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ag 556

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Description

AG 556: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5328775
CHEMBL ID440298
SCHEMBL ID2533402
MeSH IDM0259934

Synonyms (32)

Synonym
bdbm4308
tyrphostin deriv. 56
(2e)-2-cyano-3-(3,4-dihydroxyphenyl)-n-(4-phenylbutyl)prop-2-enamide
chembl440298 ,
BRD-K81048131-001-01-6
(e)-2-cyano-3-(3,4-dihydroxyphenyl)-n-(4-phenylbutyl)prop-2-enamide
2-cyano-3-(3,4-dihydroxyphenyl)-n-(4-phenylbutyl)acrylamide
tocris-0616
NCGC00024686-01
HSCI1_000058
tyrphostin b56
SR-01000597669 ,
SR-01000597669-2
ag 556
133550-41-1
tyrphostin ag556
ag556
2-propenamide, 2-cyano-3-(3,4-dihydroxyphenyl)-n-(4-phenylbutyl)-
alpha-cyano-(3,4-dihydroxy)-n-(4-phenylbutyl)cinnamide
149092-35-3
ag-556
AKOS024458582
SCHEMBL2533402
(e)-2-cyano-3-(3,4-dihydroxyphenyl)-n-(4-phenylbutyl)-2-propenamide
2-propenamide,2-cyano-3-(3,4-dihydroxyphenyl)-n-(4-phenylbutyl)-,(2e)-
SR-01000597669-1
J-006405
(e)-2-cyano-3-(3,4-dihydroxyphenyl)-n-(4-phenylbutyl)acrylamide
HMS3678I03
n-(4-phenylbutyl)-3,4-dihydroxybenzylidene-cyanoacetamide
HMS3414I03
F81725

Research Excerpts

Treatment

AG 556 treatment restored the depressed cardiovascular and hepatocellular functions after trauma-hemorrhage and resuscitation. Treatment decreased the survival of ad libitum, but not in diet-restricted mice in both survival experiments.

ExcerptReferenceRelevance
"AG 556 treatment restored the depressed cardiovascular and hepatocellular functions after trauma-hemorrhage and resuscitation, which was associated with reduced phosphorylation of mitogen-activated protein kinases p44/42 and p38. "( Inhibition of tyrosine kinase signaling after trauma-hemorrhage: a novel approach for improving organ function and decreasing susceptibility to subsequent sepsis.
Bland, KI; Chaudry, IH; Cioffi, WG; Jarrar, D; Song, GY; Wang, P, 2000
)
1.75
"AG 556 treatment decreased the survival of ad libitum, but not in diet-restricted mice in both survival experiments."( Effects of tyrosine kinase signaling inhibition on survival after cecal ligation and puncture in diet-restricted mice.
Fukatsu, K; Hidemura, A; Kang, W; Koyama, H; Maekawa, K; Saito, H; Sakamoto, T,
)
0.85
"Treatment with AG 556 had no effect on clearance of endotoxin or bacteria from the blood (both P = NS); however, AG 556 did significantly lower serum TNF levels (P = 0.03)."( Tyrphostin AG 556 improves survival and reduces multiorgan failure in canine Escherichia coli peritonitis.
Bacher, J; Banks, SM; Danner, RL; Eichacker, PQ; Elin, RJ; Freeman, BD; Gazit, A; Hoffman, A; Levitzki, A; Natanson, C; Novogrodsky, A; Quezado, ZM; Sevransky, JE; Shaked, G; Thomas, ML, 1997
)
1.03

