Page last updated: 2024-11-06

carbobenzoxyvalylphenylalanine aldehyde

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Description

Z-Val-Phe-H : A dipeptide resulting from the formal condensation of the carboxy group of N-benzyloxycarbonyl-L-valine with the amino group of L-phenylalanine aldehyde. It is a potent cell-permeable inhibitor of calpain I and II, and is also a gamma-secretase inhibitor. [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 CID72430
CHEMBL ID286722
CHEBI ID82818
SCHEMBL ID5133312
MeSH IDM0162148

Synonyms (74)

Synonym
BRD-K43245338-001-02-4
EU-0100730
lopac-m-6690
NCGC00015696-01
BIO2_000757
BIO2_000277
BSPBIO_001557
IDI1_034027
LOPAC0_000730
MDL 28170 ,
n-[n-[(phenylmethoxy)carbonyl]-l-valyl]-l-phenylalanine, aldehyde deriv.
cbz-val-phe-cho
BCBCMAP01_000248
NCGC00094076-03
cbz-val-phe-h
cbz-valpheh
carbamic acid, (1-(((1-formyl-2-phenylethyl)amino)carbonyl)-2-methylpropyl)-, phenylmethyl ester, (s-(r*,r*))-
phenylmethyl ((1s)-1-((((1s)-1-formyl-2-phenylethyl)amino)carbonyl)-2-methylpropyl)carbamate
n-cbz-val-phe-al
carbobenzoxyvalylphenylalanine aldehyde
n-benzyloxycarbonylvalylphenylalaninal
n-benzyloxycarbonylvalylphenylalanine aldehyde
carbamic acid, ((1s)-1-((((1s)-1-formyl-2-phenylethyl)amino)carbonyl)-2-methylpropyl)-, phenyl ester
KBIOSS_000277
KBIO3_000553
KBIO2_005413
KBIO2_002845
KBIOGR_000277
KBIO3_000554
KBIO2_000277
NCGC00094076-01
NCGC00094076-04
NCGC00094076-02
HMS1989N19
M 6690
NCGC00094076-05
CHEMBL286722 ,
chebi:82818 ,
benzyl n-[(2s)-3-methyl-1-oxo-1-[[(2s)-1-oxo-3-phenylpropan-2-yl]amino]butan-2-yl]carbamate
HMS1361N19
HMS1791N19
mdl-2170
benzyl (s)-3-methyl-1-oxo-1-((s)-1-oxo-3-phenylpropan-2-ylamino)butan-2-ylcarbamate
[(s)-1-((s)-1-benzyl-2-oxo-ethylcarbamoyl)-2-methyl-propyl]-carbamic acid benzyl ester
bdbm50014577
z-val-phe-h
HMS3262A22
CCG-204815
unii-wcj9lq197s
wcj9lq197s ,
LP00730
carbamic acid, n-((1s)-1-(((1-formyl-2-phenylethyl)amino)carbonyl)-2-methylpropyl)-, phenylmethyl ester
mdl 28,170
z-val-phe-al
benzyl [(2s)-3-methyl-1-oxo-1-{[(2s)-1-oxo-3-phenylpropan-2-yl]amino}butan-2-yl]carbamate
l-benzyloxycarbonyl-l-valyl-l-phenylalaninal
tox21_500730
NCGC00261415-01
SCHEMBL5133312
HMS3402N19
sr-01000076004
SR-01000076004-1
Q27156387
benzyl ((s)-3-methyl-1-oxo-1-(((s)-1-oxo-3-phenylpropan-2-yl)amino)butan-2-yl)carbamate
NGBKFLTYGSREKK-PMACEKPBSA-N
cbz(l)-val-phe-h
756485-04-8
SDCCGSBI-0050708.P003
NCGC00094076-06
n-benzyloxycarbonyl-l-valyl-l-phenylalaninal
gtpl10745
2-{[(benzyloxy)(hydroxy)methylidene]amino}-3-methyl-n-(1-oxo-3-phenylpropan-2-yl)butanimidic acid
DTXSID801007990
mdl-28170; z-val-phe-cho
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (5)

