Compounds > m475271
Page last updated: 2024-12-11

m475271

Description

AZM475271: a Src family kinase inhibitor [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5330175
CHEMBL ID426161
SCHEMBL ID3195079
MeSH IDM0493488

Synonyms (28)

Synonym
methoxy aniline 7
m475271
bdbm6198
n-(2-chloro-5-methoxyphenyl)-6-methoxy-7-[(1-methylpiperidin-4-yl)methoxy]quinazolin-4-amine
CHEMBL426161
n-(2-chloro-5-methoxyphenyl)-6-methoxy-7-((1-methylpiperidin-4-yl)methoxy)quinazolin-4-amine
4-quinazolinamine, n-(2-chloro-5-methoxyphenyl)-6-methoxy-7-((1-methyl-4-piperidinyl)methoxy)-
unii-0361z8214o
azm-475271
m-475271
0361z8214o ,
476159-98-5
azm 475271
azm 475271 [who-dd]
SCHEMBL3195079
c23h27cln4o3
n-(2-chloro-5-methoxyphenyl)-6-methoxy
azm475271
HY-13561
AKOS024457900
DTXSID00197222
NCGC00370984-01
Q21547118
A914756
F85123
MS-27972
NCGC00370984-02
BUA15998

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)		0.51

Dosage Studied

ExcerptRelevanceReference
" AZD0530 is a potent inhibitor of tumor growth in a c-Src-transfected 3T3-fibroblast xenograft model in vivo and led to a significant increase in survival in a highly aggressive, orthotopic model of human pancreatic cancer when dosed orally once daily."( N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor.
Allen, J; Breed, J; Costello, G; Curwen, J; Fennell, M; Green, TP; Hennequin, LF; Lambert-van der Brempt, C; Morgentin, R; Norman, RA; Olivier, A; Otterbein, L; Plé, PA; Warin, N, 2006)		0.33
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (6)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
PPM1D proteinHomo sapiens (human)Potency20.82120.00529.466132.9993AID1347411
Interferon betaHomo sapiens (human)Potency20.82120.00339.158239.8107AID1347411
[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)
Fibroblast growth factor receptor 1Homo sapiens (human)IC50 (µMol)0.01000.00020.942010.0000AID1795857
Proto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)IC50 (µMol)0.27210.00020.533510.0000AID1545500; AID1795857; AID1795858; AID1796878; AID272211; AID272213
Vascular endothelial growth factor receptor 1 Homo sapiens (human)IC50 (µMol)0.01000.00010.29147.0000AID1795857
Vascular endothelial growth factor receptor 2Homo sapiens (human)IC50 (µMol)0.40600.00000.48308.8000AID1795857; AID1795858; AID1796878; AID272212
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (262)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of cell population proliferationFibroblast growth factor receptor 1Homo sapiens (human)
fibroblast growth factor receptor signaling pathwayFibroblast growth factor receptor 1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIFibroblast growth factor receptor 1Homo sapiens (human)
MAPK cascadeFibroblast growth factor receptor 1Homo sapiens (human)
skeletal system developmentFibroblast growth factor receptor 1Homo sapiens (human)
angiogenesisFibroblast growth factor receptor 1Homo sapiens (human)
ureteric bud developmentFibroblast growth factor receptor 1Homo sapiens (human)
in utero embryonic developmentFibroblast growth factor receptor 1Homo sapiens (human)
organ inductionFibroblast growth factor receptor 1Homo sapiens (human)
neuron migrationFibroblast growth factor receptor 1Homo sapiens (human)
epithelial to mesenchymal transitionFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of mesenchymal cell proliferationFibroblast growth factor receptor 1Homo sapiens (human)
chondrocyte differentiationFibroblast growth factor receptor 1Homo sapiens (human)
protein phosphorylationFibroblast growth factor receptor 1Homo sapiens (human)
sensory perception of soundFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of cell population proliferationFibroblast growth factor receptor 1Homo sapiens (human)
fibroblast growth factor receptor signaling pathwayFibroblast growth factor receptor 1Homo sapiens (human)
mesenchymal cell proliferationFibroblast growth factor receptor 1Homo sapiens (human)
gene expressionFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of phospholipase activityFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of phospholipase C activityFibroblast growth factor receptor 1Homo sapiens (human)
regulation of phosphate transportFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of neuron projection developmentFibroblast growth factor receptor 1Homo sapiens (human)
cell migrationFibroblast growth factor receptor 1Homo sapiens (human)
peptidyl-tyrosine phosphorylationFibroblast growth factor receptor 1Homo sapiens (human)
ventricular zone neuroblast divisionFibroblast growth factor receptor 1Homo sapiens (human)
cell projection assemblyFibroblast growth factor receptor 1Homo sapiens (human)
embryonic limb morphogenesisFibroblast growth factor receptor 1Homo sapiens (human)
midbrain developmentFibroblast growth factor receptor 1Homo sapiens (human)
neuron projection developmentFibroblast growth factor receptor 1Homo sapiens (human)
fibroblast growth factor receptor signaling pathway involved in orbitofrontal cortex developmentFibroblast growth factor receptor 1Homo sapiens (human)
inner ear morphogenesisFibroblast growth factor receptor 1Homo sapiens (human)
outer ear morphogenesisFibroblast growth factor receptor 1Homo sapiens (human)
middle ear morphogenesisFibroblast growth factor receptor 1Homo sapiens (human)
chordate embryonic developmentFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of MAP kinase activityFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of MAPK cascadeFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of blood vessel endothelial cell migrationFibroblast growth factor receptor 1Homo sapiens (human)
cellular response to fibroblast growth factor stimulusFibroblast growth factor receptor 1Homo sapiens (human)
regulation of cell differentiationFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of neuron differentiationFibroblast growth factor receptor 1Homo sapiens (human)
protein autophosphorylationFibroblast growth factor receptor 1Homo sapiens (human)
phosphatidylinositol-mediated signalingFibroblast growth factor receptor 1Homo sapiens (human)
paraxial mesoderm developmentFibroblast growth factor receptor 1Homo sapiens (human)
regulation of lateral mesodermal cell fate specificationFibroblast growth factor receptor 1Homo sapiens (human)
cell maturationFibroblast growth factor receptor 1Homo sapiens (human)
skeletal system morphogenesisFibroblast growth factor receptor 1Homo sapiens (human)
stem cell differentiationFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionFibroblast growth factor receptor 1Homo sapiens (human)
calcium ion homeostasisFibroblast growth factor receptor 1Homo sapiens (human)
cardiac muscle cell proliferationFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of cardiac muscle cell proliferationFibroblast growth factor receptor 1Homo sapiens (human)
auditory receptor cell developmentFibroblast growth factor receptor 1Homo sapiens (human)
branching involved in salivary gland morphogenesisFibroblast growth factor receptor 1Homo sapiens (human)
