Page last updated: 2024-11-08

amastatin

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

Description

amastatin: structure; inhibits aminopeptidase [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

amastatin : A tetrapeptide comprising (2S,3R)-3-amino-2-hydroxy-5-methylhexanoyl, L-valyl, L-valyl and L-aspartic acid units joined in sequence [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID439518
CHEMBL ID28650
CHEBI ID2624
SCHEMBL ID163492
MeSH IDM0067389

Synonyms (29)

Synonym
l-aspartic acid, n-(n-(n-(3-amino-2-hydroxy-5-methyl-1-oxohexyl)-l-valyl)-l-valyl)-, (s-(r*,s*))-
l-aspartic acid, n-((2s,3r)-3-amino-2-hydroxy-5-methyl-1-oxohexyl)-l-valyl-l-valyl-
n-((2s,3r)-3-amino-2-hydroxy-5-methyl-1-oxohexyl)-l-valyl-l-valyl-l-aspartic acid
l-aspartic acid, n-(n-(3-amino-2-hydroxy-5-methyl-1-oxohexyl)-l-valyl)-l-valyl)-, (s-(r*,s*))-
brn 4727847
leu[1psi,chohconh]valvalasp
n-[(2s,3r)-3-amino-2-hydroxy-5-methylhexanoyl]-l-valyl-l-valyl-l-aspartic acid
CHEBI:2624 ,
C01552
amastatin
(2s)-2-[[(2s)-2-[[(2s)-2-[[(2s,3r)-3-amino-2-hydroxy-5-methyl-hexanoyl]amino]-3-methyl-butanoyl]amino]-3-methyl-butanoyl]amino]butanedioic acid
[(2s,3r)-3-amino-2-hydroxy-5-methylhexanoyl]-val-val-asp
67655-94-1
CHEMBL28650 ,
(2s)-2-[[(2s)-2-[[(2s)-2-[[(2s,3r)-3-amino-2-hydroxy-5-methylhexanoyl]amino]-3-methylbutanoyl]amino]-3-methylbutanoyl]amino]butanedioic acid
bdbm50017478
3-amino-2-hydroxy-5-methylhexanoyl-l-valyl-l-valyl-l-aspartic acid
NCGC00346895-01
MLS006010001
smr000058546
SCHEMBL163492
QFAADIRHLBXJJS-ZAZJUGBXSA-N
l-aspartic acid, n-[(2s,3r)-3-amino-2-hydroxy-5-methyl-1-oxohexyl]-l-valyl-l-valyl-
(s)-2-((s)-2-((s)-2-((2s,3r)-3-amino-2-hydroxy-5-methylhexanamido)-3-methylbutanamido)-3-methylbutanamido)succinic acid
Q21098987
DTXSID10987015
n-[2-({2-[(3-amino-1,2-dihydroxy-5-methylhexylidene)amino]-1-hydroxy-3-methylbutylidene}amino)-1-hydroxy-3-methylbutylidene]aspartic acid
((2s,3r)-3-amino-2-hydroxy-5-methylhexanoyl)-l-valyl-l-valyl-l-aspartic acid
AKOS040745009

Research Excerpts

Overview

Amastatin is a selective, but not totally specific aminopeptidase inhibitor. Bestatin selectively blocks aminopesidase B, which cleaves basic amino acids.

ExcerptReferenceRelevance
"Amastatin is a selective, but not totally specific aminopeptidase inhibitor that blocks aminopeptidase A, which cleaves acidic amino acids, while bestatin selectively blocks aminopeptidase B, which cleaves basic amino acids."( Amastatin and bestatin-induced dipsogenicity in the Sprague-Dawley rat.
Harding, JW; Quirk, WS; Wright, JW, 1987
)
2.44

Actions

ExcerptReferenceRelevance
"Amastatin did not inhibit the holo-antibiotic to cleave isolated DNA."( Aminopeptidase activity of an antitumor antibiotic, C-1027.
Aoyagi, T; Hayashi, H; Hori, M; Moriya, Y; Nagai, M; Otani, T; Sakata, N; Tsuchiya, KS, 1992
)
1