Dosage Studied

ExcerptRelevanceReference
"MiaPaCa-2 responded with increased cell number to stimulation with EGF, and at 10(-8) M or higher concentrations a dose-response pattern was seen."( The inhibitory effect of an EGF receptor-specific tyrosine kinase inhibitor on pancreatic cancer cell lines was more potent than inhibitory antibodies against the receptors for EGF and IGF I.
Axelson, J; Björkman, A; Ihse, I; Kobari, M; Kullenberg, B; Matsuno, S, 1998
)
0.3
" AG-556 dissolved in DMSO was injected intraperitoneally daily to the injured mice in a dosage of 2 mg/mouse."( The effect of tyrphostin AG-556 on intimal thickening in a mouse model of arterial injury.
Barshack, I; Gazit, A; George, J; Keren, G; Keren, P; Levitzki, A; Roth, A, 2005
)
0.33
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (52)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency39.81070.003245.467312,589.2998AID2517
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency0.56230.004023.8416100.0000AID485290
Chain A, HADH2 proteinHomo sapiens (human)Potency31.62280.025120.237639.8107AID886
Chain B, HADH2 proteinHomo sapiens (human)Potency31.62280.025120.237639.8107AID886
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency4.46680.177814.390939.8107AID2147
Chain A, ATP-DEPENDENT DNA HELICASE Q1Homo sapiens (human)Potency10.00000.125919.1169125.8920AID2549
Chain A, CruzipainTrypanosoma cruziPotency31.62280.002014.677939.8107AID1476; AID1478
15-lipoxygenase, partialHomo sapiens (human)Potency1.58490.012610.691788.5700AID887
phosphopantetheinyl transferaseBacillus subtilisPotency79.43280.141337.9142100.0000AID1490
USP1 protein, partialHomo sapiens (human)Potency35.48130.031637.5844354.8130AID504865
TDP1 proteinHomo sapiens (human)Potency7.54910.000811.382244.6684AID686978; AID686979
Microtubule-associated protein tauHomo sapiens (human)Potency15.84890.180013.557439.8107AID1460
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency8.91250.011212.4002100.0000AID1030
alpha-galactosidaseHomo sapiens (human)Potency39.81074.466818.391635.4813AID1467
Bloom syndrome protein isoform 1Homo sapiens (human)Potency28.18380.540617.639296.1227AID2528
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency31.62280.00207.533739.8107AID891
polyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)Potency22.38721.000012.232631.6228AID1452
cytochrome P450 2C19 precursorHomo sapiens (human)Potency5.01190.00255.840031.6228AID899
cytochrome P450 2C9 precursorHomo sapiens (human)Potency0.01580.00636.904339.8107AID883
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency8.91250.001815.663839.8107AID894
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency39.81070.354828.065989.1251AID504847
mitogen-activated protein kinase 1Homo sapiens (human)Potency39.81070.039816.784239.8107AID995
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency23.73590.00798.23321,122.0200AID2546; AID2551
DNA polymerase kappa isoform 1Homo sapiens (human)Potency11.22020.031622.3146100.0000AID588579
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency3.16230.031610.279239.8107AID884; AID885
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency28.18380.251215.843239.8107AID504327
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency3.16231.000012.224831.6228AID885
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency15.84890.316212.765731.6228AID881
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency3.16231.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency3.16231.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency3.16231.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency3.16231.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency3.16231.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency3.16231.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency3.16231.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency3.16231.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency3.16231.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency3.16231.000012.224831.6228AID885
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency6.34900.00638.235039.8107AID881; AID883
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency3.16231.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency3.16231.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency3.16231.000012.224831.6228AID885
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency28.18381.000010.475628.1838AID1457
GABA theta subunitRattus norvegicus (Norway rat)Potency3.16231.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency3.16231.000012.224831.6228AID885
[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)
Epidermal growth factor receptorHomo sapiens (human)IC50 (µMol)3.36860.00000.536910.0000AID162571; AID1795628; AID66448; AID69711; AID69890; AID89322
Receptor tyrosine-protein kinase erbB-2Homo sapiens (human)IC50 (µMol)500.39570.00010.545310.0000AID164335; AID68095; AID68103
Alpha-1A adrenergic receptorHomo sapiens (human)IC50 (µMol)100.00000.00020.56145.4000AID36306
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)IC50 (µMol)66.85330.00071.600310.0000AID143779; AID143785; AID143788
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)IC50 (µMol)100.00000.00071.630610.0000AID143779
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)IC50 (µMol)0.56000.00061.525710.0000AID143785
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)IC50 (µMol)100.00000.00071.747210.0000AID143788
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (161)