lung-associated mesenchyme developmentFibroblast growth factor receptor 1Homo sapiens (human)
regulation of branching involved in salivary gland morphogenesis by mesenchymal-epithelial signalingFibroblast growth factor receptor 1Homo sapiens (human)
vitamin D3 metabolic processFibroblast growth factor receptor 1Homo sapiens (human)
diphosphate metabolic processFibroblast growth factor receptor 1Homo sapiens (human)
cementum mineralizationFibroblast growth factor receptor 1Homo sapiens (human)
stem cell proliferationFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of MAPKKK cascade by fibroblast growth factor receptor signaling pathwayFibroblast growth factor receptor 1Homo sapiens (human)
negative regulation of fibroblast growth factor productionFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of mitotic cell cycle DNA replicationFibroblast growth factor receptor 1Homo sapiens (human)
response to sodium phosphateFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of vascular endothelial cell proliferationFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of stem cell proliferationFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of parathyroid hormone secretionFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of endothelial cell chemotaxisFibroblast growth factor receptor 1Homo sapiens (human)
regulation of extrinsic apoptotic signaling pathway in absence of ligandFibroblast growth factor receptor 1Homo sapiens (human)
multicellular organism developmentFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of cell differentiationFibroblast growth factor receptor 1Homo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of kinase activityFibroblast growth factor receptor 1Homo sapiens (human)
peptidyl-tyrosine phosphorylationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
primary ovarian follicle growthProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of cytokine productionProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
stimulatory C-type lectin receptor signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
negative regulation of inflammatory response to antigenic stimulusProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
signal transductionProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
signal complex assemblyProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
epidermal growth factor receptor signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
transforming growth factor beta receptor signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
integrin-mediated signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
spermatogenesisProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
learning or memoryProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
response to xenobiotic stimulusProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
response to mechanical stimulusProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
response to acidic pHProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
negative regulation of gene expressionProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
regulation of epithelial cell migrationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of epithelial cell migrationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of glucose metabolic processProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of protein processingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
skeletal muscle cell proliferationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of smooth muscle cell migrationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
macroautophagyProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
peptidyl-tyrosine phosphorylationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
regulation of cell-cell adhesionProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
platelet activationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
forebrain developmentProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
T cell costimulationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
negative regulation of protein-containing complex assemblyProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
protein destabilizationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
response to nutrient levelsProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
negative regulation of telomere maintenance via telomeraseProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
cellular response to insulin stimulusProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
regulation of intracellular estrogen receptor signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of integrin activationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
regulation of toll-like receptor 3 signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
adherens junction organizationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
substrate adhesion-dependent cell spreadingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of dephosphorylationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
negative regulation of hippo signalingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
intracellular signal transductionProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
entry of bacterium into host cellProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
osteoclast developmentProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
cellular response to platelet-derived growth factor stimulusProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
Fc-gamma receptor signaling pathway involved in phagocytosisProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
ERBB2 signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
angiotensin-activated signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
odontogenesisProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of apoptotic processProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
negative regulation of apoptotic processProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
regulation of vascular permeabilityProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
stress fiber assemblyProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
negative regulation of cysteine-type endopeptidase activity involved in apoptotic processProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
transcytosisProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
regulation of bone resorptionProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
bone resorptionProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of Notch signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of bone resorptionProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of Ras protein signal transductionProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of insulin receptor signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