Treatment

ExcerptReferenceRelevance
"Amastatin treatment caused only a slight decrease in cytotoxicity against YAC-1 targets, but a significant decrease in cytotoxicity against P815 targets."( Surface aminopeptidase activity of rat natural killer cells. I. Biochemical and biological properties.
Amoscato, AA; Brumfield, AM; Chambers, WH; Herberman, RB; Spiess, RR, 1994
)
1.01

Compound-Compound Interactions

ExcerptReferenceRelevance
"The application of reversed-phase HPLC in combination with micro-electrospray mass spectrometry to study a substance P (SP)-hydrolysing endoprotease in human cerebrospinal fluid (hCSF) is reported."( Reversed-phase high-performance liquid chromatography combined with tandem mass spectrometry in studies of a substance P-converting enzyme from human cerebrospinal fluid.
Andrén, PE; Caprioli, RM; Eriksson, U; Nyberg, F, 1996
)
0.29

Bioavailability

ExcerptReferenceRelevance
" The inclusion of aminopeptidase inhibitors in buccal bioadhesive delivery systems could improve buccal bioavailability of Leu-enkephalin."( Peptidase activity on the surface of the porcine buccal mucosa.
Bernkop-Schnürch, A; Langoth, N; Walker, GF, 2002
)
0.31
"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 amount of IV SP, IV ACh, or inhaled capsaicin necessary to increase baseline specific airway resistance by 100% (ED200ACh or ED200SP) or 35% (ED135CAP) was determined by interpolation from dose-response curves."( Dexamethasone reduces tachykinin but not ACh airway hyperreactivity after O3.
Chodimella, V; Lang, Z; Murlas, CG, 1993
)
0.29
" Effects of PIs on antinociception were evaluated by dose-response study (ME, 1-20 nmol; PIs, 1-20 nmol each), by comparison of differences among two combinations of PIs (amastatin and captopril; captopril and phosphoramidon; amastatin and phosphoramidon) and three PIs (amastatin, captopril, and phosphoramidon), and by using opioid receptor selective antagonists."( Potentiation of [Met5]enkephalin-induced antinociception by mixture of three peptidase inhibitors in rat.
Kawaguchi, M; Kobayashi, H; Murata, T; Suzuki, T; Takahashi, S; Watanabe, M; Yoshikawa, M, 2014
)
0.6
" The effects of the PIs on antinociception and toxicity were evaluated by a dose-response study and a comparison of differences among various combinations of Dyn A (1-17) or Dyn A (1-13) and the three PIs and p-hydroxymercuribenzoate."( Effect of three peptidase inhibitors on antinociceptive potential and toxicity with intracerebroventricular administration of dynorphin A (1-17) or (1-13) in the rat.
Ajimi, J; Kawaguchi, M; Kobayashi, H; Miura, M; Suzuki, T; Takahashi, S; Tsukamoto, H; Yoshikawa, M, 2015
)
0.42
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
protease inhibitorA compound which inhibits or antagonizes the biosynthesis or actions of proteases (endopeptidases).
EC 3.4.11.* (aminopeptidase) inhibitorAn EC 3.4.* (hydrolases acting on peptide bond) inhibitor that interferes wtih the action of any aminopeptidase (EC 3.4.11.*).
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (1)

