Page last updated: 2024-12-11

ca 074

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Cross-References

ID SourceID
PubMed CID9821383
CHEMBL ID490920
SCHEMBL ID4323476
MeSH IDM0480921

Synonyms (18)

Synonym
cathepsin b inhibitor iii
(2s)-1-[(2s,3s)-3-methyl-2-{[(2s,3s)-3-(propylcarbamoyl)oxiran-2-yl]formamido}pentanoyl]pyrrolidine-2-carboxylic acid
prnh-tes-ile-pro-oh
epoxysuccinyl derivative ca074
ca074
bdbm16509
n-{[(2s,3s)-3-(propylcarbamoyl)oxiran-2-yl]carbonyl}-l-isoleucyl-l-proline
chembl490920 ,
SCHEMBL4323476
l-proline,n-[[(2s,3s)-3-[(propylamino)carbonyl]-2-oxiranyl]carbonyl]-l-isoleucyl-
n-[[(2s,3s)-3-[(propylamino)carbonyl]-2-oxiranyl]carbonyl]-l-isoleucyl-l-proline
AKOS024458382
mfcd00797531
HY-103350
CS-7886
MS-26297
EX-A6724
AC-37063
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (7)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cathepsin DHomo sapiens (human)IC50 (µMol)100.00000.00000.931610.0000AID350740
Calpain-1 catalytic subunitHomo sapiens (human)IC50 (µMol)100.00000.00021.059210.0000AID1712997; AID1800259
Cathepsin BBos taurus (cattle)IC50 (µMol)0.03800.02000.09130.3100AID1797510
Procathepsin LHomo sapiens (human)IC50 (µMol)67.69670.00021.66619.5100AID1712999; AID1800262; AID350738
Cathepsin BHomo sapiens (human)IC50 (µMol)1.51460.00021.845310.0000AID1545139; AID1712998; AID1713008; AID1800261; AID350737
Pro-cathepsin HHomo sapiens (human)IC50 (µMol)100.00000.12592.740410.0000AID350739
Calpain-2 catalytic subunitHomo sapiens (human)IC50 (µMol)100.00000.00200.24300.6000AID1800260
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (71)

Processvia Protein(s)Taxonomy
autophagosome assemblyCathepsin DHomo sapiens (human)
proteolysisCathepsin DHomo sapiens (human)
antigen processing and presentation of exogenous peptide antigen via MHC class IICathepsin DHomo sapiens (human)
insulin receptor recyclingCathepsin DHomo sapiens (human)
lipoprotein catabolic processCathepsin DHomo sapiens (human)
positive regulation of apoptotic processCathepsin DHomo sapiens (human)
positive regulation of cysteine-type endopeptidase activity involved in apoptotic processCathepsin DHomo sapiens (human)
regulation of establishment of protein localizationCathepsin DHomo sapiens (human)
insulin catabolic processCathepsin DHomo sapiens (human)
proteolysisCalpain-1 catalytic subunitHomo sapiens (human)
positive regulation of cell population proliferationCalpain-1 catalytic subunitHomo sapiens (human)
regulation of macroautophagyCalpain-1 catalytic subunitHomo sapiens (human)
receptor catabolic processCalpain-1 catalytic subunitHomo sapiens (human)
regulation of catalytic activityCalpain-1 catalytic subunitHomo sapiens (human)
mammary gland involutionCalpain-1 catalytic subunitHomo sapiens (human)
self proteolysisCalpain-1 catalytic subunitHomo sapiens (human)
regulation of NMDA receptor activityCalpain-1 catalytic subunitHomo sapiens (human)
adaptive immune responseProcathepsin LHomo sapiens (human)
proteolysisProcathepsin LHomo sapiens (human)
protein autoprocessingProcathepsin LHomo sapiens (human)
fusion of virus membrane with host plasma membraneProcathepsin LHomo sapiens (human)
receptor-mediated endocytosis of virus by host cellProcathepsin LHomo sapiens (human)
antigen processing and presentationProcathepsin LHomo sapiens (human)
antigen processing and presentation of exogenous peptide antigen via MHC class IIProcathepsin LHomo sapiens (human)