protein autophosphorylationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
platelet-derived growth factor receptor signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
vascular endothelial growth factor receptor signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
neurotrophin TRK receptor signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
ephrin receptor signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
focal adhesion assemblyProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
oogenesisProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
progesterone receptor signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
leukocyte migrationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of small GTPase mediated signal transductionProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of protein transportProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
response to mineralocorticoidProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
myoblast proliferationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
response to electrical stimulusProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
negative regulation of focal adhesion assemblyProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
negative regulation of mitochondrial depolarizationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
negative regulation of telomerase activityProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
uterus developmentProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
branching involved in mammary gland duct morphogenesisProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
regulation of cell projection assemblyProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
intestinal epithelial cell developmentProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
interleukin-6-mediated signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
cellular response to hydrogen peroxideProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
response to interleukin-1Proto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
cellular response to lipopolysaccharideProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
cellular response to peptide hormone stimulusProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
cellular response to progesterone stimulusProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
cellular response to fatty acidProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
cellular response to hypoxiaProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
cellular response to fluid shear stressProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of podosome assemblyProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
DNA biosynthetic processProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of protein serine/threonine kinase activityProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
regulation of heart rate by cardiac conductionProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of canonical Wnt signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
cell-cell adhesionProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of protein localization to nucleusProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of non-membrane spanning protein tyrosine kinase activityProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of TORC1 signalingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
cellular response to prolactinProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of male germ cell proliferationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of ovarian follicle developmentProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of lamellipodium morphogenesisProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
positive regulation of platelet-derived growth factor receptor-beta signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
regulation of early endosome to late endosome transportProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
negative regulation of anoikisProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathwayProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
regulation of caveolin-mediated endocytosisProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
cell differentiationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
cell adhesionProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
innate immune responseProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
protein phosphorylationProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
symbiont entry into host cellProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
angiogenesisVascular endothelial growth factor receptor 1 Homo sapiens (human)
monocyte chemotaxisVascular endothelial growth factor receptor 1 Homo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayVascular endothelial growth factor receptor 1 Homo sapiens (human)
positive regulation of cell population proliferationVascular endothelial growth factor receptor 1 Homo sapiens (human)
positive regulation of phospholipase C activityVascular endothelial growth factor receptor 1 Homo sapiens (human)
cell migrationVascular endothelial growth factor receptor 1 Homo sapiens (human)
peptidyl-tyrosine phosphorylationVascular endothelial growth factor receptor 1 Homo sapiens (human)
cell differentiationVascular endothelial growth factor receptor 1 Homo sapiens (human)
positive regulation of cell migrationVascular endothelial growth factor receptor 1 Homo sapiens (human)
cellular response to vascular endothelial growth factor stimulusVascular endothelial growth factor receptor 1 Homo sapiens (human)
vascular endothelial growth factor receptor-1 signaling pathwayVascular endothelial growth factor receptor 1 Homo sapiens (human)
vascular endothelial growth factor signaling pathwayVascular endothelial growth factor receptor 1 Homo sapiens (human)
positive regulation of MAP kinase activityVascular endothelial growth factor receptor 1 Homo sapiens (human)
positive regulation of MAPK cascadeVascular endothelial growth factor receptor 1 Homo sapiens (human)
positive regulation of angiogenesisVascular endothelial growth factor receptor 1 Homo sapiens (human)
protein autophosphorylationVascular endothelial growth factor receptor 1 Homo sapiens (human)
vascular endothelial growth factor receptor signaling pathwayVascular endothelial growth factor receptor 1 Homo sapiens (human)
blood vessel morphogenesisVascular endothelial growth factor receptor 1 Homo sapiens (human)
embryonic morphogenesisVascular endothelial growth factor receptor 1 Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionVascular endothelial growth factor receptor 1 Homo sapiens (human)
negative regulation of vascular endothelial cell proliferationVascular endothelial growth factor receptor 1 Homo sapiens (human)
hyaloid vascular plexus regressionVascular endothelial growth factor receptor 1 Homo sapiens (human)