ClassDescription
tetrapeptideAny molecule that contains four amino-acid residues connected by peptide linkages.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (9)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
EWS/FLI fusion proteinHomo sapiens (human)Potency23.05060.001310.157742.8575AID1259252; AID1259253; AID1259256
[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)
Polyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)Ki0.03000.00010.03040.1570AID101207
Aminopeptidase NHomo sapiens (human)Ki0.20000.00081.956910.0000AID38376
Aminopeptidase NSus scrofa (pig)IC50 (µMol)1.10000.00053.53548.9000AID38227
Aminopeptidase NSus scrofa (pig)Ki0.68000.00052.29697.8000AID38231; AID38232; AID38233
Cytosol aminopeptidaseHomo sapiens (human)Ki5.11250.00060.16010.4200AID101207; AID101324; AID101325; AID101327
Angiotensin-converting enzymeRattus norvegicus (Norway rat)IC50 (µMol)1.10000.00090.33223.0300AID38227
Leucyl-cystinyl aminopeptidaseRattus norvegicus (Norway rat)Ki0.12000.02001.16504.4000AID101332; AID38354
Glutamyl aminopeptidaseHomo sapiens (human)Ki8.00002.30005.15008.0000AID35699
Leukotriene B4 receptor 1Homo sapiens (human)Ki0.03000.00010.51267.0000AID101207
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (49)

Processvia Protein(s)Taxonomy
negative regulation of endothelial cell proliferationPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukocyte chemotaxis involved in inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukocyte migration involved in inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukotriene production involved in inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukotriene metabolic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
humoral immune responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of angiogenesisPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukotriene biosynthetic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
lipoxygenase pathwayPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
positive regulation of bone mineralizationPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
dendritic cell migrationPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
glucose homeostasisPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
long-chain fatty acid biosynthetic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of fat cell differentiationPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of insulin secretionPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of vascular wound healingPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of wound healingPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of inflammatory response to woundingPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of cytokine production involved in inflammatory responsePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of cellular response to oxidative stressPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
leukotriene A4 biosynthetic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
regulation of reactive oxygen species biosynthetic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of response to endoplasmic reticulum stressPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
negative regulation of sprouting angiogenesisPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
positive regulation of leukocyte adhesion to arterial endothelial cellPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
lipoxin biosynthetic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
arachidonic acid metabolic processPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
lipid oxidationPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
angiogenesisAminopeptidase NHomo sapiens (human)
cell differentiationAminopeptidase NHomo sapiens (human)
symbiont entry into host cellAminopeptidase NHomo sapiens (human)
proteolysisAminopeptidase NHomo sapiens (human)
peptide catabolic processAminopeptidase NHomo sapiens (human)
proteolysisCytosol aminopeptidaseHomo sapiens (human)
cell population proliferationGlutamyl aminopeptidaseHomo sapiens (human)
cell migrationGlutamyl aminopeptidaseHomo sapiens (human)
angiogenesisGlutamyl aminopeptidaseHomo sapiens (human)
angiotensin maturationGlutamyl aminopeptidaseHomo sapiens (human)
regulation of systemic arterial blood pressure by renin-angiotensinGlutamyl aminopeptidaseHomo sapiens (human)
cell-cell signalingGlutamyl aminopeptidaseHomo sapiens (human)
glomerulus developmentGlutamyl aminopeptidaseHomo sapiens (human)
regulation of blood pressureGlutamyl aminopeptidaseHomo sapiens (human)
proteolysisGlutamyl aminopeptidaseHomo sapiens (human)
peptide catabolic processGlutamyl aminopeptidaseHomo sapiens (human)
muscle contractionLeukotriene B4 receptor 1Homo sapiens (human)
inflammatory responseLeukotriene B4 receptor 1Homo sapiens (human)
immune responseLeukotriene B4 receptor 1Homo sapiens (human)
G protein-coupled receptor signaling pathwayLeukotriene B4 receptor 1Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayLeukotriene B4 receptor 1Homo sapiens (human)
leukotriene signaling pathwayLeukotriene B4 receptor 1Homo sapiens (human)
neuropeptide signaling pathwayLeukotriene B4 receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (21)

