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bms-262084

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Description

BMS-262084: an azetidinone-based tryptase inhibitor; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9802488
CHEMBL ID71037
MeSH IDM0442226

Synonyms (20)

Synonym
(r)-1-(4-tert-butylcarbamoyl-piperazine-1-carbonyl)-3-(3-guanidino-propyl)-4-oxo-azetidine-2-carboxylic acid
(3s,4r)-1-(4-tert-butylcarbamoyl-piperazine-1-carbonyl)-3-(3-guanidino-propyl)-4-oxo-azetidine-2-carboxylic acid
(2s,3r)-1-(4-tert-butylcarbamoyl-piperazine-1-carbonyl)-3-(3-guanidino-propyl)-4-oxo-azetidine-2-carboxylic acid
bdbm50120368
bms-262084
CHEMBL71037 ,
(-)-bms-262084
unii-i0ir71971g
i0ir71971g ,
2-azetidinecarboxylic acid, 3-(3-((aminoiminomethyl)amino)propyl)-1-((4-(((1,1-dimethylethyl)amino)carbonyl)-1-piperazinyl)carbonyl)-4-oxo-, (2s,3r)-
253174-92-4
bdbm50220841
253172-74-6
EX-A5488
Q27280202
HY-118969
(2s,3r)-1-[4-(tert-butylcarbamoyl)piperazine-1-carbonyl]-3-[3-(diaminomethylideneamino)propyl]-4-oxoazetidine-2-carboxylic acid
CS-0078186
AKOS040750848
(2s,3r)-1-(4-(tert-butylcarbamoyl)piperazine-1-carbonyl)-3-(3-guanidinopropyl)-4-oxoazetidine-2-carboxylic acid

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" From these studies compound 2, BMS-262084, was identified as a potent and selective tryptase inhibitor which, when dosed intratracheally in ovalbumin-sensitized guinea pigs, reduced allergen-induced bronchoconstriction and inflammatory cell infiltration into the lung."( Synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.
Bisacchi, GS; Bolton, SA; Hartl, KS; Huang, MH; Jacobs, G; Meng, W; Ogletree, ML; Pi, Z; Schumacher, WA; Seiler, SM; Slusarchyk, WA; Sutton, JC; Treuner, U; Zahler, R; Zhao, G, 2002
)
0.6
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (13)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Urokinase-type plasminogen activatorHomo sapiens (human)IC50 (µMol)0.13500.03703.385910.0000AID213436
Tissue-type plasminogen activatorHomo sapiens (human)IC50 (µMol)8.25000.03402.54256.6000AID210912
Cationic trypsinBos taurus (cattle)IC50 (µMol)0.07200.00003.479210.0000AID214871
Coagulation factor XIHomo sapiens (human)IC50 (µMol)0.00280.00282.639110.0000AID1074166; AID1384597
Trypsin-1Homo sapiens (human)IC50 (µMol)0.02730.00351.532110.0000AID1384599; AID215727
Trypsin-2Homo sapiens (human)IC50 (µMol)0.05000.00351.58464.4000AID1384599
Trypsin-3Homo sapiens (human)IC50 (µMol)0.05000.00351.58464.4000AID1384599
Plasminogen Rattus norvegicus (Norway rat)IC50 (µMol)0.43000.43001.52502.6200AID158331
Tryptase alpha/beta-1Homo sapiens (human)IC50 (µMol)0.00420.00401.438910.0000AID1384598; AID213371; AID213372; AID213382; AID91664
Tryptase deltaHomo sapiens (human)IC50 (µMol)0.00420.00400.00420.0050AID1384598; AID213371; AID213372; AID213382; AID91664
Tryptase gammaHomo sapiens (human)IC50 (µMol)0.00420.00401.670210.0000AID1384598; AID213371; AID213372; AID213382; AID91664
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ProthrombinHomo sapiens (human)Selectivity2.62502.62502.62502.6250AID211916
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (64)

Processvia Protein(s)Taxonomy
positive regulation of protein phosphorylationProthrombinHomo sapiens (human)
proteolysisProthrombinHomo sapiens (human)
acute-phase responseProthrombinHomo sapiens (human)
cell surface receptor signaling pathwayProthrombinHomo sapiens (human)
G protein-coupled receptor signaling pathwayProthrombinHomo sapiens (human)
blood coagulationProthrombinHomo sapiens (human)
positive regulation of cell population proliferationProthrombinHomo sapiens (human)
regulation of cell shapeProthrombinHomo sapiens (human)
response to woundingProthrombinHomo sapiens (human)
negative regulation of platelet activationProthrombinHomo sapiens (human)
platelet activationProthrombinHomo sapiens (human)
regulation of blood coagulationProthrombinHomo sapiens (human)