RoleDescription
EC 3.4.22.53 (calpain-2) inhibitorA calpain inhibitor that interferes with the action of calpain-2 (EC 3.4.22.53).
EC 3.4.22.52 (calpain-1) inhibitorA calpain inhibitor that interferes with the action of calpain-1 (EC 3.4.22.52).
EC 3.4.23.46 (memapsin 2) inhibitorAn EC 3.4.23.* (aspartic endopeptidase) inhibitor that interferes with the activity of memapsin 2 (EC 3.4.23.46).
antileishmanial agentAn antiprotozoal drug used to treat or prevent infections caused by protozoan parasites that belong to the genus Leishmania.
apoptosis inhibitorAny substance that inhibits the process of apoptosis (programmed cell death) in multi-celled organisms.
[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 (3)

ClassDescription
aldehydeA compound RC(=O)H, in which a carbonyl group is bonded to one hydrogen atom and to one R group.
dipeptideAny molecule that contains two amino-acid residues connected by peptide linkages.
carbamate esterAny ester of carbamic acid or its N-substituted derivatives.
[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 (44)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, CruzipainTrypanosoma cruziPotency0.03160.002014.677939.8107AID1476; AID1478
thioredoxin reductaseRattus norvegicus (Norway rat)Potency0.50120.100020.879379.4328AID588453
NFKB1 protein, partialHomo sapiens (human)Potency1.77830.02827.055915.8489AID895; AID928
TDP1 proteinHomo sapiens (human)Potency34.30430.000811.382244.6684AID686978; AID686979
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency22.38720.011212.4002100.0000AID1030
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency15.56860.001530.607315,848.9004AID1224819; AID1224820; AID1224821
arylsulfatase AHomo sapiens (human)Potency2.39341.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency41.45680.035520.977089.1251AID504332
Bloom syndrome protein isoform 1Homo sapiens (human)Potency0.00040.540617.639296.1227AID2364; AID2528
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency10.691023.934123.934123.9341AID1967
cytochrome P450 2C9 precursorHomo sapiens (human)Potency39.81070.00636.904339.8107AID883
D(1A) dopamine receptorHomo sapiens (human)Potency2.05950.02245.944922.3872AID488982
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency70.79460.354828.065989.1251AID504847
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency1.58490.010039.53711,122.0200AID1479
DNA polymerase eta isoform 1Homo sapiens (human)Potency0.28180.100028.9256213.3130AID588591
gemininHomo sapiens (human)Potency14.12540.004611.374133.4983AID463097
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency6.30960.031610.279239.8107AID884; AID885
M-phase phosphoprotein 8Homo sapiens (human)Potency56.23410.177824.735279.4328AID488949
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency35.48130.251215.843239.8107AID504327
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency0.01410.00106.000935.4813AID944
lamin isoform A-delta10Homo sapiens (human)Potency18.85410.891312.067628.1838AID1459; AID1487
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency39.81070.00638.235039.8107AID883
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency6.30961.000012.224831.6228AID885
[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)
Chymotrypsinogen ABos taurus (cattle)Ki54.00000.90004.00008.7000AID219281
Calpain-1 catalytic subunitHomo sapiens (human)IC50 (µMol)0.30000.00021.059210.0000AID46723
Calpain-1 catalytic subunitHomo sapiens (human)Ki0.00800.00700.01810.0560AID46727
Cathepsin BHomo sapiens (human)Ki0.02400.00001.21808.6000AID50287
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2IC50 (µMol)20.00000.00022.45859.9600AID1845236
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)IC50 (µMol)0.30000.00051.48357.8000AID46723
Calpain-1 catalytic subunitSus scrofa (pig)Ki0.01000.01000.86403.9600AID1662230
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (17)

Processvia Protein(s)Taxonomy
digestionChymotrypsinogen ABos taurus (cattle)
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)
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (18)

Processvia Protein(s)Taxonomy
protein bindingChymotrypsinogen ABos taurus (cattle)
serpin family protein bindingChymotrypsinogen ABos taurus (cattle)
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)
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)
3'-5'-RNA exonuclease activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
RNA-dependent RNA polymerase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
cysteine-type endopeptidase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
mRNA 5'-cap (guanine-N7-)-methyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
mRNA (nucleoside-2'-O-)-methyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
mRNA guanylyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
RNA endonuclease activity, producing 3'-phosphomonoestersReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
ISG15-specific peptidase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
5'-3' RNA helicase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
protein guanylyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (22)

Processvia Protein(s)Taxonomy
extracellular regionChymotrypsinogen ABos taurus (cattle)
serine protease inhibitor complexChymotrypsinogen ABos taurus (cattle)
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)
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)
double membrane vesicle viral factory outer membraneReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (40)

