Page last updated: 2024-11-08

l 694,458

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Description

DMP 777: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID177992
CHEMBL ID310871
SCHEMBL ID6538142
MeSH IDM0276340

Synonyms (31)

Synonym
CHEMBL310871 ,
l-694458
157341-41-8
HY-75957
dmp 777
(2s)-n-[(1r)-1-(1,3-benzodioxol-5-yl)butyl]-3,3-diethyl-2-[4-(4-methylpiperazine-1-carbonyl)phenoxy]-4-oxoazetidine-1-carboxamide
bdbm50066999
(s)-n-((r)-1-(benzo[d][1,3]dioxol-5-yl)butyl)-3,3-diethyl-2-(4-(1-methylpiperazine-4-carbonyl)phenoxy)-4-oxoazetidine-1-carboxamide
(s)-3,3-diethyl-2-[4-(4-methyl-piperazine-1-carbonyl)-phenoxy]-4-oxo-azetidine-1-carboxylic acid ((r)-1-benzo[1,3]dioxol-5-yl-butyl)-amide
3q0469283p ,
l 694,458
2-(4-(((4-methyl)piperazin-1-yl)carbonyl)phenoxy)-3,3-diethyl-n-(1-(3,4-methylenedioxyphenyl)butyl)-4-oxo-1-azetidinecarboxamide
1-azetidinecarboxamide, n-((1r)-1-(1,3-benzodioxol-5-yl)butyl)-3,3-diethyl-2-(4-((4-methyl-1-piperazinyl)carbonyl)phenoxy)-4-oxo-, (2s)-
l-694,458
1-azetidinecarboxamide, n-(1-(1,3-benzodioxol-5-yl)butyl)-3,3-diethyl-2-(4-((4-methyl-1-piperazinyl)carbonyl)phenoxy)-4-oxo-, (s-(r*,s*))-
dmp-777
unii-3q0469283p
n-(1-(1,3-benzodioxol-5-yl)butyl)-3,3-diethyl-2-(4-((4-methyl-1-piperazinyl)carbonyl)phenoxy)-4-oxo-1-azetidinecarboxamide
l 694458
dmp777
(s)-n-((r)-1-(benzo[d][1,3]dioxol-5-yl)butyl)-3,3-diethyl-2-(4-(4-methylpiperazine-1-carbonyl)phenoxy)-4-oxoazetidine-1-carboxamide
AKOS016005343
CS-0355
SCHEMBL6538142
DTXSID00166251
NCGC00378760-01
BCP02269
1-azetidinecarboxamide, n-[(1r)-1-(1,3-benzodioxol-5-yl)butyl]-3,3-diethyl-2-[4-[(4-methyl-1-piperazinyl)carbonyl]phenoxy]-4-oxo-, (2s)-
Q27257882
F83763
MS-30232

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" The bioavailability of a 10 mg/kg oral dose was higher in rats (65%) than in rhesus monkeys (39%)."( Orally active inhibitors of human leukocyte elastase. II. Disposition of L-694,458 in rats and rhesus monkeys.
Chiu, SH; Cioffe, C; Doss, G; Karanam, BV; Luffer-Atlas, D; McGowan, E; Painter, SK; Vincent, SH, 1997
)
0.3
"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

ExcerptRelevanceReference
"The degradation profile indicates that development of a solution dosage form of DMP 777 with adequate shelf-life stability at room temperature is feasible."( Degradation kinetics of DMP 777, an elastase inhibitor.
Gray, DB; Hussain, MA; Nemeth, GA; Raghavan, KS; Scholz, TH, 1996
)
0.29
" [3H]L-694,458 was well absorbed after oral dosing to rats at 10 mg/kg, as indicated by the high recovery of radioactivity in bile (83%) and urine (6%) of bile duct-cannulated rats."( Orally active inhibitors of human leukocyte elastase. II. Disposition of L-694,458 in rats and rhesus monkeys.
Chiu, SH; Cioffe, C; Doss, G; Karanam, BV; Luffer-Atlas, D; McGowan, E; Painter, SK; Vincent, SH, 1997
)
0.3
" Bile obtained from orally dosed rats contained more than 40 parent-related components, and many of these metabolites had arisen from piperazine ring cleavage."( Orally active inhibitors of human leukocyte elastase. III. Identification and characterization of metabolites of L-694,458 by liquid chromatography-tandem mass spectrometry.
Arison, BH; Chiu, SH; Luffer-Atlas, D; Painter, SK; Stearns, RA; Vincent, SH, 1997
)
0.3
" Using this method, it was demonstrated that after oral dosing of monkeys at 40 mg kg(-1) with 1 the only stereoisomer detected in the post-dose plasma samples was the starting material 1, and no inversion of the configuration at positions 'a' and 'b' of 1 had occurred in vivo."( Separation of the four stereoisomers of a potent inhibitor (L-694,458) of human leukocyte elastase and its determination in human plasma using achiral/chiral chromatography with column switching.
Kline, WF; Matuszewski, BK; Vincent, SH; Zagrobelny, J, 1998
)
0.3
"Oral dosing with DMP 777 caused a rapid increase in serum gastrin levels and severe hypochlorhydria."( Reversible drug-induced oxyntic atrophy in rats.
Barnes, TB; Car, BD; Coffey, RJ; Goldenring, JR; Haley, PJ; Meunier, PC; Ray, GS, 2000
)
0.31
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (10)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency0.47720.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency3.37860.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency16.93300.00108.379861.1304AID1645840
Interferon betaHomo sapiens (human)Potency3.37860.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency3.37860.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency3.37860.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency3.37860.01238.964839.8107AID1645842
[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)
ProthrombinHomo sapiens (human)IC50 (µMol)78.76000.00000.710710.0000AID211763
Chymotrypsinogen ABos taurus (cattle)IC50 (µMol)0.98000.98004.05607.2000AID52784
Neutrophil elastaseHomo sapiens (human)IC50 (µMol)0.02950.00632.073422.3780AID66657; AID66659
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (101)