positive regulation of blood coagulationProthrombinHomo sapiens (human)
positive regulation of cell growthProthrombinHomo sapiens (human)
positive regulation of insulin secretionProthrombinHomo sapiens (human)
positive regulation of collagen biosynthetic processProthrombinHomo sapiens (human)
fibrinolysisProthrombinHomo sapiens (human)
negative regulation of proteolysisProthrombinHomo sapiens (human)
positive regulation of receptor signaling pathway via JAK-STATProthrombinHomo sapiens (human)
negative regulation of astrocyte differentiationProthrombinHomo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosolProthrombinHomo sapiens (human)
regulation of cytosolic calcium ion concentrationProthrombinHomo sapiens (human)
cytolysis by host of symbiont cellsProthrombinHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionProthrombinHomo sapiens (human)
negative regulation of fibrinolysisProthrombinHomo sapiens (human)
antimicrobial humoral immune response mediated by antimicrobial peptideProthrombinHomo sapiens (human)
neutrophil-mediated killing of gram-negative bacteriumProthrombinHomo sapiens (human)
positive regulation of lipid kinase activityProthrombinHomo sapiens (human)
negative regulation of cytokine production involved in inflammatory responseProthrombinHomo sapiens (human)
positive regulation of protein localization to nucleusProthrombinHomo sapiens (human)
positive regulation of phospholipase C-activating G protein-coupled receptor signaling pathwayProthrombinHomo sapiens (human)
ligand-gated ion channel signaling pathwayProthrombinHomo sapiens (human)
positive regulation of reactive oxygen species metabolic processProthrombinHomo sapiens (human)
proteolysisCoagulation factor XHomo sapiens (human)
blood coagulationCoagulation factor XHomo sapiens (human)
positive regulation of cell migrationCoagulation factor XHomo sapiens (human)
positive regulation of TOR signalingCoagulation factor XHomo sapiens (human)
positive regulation of cell migrationUrokinase-type plasminogen activatorHomo sapiens (human)
response to hypoxiaUrokinase-type plasminogen activatorHomo sapiens (human)
proteolysisUrokinase-type plasminogen activatorHomo sapiens (human)
chemotaxisUrokinase-type plasminogen activatorHomo sapiens (human)
signal transductionUrokinase-type plasminogen activatorHomo sapiens (human)
blood coagulationUrokinase-type plasminogen activatorHomo sapiens (human)
regulation of signaling receptor activityUrokinase-type plasminogen activatorHomo sapiens (human)
regulation of plasminogen activationUrokinase-type plasminogen activatorHomo sapiens (human)
negative regulation of plasminogen activationUrokinase-type plasminogen activatorHomo sapiens (human)
smooth muscle cell migrationUrokinase-type plasminogen activatorHomo sapiens (human)
regulation of smooth muscle cell migrationUrokinase-type plasminogen activatorHomo sapiens (human)
regulation of cell adhesionUrokinase-type plasminogen activatorHomo sapiens (human)
plasminogen activationUrokinase-type plasminogen activatorHomo sapiens (human)
regulation of cell adhesion mediated by integrinUrokinase-type plasminogen activatorHomo sapiens (human)
urokinase plasminogen activator signaling pathwayUrokinase-type plasminogen activatorHomo sapiens (human)
regulation of cell population proliferationUrokinase-type plasminogen activatorHomo sapiens (human)
fibrinolysisUrokinase-type plasminogen activatorHomo sapiens (human)
regulation of fibrinolysisUrokinase-type plasminogen activatorHomo sapiens (human)
negative regulation of fibrinolysisUrokinase-type plasminogen activatorHomo sapiens (human)
regulation of wound healingUrokinase-type plasminogen activatorHomo sapiens (human)
regulation of smooth muscle cell-matrix adhesionUrokinase-type plasminogen activatorHomo sapiens (human)
response to hypoxiaTissue-type plasminogen activatorHomo sapiens (human)
