Page last updated: 2024-12-11

erbstatin

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Description

erbstatin: from actinomycetes; an inhibitor of EGF-receptor kinase & other protein-tyrosine kinases; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5328552
CHEMBL ID47986
SCHEMBL ID9320680
SCHEMBL ID9320673
MeSH IDM0138849

Synonyms (33)

Synonym
n-[(e)-2-(2,5-dihydroxyphenyl)ethenyl]formamide
bdbm3973
cid_58035
nsc606641
erbstatin, synthetic non-solvated
100827-28-9
nsc610187
nsc-606641
nsc-610187
erbstatin
n-[(e)-2-(2,5-dihydroxyphenyl)vinyl]formamide
formamide, n-[(1e)-2-(2,5-dihydroxyphenyl)ethenyl]-
formamide, n-(2-(2,5-dihydroxyphenyl)ethenyl)-, (e)-
(e)-n-(2-(2,5-dihydroxyphenyl)ethenyl)formamide
nsc 610187
smr000529090
CHEMBL47986
NCGC00246858-01
AKOS006273458
wdh83k6t5p ,
unii-wdh83k6t5p
HMS2270A13
n-((e)-2-(2,5-dihydroxyphenyl)ethenyl)formamide
REGID_FOR_CID_5328552
SIHZWGODIRRSRA-ONEGZZNKSA-N
SCHEMBL9320680
SCHEMBL9320673
(e)-n-(2,5-dihydroxystyryl)formamide
Q27292578
STARBLD0005202
DTXSID801318622
HY-113549
CS-0062676

Research Excerpts

Overview

Erbstatin is an inhibitor of epidermal growth factor (EGF) receptor and p60v-src-associated tyrosine kinase.

ExcerptReferenceRelevance
"Erbstatin is an inhibitor of epidermal growth factor (EGF) receptor and p60v-src-associated tyrosine kinase."( [Inhibitors of oncogene product functions].
Umezawa, K, 1990
)
1

Actions

Erbstatin was found to inhibit protein kinase C (PKC) with an IC50 of 19.8 +/- 3.2 microM. It did not inhibit the binding of epidermal growth factor to its receptor.

ExcerptReferenceRelevance
"Erbstatin did not inhibit serum-induced DNA synthesis at all."( Inhibition of serum-induced M-phase progression by a tyrosine kinase inhibitor, erbstatin.
Sugata, D; Umezawa, K; Yamashita, K, 1993
)
1.23
"Erbstatin was found to inhibit protein kinase C (PKC) with an IC50 of 19.8 +/- 3.2 microM."( Inhibition of protein kinase C by the tyrosine kinase inhibitor erbstatin.
Bishop, WR; Doll, RJ; Petrin, J; Ramesh, U; Wang, L, 1990
)
1.24
"Erbstatin did not inhibit the binding of epidermal growth factor to its receptor but did inhibit internalization of epidermal growth factor-receptor complexes."( In situ inhibition of tyrosine protein kinase by erbstatin.
Imoto, M; Sawa, T; Takeuchi, T; Umezawa, H; Umezawa, K, 1987
)
1.25