Assay IDTitleYearJournalArticle
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
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.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
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.
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS 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.
AID1347151Optimization of GU AMC 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.
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.
AID46729Inhibitory activity against Calpain-II receptor in porcine kidney; Not determined1998Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15
D-amino acid containing, high-affinity inhibitors of recombinant human calpain I.
AID1916513Antileishmanial activity against Leishmania amazonensis promastigotes assessed as reduction in parasite survival measured after 48 hrs by Neubauer counting chamber based analysis2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Cysteine proteases as potential targets for anti-trypanosomatid drug discovery.
AID46333Inhibition of Calpain1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
Alpha-diketone and alpha-keto ester derivatives of N-protected amino acids and peptides as novel inhibitors of cysteine and serine proteinases.
AID219281Inhibition of alpha-chymotrypsin1990Journal of medicinal chemistry, Jan, Volume: 33, Issue:1
Alpha-diketone and alpha-keto ester derivatives of N-protected amino acids and peptides as novel inhibitors of cysteine and serine proteinases.
AID36978Inhibitory activity against Bovine pancreas alpha-chymotrypsin at 10 uM; Not determined1998Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15
D-amino acid containing, high-affinity inhibitors of recombinant human calpain I.
AID1916516Antitrypanosomal activity against bloodstream Trypanosoma cruzi Y strain trypomastigote assessed as reduction in parasite viability incubated for 24 hrs by Neubauer chamber based analysis2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Cysteine proteases as potential targets for anti-trypanosomatid drug discovery.
AID1662229Antiproliferative activity against human A375 cells assessed as inhibition of cell growth after 48 hrs by sulforhodamine B colorimetric assay2020Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
Synthesis and antiproliferative activity of sulfonamide-based peptidomimetic calpain inhibitors.
AID210832Inhibitory activity against human plasma thrombin at 10 uM; Not determined1998Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15
D-amino acid containing, high-affinity inhibitors of recombinant human calpain I.
AID1662227Antiproliferative activity against human PC3 cells assessed as inhibition of cell growth after 72 hrs by MTT assay2020Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
Synthesis and antiproliferative activity of sulfonamide-based peptidomimetic calpain inhibitors.
AID1845236Inhibition of SARS-CoV-2 MPro2021Bioorganic & medicinal chemistry, 01-01, Volume: 29Protease targeted COVID-19 drug discovery and its challenges: Insight into viral main protease (Mpro) and papain-like protease (PLpro) inhibitors.
AID1916515Antitrypanosomal activity against Trypanosoma cruzi Dm28c epimastigotes assessed as reduction in parasite viability incubated for 48 hrs by trypan blue staining based Neubauer counting chamber analysis2021Bioorganic & medicinal chemistry, 09-15, Volume: 46Cysteine proteases as potential targets for anti-trypanosomatid drug discovery.
AID46727Inhibitory activity against recombinant human Calpain-I receptor1998Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15
D-amino acid containing, high-affinity inhibitors of recombinant human calpain I.
AID46723Inhibition of intracellular Calpain-I receptor using intact cell assay system1998Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15
D-amino acid containing, high-affinity inhibitors of recombinant human calpain I.
AID50287Inhibitory activity against cathepsin B receptor in human liver1998Journal of medicinal chemistry, Jul-16, Volume: 41, Issue:15
D-amino acid containing, high-affinity inhibitors of recombinant human calpain I.
AID1662230Inhibition of mu-calpain in porcine erythrocyte using Suc-Leu-Tyr-AMC as substrate by microtiter plate assay based Dixon plot analysis2020Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
Synthesis and antiproliferative activity of sulfonamide-based peptidomimetic calpain inhibitors.
AID1662228Antiproliferative activity against mouse B16-F1 cells assessed as inhibition of cell growth after 48 hrs by sulforhodamine B colorimetric assay2020Bioorganic & medicinal chemistry, 05-01, Volume: 28, Issue:9
Synthesis and antiproliferative activity of sulfonamide-based peptidomimetic calpain inhibitors.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (20)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's2 (10.00)18.2507
2000's1 (5.00)29.6817
2010's8 (40.00)24.3611
2020's9 (45.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.04

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 Index12.04 (24.57)
Research Supply Index3.04 (2.92)
Research Growth Index5.08 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.04)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (10.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other18 (90.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]