Page last updated: 2024-11-12

verubulin

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

verubulin: antineoplastic; a small-molecule inhibitor of microtubule formation that is not a substrate for multidrug resistance pumps; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID11414799
CHEMBL ID492399
SCHEMBL ID2232326
MeSH IDM0513767

Synonyms (38)

Synonym
n-(4-methoxyphenyl)-n,2-dimethyl-quinazolin-4-amine
verubulin
CHEMBL492399
mx-128495
azixa
verubulin (usan/inn)
D10029
827031-83-4
mpc 6827
verubulin [usan:inn]
unii-x97o9ftb92
x97o9ftb92 ,
n-(4-methoxyphenyl)-n,2-dimethylquinazolin-4-amine
4-quinazolinamine, n-(4-methoxyphenyl)-n,2-dimethyl-
AKOS015994561
verubulin [who-dd]
verubulin [usan]
verubulin [inn]
verubulin, mpc-6827
EE-0048
SCHEMBL2232326
AC-25267
88U ,
NCGC00387248-01
FT-0703165
DB05585
BCP09127
mpc-6827 (hydrochloride)
SB19790
AMY32185
HY-14907
CS-0003626
nsc-758773
nsc758773
Q27293718
A864363
bdbm50557539
CIB03183

Research Excerpts

Overview

Verubulin (MPC-6827) is a microtubule-destabilizing agent that achieves high concentrations in the brain.

ExcerptReferenceRelevance
"Verubulin is a microtubule destabilizer and vascular disrupting agent that achieve high brain concentration relative to plasma in animals."( A phase 2 trial of verubulin for recurrent glioblastoma: a prospective study by the Brain Tumor Investigational Consortium (BTIC).
Chamberlain, MC; Fadul, CE; Grimm, S; Kim, L; Phuphanich, S; Recht, L; Rosenfeld, S; Zhu, JZ, 2014
)
1.45
"Verubulin (MPC-6827) is a microtubule-destabilizing agent that achieves high concentrations in the brain. "( Phase I trial of verubulin (MPC-6827) plus carboplatin in patients with relapsed glioblastoma multiforme.
Aiken, RD; Akerley, WA; Beelen, AP; Colman, H; De Groot, JF; Evans, BA; Glantz, M; Grossmann, KF; Jensen, RL; Matsuoko, Y; Olsen, JJ; Olson, JJ; Yu, M, 2012
)
2.16

Toxicity

ExcerptReferenceRelevance
" Close collaboration with cardiology colleagues for early indicators of serious cardiac adverse events will likely minimize toxicity while optimizing the therapeutic potential of VDAs and ultimately enhancing patient outcomes."( Cardiovascular toxicity profiles of vascular-disrupting agents.
Lenihan, DJ; Subbiah, IM; Tsimberidou, AM, 2011
)
0.37