Dosage Studied

ExcerptRelevanceReference
" By contrast, phenylephrine-induced dose-response curves in rabbit aorta were largely unaffected by tyrosine kinase inhibitors at 50 microM."( Alpha 2-adrenoceptor-mediated vasoconstriction requires a tyrosine kinase.
Deth, RC; Jinsi, A, 1995
)
0.29
" The dose-response curves showed that tyrosine phosphorylation and O2- release were stimulated in parallel by PMA, whereas tyrosine phosphorylation and an increase in [Ca2+]i, but not O2- release, were stimulated in parallel by FMLP or ionomycin."( Activation of the respiratory burst and tyrosine phosphorylation of proteins in human neutrophils: no direct relationship and involvement of protein kinase C-dependent and -independent signaling pathways.
Azuma, EK; Kitagawa, S; Mizoguchi, H; Saito, M; Takaku, F; Umezawa, K; Yuo, A, 1993
)
0.29
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (46)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency10.00000.003245.467312,589.2998AID2517
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency7.94330.004023.8416100.0000AID485290
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency14.09190.140911.194039.8107AID2451
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency3.16230.631035.7641100.0000AID504339
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency28.18380.177814.390939.8107AID2147
LuciferasePhotinus pyralis (common eastern firefly)Potency23.93410.007215.758889.3584AID588342
thioredoxin reductaseRattus norvegicus (Norway rat)Potency70.79460.100020.879379.4328AID588453
ClpPBacillus subtilisPotency22.38721.995322.673039.8107AID651965
phosphopantetheinyl transferaseBacillus subtilisPotency14.12540.141337.9142100.0000AID1490
USP1 protein, partialHomo sapiens (human)Potency50.11870.031637.5844354.8130AID743255
GLS proteinHomo sapiens (human)Potency35.48130.35487.935539.8107AID624170
TDP1 proteinHomo sapiens (human)Potency4.36020.000811.382244.6684AID686978; AID686979
Microtubule-associated protein tauHomo sapiens (human)Potency28.37090.180013.557439.8107AID1460; AID1468
thioredoxin glutathione reductaseSchistosoma mansoniPotency6.30960.100022.9075100.0000AID485364
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency14.12540.707912.194339.8107AID720542
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency15.84890.011212.4002100.0000AID1030
regulator of G-protein signaling 4Homo sapiens (human)Potency50.11870.531815.435837.6858AID504845
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency79.43280.707936.904389.1251AID504333
pyruvate kinaseLeishmania mexicana mexicanaPotency16.66210.398113.744731.6228AID1721; AID1722; AID2559
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency1.41250.035520.977089.1251AID504332
lysosomal alpha-glucosidase preproproteinHomo sapiens (human)Potency22.38720.036619.637650.1187AID2100
chromobox protein homolog 1Homo sapiens (human)Potency3.98110.006026.168889.1251AID540317
pyruvate kinase PKM isoform aHomo sapiens (human)Potency10.00000.04017.459031.6228AID1631; AID1634
DNA polymerase betaHomo sapiens (human)Potency56.23410.022421.010289.1251AID485314
flap endonuclease 1Homo sapiens (human)Potency17.78280.133725.412989.1251AID588795
serine/threonine-protein kinase PLK1Homo sapiens (human)Potency37.68580.168316.404067.0158AID720504
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency35.48130.425612.059128.1838AID504891
DNA polymerase eta isoform 1Homo sapiens (human)Potency50.11870.100028.9256213.3130AID588591
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency22.38720.050127.073689.1251AID588590
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency3.16230.15855.287912.5893AID540303
plasminogen precursorMus musculus (house mouse)Potency3.16230.15855.287912.5893AID540303
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency3.16230.15855.287912.5893AID540303
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency13.53450.00798.23321,122.0200AID2546; AID2551
lethal(3)malignant brain tumor-like protein 1 isoform IHomo sapiens (human)Potency15.84890.075215.225339.8107AID485360
gemininHomo sapiens (human)Potency25.92900.004611.374133.4983AID624296; AID624297
DNA polymerase kappa isoform 1Homo sapiens (human)Potency44.66840.031622.3146100.0000AID588579
DNA dC->dU-editing enzyme APOBEC-3G isoform 1Homo sapiens (human)Potency22.38720.058010.694926.6086AID602310
Endothelin receptor type BRattus norvegicus (Norway rat)Potency4.46680.562315.160931.6228AID1721
Endothelin-1 receptorRattus norvegicus (Norway rat)Potency4.46680.562315.160931.6228AID1721
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency30.13130.060110.745337.9330AID485367
[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)
M18 aspartyl aminopeptidasePlasmodium falciparum 3D7IC50 (µMol)3.71900.385113.0782100.0000AID2195
VifHuman immunodeficiency virus 1IC50 (µMol)1.72000.270034.0015100.0000AID1117319
TatHuman immunodeficiency virus 1IC50 (µMol)10.97000.996039.8009100.0000AID1117361
high affinity choline transporter 1 isoform aHomo sapiens (human)IC50 (µMol)2.46210.00036.210228.8403AID504840; AID588401
DNA dC->dU-editing enzyme APOBEC-3G isoform 1Homo sapiens (human)IC50 (µMol)1.72000.270026.3638100.0000AID1117319
Epidermal growth factor receptorHomo sapiens (human)IC50 (µMol)8.00000.00000.536910.0000AID1795584; AID1795632; AID67293; AID69555
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (89)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
epidermal growth factor receptor signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cell population proliferationEpidermal growth factor receptorHomo sapiens (human)
MAPK cascadeEpidermal growth factor receptorHomo sapiens (human)
ossificationEpidermal growth factor receptorHomo sapiens (human)
embryonic placenta developmentEpidermal growth factor receptorHomo sapiens (human)
positive regulation of protein phosphorylationEpidermal growth factor receptorHomo sapiens (human)
hair follicle developmentEpidermal growth factor receptorHomo sapiens (human)
translationEpidermal growth factor receptorHomo sapiens (human)
signal transductionEpidermal growth factor receptorHomo sapiens (human)
epidermal growth factor receptor signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
activation of phospholipase C activityEpidermal growth factor receptorHomo sapiens (human)
salivary gland morphogenesisEpidermal growth factor receptorHomo sapiens (human)
midgut developmentEpidermal growth factor receptorHomo sapiens (human)
learning or memoryEpidermal growth factor receptorHomo sapiens (human)
circadian rhythmEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cell population proliferationEpidermal growth factor receptorHomo sapiens (human)
diterpenoid metabolic processEpidermal growth factor receptorHomo sapiens (human)
peptidyl-tyrosine phosphorylationEpidermal growth factor receptorHomo sapiens (human)
cerebral cortex cell migrationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cell growthEpidermal growth factor receptorHomo sapiens (human)
lung developmentEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cell migrationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of superoxide anion generationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationEpidermal growth factor receptorHomo sapiens (human)
response to cobalaminEpidermal growth factor receptorHomo sapiens (human)
response to hydroxyisoflavoneEpidermal growth factor receptorHomo sapiens (human)
cellular response to reactive oxygen speciesEpidermal growth factor receptorHomo sapiens (human)
peptidyl-tyrosine autophosphorylationEpidermal growth factor receptorHomo sapiens (human)
ERBB2-EGFR signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
negative regulation of epidermal growth factor receptor signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
negative regulation of protein catabolic processEpidermal growth factor receptorHomo sapiens (human)
vasodilationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of phosphorylationEpidermal growth factor receptorHomo sapiens (human)
ovulation cycleEpidermal growth factor receptorHomo sapiens (human)
hydrogen peroxide metabolic processEpidermal growth factor receptorHomo sapiens (human)
negative regulation of apoptotic processEpidermal growth factor receptorHomo sapiens (human)
positive regulation of MAP kinase activityEpidermal growth factor receptorHomo sapiens (human)
tongue developmentEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cyclin-dependent protein serine/threonine kinase activityEpidermal growth factor receptorHomo sapiens (human)
positive regulation of DNA repairEpidermal growth factor receptorHomo sapiens (human)
positive regulation of DNA replicationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of bone resorptionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of DNA-templated transcriptionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of vasoconstrictionEpidermal growth factor receptorHomo sapiens (human)
negative regulation of mitotic cell cycleEpidermal growth factor receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIEpidermal growth factor receptorHomo sapiens (human)
regulation of JNK cascadeEpidermal growth factor receptorHomo sapiens (human)
symbiont entry into host cellEpidermal growth factor receptorHomo sapiens (human)
protein autophosphorylationEpidermal growth factor receptorHomo sapiens (human)
astrocyte activationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of fibroblast proliferationEpidermal growth factor receptorHomo sapiens (human)
digestive tract morphogenesisEpidermal growth factor receptorHomo sapiens (human)
positive regulation of smooth muscle cell proliferationEpidermal growth factor receptorHomo sapiens (human)
neuron projection morphogenesisEpidermal growth factor receptorHomo sapiens (human)
epithelial cell proliferationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of epithelial cell proliferationEpidermal growth factor receptorHomo sapiens (human)
regulation of peptidyl-tyrosine phosphorylationEpidermal growth factor receptorHomo sapiens (human)
protein insertion into membraneEpidermal growth factor receptorHomo sapiens (human)
response to calcium ionEpidermal growth factor receptorHomo sapiens (human)
regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of synaptic transmission, glutamatergicEpidermal growth factor receptorHomo sapiens (human)
positive regulation of glial cell proliferationEpidermal growth factor receptorHomo sapiens (human)
morphogenesis of an epithelial foldEpidermal growth factor receptorHomo sapiens (human)
eyelid development in camera-type eyeEpidermal growth factor receptorHomo sapiens (human)
response to UV-AEpidermal growth factor receptorHomo sapiens (human)
positive regulation of mucus secretionEpidermal growth factor receptorHomo sapiens (human)
regulation of ERK1 and ERK2 cascadeEpidermal growth factor receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeEpidermal growth factor receptorHomo sapiens (human)
cellular response to amino acid stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to mechanical stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to cadmium ionEpidermal growth factor receptorHomo sapiens (human)
cellular response to epidermal growth factor stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to estradiol stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to xenobiotic stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to dexamethasone stimulusEpidermal growth factor receptorHomo sapiens (human)
positive regulation of canonical Wnt signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
liver regenerationEpidermal growth factor receptorHomo sapiens (human)
cell-cell adhesionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of protein kinase C activityEpidermal growth factor receptorHomo sapiens (human)
positive regulation of G1/S transition of mitotic cell cycleEpidermal growth factor receptorHomo sapiens (human)
positive regulation of non-canonical NF-kappaB signal transductionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of prolactin secretionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of miRNA transcriptionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of protein localization to plasma membraneEpidermal growth factor receptorHomo sapiens (human)
negative regulation of cardiocyte differentiationEpidermal growth factor receptorHomo sapiens (human)
neurogenesisEpidermal growth factor receptorHomo sapiens (human)
multicellular organism developmentEpidermal growth factor receptorHomo sapiens (human)
positive regulation of kinase activityEpidermal growth factor receptorHomo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (24)