Processvia Protein(s)Taxonomy
lipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
phospholipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
apoptotic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell population proliferationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of macrophage derived foam cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell migrationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
prostate gland developmentPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
regulation of epithelial cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of chemokine productionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of peroxisome proliferator activated receptor signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of keratinocyte differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell cyclePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of growthPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
hepoxilin biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
endocannabinoid signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cannabinoid biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxin A4 biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid oxidationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxygenase pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
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)
cell surface receptor signaling pathwayReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
positive regulation of protein phosphorylationReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
protein phosphorylationReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
signal transductionReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
enzyme-linked receptor protein signaling pathwayReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
heart developmentReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
neuromuscular junction developmentReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
motor neuron axon guidanceReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
Schwann cell developmentReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
peptidyl-tyrosine phosphorylationReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
positive regulation of cell growthReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
regulation of microtubule-based processReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
immature T cell proliferation in thymusReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
negative regulation of immature T cell proliferation in thymusReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
positive regulation of Rho protein signal transductionReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
intracellular signal transductionReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
ERBB2-ERBB3 signaling pathwayReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
ERBB2-EGFR signaling pathwayReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
ERBB2-ERBB4 signaling pathwayReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
wound healingReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
myelinationReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
positive regulation of MAP kinase activityReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transductionReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
positive regulation of translationReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
regulation of angiogenesisReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
positive regulation of cell adhesionReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
positive regulation of transcription by RNA polymerase IReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
oligodendrocyte differentiationReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
positive regulation of epithelial cell proliferationReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
regulation of ERK1 and ERK2 cascadeReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
cellular response to growth factor stimulusReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
cellular response to epidermal growth factor stimulusReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
semaphorin-plexin signaling pathwayReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
positive regulation of protein targeting to membraneReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
neurotransmitter receptor localization to postsynaptic specialization membraneReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
neurogenesisReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
positive regulation of MAPK cascadeReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
negative regulation of apoptotic processReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
positive regulation of kinase activityReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
multicellular organism developmentReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
positive regulation of cell population proliferationReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
neuron differentiationReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
MAPK cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of heart rate involved in baroreceptor response to increased systemic arterial blood pressureAlpha-1A adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine vasoconstriction involved in regulation of systemic arterial blood pressureAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of heart rate by epinephrine-norepinephrineAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of the force of heart contraction by epinephrine-norepinephrineAlpha-1A adrenergic receptorHomo sapiens (human)
apoptotic processAlpha-1A adrenergic receptorHomo sapiens (human)
smooth muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
signal transductionAlpha-1A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
activation of phospholipase C activityAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1A adrenergic receptorHomo sapiens (human)
adult heart developmentAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of cell population proliferationAlpha-1A adrenergic receptorHomo sapiens (human)
response to xenobiotic stimulusAlpha-1A adrenergic receptorHomo sapiens (human)
response to hormoneAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of autophagyAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cardiac muscle hypertrophyAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicAlpha-1A adrenergic receptorHomo sapiens (human)
intracellular signal transductionAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of action potentialAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of vasoconstrictionAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of smooth muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
calcium ion transport into cytosolAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cardiac muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
cell growth involved in cardiac muscle cell developmentAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of protein kinase C signalingAlpha-1A adrenergic receptorHomo sapiens (human)
pilomotor reflexAlpha-1A adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1A adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1A adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (39)

Processvia Protein(s)Taxonomy
iron ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
calcium ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
protein bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 13S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 8(S)-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 15-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 9S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
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)
growth factor bindingReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
RNA polymerase I core bindingReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
protein tyrosine kinase activityReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
transmembrane receptor protein tyrosine kinase activityReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
transmembrane signaling receptor activityReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
signaling receptor bindingReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
protein bindingReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
ATP bindingReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
coreceptor activityReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
receptor tyrosine kinase bindingReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
identical protein bindingReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
ErbB-3 class receptor bindingReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
protein heterodimerization activityReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-1A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1A adrenergic receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (39)

Processvia Protein(s)Taxonomy
nucleusPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytosolPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytoskeletonPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
plasma membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
adherens junctionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
focal adhesionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
extracellular exosomePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
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)
semaphorin receptor complexReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
nucleusReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
nucleoplasmReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
early endosomeReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
cytosolReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
plasma membraneReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
endosome membraneReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
membraneReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
basolateral plasma membraneReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
apical plasma membraneReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
neuromuscular junctionReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
ruffle membraneReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
presynaptic membraneReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
myelin sheathReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
perinuclear region of cytoplasmReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
ERBB3:ERBB2 complexReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
receptor complexReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
plasma membraneReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
basal plasma membraneReceptor tyrosine-protein kinase erbB-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
nucleusAlpha-1A adrenergic receptorHomo sapiens (human)
nucleoplasmAlpha-1A adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-1A adrenergic receptorHomo sapiens (human)
cytosolAlpha-1A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1A adrenergic receptorHomo sapiens (human)
caveolaAlpha-1A adrenergic receptorHomo sapiens (human)
nuclear membraneAlpha-1A adrenergic receptorHomo sapiens (human)
intracellular membrane-bounded organelleAlpha-1A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1A adrenergic receptorHomo sapiens (human)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 1 Rattus 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)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (18)

