Page last updated: 2024-10-15

tyrphostin ag 1112

Description

tyrphostin AG 1112: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID135402851
CHEMBL ID65827
SCHEMBL ID18045510
SCHEMBL ID6055081
MeSH IDM0225525

Synonyms (19)

Synonym
indole-containing inhibitor 11
3-amino-5-[(1z)-1-cyano-2-(1h-indol-3-yl)eth-1-en-1-yl]-1h-pyrazole-4-carbonitrile
bdbm5177
tyrphostin ag 1112
AKOS000112967
CHEMBL65827
ag-1112
1h-pyrazole-3-acetonitrile, 5-amino-4-cyano-alpha-(1h-indol-3-ylmethylene), (z)-
153150-84-6
ag 1112
SCHEMBL18045510
SCHEMBL6055081
tyrphostin ag 1112, >=98%, solid
5-azanyl-3-[(~{z})-1-cyano-2-(1~{h}-indol-3-yl)ethenyl]-1~{h}-pyrazole-4-carbonitrile
3-amino-5-[(z)-1-cyano-2-(1h-indol-3-yl)ethenyl]-1h-pyrazole-4-carbonitrile
tyrphostin ag-1112
tyrphostin ag1112
HY-120036
CS-0069341
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Epidermal growth factor receptorHomo sapiens (human)IC50 (µMol)100.00000.00000.536910.0000AID1795753
Platelet-derived growth factor receptor betaHomo sapiens (human)IC50 (µMol)100.00000.00060.80078.5000AID1795753
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (116)

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)
signal transductionPlatelet-derived growth factor receptor betaHomo sapiens (human)
G protein-coupled receptor signaling pathwayPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of cell population proliferationPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of phospholipase C activityPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of smooth muscle cell migrationPlatelet-derived growth factor receptor betaHomo sapiens (human)
peptidyl-tyrosine phosphorylationPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of cell migrationPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of phosphoprotein phosphatase activityPlatelet-derived growth factor receptor betaHomo sapiens (human)
regulation of actin cytoskeleton organizationPlatelet-derived growth factor receptor betaHomo sapiens (human)
cell migration involved in vasculogenesisPlatelet-derived growth factor receptor betaHomo sapiens (human)
platelet-derived growth factor receptor-beta signaling pathwayPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of metanephric mesenchymal cell migration by platelet-derived growth factor receptor-beta signaling pathwayPlatelet-derived growth factor receptor betaHomo sapiens (human)
aorta morphogenesisPlatelet-derived growth factor receptor betaHomo sapiens (human)
cellular response to platelet-derived growth factor stimulusPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of cell proliferation by VEGF-activated platelet derived growth factor receptor signaling pathwayPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of MAP kinase activityPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of mitotic nuclear divisionPlatelet-derived growth factor receptor betaHomo sapiens (human)
phosphatidylinositol metabolic processPlatelet-derived growth factor receptor betaHomo sapiens (human)
protein autophosphorylationPlatelet-derived growth factor receptor betaHomo sapiens (human)
platelet-derived growth factor receptor signaling pathwayPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of smooth muscle cell proliferationPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of calcium-mediated signalingPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of chemotaxisPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionPlatelet-derived growth factor receptor betaHomo sapiens (human)
cardiac myofibril assemblyPlatelet-derived growth factor receptor betaHomo sapiens (human)
cell chemotaxisPlatelet-derived growth factor receptor betaHomo sapiens (human)
cell migration involved in coronary angiogenesisPlatelet-derived growth factor receptor betaHomo sapiens (human)
retina vasculature development in camera-type eyePlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadePlatelet-derived growth factor receptor betaHomo sapiens (human)
smooth muscle cell chemotaxisPlatelet-derived growth factor receptor betaHomo sapiens (human)
metanephric glomerular mesangial cell proliferation involved in metanephros developmentPlatelet-derived growth factor receptor betaHomo sapiens (human)
metanephric glomerular capillary formationPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of calcium ion importPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of reactive oxygen species metabolic processPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of DNA biosynthetic processPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of kinase activityPlatelet-derived growth factor receptor betaHomo sapiens (human)
angiogenesisPlatelet-derived growth factor receptor betaHomo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayPlatelet-derived growth factor receptor betaHomo sapiens (human)
multicellular organism developmentPlatelet-derived growth factor receptor betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (32)

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)
protein kinase activityPlatelet-derived growth factor receptor betaHomo sapiens (human)
protein tyrosine kinase activityPlatelet-derived growth factor receptor betaHomo sapiens (human)
platelet activating factor receptor activityPlatelet-derived growth factor receptor betaHomo sapiens (human)
platelet-derived growth factor receptor activityPlatelet-derived growth factor receptor betaHomo sapiens (human)
platelet-derived growth factor beta-receptor activityPlatelet-derived growth factor receptor betaHomo sapiens (human)
signaling receptor bindingPlatelet-derived growth factor receptor betaHomo sapiens (human)
platelet-derived growth factor receptor bindingPlatelet-derived growth factor receptor betaHomo sapiens (human)
protein bindingPlatelet-derived growth factor receptor betaHomo sapiens (human)
ATP bindingPlatelet-derived growth factor receptor betaHomo sapiens (human)
enzyme bindingPlatelet-derived growth factor receptor betaHomo sapiens (human)
protein kinase bindingPlatelet-derived growth factor receptor betaHomo sapiens (human)
vascular endothelial growth factor bindingPlatelet-derived growth factor receptor betaHomo sapiens (human)
platelet-derived growth factor bindingPlatelet-derived growth factor receptor betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (30)

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)
nucleusPlatelet-derived growth factor receptor betaHomo sapiens (human)
cytoplasmPlatelet-derived growth factor receptor betaHomo sapiens (human)
Golgi apparatusPlatelet-derived growth factor receptor betaHomo sapiens (human)
plasma membranePlatelet-derived growth factor receptor betaHomo sapiens (human)
focal adhesionPlatelet-derived growth factor receptor betaHomo sapiens (human)
membranePlatelet-derived growth factor receptor betaHomo sapiens (human)
apical plasma membranePlatelet-derived growth factor receptor betaHomo sapiens (human)
cytoplasmic vesiclePlatelet-derived growth factor receptor betaHomo sapiens (human)
lysosomal lumenPlatelet-derived growth factor receptor betaHomo sapiens (human)
intracellular membrane-bounded organellePlatelet-derived growth factor receptor betaHomo sapiens (human)
plasma membranePlatelet-derived growth factor receptor betaHomo sapiens (human)
receptor complexPlatelet-derived growth factor receptor betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (3)

Assay IDTitleYearJournalArticle
AID1795753Membrane Autophosphorylation Assay. from Article 10.1021/jm950727b: \\Tyrphostins. 5. Potent inhibitors of platelet-derived growth factor receptor tyrosine kinase: structure-activity relationships in quinoxalines, quinolines, and indole tyrphostins.\\1996Journal of medicinal chemistry, May-24, Volume: 39, Issue:11
Tyrphostins. 5. Potent inhibitors of platelet-derived growth factor receptor tyrosine kinase: structure-activity relationships in quinoxalines, quinolines, and indole tyrphostins.
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).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's3 (60.00)18.2507
2000's0 (0.00)29.6817
2010's1 (20.00)24.3611
2020's1 (20.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other5 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]