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
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (6)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Epidermal growth factor receptorHomo sapiens (human)IC50 (µMol)0.00280.00000.536910.0000AID1709289
Platelet-derived growth factor receptor betaHomo sapiens (human)IC50 (µMol)0.00560.00060.80078.5000AID1709291
Vascular endothelial growth factor receptor 2Homo sapiens (human)IC50 (µMol)0.00840.00000.48308.8000AID1709290
Tubulin beta-2B chainBos taurus (cattle)IC50 (µMol)1.00000.25001.88388.7000AID1339685
Similar to alpha-tubulin isoform 1 Bos taurus (cattle)IC50 (µMol)1.00000.25001.87798.7000AID1339685
Similar to alpha-tubulin isoform 1 Bos taurus (cattle)IC50 (µMol)1.00000.25001.86568.7000AID1339685
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (169)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
epidermal growth factor receptor signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cell population proliferationEpidermal growth factor receptorHomo sapiens (human)
MAPK cascadeEpidermal growth factor receptorHomo sapiens (human)
ossificationEpidermal growth factor receptorHomo sapiens (human)
embryonic placenta developmentEpidermal growth factor receptorHomo sapiens (human)
positive regulation of protein phosphorylationEpidermal growth factor receptorHomo sapiens (human)
hair follicle developmentEpidermal growth factor receptorHomo sapiens (human)
translationEpidermal growth factor receptorHomo sapiens (human)
signal transductionEpidermal growth factor receptorHomo sapiens (human)
epidermal growth factor receptor signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
activation of phospholipase C activityEpidermal growth factor receptorHomo sapiens (human)
salivary gland morphogenesisEpidermal growth factor receptorHomo sapiens (human)
midgut developmentEpidermal growth factor receptorHomo sapiens (human)
learning or memoryEpidermal growth factor receptorHomo sapiens (human)
circadian rhythmEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cell population proliferationEpidermal growth factor receptorHomo sapiens (human)
diterpenoid metabolic processEpidermal growth factor receptorHomo sapiens (human)
peptidyl-tyrosine phosphorylationEpidermal growth factor receptorHomo sapiens (human)
cerebral cortex cell migrationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cell growthEpidermal growth factor receptorHomo sapiens (human)
lung developmentEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cell migrationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of superoxide anion generationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationEpidermal growth factor receptorHomo sapiens (human)
response to cobalaminEpidermal growth factor receptorHomo sapiens (human)
response to hydroxyisoflavoneEpidermal growth factor receptorHomo sapiens (human)
cellular response to reactive oxygen speciesEpidermal growth factor receptorHomo sapiens (human)
peptidyl-tyrosine autophosphorylationEpidermal growth factor receptorHomo sapiens (human)
ERBB2-EGFR signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
negative regulation of epidermal growth factor receptor signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
negative regulation of protein catabolic processEpidermal growth factor receptorHomo sapiens (human)
vasodilationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of phosphorylationEpidermal growth factor receptorHomo sapiens (human)
ovulation cycleEpidermal growth factor receptorHomo sapiens (human)
hydrogen peroxide metabolic processEpidermal growth factor receptorHomo sapiens (human)
negative regulation of apoptotic processEpidermal growth factor receptorHomo sapiens (human)
positive regulation of MAP kinase activityEpidermal growth factor receptorHomo sapiens (human)
tongue developmentEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cyclin-dependent protein serine/threonine kinase activityEpidermal growth factor receptorHomo sapiens (human)
positive regulation of DNA repairEpidermal growth factor receptorHomo sapiens (human)
positive regulation of DNA replicationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of bone resorptionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of DNA-templated transcriptionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of vasoconstrictionEpidermal growth factor receptorHomo sapiens (human)
negative regulation of mitotic cell cycleEpidermal growth factor receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIEpidermal growth factor receptorHomo sapiens (human)
regulation of JNK cascadeEpidermal growth factor receptorHomo sapiens (human)
symbiont entry into host cellEpidermal growth factor receptorHomo sapiens (human)
protein autophosphorylationEpidermal growth factor receptorHomo sapiens (human)
astrocyte activationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of fibroblast proliferationEpidermal growth factor receptorHomo sapiens (human)
digestive tract morphogenesisEpidermal growth factor receptorHomo sapiens (human)
positive regulation of smooth muscle cell proliferationEpidermal growth factor receptorHomo sapiens (human)
neuron projection morphogenesisEpidermal growth factor receptorHomo sapiens (human)
epithelial cell proliferationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of epithelial cell proliferationEpidermal growth factor receptorHomo sapiens (human)
regulation of peptidyl-tyrosine phosphorylationEpidermal growth factor receptorHomo sapiens (human)
protein insertion into membraneEpidermal growth factor receptorHomo sapiens (human)
response to calcium ionEpidermal growth factor receptorHomo sapiens (human)
regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of synaptic transmission, glutamatergicEpidermal growth factor receptorHomo sapiens (human)
positive regulation of glial cell proliferationEpidermal growth factor receptorHomo sapiens (human)
morphogenesis of an epithelial foldEpidermal growth factor receptorHomo sapiens (human)
eyelid development in camera-type eyeEpidermal growth factor receptorHomo sapiens (human)
