Compounds > xr 334
Page last updated: 2024-12-11

xr 334

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

Description

XR 334: a low molecular weight modulator of human plasminogen activator inhibitor-1 activity; structure given in first source; RN given refers to (Z,Z)-isomer [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9797139
CHEMBL ID49073
SCHEMBL ID6372616
MeSH IDM0269400

Synonyms (15)

Synonym
(3z,6z)-3-benzylidene-6-[(4-methoxyphenyl)methylidene]piperazine-2,5-dione
3-[1-(4-methoxy-phenyl)-meth-(z)-ylidene]-6-[1-phenyl-meth-(z)-ylidene]-piperazine-2,5-dione
bdbm50127731
3-(4-methoxy-benzylidene)-6-[1-phenyl-meth-(z)-ylidene]-piperazine-2,5-dione
CHEMBL49073 ,
74720-35-7
2,5-piperazinedione, 3-((4-methoxyphenyl)methylene)-6-(phenylmethylene)-, (z,z)-
3-benzylidene-6-(4'-methoxybenzylidene)piperazine-2,5-dione
xr-334
xr334
xr 334
SCHEMBL6372616
(3z,6z)-6-benzylidene-3-(4-methoxybenzylidene)-2,5-piperazinedione
QMUALMJMQXNBIA-LSQIQBGYSA-N ,
AKOS040754469
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Plasminogen activator inhibitor 1Homo sapiens (human)IC50 (µMol)59.40000.09104.892810.0000AID158355
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (27)

Processvia Protein(s)Taxonomy
angiogenesisPlasminogen activator inhibitor 1Homo sapiens (human)
regulation of signaling receptor activityPlasminogen activator inhibitor 1Homo sapiens (human)
negative regulation of plasminogen activationPlasminogen activator inhibitor 1Homo sapiens (human)
negative regulation of endopeptidase activityPlasminogen activator inhibitor 1Homo sapiens (human)
negative regulation of smooth muscle cell migrationPlasminogen activator inhibitor 1Homo sapiens (human)
positive regulation of blood coagulationPlasminogen activator inhibitor 1Homo sapiens (human)
negative regulation of blood coagulationPlasminogen activator inhibitor 1Homo sapiens (human)
negative regulation of cell migrationPlasminogen activator inhibitor 1Homo sapiens (human)
positive regulation of interleukin-8 productionPlasminogen activator inhibitor 1Homo sapiens (human)
negative regulation of cell adhesion mediated by integrinPlasminogen activator inhibitor 1Homo sapiens (human)
positive regulation of leukotriene production involved in inflammatory responsePlasminogen activator inhibitor 1Homo sapiens (human)
fibrinolysisPlasminogen activator inhibitor 1Homo sapiens (human)
positive regulation of angiogenesisPlasminogen activator inhibitor 1Homo sapiens (human)
positive regulation of receptor-mediated endocytosisPlasminogen activator inhibitor 1Homo sapiens (human)
positive regulation of inflammatory responsePlasminogen activator inhibitor 1Homo sapiens (human)
defense response to Gram-negative bacteriumPlasminogen activator inhibitor 1Homo sapiens (human)
negative regulation of fibrinolysisPlasminogen activator inhibitor 1Homo sapiens (human)
negative regulation of vascular wound healingPlasminogen activator inhibitor 1Homo sapiens (human)
negative regulation of wound healingPlasminogen activator inhibitor 1Homo sapiens (human)
cellular response to lipopolysaccharidePlasminogen activator inhibitor 1Homo sapiens (human)
positive regulation of monocyte chemotaxisPlasminogen activator inhibitor 1Homo sapiens (human)
replicative senescencePlasminogen activator inhibitor 1Homo sapiens (human)
dentinogenesisPlasminogen activator inhibitor 1Homo sapiens (human)
positive regulation of odontoblast differentiationPlasminogen activator inhibitor 1Homo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathway via death domain receptorsPlasminogen activator inhibitor 1Homo sapiens (human)
negative regulation of smooth muscle cell-matrix adhesionPlasminogen activator inhibitor 1Homo sapiens (human)
negative regulation of endothelial cell apoptotic processPlasminogen activator inhibitor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (4)

Processvia Protein(s)Taxonomy
protease bindingPlasminogen activator inhibitor 1Homo sapiens (human)
serine-type endopeptidase inhibitor activityPlasminogen activator inhibitor 1Homo sapiens (human)
signaling receptor bindingPlasminogen activator inhibitor 1Homo sapiens (human)
protein bindingPlasminogen activator inhibitor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (8)

Processvia Protein(s)Taxonomy
collagen-containing extracellular matrixPlasminogen activator inhibitor 1Homo sapiens (human)
extracellular regionPlasminogen activator inhibitor 1Homo sapiens (human)
extracellular spacePlasminogen activator inhibitor 1Homo sapiens (human)
plasma membranePlasminogen activator inhibitor 1Homo sapiens (human)
platelet alpha granule lumenPlasminogen activator inhibitor 1Homo sapiens (human)
collagen-containing extracellular matrixPlasminogen activator inhibitor 1Homo sapiens (human)
extracellular exosomePlasminogen activator inhibitor 1Homo sapiens (human)
serine protease inhibitor complexPlasminogen activator inhibitor 1Homo sapiens (human)
peptidase inhibitor complexPlasminogen activator inhibitor 1Homo sapiens (human)
extracellular spacePlasminogen activator inhibitor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (2)

Assay IDTitleYearJournalArticle
AID39065Compound was tested for brine shrimp (Artemia salina) toxicity measured as the lowest value at which severe inhibition of nauplii movement was observed2000Bioorganic & medicinal chemistry letters, Jan-17, Volume: 10, Issue:2
Solution-phase combinatorial synthesis and evaluation of piperazine-2,5-dione derivatives.
AID158355Inhibitory activity against plasminogen activator inhibitor 1 (PAI-1) was evaluated by inhibition of tissue plasminogen activator/PAI-1 complex formation in t-PA-induced fibrin clot lysis assay2003Bioorganic & medicinal chemistry letters, May-19, Volume: 13, Issue:10
New fibrinolytic agents: benzothiophene derivatives as inhibitors of the t-PA-PAI-1 complex formation.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's2 (33.33)18.2507
2000's2 (33.33)29.6817
2010's2 (33.33)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 29.02

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 Index29.02 (24.57)
Research Supply Index1.95 (2.92)
Research Growth Index4.64 (4.65)
Search Engine Demand Index55.82 (26.88)
Search Engine Supply Index3.78 (0.95)

This Compound (29.02)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other6 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
npi 2358
NPI 2358: antineoplastic; structure in first source. plinabulin : A member of the class of 2,5-diketopiperazines that is piperazine-2,5-dione substituted by benzylidene and (5-tert-butyl-1H-imidazol-4-yl)methylidene groups at positions 3 and 6, respectively. It is a vascular disrupting agent and a microtubule destabalising agent which was in clinical trials (now discontinued) for the treatment of non-small cell lung cancer.		2.11102,5-diketopiperazines;
benzenes;
imidazoles;
olefinic compound		angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
microtubule-destabilising agent
ConditionIndicatedRelationship StrengthStudiesTrials