multicellular organism developmentVascular endothelial growth factor receptor 1 Homo sapiens (human)
positive regulation of kinase activityVascular endothelial growth factor receptor 1 Homo sapiens (human)
branching involved in blood vessel morphogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of macroautophagyVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of mitochondrial depolarizationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of mitochondrial fissionVascular endothelial growth factor receptor 2Homo sapiens (human)
angiogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
ovarian follicle developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
vasculogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of protein phosphorylationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of endothelial cell proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
lymph vessel developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
cell migration involved in sprouting angiogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of mesenchymal cell proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
epithelial cell maturationVascular endothelial growth factor receptor 2Homo sapiens (human)
endocardium developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
endothelium developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of cell population proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
regulation of cell shapeVascular endothelial growth factor receptor 2Homo sapiens (human)
mesenchymal cell proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of endothelial cell migrationVascular endothelial growth factor receptor 2Homo sapiens (human)
negative regulation of gene expressionVascular endothelial growth factor receptor 2Homo sapiens (human)
peptidyl-tyrosine phosphorylationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of cell migrationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of BMP signaling pathwayVascular endothelial growth factor receptor 2Homo sapiens (human)
embryonic hemopoiesisVascular endothelial growth factor receptor 2Homo sapiens (human)
cellular response to vascular endothelial growth factor stimulusVascular endothelial growth factor receptor 2Homo sapiens (human)
vascular endothelial growth factor receptor-2 signaling pathwayVascular endothelial growth factor receptor 2Homo sapiens (human)
peptidyl-tyrosine autophosphorylationVascular endothelial growth factor receptor 2Homo sapiens (human)
vascular endothelial growth factor signaling pathwayVascular endothelial growth factor receptor 2Homo sapiens (human)
surfactant homeostasisVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of MAPK cascadeVascular endothelial growth factor receptor 2Homo sapiens (human)
negative regulation of neuron apoptotic processVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of blood vessel endothelial cell migrationVascular endothelial growth factor receptor 2Homo sapiens (human)
cell fate commitmentVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of angiogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
protein autophosphorylationVascular endothelial growth factor receptor 2Homo sapiens (human)
vascular endothelial growth factor receptor signaling pathwayVascular endothelial growth factor receptor 2Homo sapiens (human)
lung alveolus developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
post-embryonic camera-type eye morphogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
epithelial cell proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of positive chemotaxisVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of nitric-oxide synthase biosynthetic processVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of focal adhesion assemblyVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionVascular endothelial growth factor receptor 2Homo sapiens (human)
calcium ion homeostasisVascular endothelial growth factor receptor 2Homo sapiens (human)
blood vessel endothelial cell differentiationVascular endothelial growth factor receptor 2Homo sapiens (human)
vascular wound healingVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeVascular endothelial growth factor receptor 2Homo sapiens (human)
semaphorin-plexin signaling pathwayVascular endothelial growth factor receptor 2Homo sapiens (human)
stem cell proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
regulation of hematopoietic progenitor cell differentiationVascular endothelial growth factor receptor 2Homo sapiens (human)
regulation of bone developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
cellular response to hydrogen sulfideVascular endothelial growth factor receptor 2Homo sapiens (human)
negative regulation of endothelial cell apoptotic processVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of stem cell proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of endothelial cell chemotaxisVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of vasculogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
regulation of MAPK cascadeVascular endothelial growth factor receptor 2Homo sapiens (human)
multicellular organism developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
cell migrationVascular endothelial growth factor receptor 2Homo sapiens (human)
endothelial cell differentiationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of kinase activityVascular endothelial growth factor receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (40)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
protein tyrosine kinase activityFibroblast growth factor receptor 1Homo sapiens (human)
fibroblast growth factor receptor activityFibroblast growth factor receptor 1Homo sapiens (human)
protein bindingFibroblast growth factor receptor 1Homo sapiens (human)
ATP bindingFibroblast growth factor receptor 1Homo sapiens (human)
heparin bindingFibroblast growth factor receptor 1Homo sapiens (human)
fibroblast growth factor bindingFibroblast growth factor receptor 1Homo sapiens (human)
SH2 domain bindingFibroblast growth factor receptor 1Homo sapiens (human)
identical protein bindingFibroblast growth factor receptor 1Homo sapiens (human)
protein homodimerization activityFibroblast growth factor receptor 1Homo sapiens (human)
receptor-receptor interactionFibroblast growth factor receptor 1Homo sapiens (human)
protein kinase activityProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
protein tyrosine kinase activityProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
non-membrane spanning protein tyrosine kinase activityProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
protein kinase C bindingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
signaling receptor bindingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
insulin receptor bindingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
integrin bindingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
protein bindingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
