Compounds > l 659286
Page last updated: 2024-12-07

l 659286

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

Description

L 659286: structure given in first source; RN given from Toxlit 6/89 [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID128954
CHEMBL ID123153
MeSH IDM0165708

Synonyms (14)

Synonym
l 659,286
l 659286
CHEMBL123153 ,
3-(6-hydroxy-2-methyl-5-oxo-2,5-dihydro-[1,2,4]triazin-3-ylsulfanylmethyl)-7-methoxy-5,5-dioxo-2-(pyrrolidine-1-carbonyl)-5lambda*6*-thia-1-aza-bicyclo[4.2.0]oct-2-en-8-one
bdbm50003159
l-659,286
7-methoxy-8-oxo-3-(((1,2,5,6-tetrahydro-2-methyl-5,6-dioxo-1,2,4-triazin-3-yl)thio)methyl)-5-thia-1-aza-6-bicyclo(4.2.0)oct-2-ene-2-pyrrolidenecarboxamide-5-dioxide
pyrrolidine, 1-((7-methoxy-8-oxo-3-(((1,2,5,6-tetrahydro-2-methyl-5,6-dioxo-1,2,4-triazin-3-yl)thio)methyl)-5-thia-1-azabicyclo(4.2.0)oct-2-en-2-yl)carbonyl)-, s,s-dioxide, (6r-cis)-
l-659286
119742-06-2
DTXSID80152571
3-((((6r,7s)-7-methoxy-5,5-dioxido-8-oxo-2-(pyrrolidine-1-carbonyl)-5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl)methyl)thio)-2-methyl-1,2-dihydro-1,2,4-triazine-5,6-dione
3-[[(6r,7s)-7-methoxy-5,5,8-trioxo-2-(pyrrolidine-1-carbonyl)-5lambda6-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl]methylsulfanyl]-2-methyl-1h-1,2,4-triazine-5,6-dione
AKOS040752316
[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)
Neutrophil elastaseHomo sapiens (human)IC50 (µMol)2.00000.00632.073422.3780AID66502
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (25)

Processvia Protein(s)Taxonomy
proteolysisNeutrophil elastaseHomo sapiens (human)
negative regulation of transcription by RNA polymerase IINeutrophil elastaseHomo sapiens (human)
response to yeastNeutrophil elastaseHomo sapiens (human)
leukocyte migration involved in inflammatory responseNeutrophil elastaseHomo sapiens (human)
biosynthetic process of antibacterial peptides active against Gram-negative bacteriaNeutrophil elastaseHomo sapiens (human)
proteolysisNeutrophil elastaseHomo sapiens (human)
intracellular calcium ion homeostasisNeutrophil elastaseHomo sapiens (human)
response to UVNeutrophil elastaseHomo sapiens (human)
extracellular matrix disassemblyNeutrophil elastaseHomo sapiens (human)
protein catabolic processNeutrophil elastaseHomo sapiens (human)
response to lipopolysaccharideNeutrophil elastaseHomo sapiens (human)
negative regulation of chemokine productionNeutrophil elastaseHomo sapiens (human)
negative regulation of interleukin-8 productionNeutrophil elastaseHomo sapiens (human)
positive regulation of interleukin-8 productionNeutrophil elastaseHomo sapiens (human)
defense response to bacteriumNeutrophil elastaseHomo sapiens (human)
positive regulation of MAP kinase activityNeutrophil elastaseHomo sapiens (human)
positive regulation of smooth muscle cell proliferationNeutrophil elastaseHomo sapiens (human)
negative regulation of inflammatory responseNeutrophil elastaseHomo sapiens (human)
positive regulation of immune responseNeutrophil elastaseHomo sapiens (human)
negative regulation of chemotaxisNeutrophil elastaseHomo sapiens (human)
pyroptosisNeutrophil elastaseHomo sapiens (human)
neutrophil-mediated killing of gram-negative bacteriumNeutrophil elastaseHomo sapiens (human)
neutrophil-mediated killing of fungusNeutrophil elastaseHomo sapiens (human)
positive regulation of leukocyte tethering or rollingNeutrophil elastaseHomo sapiens (human)
phagocytosisNeutrophil elastaseHomo sapiens (human)
acute inflammatory response to antigenic stimulusNeutrophil elastaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (8)

Processvia Protein(s)Taxonomy
protease bindingNeutrophil elastaseHomo sapiens (human)
transcription corepressor activityNeutrophil elastaseHomo sapiens (human)
endopeptidase activityNeutrophil elastaseHomo sapiens (human)
serine-type endopeptidase activityNeutrophil elastaseHomo sapiens (human)
protein bindingNeutrophil elastaseHomo sapiens (human)
heparin bindingNeutrophil elastaseHomo sapiens (human)
peptidase activityNeutrophil elastaseHomo sapiens (human)
cytokine bindingNeutrophil elastaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (12)

Processvia Protein(s)Taxonomy
extracellular regionNeutrophil elastaseHomo sapiens (human)
extracellular spaceNeutrophil elastaseHomo sapiens (human)
cytoplasmNeutrophil elastaseHomo sapiens (human)
cytosolNeutrophil elastaseHomo sapiens (human)
cell surfaceNeutrophil elastaseHomo sapiens (human)
secretory granuleNeutrophil elastaseHomo sapiens (human)
azurophil granule lumenNeutrophil elastaseHomo sapiens (human)
specific granule lumenNeutrophil elastaseHomo sapiens (human)
phagocytic vesicleNeutrophil elastaseHomo sapiens (human)
collagen-containing extracellular matrixNeutrophil elastaseHomo sapiens (human)
extracellular exosomeNeutrophil elastaseHomo sapiens (human)
transcription repressor complexNeutrophil elastaseHomo sapiens (human)
extracellular spaceNeutrophil elastaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (16)