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)
digestionChymotrypsinogen ABos taurus (cattle)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
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)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (30)

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)
protein bindingChymotrypsinogen ABos taurus (cattle)
serpin family protein bindingChymotrypsinogen ABos taurus (cattle)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
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)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (32)

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 regionChymotrypsinogen ABos taurus (cattle)
serine protease inhibitor complexChymotrypsinogen ABos taurus (cattle)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
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)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (15)

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.
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.
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.
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.
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.
AID66659The compound was tested for inhibition of human neutrophil elastase enzyme with a pre-incubation time of 40 min.1998Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21
Syntheses of trans-5-oxo-hexahydro-pyrrolo[3,2-b]pyrroles and trans-5-oxo-hexahydro-furo[3,2-b]pyrroles (pyrrolidine trans-lactams and trans-lactones): new pharmacophores for elastase inhibition.
AID360118Inhibition of human U937 cellular [35S]methionine-labeled cathepsin G binding to aprotinin by aprotinin-agarose silver-stained SDS-PAGE method2007The Journal of biological chemistry, Jul-20, Volume: 282, Issue:29
Inhibition of the activation of multiple serine proteases with a cathepsin C inhibitor requires sustained exposure to prevent pro-enzyme processing.
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.
AID589140Mechanism based inhibition of human cytochrome P450 3A4 measured by testosterone 6-beta hydroxylation2005Current drug metabolism, Oct, Volume: 6, Issue:5
Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity.
AID223087In vitro inhibitory activity in human whole blood (HWB) elastase at a concentration of 102001Bioorganic & medicinal chemistry letters, Jan-22, Volume: 11, Issue:2
Intracellular inhibition of human neutrophil elastase by orally active pyrrolidine-trans-lactams.
AID588208Literature-mined public compounds from Lowe et al phospholipidosis modelling dataset2010Molecular pharmaceutics, Oct-04, Volume: 7, Issue:5
Predicting phospholipidosis using machine learning.
AID211763The compound was tested for inhibition of thrombin with a preincubation time of 15 min1998Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21
Syntheses of trans-5-oxo-hexahydro-pyrrolo[3,2-b]pyrroles and trans-5-oxo-hexahydro-furo[3,2-b]pyrroles (pyrrolidine trans-lactams and trans-lactones): new pharmacophores for elastase inhibition.
AID360117Inhibition of human sputum neutrophil elastase binding to aprotinin at 1 uM by aprotinin-agarose silver-stained SDS-PAGE method2007The Journal of biological chemistry, Jul-20, Volume: 282, Issue:29
Inhibition of the activation of multiple serine proteases with a cathepsin C inhibitor requires sustained exposure to prevent pro-enzyme processing.
AID52784The compound was tested for inhibition of Chymotrypsinogen with a pre-incubation time of 15 min1998Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21
Syntheses of trans-5-oxo-hexahydro-pyrrolo[3,2-b]pyrroles and trans-5-oxo-hexahydro-furo[3,2-b]pyrroles (pyrrolidine trans-lactams and trans-lactones): new pharmacophores for elastase inhibition.
AID66657The compound was tested for inhibition of human neutrophil elastase enzyme with a pre-incubation time of 0 min.1998Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21
Syntheses of trans-5-oxo-hexahydro-pyrrolo[3,2-b]pyrroles and trans-5-oxo-hexahydro-furo[3,2-b]pyrroles (pyrrolidine trans-lactams and trans-lactones): new pharmacophores for elastase inhibition.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (29)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's5 (17.24)18.2507
2000's13 (44.83)29.6817
2010's7 (24.14)24.3611
2020's4 (13.79)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.18

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 Index11.18 (24.57)
Research Supply Index3.40 (2.92)
Research Growth Index4.58 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.18)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (3.45%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other28 (96.55%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]