/threonine-protein kinase Chk1Homo sapiens (human)
regulation of signal transduction by p53 class mediatorSerine/threonine-protein kinase Chk1Homo sapiens (human)
apoptotic process involved in developmentSerine/threonine-protein kinase Chk1Homo sapiens (human)
negative regulation of DNA biosynthetic processSerine/threonine-protein kinase Chk1Homo sapiens (human)
cytoskeleton organizationG-protein coupled receptor 35Homo sapiens (human)
G protein-coupled receptor signaling pathwayG-protein coupled receptor 35Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationG-protein coupled receptor 35Homo sapiens (human)
chemokine-mediated signaling pathwayG-protein coupled receptor 35Homo sapiens (human)
negative regulation of voltage-gated calcium channel activityG-protein coupled receptor 35Homo sapiens (human)
negative regulation of neuronal action potentialG-protein coupled receptor 35Homo sapiens (human)
positive regulation of Rho protein signal transductionG-protein coupled receptor 35Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayG-protein coupled receptor 35Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (9)

Processvia Protein(s)Taxonomy
protein kinase activitySerine/threonine-protein kinase Chk1Homo sapiens (human)
protein serine/threonine kinase activitySerine/threonine-protein kinase Chk1Homo sapiens (human)
protein bindingSerine/threonine-protein kinase Chk1Homo sapiens (human)
ATP bindingSerine/threonine-protein kinase Chk1Homo sapiens (human)
protein domain specific bindingSerine/threonine-protein kinase Chk1Homo sapiens (human)
histone H3T11 kinase activitySerine/threonine-protein kinase Chk1Homo sapiens (human)
protein serine kinase activitySerine/threonine-protein kinase Chk1Homo sapiens (human)
C-X-C chemokine receptor activityG-protein coupled receptor 35Homo sapiens (human)
G protein-coupled receptor activityG-protein coupled receptor 35Homo sapiens (human)
C-X-C chemokine receptor activityG-protein coupled receptor 35Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (13)

Processvia Protein(s)Taxonomy
chromosome, telomeric regionSerine/threonine-protein kinase Chk1Homo sapiens (human)
condensed nuclear chromosomeSerine/threonine-protein kinase Chk1Homo sapiens (human)
extracellular spaceSerine/threonine-protein kinase Chk1Homo sapiens (human)
nucleusSerine/threonine-protein kinase Chk1Homo sapiens (human)
nucleoplasmSerine/threonine-protein kinase Chk1Homo sapiens (human)
replication forkSerine/threonine-protein kinase Chk1Homo sapiens (human)
cytoplasmSerine/threonine-protein kinase Chk1Homo sapiens (human)
centrosomeSerine/threonine-protein kinase Chk1Homo sapiens (human)
cytosolSerine/threonine-protein kinase Chk1Homo sapiens (human)
intracellular membrane-bounded organelleSerine/threonine-protein kinase Chk1Homo sapiens (human)
chromatinSerine/threonine-protein kinase Chk1Homo sapiens (human)
protein-containing complexSerine/threonine-protein kinase Chk1Homo sapiens (human)
nucleusSerine/threonine-protein kinase Chk1Homo sapiens (human)
plasma membraneG-protein coupled receptor 35Homo sapiens (human)
plasma membraneG-protein coupled receptor 35Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (33)