proteolysisTissue-type plasminogen activatorHomo sapiens (human)
blood coagulationTissue-type plasminogen activatorHomo sapiens (human)
negative regulation of plasminogen activationTissue-type plasminogen activatorHomo sapiens (human)
plasminogen activationTissue-type plasminogen activatorHomo sapiens (human)
protein modification processTissue-type plasminogen activatorHomo sapiens (human)
fibrinolysisTissue-type plasminogen activatorHomo sapiens (human)
negative regulation of proteolysisTissue-type plasminogen activatorHomo sapiens (human)
negative regulation of fibrinolysisTissue-type plasminogen activatorHomo sapiens (human)
prevention of polyspermyTissue-type plasminogen activatorHomo sapiens (human)
trans-synaptic signaling by BDNF, modulating synaptic transmissionTissue-type plasminogen activatorHomo sapiens (human)
platelet-derived growth factor receptor signaling pathwayTissue-type plasminogen activatorHomo sapiens (human)
smooth muscle cell migrationTissue-type plasminogen activatorHomo sapiens (human)
proteolysisCationic trypsinBos taurus (cattle)
digestionCationic trypsinBos taurus (cattle)
blood coagulationCoagulation factor XIHomo sapiens (human)
plasminogen activationCoagulation factor XIHomo sapiens (human)
positive regulation of fibrinolysisCoagulation factor XIHomo sapiens (human)
digestionTrypsin-1Homo sapiens (human)
extracellular matrix disassemblyTrypsin-1Homo sapiens (human)
proteolysisTrypsin-1Homo sapiens (human)
proteolysisTrypsin-2Homo sapiens (human)
digestionTrypsin-2Homo sapiens (human)
antimicrobial humoral responseTrypsin-2Homo sapiens (human)
extracellular matrix disassemblyTrypsin-2Homo sapiens (human)
positive regulation of cell growthTrypsin-2Homo sapiens (human)
collagen catabolic processTrypsin-2Homo sapiens (human)
positive regulation of cell adhesionTrypsin-2Homo sapiens (human)
proteolysisTrypsin-3Homo sapiens (human)
digestionTrypsin-3Homo sapiens (human)
antimicrobial humoral responseTrypsin-3Homo sapiens (human)
zymogen activationTrypsin-3Homo sapiens (human)
endothelial cell migrationTrypsin-3Homo sapiens (human)
defense responseTryptase alpha/beta-1Homo sapiens (human)
extracellular matrix disassemblyTryptase alpha/beta-1Homo sapiens (human)
proteolysisTryptase alpha/beta-1Homo sapiens (human)
proteolysisTryptase deltaHomo sapiens (human)
proteolysisTryptase gammaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (17)

Processvia Protein(s)Taxonomy
lipopolysaccharide bindingProthrombinHomo sapiens (human)
serine-type endopeptidase activityProthrombinHomo sapiens (human)
signaling receptor bindingProthrombinHomo sapiens (human)
calcium ion bindingProthrombinHomo sapiens (human)
protein bindingProthrombinHomo sapiens (human)
growth factor activityProthrombinHomo sapiens (human)
heparin bindingProthrombinHomo sapiens (human)
thrombospondin receptor activityProthrombinHomo sapiens (human)
serine-type endopeptidase activityCoagulation factor XHomo sapiens (human)
calcium ion bindingCoagulation factor XHomo sapiens (human)
protein bindingCoagulation factor XHomo sapiens (human)
phospholipid bindingCoagulation factor XHomo sapiens (human)
serine-type endopeptidase activityUrokinase-type plasminogen activatorHomo sapiens (human)
protein bindingUrokinase-type plasminogen activatorHomo sapiens (human)
serine-type endopeptidase activityTissue-type plasminogen activatorHomo sapiens (human)
signaling receptor bindingTissue-type plasminogen activatorHomo sapiens (human)
protein bindingTissue-type plasminogen activatorHomo sapiens (human)
phosphoprotein bindingTissue-type plasminogen activatorHomo sapiens (human)
endopeptidase activityCationic trypsinBos taurus (cattle)
serine-type endopeptidase activityCationic trypsinBos taurus (cattle)
protein bindingCationic trypsinBos taurus (cattle)
metal ion bindingCationic trypsinBos taurus (cattle)
serpin family protein bindingCationic trypsinBos taurus (cattle)