collagen catabolic processProcathepsin LHomo sapiens (human)
zymogen activationProcathepsin LHomo sapiens (human)
enkephalin processingProcathepsin LHomo sapiens (human)
fusion of virus membrane with host endosome membraneProcathepsin LHomo sapiens (human)
CD4-positive, alpha-beta T cell lineage commitmentProcathepsin LHomo sapiens (human)
symbiont entry into host cellProcathepsin LHomo sapiens (human)
antigen processing and presentation of peptide antigenProcathepsin LHomo sapiens (human)
proteolysis involved in protein catabolic processProcathepsin LHomo sapiens (human)
elastin catabolic processProcathepsin LHomo sapiens (human)
macrophage apoptotic processProcathepsin LHomo sapiens (human)
cellular response to thyroid hormone stimulusProcathepsin LHomo sapiens (human)
positive regulation of apoptotic signaling pathwayProcathepsin LHomo sapiens (human)
positive regulation of peptidase activityProcathepsin LHomo sapiens (human)
immune responseProcathepsin LHomo sapiens (human)
proteolysisCathepsin BHomo sapiens (human)
thyroid hormone generationCathepsin BHomo sapiens (human)
collagen catabolic processCathepsin BHomo sapiens (human)
epithelial cell differentiationCathepsin BHomo sapiens (human)
regulation of apoptotic processCathepsin BHomo sapiens (human)
decidualizationCathepsin BHomo sapiens (human)
symbiont entry into host cellCathepsin BHomo sapiens (human)
proteolysis involved in protein catabolic processCathepsin BHomo sapiens (human)
cellular response to thyroid hormone stimulusCathepsin BHomo sapiens (human)
metanephros developmentPro-cathepsin HHomo sapiens (human)
T cell mediated cytotoxicityPro-cathepsin HHomo sapiens (human)
adaptive immune responsePro-cathepsin HHomo sapiens (human)
immune response-regulating signaling pathwayPro-cathepsin HHomo sapiens (human)
proteolysisPro-cathepsin HHomo sapiens (human)
apoptotic processPro-cathepsin HHomo sapiens (human)
positive regulation of cell population proliferationPro-cathepsin HHomo sapiens (human)
positive regulation of gene expressionPro-cathepsin HHomo sapiens (human)
positive regulation of epithelial cell migrationPro-cathepsin HHomo sapiens (human)
neuropeptide catabolic processPro-cathepsin HHomo sapiens (human)
bradykinin catabolic processPro-cathepsin HHomo sapiens (human)
positive regulation of peptidase activityPro-cathepsin HHomo sapiens (human)
antigen processing and presentationPro-cathepsin HHomo sapiens (human)
positive regulation of cell migrationPro-cathepsin HHomo sapiens (human)
zymogen activationPro-cathepsin HHomo sapiens (human)
protein destabilizationPro-cathepsin HHomo sapiens (human)
response to retinoic acidPro-cathepsin HHomo sapiens (human)
membrane protein proteolysisPro-cathepsin HHomo sapiens (human)
negative regulation of apoptotic processPro-cathepsin HHomo sapiens (human)
surfactant homeostasisPro-cathepsin HHomo sapiens (human)
positive regulation of angiogenesisPro-cathepsin HHomo sapiens (human)
dichotomous subdivision of terminal units involved in lung branchingPro-cathepsin HHomo sapiens (human)
ERK1 and ERK2 cascadePro-cathepsin HHomo sapiens (human)
cellular response to thyroid hormone stimulusPro-cathepsin HHomo sapiens (human)
positive regulation of apoptotic signaling pathwayPro-cathepsin HHomo sapiens (human)
proteolysis involved in protein catabolic processPro-cathepsin HHomo sapiens (human)
immune responsePro-cathepsin HHomo sapiens (human)
response to hypoxiaCalpain-2 catalytic subunitHomo sapiens (human)