Assay IDTitleYearJournalArticle
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.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1354835Agonist activity at recombinant human N-terminal FLAG/eYFP-fused GPR35a expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment by path hunter assay2018ACS medicinal chemistry letters, May-10, Volume: 9, Issue:5
SAR Studies of
AID1134494Antiallergic activity in rat peritoneal mast cells assessed as inhibition of ovalbumin-induced histamine release after 15 mins1979Journal of medicinal chemistry, Jun, Volume: 22, Issue:6
Antiallergy activity of substituted 11-oxo-11 H-pyrido[2,1-b]quinazoline-8-carboxylic acids.
AID80624Percent relaxation using isolated guinea pig trachea.1998Bioorganic & medicinal chemistry letters, Mar-03, Volume: 8, Issue:5
New bronchodilators selected by molecular topology.
AID80631Percent relaxation of isolated guinea pig trachea.1998Bioorganic & medicinal chemistry letters, Mar-03, Volume: 8, Issue:5
New bronchodilators selected by molecular topology.
AID178099Antiallergic activity is evaluated for its ability to inhibit reaginic passive cutaneous anaphylaxis (PCA) in rats dosed intravenously1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
Antiallergy activity of 10-oxo-10-H-pyridazino[6,1-b]quinazoline-2-carboxylic acids.
AID127166Inhibitory activity against rat brain mitochondrial Monoamine oxidase B at 10 uM1996Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9
Selective inhibitors of monoamine oxidase. 3. Structure-activity relationship of tricyclics bearing imidazoline, oxadiazole, or tetrazole groups.
AID1123059Inhibition of passive cutaneous anaphylaxis in po dosed Sprague-Dawley rat1979Journal of medicinal chemistry, Jul, Volume: 22, Issue:7
Inhibition of rat passive cutaneous anaphylaxis by 3-(tetrazol-5-yl)quinolines.
AID419415Inhibition of Chk12009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Large-scale application of high-throughput molecular mechanics with Poisson-Boltzmann surface area for routine physics-based scoring of protein-ligand complexes.
AID185145The compound was tested for inhibition of rat passive cutaneous anaphylaxis at 10 mg/kg dose after intraperitoneal administration1980Journal of medicinal chemistry, Nov, Volume: 23, Issue:11
Synthesis and antiallergy activity of 4-oxopyrano[3,2-b]indoles.
AID1134495Antiallergic activity in po dosed rat allergic bronchoconstriction model assessed as reduction in respiratory flow rate administered 15 to 30 mins prior to ovalbumin challenge measured after 10 mins1979Journal of medicinal chemistry, Jun, Volume: 22, Issue:6
Antiallergy activity of substituted 11-oxo-11 H-pyrido[2,1-b]quinazoline-8-carboxylic acids.
AID1134493Antiallergic activity in po dosed rat assessed as inhibition of ovalbumin-induced passive cutaneous anaphylaxis1979Journal of medicinal chemistry, Jun, Volume: 22, Issue:6
Antiallergy activity of substituted 11-oxo-11 H-pyrido[2,1-b]quinazoline-8-carboxylic acids.
AID1123585Antiallergic activity in po dosed rat assessed as inhibition of ovalbumin-induced passive cutaneous anaphylaxis pretreated for 10 to 15 mins followed by ovalbumin challenge1979Journal of medicinal chemistry, Jan, Volume: 22, Issue:1
11-Oxo-11H-pyrido[2,1-b]quinazoline-8-carboxylic acid, an orally active antiallergy agent.
AID185143Inhibition of rat passive cutaneous anaphylaxis at 1.0 mg/kg dose after intraperitoneal administration1980Journal of medicinal chemistry, Nov, Volume: 23, Issue:11
Synthesis and antiallergy activity of 4-oxopyrano[3,2-b]indoles.
AID1134492Antiallergic activity in iv dosed rat assessed as inhibition of ovalbumin-induced passive cutaneous anaphylaxis1979Journal of medicinal chemistry, Jun, Volume: 22, Issue:6
Antiallergy activity of substituted 11-oxo-11 H-pyrido[2,1-b]quinazoline-8-carboxylic acids.
AID1134496Antiallergic activity in po dosed rat allergic bronchoconstriction model assessed as survival from death by bronchoconstriction administered 15 to 30 mins prior to ovalbumin challenge measured after 10 mins1979Journal of medicinal chemistry, Jun, Volume: 22, Issue:6
Antiallergy activity of substituted 11-oxo-11 H-pyrido[2,1-b]quinazoline-8-carboxylic acids.
AID178101Antiallergic activity is evaluated for its ability to inhibit reaginic passive cutaneous anaphylaxis (PCA) in rats dosed perorally1980Journal of medicinal chemistry, Aug, Volume: 23, Issue:8
Antiallergy activity of 10-oxo-10-H-pyridazino[6,1-b]quinazoline-2-carboxylic acids.
AID1123583Antiallergic activity in iv dosed rat assessed as inhibition of ovalbumin-induced passive cutaneous anaphylaxis dosed along with ovalbumin challenge1979Journal of medicinal chemistry, Jan, Volume: 22, Issue:1
11-Oxo-11H-pyrido[2,1-b]quinazoline-8-carboxylic acid, an orally active antiallergy agent.
AID182775Compound was tested for antiallergic activity in the rat passive cutaneous anaphylaxis, after intravenous administration1981Journal of medicinal chemistry, Jul, Volume: 24, Issue:7
Synthesis and antiallergy activity of 4-oxo-4H-pyrido[1,2-a]thieno[2,3-d]pyrimidines.
AID185273Inhibition of rat passive cutaneous anaphylaxis at 5.0 mg/kg dose after peroral administration1980Journal of medicinal chemistry, Nov, Volume: 23, Issue:11
Synthesis and antiallergy activity of 4-oxopyrano[3,2-b]indoles.
AID182774Compound was tested for antiallergic activity in the rat passive cutaneous anaphylaxis, after peroral administration1981Journal of medicinal chemistry, Jul, Volume: 24, Issue:7
Synthesis and antiallergy activity of 4-oxo-4H-pyrido[1,2-a]thieno[2,3-d]pyrimidines.
AID126204Inhibitory concentration against rat brain mitochondrial Monoamine oxidase A at 10 uM1996Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9
Selective inhibitors of monoamine oxidase. 3. Structure-activity relationship of tricyclics bearing imidazoline, oxadiazole, or tetrazole groups.
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.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (82)

TimeframeStudies, This Drug (%)All Drugs %
pre-199034 (41.46)18.7374
1990's16 (19.51)18.2507
2000's17 (20.73)29.6817
2010's14 (17.07)24.3611
2020's1 (1.22)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 19.13

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index19.13 (24.57)
Research Supply Index4.45 (2.92)
Research Growth Index4.28 (4.65)
Search Engine Demand Index18.60 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (19.13)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials3 (3.66%)5.53%
Reviews1 (1.22%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other78 (95.12%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]