Processvia Protein(s)Taxonomy
epidermal growth factor receptor activityEpidermal growth factor receptorHomo sapiens (human)
virus receptor activityEpidermal growth factor receptorHomo sapiens (human)
chromatin bindingEpidermal growth factor receptorHomo sapiens (human)
double-stranded DNA bindingEpidermal growth factor receptorHomo sapiens (human)
MAP kinase kinase kinase activityEpidermal growth factor receptorHomo sapiens (human)
protein tyrosine kinase activityEpidermal growth factor receptorHomo sapiens (human)
transmembrane receptor protein tyrosine kinase activityEpidermal growth factor receptorHomo sapiens (human)
transmembrane signaling receptor activityEpidermal growth factor receptorHomo sapiens (human)
epidermal growth factor receptor activityEpidermal growth factor receptorHomo sapiens (human)
integrin bindingEpidermal growth factor receptorHomo sapiens (human)
protein bindingEpidermal growth factor receptorHomo sapiens (human)
calmodulin bindingEpidermal growth factor receptorHomo sapiens (human)
ATP bindingEpidermal growth factor receptorHomo sapiens (human)
enzyme bindingEpidermal growth factor receptorHomo sapiens (human)
kinase bindingEpidermal growth factor receptorHomo sapiens (human)
protein kinase bindingEpidermal growth factor receptorHomo sapiens (human)
protein phosphatase bindingEpidermal growth factor receptorHomo sapiens (human)
protein tyrosine kinase activator activityEpidermal growth factor receptorHomo sapiens (human)
transmembrane receptor protein tyrosine kinase activator activityEpidermal growth factor receptorHomo sapiens (human)
ubiquitin protein ligase bindingEpidermal growth factor receptorHomo sapiens (human)
identical protein bindingEpidermal growth factor receptorHomo sapiens (human)
cadherin bindingEpidermal growth factor receptorHomo sapiens (human)
actin filament bindingEpidermal growth factor receptorHomo sapiens (human)
ATPase bindingEpidermal growth factor receptorHomo sapiens (human)
epidermal growth factor bindingEpidermal growth factor receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (26)