response to UV-AEpidermal growth factor receptorHomo sapiens (human)
positive regulation of mucus secretionEpidermal growth factor receptorHomo sapiens (human)
regulation of ERK1 and ERK2 cascadeEpidermal growth factor receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeEpidermal growth factor receptorHomo sapiens (human)
cellular response to amino acid stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to mechanical stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to cadmium ionEpidermal growth factor receptorHomo sapiens (human)
cellular response to epidermal growth factor stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to estradiol stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to xenobiotic stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to dexamethasone stimulusEpidermal growth factor receptorHomo sapiens (human)
positive regulation of canonical Wnt signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
liver regenerationEpidermal growth factor receptorHomo sapiens (human)
cell-cell adhesionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of protein kinase C activityEpidermal growth factor receptorHomo sapiens (human)
positive regulation of G1/S transition of mitotic cell cycleEpidermal growth factor receptorHomo sapiens (human)
positive regulation of non-canonical NF-kappaB signal transductionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of prolactin secretionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of miRNA transcriptionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of protein localization to plasma membraneEpidermal growth factor receptorHomo sapiens (human)
negative regulation of cardiocyte differentiationEpidermal growth factor receptorHomo sapiens (human)
neurogenesisEpidermal growth factor receptorHomo sapiens (human)
multicellular organism developmentEpidermal growth factor receptorHomo sapiens (human)
positive regulation of kinase activityEpidermal growth factor receptorHomo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
signal transductionPlatelet-derived growth factor receptor betaHomo sapiens (human)
G protein-coupled receptor signaling pathwayPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of cell population proliferationPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of phospholipase C activityPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of smooth muscle cell migrationPlatelet-derived growth factor receptor betaHomo sapiens (human)
peptidyl-tyrosine phosphorylationPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of cell migrationPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of phosphoprotein phosphatase activityPlatelet-derived growth factor receptor betaHomo sapiens (human)
regulation of actin cytoskeleton organizationPlatelet-derived growth factor receptor betaHomo sapiens (human)
cell migration involved in vasculogenesisPlatelet-derived growth factor receptor betaHomo sapiens (human)
platelet-derived growth factor receptor-beta signaling pathwayPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of metanephric mesenchymal cell migration by platelet-derived growth factor receptor-beta signaling pathwayPlatelet-derived growth factor receptor betaHomo sapiens (human)
aorta morphogenesisPlatelet-derived growth factor receptor betaHomo sapiens (human)
cellular response to platelet-derived growth factor stimulusPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of cell proliferation by VEGF-activated platelet derived growth factor receptor signaling pathwayPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of MAP kinase activityPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of mitotic nuclear divisionPlatelet-derived growth factor receptor betaHomo sapiens (human)
phosphatidylinositol metabolic processPlatelet-derived growth factor receptor betaHomo sapiens (human)
protein autophosphorylationPlatelet-derived growth factor receptor betaHomo sapiens (human)
platelet-derived growth factor receptor signaling pathwayPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of smooth muscle cell proliferationPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of calcium-mediated signalingPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of chemotaxisPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionPlatelet-derived growth factor receptor betaHomo sapiens (human)
cardiac myofibril assemblyPlatelet-derived growth factor receptor betaHomo sapiens (human)
cell chemotaxisPlatelet-derived growth factor receptor betaHomo sapiens (human)
cell migration involved in coronary angiogenesisPlatelet-derived growth factor receptor betaHomo sapiens (human)
retina vasculature development in camera-type eyePlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadePlatelet-derived growth factor receptor betaHomo sapiens (human)
smooth muscle cell chemotaxisPlatelet-derived growth factor receptor betaHomo sapiens (human)
metanephric glomerular mesangial cell proliferation involved in metanephros developmentPlatelet-derived growth factor receptor betaHomo sapiens (human)
metanephric glomerular capillary formationPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of calcium ion importPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of reactive oxygen species metabolic processPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of DNA biosynthetic processPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of kinase activityPlatelet-derived growth factor receptor betaHomo sapiens (human)
angiogenesisPlatelet-derived growth factor receptor betaHomo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayPlatelet-derived growth factor receptor betaHomo sapiens (human)
multicellular organism developmentPlatelet-derived growth factor receptor betaHomo sapiens (human)
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)
microtubule-based processTubulin beta-2B chainBos taurus (cattle)
nervous system developmentTubulin beta-2B chainBos taurus (cattle)
positive regulation of axon guidanceTubulin beta-2B chainBos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (39)