blastocyst developmentCalpain-2 catalytic subunitHomo sapiens (human)
proteolysisCalpain-2 catalytic subunitHomo sapiens (human)
myoblast fusionCalpain-2 catalytic subunitHomo sapiens (human)
female pregnancyCalpain-2 catalytic subunitHomo sapiens (human)
response to mechanical stimulusCalpain-2 catalytic subunitHomo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCalpain-2 catalytic subunitHomo sapiens (human)
protein autoprocessingCalpain-2 catalytic subunitHomo sapiens (human)
regulation of interleukin-6 productionCalpain-2 catalytic subunitHomo sapiens (human)
cellular response to interferon-betaCalpain-2 catalytic subunitHomo sapiens (human)
response to hydrogen peroxideCalpain-2 catalytic subunitHomo sapiens (human)
behavioral response to painCalpain-2 catalytic subunitHomo sapiens (human)
regulation of cytoskeleton organizationCalpain-2 catalytic subunitHomo sapiens (human)
proteolysis involved in protein catabolic processCalpain-2 catalytic subunitHomo sapiens (human)
cellular response to lipopolysaccharideCalpain-2 catalytic subunitHomo sapiens (human)
cellular response to amino acid stimulusCalpain-2 catalytic subunitHomo sapiens (human)
positive regulation of myoblast fusionCalpain-2 catalytic subunitHomo sapiens (human)
positive regulation of phosphatidylcholine biosynthetic processCalpain-2 catalytic subunitHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (22)

Processvia Protein(s)Taxonomy
cysteine-type endopeptidase activityCathepsin DHomo sapiens (human)
protein bindingCathepsin DHomo sapiens (human)
peptidase activityCathepsin DHomo sapiens (human)
aspartic-type peptidase activityCathepsin DHomo sapiens (human)
aspartic-type endopeptidase activityCathepsin DHomo sapiens (human)
calcium-dependent cysteine-type endopeptidase activityCalpain-1 catalytic subunitHomo sapiens (human)
calcium ion bindingCalpain-1 catalytic subunitHomo sapiens (human)
protein bindingCalpain-1 catalytic subunitHomo sapiens (human)
peptidase activityCalpain-1 catalytic subunitHomo sapiens (human)
endopeptidase activityCathepsin BBos taurus (cattle)
fibronectin bindingProcathepsin LHomo sapiens (human)
cysteine-type endopeptidase activityProcathepsin LHomo sapiens (human)
protein bindingProcathepsin LHomo sapiens (human)
collagen bindingProcathepsin LHomo sapiens (human)
cysteine-type peptidase activityProcathepsin LHomo sapiens (human)
histone bindingProcathepsin LHomo sapiens (human)
proteoglycan bindingProcathepsin LHomo sapiens (human)
serpin family protein bindingProcathepsin LHomo sapiens (human)
cysteine-type endopeptidase activator activity involved in apoptotic processProcathepsin LHomo sapiens (human)
cysteine-type endopeptidase activityCathepsin BHomo sapiens (human)
protein bindingCathepsin BHomo sapiens (human)
collagen bindingCathepsin BHomo sapiens (human)
peptidase activityCathepsin BHomo sapiens (human)
cysteine-type peptidase activityCathepsin BHomo sapiens (human)
proteoglycan bindingCathepsin BHomo sapiens (human)
endopeptidase activityPro-cathepsin HHomo sapiens (human)
aminopeptidase activityPro-cathepsin HHomo sapiens (human)
cysteine-type endopeptidase activityPro-cathepsin HHomo sapiens (human)
serine-type endopeptidase activityPro-cathepsin HHomo sapiens (human)
protein bindingPro-cathepsin HHomo sapiens (human)
peptidase activityPro-cathepsin HHomo sapiens (human)
cysteine-type peptidase activityPro-cathepsin HHomo sapiens (human)