Assay IDTitleYearJournalArticle
AID85168Compound was evaluated in vivo for inhibition of HLE-induced hemorrhage in hamster lung at 10 ug 30 min after administration prior to HLE1992Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
Inhibition of human leukocyte elastase. 4. Selection of a substituted cephalosporin (L-658,758) as a topical aerosol.
AID22754Reactivation time of the compound1992Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
Inhibition of human leukocyte elastase. 4. Selection of a substituted cephalosporin (L-658,758) as a topical aerosol.
AID226713Partion ratio of the compound1992Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
Inhibition of human leukocyte elastase. 4. Selection of a substituted cephalosporin (L-658,758) as a topical aerosol.
AID99429Inhibitory activity against Human Leukocyte Elastase by Lung Hemorrhage assay1992Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
Inhibition of human leukocyte elastase. 4. Selection of a substituted cephalosporin (L-658,758) as a topical aerosol.
AID85175Compound was evaluated in vivo for inhibition of HLE-induced hemorrhage in hamster lung at 200 microg 4 hr after administration prior to HLE1992Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
Inhibition of human leukocyte elastase. 4. Selection of a substituted cephalosporin (L-658,758) as a topical aerosol.
AID83854Inhibitory activity against Human Leukocyte Elastase by Lung Hemorrhage assay ( at 200 ug/animal)1992Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
Inhibition of human leukocyte elastase. 4. Selection of a substituted cephalosporin (L-658,758) as a topical aerosol.
AID85172Compound was evaluated in vivo for inhibition of HLE-induced hemorrhage in hamster lung at 200 microg 1 hr after administration prior to HLE1992Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
Inhibition of human leukocyte elastase. 4. Selection of a substituted cephalosporin (L-658,758) as a topical aerosol.
AID67477In vitro inhibitory activity against human leukocyte elastase1992Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
Inhibition of human leukocyte elastase. 4. Selection of a substituted cephalosporin (L-658,758) as a topical aerosol.
AID84853Inhibitory activity against Human Leukocyte Elastase by Lung Hemorrhage assay (Effective dose at 15 microg)1992Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
Inhibition of human leukocyte elastase. 4. Selection of a substituted cephalosporin (L-658,758) as a topical aerosol.
AID85173Compound was evaluated in vivo for inhibition of HLE-induced hemorrhage in hamster lung at 200 microg 2 hr after administration prior to HLE1992Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
Inhibition of human leukocyte elastase. 4. Selection of a substituted cephalosporin (L-658,758) as a topical aerosol.
AID85174Compound was evaluated in vivo for inhibition of HLE-induced hemorrhage in hamster lung at 200 microg 3h after administration prior to HLE1992Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
Inhibition of human leukocyte elastase. 4. Selection of a substituted cephalosporin (L-658,758) as a topical aerosol.
AID84852Inhibitory activity against Human Leukocyte Elastase by Lung Hemorrhage assay (at 30 min)1992Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
Inhibition of human leukocyte elastase. 4. Selection of a substituted cephalosporin (L-658,758) as a topical aerosol.
AID66502Inhibitory activity against Human Leukocyte Elastase1992Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
Inhibition of human leukocyte elastase. 4. Selection of a substituted cephalosporin (L-658,758) as a topical aerosol.
AID85036Compound was evaluated in vivo for inhibition of HLE-induced hemorrhage in hamster lung at 100 microg 30 min after administration prior to HLE1992Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
Inhibition of human leukocyte elastase. 4. Selection of a substituted cephalosporin (L-658,758) as a topical aerosol.
AID85185Compound was evaluated in vivo for inhibition of HLE-induced hemorrhage in hamster lung at 30 ug 30 min after administration prior to HLE1992Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
Inhibition of human leukocyte elastase. 4. Selection of a substituted cephalosporin (L-658,758) as a topical aerosol.
AID23172Half-life value of the compound.1992Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
Inhibition of human leukocyte elastase. 4. Selection of a substituted cephalosporin (L-658,758) as a topical aerosol.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (20.00)18.7374
1990's4 (80.00)18.2507
2000's0 (0.00)29.6817
2010's0 (0.00)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: 13.09

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

MetricThis Compound (vs All)
Research Demand Index13.09 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.88 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (13.09)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (20.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other4 (80.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
cephalosporin c
cephalosporin C: RN given refers to parent cpd; structure in Merck, 9th ed, #1937. cephalosporin C : A cephalosporin antibiotic carrying a 3-acetoxymethyl substituent and a 6-oxo-N(6)-L-lysino group at position 7.		3.9940cephalosporinfungal metabolite
l 658758
L 658758: structure & chemical name given in UD		3.9940
ConditionIndicatedRelationship StrengthStudiesTrials
Bleeding
[description not available]		01.9710
Disease, Pulmonary
[description not available]		01.9710
Hemorrhage
Bleeding or escape of blood from a vessel.		01.9710
Lung Diseases
Pathological processes involving any part of the LUNG.		01.9710