Processvia Protein(s)Taxonomy
epidermal growth factor receptor activityEpidermal growth factor receptorHomo sapiens (human)
virus receptor activityEpidermal growth factor receptorHomo sapiens (human)
chromatin bindingEpidermal growth factor receptorHomo sapiens (human)
double-stranded DNA bindingEpidermal growth factor receptorHomo sapiens (human)
MAP kinase kinase kinase activityEpidermal growth factor receptorHomo sapiens (human)
protein tyrosine kinase activityEpidermal growth factor receptorHomo sapiens (human)
transmembrane receptor protein tyrosine kinase activityEpidermal growth factor receptorHomo sapiens (human)
transmembrane signaling receptor activityEpidermal growth factor receptorHomo sapiens (human)
epidermal growth factor receptor activityEpidermal growth factor receptorHomo sapiens (human)
integrin bindingEpidermal growth factor receptorHomo sapiens (human)
protein bindingEpidermal growth factor receptorHomo sapiens (human)
calmodulin bindingEpidermal growth factor receptorHomo sapiens (human)
ATP bindingEpidermal growth factor receptorHomo sapiens (human)
enzyme bindingEpidermal growth factor receptorHomo sapiens (human)
kinase bindingEpidermal growth factor receptorHomo sapiens (human)
protein kinase bindingEpidermal growth factor receptorHomo sapiens (human)
protein phosphatase bindingEpidermal growth factor receptorHomo sapiens (human)
protein tyrosine kinase activator activityEpidermal growth factor receptorHomo sapiens (human)
transmembrane receptor protein tyrosine kinase activator activityEpidermal growth factor receptorHomo sapiens (human)
ubiquitin protein ligase bindingEpidermal growth factor receptorHomo sapiens (human)
identical protein bindingEpidermal growth factor receptorHomo sapiens (human)
cadherin bindingEpidermal growth factor receptorHomo sapiens (human)
actin filament bindingEpidermal growth factor receptorHomo sapiens (human)
ATPase bindingEpidermal growth factor receptorHomo sapiens (human)
epidermal growth factor bindingEpidermal growth factor receptorHomo sapiens (human)
protein kinase activityPlatelet-derived growth factor receptor betaHomo sapiens (human)
protein tyrosine kinase activityPlatelet-derived growth factor receptor betaHomo sapiens (human)
platelet activating factor receptor activityPlatelet-derived growth factor receptor betaHomo sapiens (human)
platelet-derived growth factor receptor activityPlatelet-derived growth factor receptor betaHomo sapiens (human)
platelet-derived growth factor beta-receptor activityPlatelet-derived growth factor receptor betaHomo sapiens (human)
signaling receptor bindingPlatelet-derived growth factor receptor betaHomo sapiens (human)
platelet-derived growth factor receptor bindingPlatelet-derived growth factor receptor betaHomo sapiens (human)
protein bindingPlatelet-derived growth factor receptor betaHomo sapiens (human)
ATP bindingPlatelet-derived growth factor receptor betaHomo sapiens (human)
enzyme bindingPlatelet-derived growth factor receptor betaHomo sapiens (human)
protein kinase bindingPlatelet-derived growth factor receptor betaHomo sapiens (human)
vascular endothelial growth factor bindingPlatelet-derived growth factor receptor betaHomo sapiens (human)
platelet-derived growth factor bindingPlatelet-derived growth factor receptor betaHomo sapiens (human)
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)
GTPase activityTubulin beta-2B chainBos taurus (cattle)
metal ion bindingTubulin beta-2B chainBos taurus (cattle)
protein heterodimerization activityTubulin beta-2B chainBos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (37)