cysteine-type endopeptidase activator activity involved in apoptotic processPro-cathepsin HHomo sapiens (human)
HLA-A specific activating MHC class I receptor activityPro-cathepsin HHomo sapiens (human)
thyroid hormone bindingPro-cathepsin HHomo sapiens (human)
calcium-dependent cysteine-type endopeptidase activityCalpain-2 catalytic subunitHomo sapiens (human)
calcium ion bindingCalpain-2 catalytic subunitHomo sapiens (human)
protein bindingCalpain-2 catalytic subunitHomo sapiens (human)
cytoskeletal protein bindingCalpain-2 catalytic subunitHomo sapiens (human)
cysteine-type peptidase activityCalpain-2 catalytic subunitHomo sapiens (human)
enzyme bindingCalpain-2 catalytic subunitHomo sapiens (human)
protein-containing complex bindingCalpain-2 catalytic subunitHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (44)

Processvia Protein(s)Taxonomy
collagen-containing extracellular matrixCathepsin DHomo sapiens (human)
extracellular regionCathepsin DHomo sapiens (human)
extracellular spaceCathepsin DHomo sapiens (human)
lysosomeCathepsin DHomo sapiens (human)
lysosomal membraneCathepsin DHomo sapiens (human)
endosome membraneCathepsin DHomo sapiens (human)
endosome lumenCathepsin DHomo sapiens (human)
specific granule lumenCathepsin DHomo sapiens (human)
melanosomeCathepsin DHomo sapiens (human)
lysosomal lumenCathepsin DHomo sapiens (human)
membrane raftCathepsin DHomo sapiens (human)
collagen-containing extracellular matrixCathepsin DHomo sapiens (human)
extracellular exosomeCathepsin DHomo sapiens (human)
tertiary granule lumenCathepsin DHomo sapiens (human)
ficolin-1-rich granule lumenCathepsin DHomo sapiens (human)
cornified envelopeCalpain-1 catalytic subunitHomo sapiens (human)
extracellular regionCalpain-1 catalytic subunitHomo sapiens (human)
mitochondrionCalpain-1 catalytic subunitHomo sapiens (human)
lysosomeCalpain-1 catalytic subunitHomo sapiens (human)
cytosolCalpain-1 catalytic subunitHomo sapiens (human)
plasma membraneCalpain-1 catalytic subunitHomo sapiens (human)
focal adhesionCalpain-1 catalytic subunitHomo sapiens (human)
membraneCalpain-1 catalytic subunitHomo sapiens (human)
extracellular exosomeCalpain-1 catalytic subunitHomo sapiens (human)
calpain complexCalpain-1 catalytic subunitHomo sapiens (human)
ficolin-1-rich granule lumenCalpain-1 catalytic subunitHomo sapiens (human)
cytoplasmCalpain-1 catalytic subunitHomo sapiens (human)
lysosomeCathepsin BBos taurus (cattle)
apical plasma membraneCathepsin BBos taurus (cattle)
melanosomeCathepsin BBos taurus (cattle)
extracellular regionProcathepsin LHomo sapiens (human)
extracellular spaceProcathepsin LHomo sapiens (human)
nucleusProcathepsin LHomo sapiens (human)
lysosomeProcathepsin LHomo sapiens (human)
multivesicular bodyProcathepsin LHomo sapiens (human)
Golgi apparatusProcathepsin LHomo sapiens (human)
plasma membraneProcathepsin LHomo sapiens (human)
apical plasma membraneProcathepsin LHomo sapiens (human)
endolysosome lumenProcathepsin LHomo sapiens (human)
chromaffin granuleProcathepsin LHomo sapiens (human)
lysosomal lumenProcathepsin LHomo sapiens (human)
intracellular membrane-bounded organelleProcathepsin LHomo sapiens (human)
collagen-containing extracellular matrixProcathepsin LHomo sapiens (human)
extracellular exosomeProcathepsin LHomo sapiens (human)
endocytic vesicle lumenProcathepsin LHomo sapiens (human)
extracellular spaceProcathepsin LHomo sapiens (human)