Processvia Protein(s)Taxonomy
arachidonate 5-lipoxygenase activityPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
arachidonate 12(S)-lipoxygenase activityPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
iron ion bindingPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
protein bindingPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
hydrolase activityPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
arachidonate 8(S)-lipoxygenase activityPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
virus receptor activityAminopeptidase NHomo sapiens (human)
aminopeptidase activityAminopeptidase NHomo sapiens (human)
metallopeptidase activityAminopeptidase NHomo sapiens (human)
signaling receptor activityAminopeptidase NHomo sapiens (human)
metalloaminopeptidase activityAminopeptidase NHomo sapiens (human)
zinc ion bindingAminopeptidase NHomo sapiens (human)
peptide bindingAminopeptidase NHomo sapiens (human)
aminopeptidase activityCytosol aminopeptidaseHomo sapiens (human)
carboxypeptidase activityCytosol aminopeptidaseHomo sapiens (human)
protein bindingCytosol aminopeptidaseHomo sapiens (human)
metalloexopeptidase activityCytosol aminopeptidaseHomo sapiens (human)
manganese ion bindingCytosol aminopeptidaseHomo sapiens (human)
metalloaminopeptidase activityCytosol aminopeptidaseHomo sapiens (human)
peptidase activityCytosol aminopeptidaseHomo sapiens (human)
aminopeptidase activityGlutamyl aminopeptidaseHomo sapiens (human)
metalloaminopeptidase activityGlutamyl aminopeptidaseHomo sapiens (human)
peptide bindingGlutamyl aminopeptidaseHomo sapiens (human)
zinc ion bindingGlutamyl aminopeptidaseHomo sapiens (human)
nucleotide bindingLeukotriene B4 receptor 1Homo sapiens (human)
leukotriene receptor activityLeukotriene B4 receptor 1Homo sapiens (human)
G protein-coupled peptide receptor activityLeukotriene B4 receptor 1Homo sapiens (human)
leukotriene B4 receptor activityLeukotriene B4 receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (25)

Processvia Protein(s)Taxonomy
extracellular regionPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
extracellular spacePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nuclear envelopePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nuclear envelope lumenPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nucleoplasmPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
cytosolPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nuclear matrixPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nuclear membranePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
secretory granule lumenPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
perinuclear region of cytoplasmPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
ficolin-1-rich granule lumenPolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
nuclear envelopePolyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)
extracellular spaceAminopeptidase NHomo sapiens (human)
lysosomal membraneAminopeptidase NHomo sapiens (human)
endoplasmic reticulum-Golgi intermediate compartmentAminopeptidase NHomo sapiens (human)
plasma membraneAminopeptidase NHomo sapiens (human)
external side of plasma membraneAminopeptidase NHomo sapiens (human)
secretory granule membraneAminopeptidase NHomo sapiens (human)
extracellular exosomeAminopeptidase NHomo sapiens (human)
cytoplasmAminopeptidase NHomo sapiens (human)
plasma membraneAminopeptidase NHomo sapiens (human)
extracellular spaceAminopeptidase NHomo sapiens (human)
nucleusCytosol aminopeptidaseHomo sapiens (human)
trans-Golgi networkCytosol aminopeptidaseHomo sapiens (human)
focal adhesionCytosol aminopeptidaseHomo sapiens (human)
extracellular exosomeCytosol aminopeptidaseHomo sapiens (human)
cytoplasmCytosol aminopeptidaseHomo sapiens (human)
lysosomal membraneGlutamyl aminopeptidaseHomo sapiens (human)
plasma membraneGlutamyl aminopeptidaseHomo sapiens (human)
brush borderGlutamyl aminopeptidaseHomo sapiens (human)
external side of plasma membraneGlutamyl aminopeptidaseHomo sapiens (human)
apical plasma membraneGlutamyl aminopeptidaseHomo sapiens (human)
cytoplasmic vesicleGlutamyl aminopeptidaseHomo sapiens (human)
apical part of cellGlutamyl aminopeptidaseHomo sapiens (human)
extracellular exosomeGlutamyl aminopeptidaseHomo sapiens (human)
cytoplasmGlutamyl aminopeptidaseHomo sapiens (human)
plasma membraneGlutamyl aminopeptidaseHomo sapiens (human)
extracellular spaceGlutamyl aminopeptidaseHomo sapiens (human)
plasma membraneLeukotriene B4 receptor 1Homo sapiens (human)
plasma membraneLeukotriene B4 receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (42)