Processvia Protein(s)Taxonomy
endosomeEpidermal growth factor receptorHomo sapiens (human)
plasma membraneEpidermal growth factor receptorHomo sapiens (human)
ruffle membraneEpidermal growth factor receptorHomo sapiens (human)
Golgi membraneEpidermal growth factor receptorHomo sapiens (human)
extracellular spaceEpidermal growth factor receptorHomo sapiens (human)
nucleusEpidermal growth factor receptorHomo sapiens (human)
cytoplasmEpidermal growth factor receptorHomo sapiens (human)
endosomeEpidermal growth factor receptorHomo sapiens (human)
endoplasmic reticulum membraneEpidermal growth factor receptorHomo sapiens (human)
plasma membraneEpidermal growth factor receptorHomo sapiens (human)
focal adhesionEpidermal growth factor receptorHomo sapiens (human)
cell surfaceEpidermal growth factor receptorHomo sapiens (human)
endosome membraneEpidermal growth factor receptorHomo sapiens (human)
membraneEpidermal growth factor receptorHomo sapiens (human)
basolateral plasma membraneEpidermal growth factor receptorHomo sapiens (human)
apical plasma membraneEpidermal growth factor receptorHomo sapiens (human)
cell junctionEpidermal growth factor receptorHomo sapiens (human)
clathrin-coated endocytic vesicle membraneEpidermal growth factor receptorHomo sapiens (human)
early endosome membraneEpidermal growth factor receptorHomo sapiens (human)
nuclear membraneEpidermal growth factor receptorHomo sapiens (human)
membrane raftEpidermal growth factor receptorHomo sapiens (human)
perinuclear region of cytoplasmEpidermal growth factor receptorHomo sapiens (human)
multivesicular body, internal vesicle lumenEpidermal growth factor receptorHomo sapiens (human)
intracellular vesicleEpidermal growth factor receptorHomo sapiens (human)
protein-containing complexEpidermal growth factor receptorHomo sapiens (human)
receptor complexEpidermal growth factor receptorHomo sapiens (human)
Shc-EGFR complexEpidermal growth factor receptorHomo sapiens (human)
basal plasma membraneEpidermal growth factor receptorHomo sapiens (human)
nucleusPlatelet-derived growth factor receptor betaHomo sapiens (human)
cytoplasmPlatelet-derived growth factor receptor betaHomo sapiens (human)
Golgi apparatusPlatelet-derived growth factor receptor betaHomo sapiens (human)
plasma membranePlatelet-derived growth factor receptor betaHomo sapiens (human)
focal adhesionPlatelet-derived growth factor receptor betaHomo sapiens (human)
membranePlatelet-derived growth factor receptor betaHomo sapiens (human)
apical plasma membranePlatelet-derived growth factor receptor betaHomo sapiens (human)
cytoplasmic vesiclePlatelet-derived growth factor receptor betaHomo sapiens (human)
lysosomal lumenPlatelet-derived growth factor receptor betaHomo sapiens (human)
intracellular membrane-bounded organellePlatelet-derived growth factor receptor betaHomo sapiens (human)
plasma membranePlatelet-derived growth factor receptor betaHomo sapiens (human)
receptor complexPlatelet-derived growth factor receptor betaHomo sapiens (human)
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)
microtubule cytoskeletonTubulin beta-2B chainBos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (113)