ATP bindingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
phospholipase activator activityProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
enzyme bindingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
heme bindingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
nuclear estrogen receptor bindingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
SH2 domain bindingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
phospholipase bindingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
transmembrane transporter bindingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
cadherin bindingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
ephrin receptor bindingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
ATPase bindingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
phosphoprotein bindingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
BMP receptor bindingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
connexin bindingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
scaffold protein bindingProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
transmembrane receptor protein tyrosine kinase activityVascular endothelial growth factor receptor 1 Homo sapiens (human)
vascular endothelial growth factor receptor activityVascular endothelial growth factor receptor 1 Homo sapiens (human)
protein bindingVascular endothelial growth factor receptor 1 Homo sapiens (human)
ATP bindingVascular endothelial growth factor receptor 1 Homo sapiens (human)
growth factor bindingVascular endothelial growth factor receptor 1 Homo sapiens (human)
placental growth factor receptor activityVascular endothelial growth factor receptor 1 Homo sapiens (human)
protein tyrosine kinase activityVascular endothelial growth factor receptor 2Homo sapiens (human)
transmembrane receptor protein tyrosine kinase activityVascular endothelial growth factor receptor 2Homo sapiens (human)
vascular endothelial growth factor receptor activityVascular endothelial growth factor receptor 2Homo sapiens (human)
integrin bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
protein bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
ATP bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
coreceptor activityVascular endothelial growth factor receptor 2Homo sapiens (human)
growth factor bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
vascular endothelial growth factor bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
identical protein bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
cadherin bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
Hsp90 protein bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (37)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
extracellular regionFibroblast growth factor receptor 1Homo sapiens (human)
nucleusFibroblast growth factor receptor 1Homo sapiens (human)
cytosolFibroblast growth factor receptor 1Homo sapiens (human)
plasma membraneFibroblast growth factor receptor 1Homo sapiens (human)
membraneFibroblast growth factor receptor 1Homo sapiens (human)
cytoplasmic vesicleFibroblast growth factor receptor 1Homo sapiens (human)
receptor complexFibroblast growth factor receptor 1Homo sapiens (human)
plasma membraneFibroblast growth factor receptor 1Homo sapiens (human)
podosomeProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
nucleoplasmProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
cytoplasmProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
mitochondrionProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
mitochondrial inner membraneProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
lysosomeProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
late endosomeProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
cytosolProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
actin filamentProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
plasma membraneProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
caveolaProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
focal adhesionProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
cell junctionProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
ruffle membraneProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
neuronal cell bodyProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
dendritic growth coneProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
membrane raftProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
perinuclear region of cytoplasmProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
extracellular exosomeProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
synaptic membraneProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
glutamatergic synapseProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
postsynaptic specialization, intracellular componentProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
dendritic filopodiumProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
plasma membraneProto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)
extracellular spaceVascular endothelial growth factor receptor 1 Homo sapiens (human)
endosomeVascular endothelial growth factor receptor 1 Homo sapiens (human)
plasma membraneVascular endothelial growth factor receptor 1 Homo sapiens (human)
focal adhesionVascular endothelial growth factor receptor 1 Homo sapiens (human)
actin cytoskeletonVascular endothelial growth factor receptor 1 Homo sapiens (human)
receptor complexVascular endothelial growth factor receptor 1 Homo sapiens (human)
plasma membraneVascular endothelial growth factor receptor 1 Homo sapiens (human)
extracellular regionVascular endothelial growth factor receptor 2Homo sapiens (human)
nucleusVascular endothelial growth factor receptor 2Homo sapiens (human)
endosomeVascular endothelial growth factor receptor 2Homo sapiens (human)
early endosomeVascular endothelial growth factor receptor 2Homo sapiens (human)
endoplasmic reticulumVascular endothelial growth factor receptor 2Homo sapiens (human)
Golgi apparatusVascular endothelial growth factor receptor 2Homo sapiens (human)
plasma membraneVascular endothelial growth factor receptor 2Homo sapiens (human)
external side of plasma membraneVascular endothelial growth factor receptor 2Homo sapiens (human)
cell junctionVascular endothelial growth factor receptor 2Homo sapiens (human)
membrane raftVascular endothelial growth factor receptor 2Homo sapiens (human)
anchoring junctionVascular endothelial growth factor receptor 2Homo sapiens (human)
sorting endosomeVascular endothelial growth factor receptor 2Homo sapiens (human)
plasma membraneVascular endothelial growth factor receptor 2Homo sapiens (human)
receptor complexVascular endothelial growth factor receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (36)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID272218Aqueous solubility at pH 7.42006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor.