serine-type endopeptidase activityCoagulation factor XIHomo sapiens (human)
protein bindingCoagulation factor XIHomo sapiens (human)
heparin bindingCoagulation factor XIHomo sapiens (human)
serine-type aminopeptidase activityCoagulation factor XIHomo sapiens (human)
serine-type endopeptidase activityTrypsin-1Homo sapiens (human)
metal ion bindingTrypsin-1Homo sapiens (human)
metalloendopeptidase activityTrypsin-2Homo sapiens (human)
serine-type endopeptidase activityTrypsin-2Homo sapiens (human)
calcium ion bindingTrypsin-2Homo sapiens (human)
protein bindingTrypsin-2Homo sapiens (human)
serine-type peptidase activityTrypsin-2Homo sapiens (human)
serine-type endopeptidase activityTrypsin-3Homo sapiens (human)
calcium ion bindingTrypsin-3Homo sapiens (human)
protein bindingTrypsin-3Homo sapiens (human)
serine-type peptidase activityTrypsin-3Homo sapiens (human)
serine-type endopeptidase activityTryptase alpha/beta-1Homo sapiens (human)
protein bindingTryptase alpha/beta-1Homo sapiens (human)
serine-type peptidase activityTryptase alpha/beta-1Homo sapiens (human)
identical protein bindingTryptase alpha/beta-1Homo sapiens (human)
serine-type peptidase activityTryptase deltaHomo sapiens (human)
serine-type endopeptidase activityTryptase deltaHomo sapiens (human)
protein bindingTryptase gammaHomo sapiens (human)
serine-type peptidase activityTryptase gammaHomo sapiens (human)
serine-type endopeptidase activityTryptase gammaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (25)

Processvia Protein(s)Taxonomy
external side of plasma membraneProthrombinHomo sapiens (human)
collagen-containing extracellular matrixProthrombinHomo sapiens (human)
extracellular regionProthrombinHomo sapiens (human)
extracellular spaceProthrombinHomo sapiens (human)
endoplasmic reticulum lumenProthrombinHomo sapiens (human)
Golgi lumenProthrombinHomo sapiens (human)
plasma membraneProthrombinHomo sapiens (human)
extracellular exosomeProthrombinHomo sapiens (human)
blood microparticleProthrombinHomo sapiens (human)
collagen-containing extracellular matrixProthrombinHomo sapiens (human)
extracellular spaceProthrombinHomo sapiens (human)
extracellular regionCoagulation factor XHomo sapiens (human)
endoplasmic reticulum lumenCoagulation factor XHomo sapiens (human)
Golgi lumenCoagulation factor XHomo sapiens (human)
plasma membraneCoagulation factor XHomo sapiens (human)
external side of plasma membraneCoagulation factor XHomo sapiens (human)
extracellular spaceCoagulation factor XHomo sapiens (human)
extracellular regionUrokinase-type plasminogen activatorHomo sapiens (human)
extracellular spaceUrokinase-type plasminogen activatorHomo sapiens (human)
plasma membraneUrokinase-type plasminogen activatorHomo sapiens (human)
focal adhesionUrokinase-type plasminogen activatorHomo sapiens (human)
external side of plasma membraneUrokinase-type plasminogen activatorHomo sapiens (human)
cell surfaceUrokinase-type plasminogen activatorHomo sapiens (human)
specific granule membraneUrokinase-type plasminogen activatorHomo sapiens (human)
extracellular exosomeUrokinase-type plasminogen activatorHomo sapiens (human)
tertiary granule membraneUrokinase-type plasminogen activatorHomo sapiens (human)
serine protease inhibitor complexUrokinase-type plasminogen activatorHomo sapiens (human)
protein complex involved in cell-matrix adhesionUrokinase-type plasminogen activatorHomo sapiens (human)
serine-type endopeptidase complexUrokinase-type plasminogen activatorHomo sapiens (human)
extracellular spaceUrokinase-type plasminogen activatorHomo sapiens (human)
collagen-containing extracellular matrixTissue-type plasminogen activatorHomo sapiens (human)
extracellular regionTissue-type plasminogen activatorHomo sapiens (human)
cytoplasmTissue-type plasminogen activatorHomo sapiens (human)
cell surfaceTissue-type plasminogen activatorHomo sapiens (human)