Assay IDTitleYearJournalArticle
AID414617Induction of apoptosis in human T47D cells assessed as G2/M DNA content at 5 nM after 24 hrs by using propidium iodide staining by flow cytometry2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration.
AID1625715Antiproliferative activity against human HepG2 cells after 24 hrs by MTT assay2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
Design, Synthesis, and Evaluation of in Vitro and in Vivo Anticancer Activity of 4-Substituted Coumarins: A Novel Class of Potent Tubulin Polymerization Inhibitors.
AID1625734Toxicity in mouse xenografted with human H460 cells assessed as mortality at 2.5 to 5 mg/kg, iv qd administered every 2 days measured daily during compound dosing2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
Design, Synthesis, and Evaluation of in Vitro and in Vivo Anticancer Activity of 4-Substituted Coumarins: A Novel Class of Potent Tubulin Polymerization Inhibitors.
AID414608Induction of apoptosis in human T47D cells assessed as G1 phase DNA content at 5 nM after 24 hrs by using propidium iodide staining by flow cytometry2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration.
AID414621AUC (0 to infinity) in C57BL/6 mouse brain at 2.5 mg/kg, iv2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration.
AID414610Induction of apoptosis in human HCT116 cells assessed as caspase activation after 24 hrs by HTS assay2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration.
AID1709295Potency index, ratio of IC50 for erlotinib to IC50 for test compound for inhibition of VEGFR2 in human U251 cells2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.
AID1380398Antiproliferative activity against human A549 cells incubated for 48 hrs by MTT assay2018Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10
Synthesis and evaluation of new 2-chloro-4-aminopyrimidine and 2,6-dimethyl-4-aminopyrimidine derivatives as tubulin polymerization inhibitors.
AID1709298Induction of microtubule depolymerization in rat A10 cells incubated for over night by immunofluorescence method2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.
AID1709302Resistant index, ratio of IC50 for cytotoxicity against human HeLa cells expressing WT-beta3 to IC50 for cytotoxicity against human HeLa cells2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.
AID1469207Growth inhibition of human MDA-MB-231 cells after 48 hrs by MTT assay2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents.
AID1469221Inhibition of porcine brain tubulin polymerization measured every 60 secs for 90 mins by DAPI staining based fluorescence assay2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents.
AID1709297Antiproliferative activity against human MDA-MB-435 cells assessed as reduction in cell viability by Sulforhodamine B assay2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.
AID414607Induction of apoptosis in human T47D cells assessed as G1 phase DNA content at 5 nM after 48 hrs by using propidium iodide staining by flow cytometry2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration.
AID1709301Cytotoxicity against human HeLa cells over expressing WT-beta3 assessed as reduction in cell viability by Sulforhodamine B assay2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.
AID1625837Toxicity in mouse allografted with mouse C26 cells assessed as body weight loss at 2.5 to 5 mg/kg, iv qd administered every 2 days measured daily during compound dosing2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
Design, Synthesis, and Evaluation of in Vitro and in Vivo Anticancer Activity of 4-Substituted Coumarins: A Novel Class of Potent Tubulin Polymerization Inhibitors.
AID414605Induction of apoptosis in human T47D cells assessed as S phase DNA content at 5 nM after 48 hrs by using propidium iodide staining by flow cytometry2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration.
AID1709291Inhibition of PDGFRbeta in human SH-SY5Y cells preincubated for 60 mins followed by PDGF stimulation and measured after 10 mins by ELISA2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.
AID1709303Cytotoxicity against human SK-OV-3 cells assessed as reduction in cell viability by Sulforhodamine B assay2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.
AID1771025Antiproliferative activity against human A-375 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay
AID1380399Antiproliferative activity against human HeLa cells incubated for 48 hrs by MTT assay2018Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10
Synthesis and evaluation of new 2-chloro-4-aminopyrimidine and 2,6-dimethyl-4-aminopyrimidine derivatives as tubulin polymerization inhibitors.
AID1709311Antiangiogenic activity in Leghorn chicken fertilized egg chorioallantoic membrane assessed as reduction in VEGF/bFGF stimulated neovascularization after 40 hrs by microscopic based CAM assay2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.
AID1771031Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay
AID1709292Potency index, ratio of IC50 for sunitinib to IC50 for test compound for inhibition of EGFR in human A431 cell2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.
AID1469222Inhibition of porcine brain tubulin polymerization at 7.5 uM measured every 60 secs for 90 mins by DAPI staining based fluorescence assay relative to control2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents.