AID1612813Inhibition of CSK (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control2019European journal of medicinal chemistry, Feb-01, Volume: 163The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series.
AID1612828Antiproliferative activity against human MCF7 cells after 72 hrs by CellTiter 96 aqueous one solution assay2019European journal of medicinal chemistry, Feb-01, Volume: 163The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series.
AID272213Antiproliferative activity against mouse NIH3T3 cell line transfected with c-SRC2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor.
AID272248Half life in male dog2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor.
AID1612814Inhibition of Fyn A (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control2019European journal of medicinal chemistry, Feb-01, Volume: 163The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series.
AID1612826Antiproliferative activity against p53+/+ human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay2019European journal of medicinal chemistry, Feb-01, Volume: 163The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series.
AID1545500Inhibition of human recombinant Src expressed in baculovirus infected Sf9 insect cells assessed as reduction in phosphorylation of polyglutamic acid/tyrosine incubated for 15 mins by ELISA2019European journal of medicinal chemistry, May-15, Volume: 170Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry.
AID1612810Inhibition of ABL1 (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control2019European journal of medicinal chemistry, Feb-01, Volume: 163The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series.
AID272211Inhibition of human c-Src in NIH3T3 cells2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor.
AID1612816Inhibition of Lyn B (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control2019European journal of medicinal chemistry, Feb-01, Volume: 163The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series.
AID272217Lipophilicity, log D at pH 7.42006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor.
AID272256Clearance in male dog2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor.
AID1612830Antiproliferative activity against human NHDF cells after 72 hrs by CellTiter 96 aqueous one solution assay2019European journal of medicinal chemistry, Feb-01, Volume: 163The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series.
AID272221Percent of unbound ligand in rat plasma2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor.
AID1612812Inhibition of BTK (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control2019European journal of medicinal chemistry, Feb-01, Volume: 163The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series.
AID1612817Inhibition of SRC (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control2019European journal of medicinal chemistry, Feb-01, Volume: 163The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series.
AID1612829Antiproliferative activity against human A549 cells after 72 hrs by CellTiter 96 aqueous one solution assay2019European journal of medicinal chemistry, Feb-01, Volume: 163The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series.
AID1612827Antiproliferative activity against p53-/- human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay2019European journal of medicinal chemistry, Feb-01, Volume: 163The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series.
AID272212Inhibition of KDR2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor.
AID272214Inhibition of A549 cell migration by microdroplet migration assay2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor.
AID272216Dissociation constant, pKa of the basic side chain of compound2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor.
AID1612811Inhibition of BRK (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control2019European journal of medicinal chemistry, Feb-01, Volume: 163The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series.
AID272252Volume of distribution in male dog2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor.
AID1612815Inhibition of LCK (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control2019European journal of medicinal chemistry, Feb-01, Volume: 163The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series.
AID272260Bioavailability in male dog2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor.
AID272269Inhibition of liver metastasis formation in nude mouse xenografted with L3.6p1 at 25 mg/kg/day, po2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor.
AID1795857In Vitro Src Kinase Inhibition Test from Article 10.1021/jm030317k: \\Discovery of a new class of anilinoquinazoline inhibitors with high affinity and specificity for the tyrosine kinase domain of c-Src.\\2004Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4
Discovery of a new class of anilinoquinazoline inhibitors with high affinity and specificity for the tyrosine kinase domain of c-Src.
AID1796878In Vitro Src Kinase Inhibition Test from Article 10.1021/jm060434q: \\N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5-(tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor.