Processvia Protein(s)Taxonomy
endosomeEpidermal growth factor receptorHomo sapiens (human)
plasma membraneEpidermal growth factor receptorHomo sapiens (human)
ruffle membraneEpidermal growth factor receptorHomo sapiens (human)
Golgi membraneEpidermal growth factor receptorHomo sapiens (human)
extracellular spaceEpidermal growth factor receptorHomo sapiens (human)
nucleusEpidermal growth factor receptorHomo sapiens (human)
cytoplasmEpidermal growth factor receptorHomo sapiens (human)
endosomeEpidermal growth factor receptorHomo sapiens (human)
endoplasmic reticulum membraneEpidermal growth factor receptorHomo sapiens (human)
plasma membraneEpidermal growth factor receptorHomo sapiens (human)
focal adhesionEpidermal growth factor receptorHomo sapiens (human)
cell surfaceEpidermal growth factor receptorHomo sapiens (human)
endosome membraneEpidermal growth factor receptorHomo sapiens (human)
membraneEpidermal growth factor receptorHomo sapiens (human)
basolateral plasma membraneEpidermal growth factor receptorHomo sapiens (human)
apical plasma membraneEpidermal growth factor receptorHomo sapiens (human)
cell junctionEpidermal growth factor receptorHomo sapiens (human)
clathrin-coated endocytic vesicle membraneEpidermal growth factor receptorHomo sapiens (human)
early endosome membraneEpidermal growth factor receptorHomo sapiens (human)
nuclear membraneEpidermal growth factor receptorHomo sapiens (human)
membrane raftEpidermal growth factor receptorHomo sapiens (human)
perinuclear region of cytoplasmEpidermal growth factor receptorHomo sapiens (human)
multivesicular body, internal vesicle lumenEpidermal growth factor receptorHomo sapiens (human)
intracellular vesicleEpidermal growth factor receptorHomo sapiens (human)
protein-containing complexEpidermal growth factor receptorHomo sapiens (human)
receptor complexEpidermal growth factor receptorHomo sapiens (human)
Shc-EGFR complexEpidermal growth factor receptorHomo sapiens (human)
basal plasma membraneEpidermal growth factor receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (27)