lysosomeProcathepsin LHomo sapiens (human)
collagen-containing extracellular matrixCathepsin BHomo sapiens (human)
extracellular regionCathepsin BHomo sapiens (human)
extracellular spaceCathepsin BHomo sapiens (human)
lysosomeCathepsin BHomo sapiens (human)
external side of plasma membraneCathepsin BHomo sapiens (human)
apical plasma membraneCathepsin BHomo sapiens (human)
endolysosome lumenCathepsin BHomo sapiens (human)
melanosomeCathepsin BHomo sapiens (human)
perinuclear region of cytoplasmCathepsin BHomo sapiens (human)
collagen-containing extracellular matrixCathepsin BHomo sapiens (human)
extracellular exosomeCathepsin BHomo sapiens (human)
peptidase inhibitor complexCathepsin BHomo sapiens (human)
ficolin-1-rich granule lumenCathepsin BHomo sapiens (human)
extracellular spaceCathepsin BHomo sapiens (human)
lysosomeCathepsin BHomo sapiens (human)
extracellular regionPro-cathepsin HHomo sapiens (human)
extracellular spacePro-cathepsin HHomo sapiens (human)
lysosomePro-cathepsin HHomo sapiens (human)
cytosolPro-cathepsin HHomo sapiens (human)
secretory granule lumenPro-cathepsin HHomo sapiens (human)
cytoplasmic ribonucleoprotein granulePro-cathepsin HHomo sapiens (human)
intracellular membrane-bounded organellePro-cathepsin HHomo sapiens (human)
collagen-containing extracellular matrixPro-cathepsin HHomo sapiens (human)
extracellular exosomePro-cathepsin HHomo sapiens (human)
alveolar lamellar bodyPro-cathepsin HHomo sapiens (human)
multivesicular body lumenPro-cathepsin HHomo sapiens (human)
tertiary granule lumenPro-cathepsin HHomo sapiens (human)
ficolin-1-rich granule lumenPro-cathepsin HHomo sapiens (human)
extracellular spacePro-cathepsin HHomo sapiens (human)
lysosomePro-cathepsin HHomo sapiens (human)
membrane raftCalpain-2 catalytic subunitHomo sapiens (human)
nucleusCalpain-2 catalytic subunitHomo sapiens (human)
cytoplasmCalpain-2 catalytic subunitHomo sapiens (human)
lysosomeCalpain-2 catalytic subunitHomo sapiens (human)
endoplasmic reticulumCalpain-2 catalytic subunitHomo sapiens (human)
Golgi apparatusCalpain-2 catalytic subunitHomo sapiens (human)
cytosolCalpain-2 catalytic subunitHomo sapiens (human)
plasma membraneCalpain-2 catalytic subunitHomo sapiens (human)
focal adhesionCalpain-2 catalytic subunitHomo sapiens (human)
external side of plasma membraneCalpain-2 catalytic subunitHomo sapiens (human)
dendriteCalpain-2 catalytic subunitHomo sapiens (human)
cortical actin cytoskeletonCalpain-2 catalytic subunitHomo sapiens (human)
pseudopodiumCalpain-2 catalytic subunitHomo sapiens (human)
neuronal cell bodyCalpain-2 catalytic subunitHomo sapiens (human)
membrane raftCalpain-2 catalytic subunitHomo sapiens (human)
extracellular exosomeCalpain-2 catalytic subunitHomo sapiens (human)
perinuclear endoplasmic reticulumCalpain-2 catalytic subunitHomo sapiens (human)
calpain complexCalpain-2 catalytic subunitHomo sapiens (human)
chromatinCalpain-2 catalytic subunitHomo sapiens (human)
cytoplasmCalpain-2 catalytic subunitHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (21)

Assay IDTitleYearJournalArticle
AID1402865Inhibition of human cathepsin K kinase activity assessed as normalized bradykinin equivalents ratio at 1 uM pre-incubated for 15 mins before bradykinin substrate addition by competitive enzyme immunoassay (Rvb = <0.5%)2018European journal of medicinal chemistry, Jan-20, Volume: 144Substrate-derived triazolo- and azapeptides as inhibitors of cathepsins K and S.