AID1795858VEGF-R Kinase Inhibition Assay from Article 10.1021/jm030317k: \\Discovery of a new class of anilinoquinazoline inhibitors with high affinity and specificity for the tyrosine kinase domain of c-Src.\\2004Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4
Discovery of a new class of anilinoquinazoline inhibitors with high affinity and specificity for the tyrosine kinase domain of c-Src.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (9)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's2 (22.22)29.6817
2010's4 (44.44)24.3611
2020's3 (33.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.70

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.70 (24.57)
Research Supply Index2.30 (2.92)
Research Growth Index5.00 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.70)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (11.11%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other8 (88.89%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
chloroquine
Chloroquine: The prototypical antimalarial agent with a mechanism that is not well understood. It has also been used to treat rheumatoid arthritis, systemic lupus erythematosus, and in the systemic therapy of amebic liver abscesses.. chloroquine : An aminoquinoline that is quinoline which is substituted at position 4 by a [5-(diethylamino)pentan-2-yl]amino group at at position 7 by chlorine. It is used for the treatment of malaria, hepatic amoebiasis, lupus erythematosus, light-sensitive skin eruptions, and rheumatoid arthritis.		3.3110aminoquinoline;
organochlorine compound;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antimalarial;
antirheumatic drug;
autophagy inhibitor;
dermatologic drug
pd 153035
4-((3-bromophenyl)amino)-6,7-dimethoxyquinazoline: structure given in first source. PD-153035 : A member of the class of quinazolines carrying a 3-bromophenylamino substituent at position 4 and two methoxy substituents at positions 6 and 7.		3.3110aromatic amine;
aromatic ether;
bromobenzenes;
quinazolines;
secondary amino compound		EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
epidermal growth factor receptor antagonist
ag 1879
3-(4-chlorophenyl)-1-(1,1-dimethylethyl)-1H-pyrazolo(3,4-d)pyrimidin-4-amine: Fyn kinase inhibitor		2.1310aromatic amine;
monochlorobenzenes;
pyrazolopyrimidine		beta-adrenergic antagonist;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
geroprotector
imatinib
[no description available]		2.2110aromatic amine;
benzamides;
N-methylpiperazine;
pyridines;
pyrimidines		antineoplastic agent;
apoptosis inducer;
tyrosine kinase inhibitor
quinazolines
Quinazolines: A group of aromatic heterocyclic compounds that contain a bicyclic structure with two fused six-membered aromatic rings, a benzene ring and a pyrimidine ring.. quinazoline : A mancude organic heterobicyclic parent that is naphthalene in which the carbon atoms at positions 1 and 3 have been replaced by nitrogen atoms.. quinazolines : Any organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives.		2.1310azaarene;
mancude organic heterobicyclic parent;
ortho-fused heteroarene;
quinazolines
gefitinib
[no description available]		3.3110aromatic ether;
monochlorobenzenes;
monofluorobenzenes;
morpholines;
quinazolines;
secondary amino compound;
tertiary amino compound		antineoplastic agent;
epidermal growth factor receptor antagonist
canertinib
[no description available]		3.3110monochlorobenzenes;
morpholines;
organofluorine compound;
quinazolines		antineoplastic agent;
tyrosine kinase inhibitor
erlotinib
[no description available]		3.3110aromatic ether;
quinazolines;
secondary amino compound;
terminal acetylenic compound		antineoplastic agent;
epidermal growth factor receptor antagonist;
protein kinase inhibitor
lapatinib
[no description available]		3.3110furans;
organochlorine compound;
organofluorine compound;
quinazolines		antineoplastic agent;
tyrosine kinase inhibitor
artenimol
[no description available]		3.3110
lch-7749944
LCH-7749944: potent p21-activated kinase 4 inhibitor, structure in first source		3.3110
dasatinib
N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)-1,3-thiazole-5-carboxamide: a dasatinib prodrug; structure in first source. dasatinib (anhydrous) : An aminopyrimidine that is 2-methylpyrimidine which is substituted at position 4 by the primary amino group of 2-amino-1,3-thiazole-5-carboxylic acid and at position 6 by a 4-(2-hydroxyethyl)piperazin-1-yl group, and in which the carboxylic acid group has been formally condensed with 2-chloro-6-methylaniline to afford the corresponding amide. A multi-targeted kinase inhibitor, it is used, particularly as the monohydrate, for the treatment of chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia. Note that the name 'dasatinib' is used to refer to the monohydrate (USAN) as well as to anhydrous dasatinib (INN).		2.21101,3-thiazoles;
aminopyrimidine;
monocarboxylic acid amide;
N-(2-hydroxyethyl)piperazine;
N-arylpiperazine;
organochlorine compound;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor
zd 6474
CH 331: structure in first source		3.3110aromatic ether;
organobromine compound;