Assay IDTitleYearJournalArticle
AID358494Iv vivo cytotoxicity against mouse L1210 cells relative to control in presence of foroxymithine1992Journal of natural products, Nov, Volume: 55, Issue:11
Protein-tyrosine kinase inhibition: mechanism-based discovery of antitumor agents.
AID69555Inhibitory concentration of EGF dependent autophosphorylation of epidermal growth factor receptor kinase1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
Tyrphostins I: synthesis and biological activity of protein tyrosine kinase inhibitors.
AID358493Cytotoxicity against mouse L1210 cells1992Journal of natural products, Nov, Volume: 55, Issue:11
Protein-tyrosine kinase inhibition: mechanism-based discovery of antitumor agents.
AID337241Inhibition of protein kinase C
AID67293Inhibition of EGF-stimulated EGFR tyrosine kinase activity using plasma membrane vesicles shed from cultured human A431 carcinoma cells1993Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
Tyrosine kinase inhibitors. 1. Structure-activity relationships for inhibition of epidermal growth factor receptor tyrosine kinase activity by 2,3-dihydro-2-thioxo-1H-indole-3-alkanoic acids and 2,2'-dithiobis(1H-indole-3-alkanoic acids).
AID358496Cytotoxicity against human A431 cells1992Journal of natural products, Nov, Volume: 55, Issue:11
Protein-tyrosine kinase inhibition: mechanism-based discovery of antitumor agents.
AID337240Inhibition of protein kinase A
AID337238Inhibition of mouse EGFR by liquid scintillation counting
AID358492Cytotoxicity against Rous sarcoma virus-infected rat kidney cells1992Journal of natural products, Nov, Volume: 55, Issue:11
Protein-tyrosine kinase inhibition: mechanism-based discovery of antitumor agents.
AID358179Inhibition of EGFR1992Journal of natural products, Nov, Volume: 55, Issue:11
Protein-tyrosine kinase inhibition: mechanism-based discovery of antitumor agents.
AID337242Inhibition of phosphatidylinositol kinase
AID337239Inhibition of EGFR
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1795584Kinase Inhibition Assay from Article 10.1021/jm00069a003: \\Tyrosine kinase inhibitors. 1. Structure-activity relationships for inhibition of epidermal growth factor receptor tyrosine kinase activity by 2,3-dihydro-2-thioxo-1H-indole-3-alkanoic acids and 21993Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
Tyrosine kinase inhibitors. 1. Structure-activity relationships for inhibition of epidermal growth factor receptor tyrosine kinase activity by 2,3-dihydro-2-thioxo-1H-indole-3-alkanoic acids and 2,2'-dithiobis(1H-indole-3-alkanoic acids).
AID1795632EGFR assay from Article 10.1021/jm00130a020: \\Tyrphostins I: synthesis and biological activity of protein tyrosine kinase inhibitors.\\1989Journal of medicinal chemistry, Oct, Volume: 32, Issue:10
Tyrphostins I: synthesis and biological activity of protein tyrosine kinase inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (140)

TimeframeStudies, This Drug (%)All Drugs %
pre-19909 (6.43)18.7374
1990's104 (74.29)18.2507
2000's21 (15.00)29.6817
2010's5 (3.57)24.3611
2020's1 (0.71)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 21.03

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 Index21.03 (24.57)
Research Supply Index4.98 (2.92)
Research Growth Index5.43 (4.65)
Search Engine Demand Index21.17 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (21.03)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews6 (4.14%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other139 (95.86%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]