AID1712998Inhibition of cathepsin B (unknown origin) using RR-AMC as substrate preincubated for 30 mins followed by substrate addition and further incubated for 30 mins under shaking condition by fluorescence assay2016European journal of medicinal chemistry, Oct-04, Volume: 121Neuroprotective effect of synthetic chalcone derivatives as competitive dual inhibitors against μ-calpain and cathepsin B through the downregulation of tau phosphorylation and insoluble Aβ peptide formation.
AID350737Inhibition of human liver cathepsin B after 30 mins by fluorometric end-point assay2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Identification of 3-acetyl-2-aminoquinolin-4-one as a novel, nonpeptidic scaffold for specific calpain inhibitory activity.
AID1402866Inhibition of human cathepsin K kinase activity assessed as normalized bradykinin equivalents ratio at 1 uM pre-incubated for 15 mins before kallidin substrate addition by competitive enzyme immunoassay (Rvb = <0.5%)2018European journal of medicinal chemistry, Jan-20, Volume: 144Substrate-derived triazolo- and azapeptides as inhibitors of cathepsins K and S.
AID1713010Neuroprotective activity in human SH-SY5Y cells assessed as reduction in GOx-induced PARP cleavage at 20 uM pretreated with GOx for 4 hrs followed by compound treatment by Western blot analysis2016European journal of medicinal chemistry, Oct-04, Volume: 121Neuroprotective effect of synthetic chalcone derivatives as competitive dual inhibitors against μ-calpain and cathepsin B through the downregulation of tau phosphorylation and insoluble Aβ peptide formation.
AID1372431Inhibition of Cathepsin-B (unknown origin) at 5 uM preincubated for 15 mins followed by Z-Arg-Arg-AMC addition measured after 30 mins by fluorescence assay relative to control2018Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
Synthesis and biological evaluation of novel synthetic chalcone derivatives as anti-tumor agents targeting Cat L and Cat K.
AID1545139Inhibition of cathepsin B (unknown origin) assessed as reduction in 7-amino-4-methylcoumarin formation using Z-Arg-Arg-MCA as substrate preincubated for 3 mins followed by substrate addition and measured after 10 mins by fluorescence spectrometric method2019Bioorganic & medicinal chemistry, 01-01, Volume: 27, Issue:1
Cathepsin B: Active site mapping with peptidic substrates and inhibitors.
AID723745Inhibition of human MCF10A neoT cell invasion expressing c-Ha-Ras oncogene at 5 uM after 30 mins relative to DMSO-treated control2013Journal of medicinal chemistry, Jan-24, Volume: 56, Issue:2
Development of new cathepsin B inhibitors: combining bioisosteric replacements and structure-based design to explore the structure-activity relationships of nitroxoline derivatives.
AID1712999Inhibition of cathepsin L (unknown origin) using Z-FR-AMC as substrate preincubated for 30 mins followed by substrate addition and further incubated for 30 mins under shaking condition by fluorescence assay2016European journal of medicinal chemistry, Oct-04, Volume: 121Neuroprotective effect of synthetic chalcone derivatives as competitive dual inhibitors against μ-calpain and cathepsin B through the downregulation of tau phosphorylation and insoluble Aβ peptide formation.
AID350740Inhibition of human liver cathepsin D after 30 mins by fluorometric end-point assay2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Identification of 3-acetyl-2-aminoquinolin-4-one as a novel, nonpeptidic scaffold for specific calpain inhibitory activity.
AID1390137Antiinvasive activity against human MCF10AneoT cells at 5 uM incubated for 1 hr measured every 15 mins for 72 hrs by real time xCELLigence assay relative to control2018Bioorganic & medicinal chemistry letters, 04-15, Volume: 28, Issue:7
Cathepsin B inhibitors: Further exploration of the nitroxoline core.