secretory granuleTissue-type plasminogen activatorHomo sapiens (human)
apical part of cellTissue-type plasminogen activatorHomo sapiens (human)
extracellular exosomeTissue-type plasminogen activatorHomo sapiens (human)
serine protease inhibitor complexTissue-type plasminogen activatorHomo sapiens (human)
Schaffer collateral - CA1 synapseTissue-type plasminogen activatorHomo sapiens (human)
glutamatergic synapseTissue-type plasminogen activatorHomo sapiens (human)
extracellular spaceTissue-type plasminogen activatorHomo sapiens (human)
serine protease inhibitor complexCationic trypsinBos taurus (cattle)
extracellular regionCoagulation factor XIHomo sapiens (human)
extracellular spaceCoagulation factor XIHomo sapiens (human)
plasma membraneCoagulation factor XIHomo sapiens (human)
membraneCoagulation factor XIHomo sapiens (human)
extracellular exosomeCoagulation factor XIHomo sapiens (human)
extracellular regionTrypsin-1Homo sapiens (human)
collagen-containing extracellular matrixTrypsin-1Homo sapiens (human)
blood microparticleTrypsin-1Homo sapiens (human)
extracellular spaceTrypsin-1Homo sapiens (human)
extracellular regionTrypsin-2Homo sapiens (human)
extracellular spaceTrypsin-2Homo sapiens (human)
extracellular matrixTrypsin-2Homo sapiens (human)
azurophil granule lumenTrypsin-2Homo sapiens (human)
extracellular spaceTrypsin-2Homo sapiens (human)
extracellular regionTrypsin-3Homo sapiens (human)
extracellular spaceTrypsin-3Homo sapiens (human)
tertiary granule lumenTrypsin-3Homo sapiens (human)
extracellular spaceTrypsin-3Homo sapiens (human)
collagen-containing extracellular matrixTryptase alpha/beta-1Homo sapiens (human)
extracellular regionTryptase alpha/beta-1Homo sapiens (human)
extracellular spaceTryptase alpha/beta-1Homo sapiens (human)
extracellular spaceTryptase alpha/beta-1Homo sapiens (human)
extracellular spaceTryptase deltaHomo sapiens (human)
plasma membraneTryptase gammaHomo sapiens (human)
extracellular spaceTryptase gammaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (39)

Assay IDTitleYearJournalArticle
AID234527Selectivity of trypsin compared to tryptase2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.
AID75209Effect (decrease in dynamic lung compliance) on pulmonary mechanics of ovalbumin-sensitized guinea pigs following allergen induced bronchoconstriction upon intratracheal dosage of 75 ug/kg 10 min prior to ovalbumin challenge2002Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
Synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.
AID91664In vitro inhibition of human tryptase.2002Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
Synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.
AID233108Selectivity for human tryptase compared to human urokinase plasminogen activator.2002Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
Synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.
AID1384601Antithrombotic activity in rabbit model of venous thrombosis2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Factor XIa Inhibitors as New Anticoagulants.
AID233106Selectivity for human tryptase compared to human tissue plasminogen activator tissue.2002Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
Synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.
AID213382Inhibitory concentration against human tryptase2002Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
Synthesis of potent and highly selective inhibitors of human tryptase.
AID547678Inhibition of human Tryptase2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
2-Azetidinone--a new profile of various pharmacological activities.
AID1384598Inhibition of human lung tryptase using Z-glypro-arg-AMC incubated for 3 mins by spectrophotometry2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Factor XIa Inhibitors as New Anticoagulants.
AID158331Inhibitory activity against plasmin2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.