AID1469223Antiproliferative activity against HLF after 48 hrs by MTT assay2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents.
AID414620Induction of apoptosis in human Jurkat cells assessed as sub-diploid DNA content at 10 nM after 18 hrs by flow cytometry in presence of caspase inhibitor MX-10132009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration.
AID1771038Half life in rat liver microsomes at 1 ug/ml measured up to 60 mins in presence of NADPH by LC-MS/MS analysis
AID1469205Growth inhibition of human HCT116 cells after 48 hrs by MTT assay2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents.
AID1469262Antiproliferative activity against human LO2 cells after 48 hrs by MTT assay2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents.
AID1469218Growth inhibition of human HepG2/DOX cells after 48 hrs by MTT assay2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents.
AID1469204Growth inhibition of human A549 cells after 48 hrs by MTT assay2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents.
AID1469210Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents.
AID1399020Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay2018Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
Evaluation of 4-phenylamino-substituted naphthalene-1,2-diones as tubulin polymerization inhibitors.
AID1469202Selectivity index, ratio of IC50 for human LO2 cells to IC50 for human A549 cells2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents.
AID1771041Intrinsic clearance in mouse liver microsomes at 1 ug/ml measured up to 60 mins in presence of NADPH by LC-MS/MS analysis
AID1469220Resistance factor, ratio of IC50 for human HepG2/DOX cells to IC50 for human HepG2 cells2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents.
AID414623Antitumor activity against human MX1 cells xenografted in Crl:Nu/Nu-nuBR mouse assessed as tumor growth inhibition at 10 mg/kg, iv administered once weekly for 3 weeks2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration.
AID1709294Potency index, ratio of IC50 for sunitinib to IC50 for test compound for inhibition of PDGFRbeta in human SH-SY5Y cells2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.
AID375808Induction of apoptosis in human H1299 cells assessed as caspase activation after 48 hrs by HTS assay2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Discovery of 4-anilino-N-methylthieno[3,2-d]pyrimidines and 4-anilino-N-methylthieno[2,3-d]pyrimidines as potent apoptosis inducers.
AID473427Ratio of AUC in brain to plasma in mouse at 2.5 mg/kg, iv2010Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7
Discovery of N-methyl-4-(4-methoxyanilino)quinazolines as potent apoptosis inducers. Structure-activity relationship of the quinazoline ring.
AID1469263Antiproliferative activity against human BJ cells after 48 hrs by MTT assay2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents.
AID1469208Growth inhibition of human LoVo cells after 48 hrs by MTT assay2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents.
AID1709299Ratio of EC50 for induction of microtubule depolymerization in rat A10 cells to IC50 for antiproliferative activity against human MDA-MB-435 cells2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.
AID1380400Antiproliferative activity against human HCT116 cells incubated for 48 hrs by MTT assay2018Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10
Synthesis and evaluation of new 2-chloro-4-aminopyrimidine and 2,6-dimethyl-4-aminopyrimidine derivatives as tubulin polymerization inhibitors.
AID414618Induction of apoptosis in human T47D cells assessed as G2/M DNA content at 5 nM after 48 hrs by using propidium iodide staining by flow cytometry2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration.
AID473426Inhibition of tubulin polymerization2010Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7
Discovery of N-methyl-4-(4-methoxyanilino)quinazolines as potent apoptosis inducers. Structure-activity relationship of the quinazoline ring.
AID1709305Resistant index, ratio of IC50 for cytotoxicity against human SK-OV-3 cells over expressing MDR1-6/6 cells to IC50 for cytotoxicity against human SK-OV-3 cells2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.
AID1625714Antiproliferative activity against human HCT116 cells after 24 hrs by MTT assay2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
Design, Synthesis, and Evaluation of in Vitro and in Vivo Anticancer Activity of 4-Substituted Coumarins: A Novel Class of Potent Tubulin Polymerization Inhibitors.
AID1709310Cytotoxicity against human U-251 cells assessed as reduction in cell viability by Sulforhodamine B assay2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.
AID1399019Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay2018Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
Evaluation of 4-phenylamino-substituted naphthalene-1,2-diones as tubulin polymerization inhibitors.
AID414626Ratio of AUC (0 to infinity) in C57BL/6 mouse brain to AUC (0 to infinity) in C57BL/6 mouse plasma at 2.5 mg/kg, iv2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration.
AID1625713Antiproliferative activity against human SKOV3 cells after 24 hrs by MTT assay2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