AID350738Inhibition of human liver cathepsin L after 30 mins by fluorometric end-point assay2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Identification of 3-acetyl-2-aminoquinolin-4-one as a novel, nonpeptidic scaffold for specific calpain inhibitory activity.
AID1713008Inhibition of cathepsin B in human SH-SY5Y cells using RR-AMC as substrate by fluorescence microplate reader assay2016European journal of medicinal chemistry, Oct-04, Volume: 121Neuroprotective effect of synthetic chalcone derivatives as competitive dual inhibitors against μ-calpain and cathepsin B through the downregulation of tau phosphorylation and insoluble Aβ peptide formation.
AID1712997Inhibition of human erythrocytes mu-calpain using Pep1 as substrate incubated for 30 mins under shaking condition in presence of CaCl2 by fluorescence assay2016European journal of medicinal chemistry, Oct-04, Volume: 121Neuroprotective effect of synthetic chalcone derivatives as competitive dual inhibitors against μ-calpain and cathepsin B through the downregulation of tau phosphorylation and insoluble Aβ peptide formation.
AID350739Inhibition of human liver cathepsin H after 30 mins by fluorometric end-point assay2009Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
Identification of 3-acetyl-2-aminoquinolin-4-one as a novel, nonpeptidic scaffold for specific calpain inhibitory activity.
AID1390127Inhibition of cathepsin B in human MCF-10A neoT cells assessed as proteolysis of extracellular membrane by measuring decrease in intracellular degradation of DQ-collagen 4 at 50 uM incubated for 2 hrs followed by DQ-collagen addition measured for 2 hrs by2018Bioorganic & medicinal chemistry letters, 04-15, Volume: 28, Issue:7
Cathepsin B inhibitors: Further exploration of the nitroxoline core.
AID1800261Cathepsin B Inhibition Assay from Article 10.1016/j.bioorg.2013.09.002: \\Synthesis and investigation of dihydroxychalcones as calpain and cathepsin inhibitors.\\2013Bioorganic chemistry, Dec, Volume: 51Synthesis and investigation of dihydroxychalcones as calpain and cathepsin inhibitors.
AID1800260m-Calpain Inhibition Assay from Article 10.1016/j.bioorg.2013.09.002: \\Synthesis and investigation of dihydroxychalcones as calpain and cathepsin inhibitors.\\2013Bioorganic chemistry, Dec, Volume: 51Synthesis and investigation of dihydroxychalcones as calpain and cathepsin inhibitors.
AID1800259µ-Calpain Inhibition Assay from Article 10.1016/j.bioorg.2013.09.002: \\Synthesis and investigation of dihydroxychalcones as calpain and cathepsin inhibitors.\\2013Bioorganic chemistry, Dec, Volume: 51Synthesis and investigation of dihydroxychalcones as calpain and cathepsin inhibitors.
AID1797510Inhibitory Activity Measurement of Bovine Cathepsin B. from Article 10.1016/j.jmb.2006.07.070: \\Quantitative evaluation of each catalytic subsite of cathepsin B for inhibitory activity based on inhibitory activity-binding mode relationship of epoxysucciny2006Journal of molecular biology, Oct-06, Volume: 362, Issue:5
Quantitative evaluation of each catalytic subsite of cathepsin B for inhibitory activity based on inhibitory activity-binding mode relationship of epoxysuccinyl inhibitors by X-ray crystal structure analyses of complexes.
AID1800262Cathepsin L Inhibition Assay from Article 10.1016/j.bioorg.2013.09.002: \\Synthesis and investigation of dihydroxychalcones as calpain and cathepsin inhibitors.\\2013Bioorganic chemistry, Dec, Volume: 51Synthesis and investigation of dihydroxychalcones as calpain and cathepsin inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (9)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's2 (22.22)29.6817
2010's7 (77.78)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: 24.34

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 Index24.34 (24.57)
Research Supply Index2.30 (2.92)
Research Growth Index5.00 (4.65)
Search Engine Demand Index23.28 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (24.34)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (11.11%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other8 (88.89%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]