AID1074166Irreversible inhibition of human factor 11a2014Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3
Tetrahydroquinoline derivatives as potent and selective factor XIa inhibitors.
AID233105Selectivity for human tryptase compared to human thrombin.2002Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
Synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.
AID24273Aqueous stability was evaluated as half life at 37 degree C at pH 92002Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
Synthesis of potent and highly selective inhibitors of human tryptase.
AID232622Ratio of inhibitory activities against human tryptase to that of human urokinase plasminogen activator (microPa)2002Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
Synthesis of potent and highly selective inhibitors of human tryptase.
AID213372Inhibitory activity against human tryptase2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.
AID77517Effect (increase in lung resistance (Rlung)) on pulmonary mechanics of ovalbumin-sensitized guinea pigs following allergen induced bronchoconstriction2002Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
Synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.
AID232621Ratio of inhibitory activities against human tryptase to that of human trypsin2002Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
Synthesis of potent and highly selective inhibitors of human tryptase.
AID24272Aqueous stability was evaluated as half life at 37 degree C at pH 72002Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
Synthesis of potent and highly selective inhibitors of human tryptase.
AID232618Ratio of inhibitory activities against human tryptase to that of human plasmin2002Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
Synthesis of potent and highly selective inhibitors of human tryptase.
AID213436Inhibitory activity against Urokinase-type plasminogen activator2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.
AID77518Effect (increase in lung resistance (Rlung)) on pulmonary mechanics of ovalbumin-sensitized guinea pigs following allergen induced bronchoconstriction upon intratracheal dosage of 75 ug/kg 10 min prior to ovalbumin challenge2002Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
Synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.
AID52005Inhibitory activity against Coagulation factor X2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.
AID24271Aqueous Stability (half-life period) at pH 9 and 37 degrees2002Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
Synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.
AID211916Inhibitory activity against thrombin2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.
AID24270Aqueous Stability (half-life period) at pH 7 and 37 degrees2002Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
Synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.
AID213371Inhibitory activity of compound against human tryptase was determined2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
Synthesis of potent and highly selective nonguanidine azetidinone inhibitors of human tryptase.
AID232620Ratio of inhibitory activities against human tryptase to that of human tissue plasminogen activator (tissue plasminogen activator)2002Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
Synthesis of potent and highly selective inhibitors of human tryptase.
AID1384602Antithrombotic activity in rabbit model of electrolytic-mediated carotid arterial thrombosis2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Factor XIa Inhibitors as New Anticoagulants.
AID233107Selectivity for human tryptase compared to human trypsin.2002Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
Synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.
AID215727Inhibitory activity against trypsin2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.
AID75208Effect (decrease in dynamic lung compliance) on pulmonary mechanics of ovalbumin-sensitized guinea pigs following allergen induced bronchoconstriction2002Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
Synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.
AID233104Selectivity for human tryptase compared to human plasmin.2002Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
Synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.
AID1384599Inhibition of trypsin (unknown origin) using Chromozyme-TRY substrate incubated for 3 mins by spectrophotometry2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Factor XIa Inhibitors as New Anticoagulants.
AID1384600Antithrombotic activity in rabbit model of arteriovenous-shunt thrombosis2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Factor XIa Inhibitors as New Anticoagulants.
AID210912Inhibitory activity against tissue type plasminogen activator2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.
AID232619Ratio of inhibitory activities against human tryptase to that of human thrombin2002Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
Synthesis of potent and highly selective inhibitors of human tryptase.
AID75653Dose required for the inhibition of the cellular inflammatory response in ovalbumin-sensitized guinea pigs was evaluated by the reduction in cell count by 70-80%2002Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
Synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.
AID214871Inhibitory activity against bovine trypsin2004Bioorganic & medicinal chemistry letters, May-03, Volume: 14, Issue:9
Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.
AID1384597Inhibition of human factor 11a using S-2366 substrate incubated for 3 mins by spectrophotometry2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Factor XIa Inhibitors as New Anticoagulants.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (12)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's7 (58.33)29.6817
2010's5 (41.67)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: 19.39

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 Index19.39 (24.57)
Research Supply Index2.56 (2.92)
Research Growth Index4.32 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (19.39)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (16.67%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other10 (83.33%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]