organofluorine compound;
piperidines;
quinazolines;
secondary amine		antineoplastic agent;
tyrosine kinase inhibitor
axitinib
[no description available]		2.2110aryl sulfide;
benzamides;
indazoles;
pyridines		antineoplastic agent;
tyrosine kinase inhibitor;
vascular endothelial growth factor receptor antagonist
artesunate
artesunic acid: RN given for (3R-(3alpha,5abeta,6beta,8abeta,9alpha,10alpha,12beta,(2aR*))-isomer; succinic ester of artemether		3.3110artemisinin derivative;
cyclic acetal;
dicarboxylic acid monoester;
hemisuccinate;
semisynthetic derivative;
sesquiterpenoid		antimalarial;
antineoplastic agent;
ferroptosis inducer
spc-839
SPC-839: an inhibitor of activator protein 1; structure in first source		3.3110
cp 724714
2-methoxy-N-(3-(4-((3-methyl-4-((6-methyl-3-pyridinyl)oxy)phenyl)amino)-6-quinazolinyl)-2-propenyl)acetamide: CP-724714 is the ((2E)-isomer, 1:1.5 succinate); structure in first source		3.31102-methoxy-N-[3-[4-[3-methyl-4-[(6-methyl-3-pyridinyl)oxy]anilino]-6-quinazolinyl]prop-2-enyl]acetamideantineoplastic agent;
apoptosis inducer;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
hepatotoxic agent
zm 447439
ZM447439 : A member of the class of quinazolines that is quinazoline which is substituted at positions 4, 6 and 7 by a (4-benzamidophenyl)nitrilo group, methoxy group and a 3-(morpholin-4-yl)propoxy group, respectively. It is an ATP-competitive inhibitor of Aurora A and Aurora B kinases with IC50 of 110 nM and 130 nM, respectively.		3.3110aromatic ether;
benzamides;
morpholines;
polyether;
quinazolines;
secondary amino compound;
tertiary amino compound		antineoplastic agent;
apoptosis inducer;
Aurora kinase inhibitor
cp 31398
CP 31398: structure in first source		2.2110
bibw 2992
[no description available]		3.3110aromatic ether;
enamide;
furans;
monochlorobenzenes;
organofluorine compound;
quinazolines;
secondary carboxamide;
tertiary amino compound		antineoplastic agent;
tyrosine kinase inhibitor
saracatinib
[no description available]		4.520aromatic ether;
benzodioxoles;
diether;
N-methylpiperazine;
organochlorine compound;
oxanes;
quinazolines;
secondary amino compound		anticoronaviral agent;
antineoplastic agent;
apoptosis inducer;
autophagy inducer;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
radiosensitizing agent
azd 8931
sapitinib : A member of the class of quinazolines that is 4-amino-7-methoxyquinazoline in which the amino group has been substituted by a 3-chloro-2-fluorophenyl group and in which position 6 of the quinoline ring has been substituted by a {1-[2-(methylamino)-2-oxoethyl]piperidin-4-yl}oxy group. Sapitinib is a dual tyrosine kinase inhibitor (TKI) of epithelial growth factor receptors (EGFR) HER2 and HER3.		3.3110aromatic ether;
monochlorobenzenes;
monofluorobenzenes;
piperidines;
quinazolines;
secondary amino compound;
tertiary amino compound		EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
epidermal growth factor receptor antagonist
pf 00299804
dacomitinib: a pan-ERBB inhibitor. dacomitinib : A member of the class of quinazolines that is 7-methoxyquinazoline-4,6-diamine in which the amino group at position 4 is substituted by a 3-chloro-4-fluorophenyl group and the amino group at position 6 is substituted by an (E)-4-(piperidin-1-yl)but-2-enoyl group.		3.3110enamide;
monochlorobenzenes;
monofluorobenzenes;
piperidines;
quinazolines;
secondary amino compound;
secondary carboxamide;
tertiary amino compound		antineoplastic agent;
epidermal growth factor receptor antagonist
jnj-26483327
JNJ-26483327: an orally active macrocyclic tyrosine kinase inhibitor for treatment of patients with advanced solid tumours; in Phase I trial, 9/2010		3.3110
azd 1152-hqpa
AZD2811: has antineoplastic activity; structure in first source		3.3110anilide;
monofluorobenzenes;
primary alcohol;
pyrazoles;
quinazolines;
secondary amino compound;
secondary carboxamide;
tertiary amino compound		antineoplastic agent;
Aurora kinase inhibitor
icotinib
[no description available]		3.3110
arry-334543
ARRY-334543: an antagonist of ATP-binding cassette subfamily G member 2 (ABCG2); structure in first source		3.3110
ganciclovir
[no description available]		3.31102-aminopurines;
oxopurine		antiinfective agent;
antiviral drug
ConditionIndicatedRelationship StrengthStudiesTrials
Invasiveness, Neoplasm
[description not available]		03.3420
Benign Neoplasms
[description not available]		03.1210
Neoplasms
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.		03.1210
Congenital Zika Syndrome
[description not available]		02.2510
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.2510
Zika Virus Infection
A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.		02.2510
Adenoma, Prostatic
[description not available]		02.1310
Muscle Contraction
A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.		07.1310
Prostatic Hyperplasia
Increase in constituent cells in the PROSTATE, leading to enlargement of the organ (hypertrophy) and adverse impact on the lower urinary tract function. This can be caused by increased rate of cell proliferation, reduced rate of cell death, or both.		02.1310
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