Assay IDTitleYearJournalArticle
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347154Primary screen GU AMC 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.
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.
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.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID35699Inhibition of aminopeptidase A (APA)1994Journal of medicinal chemistry, Apr-29, Volume: 37, Issue:9
Investigation of the active site of aminopeptidase A using a series of new thiol-containing inhibitors.
AID101327Compound was evaluated for the inhibition of Leucine aminopeptidase and the inhibition constant was determined after preincubating the enzyme and inhibitor1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Inhibition of aminopeptidases by amastatin and bestatin derivatives. Effect of inhibitor structure on slow-binding processes.
AID101332Inhibition of leucine aminopeptidase1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Inhibition of aminopeptidases by peptides containing ketomethylene and hydroxyethylene amide bond replacements.
AID38231Effect of inhibitor structure on the slow binding inhibition of aminopeptidase M was determined and Ki* was reported which is obtained by the equation Ki[k4/(k3 + k4)]1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Inhibition of aminopeptidases by amastatin and bestatin derivatives. Effect of inhibitor structure on slow-binding processes.
AID38233Compound was evaluated for the inhibition of Aminopeptidase M (AP-M) and the inhibition constant was determined after preincubating the enzyme and inhibitor1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Inhibition of aminopeptidases by amastatin and bestatin derivatives. Effect of inhibitor structure on slow-binding processes.
AID38227Compound was evaluated for the inhibitory activity against aminopeptidase M1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Inhibition of aminopeptidases by amastatin and bestatin derivatives. Effect of inhibitor structure on slow-binding processes.
AID38232Effect of inhibitor structure on the slow binding inhibition of aminopeptidase M was determined and the Ki was reported which is = k2/k11984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Inhibition of aminopeptidases by amastatin and bestatin derivatives. Effect of inhibitor structure on slow-binding processes.
AID101207Binding affinity for cytosolic leucine aminopeptidase (LAP) from porcine kidney2003Journal of medicinal chemistry, Jun-19, Volume: 46, Issue:13
The most potent organophosphorus inhibitors of leucine aminopeptidase. Structure-based design, chemistry, and activity.
AID101324Effect of inhibitor structure on the slow binding inhibition of Leucine aminopeptidase was determined and Ki* was reported which is obtained by the equation Ki[k4/(k3 + k4)]1984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Inhibition of aminopeptidases by amastatin and bestatin derivatives. Effect of inhibitor structure on slow-binding processes.
AID101325Effect of inhibitor structure on the slow binding inhibition of Leucine aminopeptidase was determined and the Ki was reported which is = k2/k11984Journal of medicinal chemistry, Apr, Volume: 27, Issue:4
Inhibition of aminopeptidases by amastatin and bestatin derivatives. Effect of inhibitor structure on slow-binding processes.
AID38354Inhibition of aminopeptidase M or membrane leucine aminopeptidase1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Inhibition of aminopeptidases by peptides containing ketomethylene and hydroxyethylene amide bond replacements.
AID38376Inhibition of aminopeptidase N (APN)1994Journal of medicinal chemistry, Apr-29, Volume: 37, Issue:9
Investigation of the active site of aminopeptidase A using a series of new thiol-containing inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (178)

TimeframeStudies, This Drug (%)All Drugs %
pre-199044 (24.72)18.7374
1990's73 (41.01)18.2507
2000's40 (22.47)29.6817
2010's13 (7.30)24.3611
2020's8 (4.49)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 30.30

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 Index30.30 (24.57)
Research Supply Index5.21 (2.92)
Research Growth Index4.43 (4.65)
Search Engine Demand Index38.40 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (30.30)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews3 (1.64%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other180 (98.36%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]