Assay IDTitleYearJournalArticle
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.
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.
AID68095In vitro inhibition of ERBB2 receptor kinase autophosphorylation.1991Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases.
AID69890Inhibition of Epidermal growth factor receptor autophosphorylation1999Journal of medicinal chemistry, Aug-26, Volume: 42, Issue:17
Structure-activity relationship of N-(phenylalkyl)cinnamides as novel NR2B subtype-selective NMDA receptor antagonists.
AID36306Inhibition of Alpha-1 adrenergic receptor1999Journal of medicinal chemistry, Aug-26, Volume: 42, Issue:17
Structure-activity relationship of N-(phenylalkyl)cinnamides as novel NR2B subtype-selective NMDA receptor antagonists.
AID143788Antagonistic activity against N-methyl-D-aspartate glutamate receptor 1/2C.1999Journal of medicinal chemistry, Aug-26, Volume: 42, Issue:17
Structure-activity relationship of N-(phenylalkyl)cinnamides as novel NR2B subtype-selective NMDA receptor antagonists.
AID69711Inhibitory activity against epidermal growth factor receptor (EGFR)2003Journal of medicinal chemistry, Oct-23, Volume: 46, Issue:22
Receptor-guided alignment-based comparative 3D-QSAR studies of benzylidene malonitrile tyrphostins as EGFR and HER-2 kinase inhibitors.
AID162571Inhibition of polyGAT phosphorylation1991Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases.
AID326316Effect on catechol-O-methyltransferase assessed as stimulation of methylation of mouse heart cytosol proteins per miligram of protein at 100 uM after 2 hrs by vapor-diffusion assay2007The Journal of biological chemistry, Oct-19, Volume: 282, Issue:42
S-adenosylmethionine-dependent protein methylation in mammalian cytosol via tyrphostin modification by catechol-O-methyltransferase.
AID66448In vitro inhibition of HER1 autophosphorylation.1991Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases.
AID143785Antagonistic activity against N-methyl-D-aspartate glutamate receptor 1/2B.1999Journal of medicinal chemistry, Aug-26, Volume: 42, Issue:17
Structure-activity relationship of N-(phenylalkyl)cinnamides as novel NR2B subtype-selective NMDA receptor antagonists.
AID54308Inhibition of HER14 (human EGFR overexpressing NIH3T3) cell growth in the absence of EGF.1991Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases.
AID68103Inhibition of ERBB2 receptor autophosphorylation1999Journal of medicinal chemistry, Aug-26, Volume: 42, Issue:17
Structure-activity relationship of N-(phenylalkyl)cinnamides as novel NR2B subtype-selective NMDA receptor antagonists.
AID143779Antagonistic activity against N-methyl-D-aspartate glutamate receptor 1/2A.1999Journal of medicinal chemistry, Aug-26, Volume: 42, Issue:17
Structure-activity relationship of N-(phenylalkyl)cinnamides as novel NR2B subtype-selective NMDA receptor antagonists.
AID326317Activity of pig recombinant catechol-O-methyltransferase assessed per unit enzyme2007The Journal of biological chemistry, Oct-19, Volume: 282, Issue:42
S-adenosylmethionine-dependent protein methylation in mammalian cytosol via tyrphostin modification by catechol-O-methyltransferase.
AID164335Inhibitory activity tested against protein kinase HER-22003Journal of medicinal chemistry, Oct-23, Volume: 46, Issue:22
Receptor-guided alignment-based comparative 3D-QSAR studies of benzylidene malonitrile tyrphostins as EGFR and HER-2 kinase inhibitors.
AID89322Inhibition of HER14 (human EGFR overexpressing) cell proliferation.1991Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases.
AID1795628EGFR assay from Article 10.1021/jm00110a022: \\Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases.\\1991Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (38)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's10 (26.32)18.2507
2000's16 (42.11)29.6817
2010's10 (26.32)24.3611
2020's2 (5.26)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%
Other39 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]