Design, Synthesis, and Evaluation of in Vitro and in Vivo Anticancer Activity of 4-Substituted Coumarins: A Novel Class of Potent Tubulin Polymerization Inhibitors.
AID1399018Antiproliferative activity against human A549 cells after 48 hrs by MTT assay2018Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
Evaluation of 4-phenylamino-substituted naphthalene-1,2-diones as tubulin polymerization inhibitors.
AID1469206Growth inhibition of human HepG2 cells after 48 hrs by MTT assay2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents.
AID1771032Antiproliferative activity against human A549/Taxol cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay
AID1771036Half life in human liver microsomes at 1 ug/ml measured up to 60 mins in presence of NADPH by LC-MS/MS analysis
AID1771034Antiproliferative activity against human LCC6MDR cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay
AID1469264Selectivity index, ratio of IC50 for human BJ cells to IC50 for human A549 cells2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents.
AID414614Growth inhibition of human SNU398 cells after 48 hrs by celltiter assay2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration.
AID414612Growth inhibition of human T47D cells after 48 hrs by celltiter assay2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration.
AID473423Induction of apoptosis in human T47D cells assessed as caspase activation2010Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7
Discovery of N-methyl-4-(4-methoxyanilino)quinazolines as potent apoptosis inducers. Structure-activity relationship of the quinazoline ring.
AID1399021Antiproliferative activity against human RKO cells after 48 hrs by MTT assay2018Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
Evaluation of 4-phenylamino-substituted naphthalene-1,2-diones as tubulin polymerization inhibitors.
AID414619Induction of apoptosis in human Jurkat cells assessed as sub-diploid DNA content at 10 nM after 18 hrs by flow cytometry2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration.
AID1709304Cytotoxicity against human SK-OV-3 cells over expressing MDR1-6/6 assessed as reduction in cell viability by Sulforhodamine B assay2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.
AID1771026Antiproliferative activity against human M14 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay
AID1625838Toxicity in mouse allografted with mouse C26 cells assessed as mortality at 2.5 to 5 mg/kg, iv qd administered every 2 days measured daily during compound dosing2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
Design, Synthesis, and Evaluation of in Vitro and in Vivo Anticancer Activity of 4-Substituted Coumarins: A Novel Class of Potent Tubulin Polymerization Inhibitors.
AID1709309Cytotoxicity against human A-431 cells assessed as reduction in cell viability by Sulforhodamine B assay2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.
AID1469219Resistance factor, ratio of IC50 for human A549/CDDP cells to IC50 for human A549 cells2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents.
AID1709293Potency index, ratio of IC50 for sunitinib to IC50 for test compound for inhibition of VEGFR2 in human U251 cells2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.
AID414609Induction of apoptosis in human T47D cells assessed as caspase activation after 24 hrs by HTS assay2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration.
AID1469209Growth inhibition of human RKO cells after 48 hrs by MTT assay2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents.
AID414624Antitumor activity against human MX1 cells xenografted in Crl:Nu/Nu-nuBR mouse assessed as tumor growth inhibition at 5 mg/kg, iv administered once weekly for 3 weeks2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration.
AID1771037Intrinsic clearance in human liver microsomes at 1 ug/ml measured up to 60 mins in presence of NADPH by LC-MS/MS analysis
AID1709289Inhibition of EGFR in human A431 cells preincubated for 60 mins followed by EGF stimulation and measured after 10 mins by ELISA2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.
AID414611Induction of apoptosis in human SNU398 cells assessed as caspase activation after 24 hrs by HTS assay2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration.
AID1771059Binding affinity to immobilized bovine brain tubulin by SPR assay
AID1380402Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by MTT assay2018Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10
Synthesis and evaluation of new 2-chloro-4-aminopyrimidine and 2,6-dimethyl-4-aminopyrimidine derivatives as tubulin polymerization inhibitors.
AID1771090Antiproliferative activity against human A375/TxR cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay
AID414613Growth inhibition of human HCT116 cells after 48 hrs by celltiter assay2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration.
AID1469261Antimigratory activity against human A549 cells assessed as suppression of wound healing at 4 nM after 24 hrs by phase contrast microscopic method2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents.
AID473425Selectivity ratio EC50 for human H1299 cells over EC50 for human T47D cells2010Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7
Discovery of N-methyl-4-(4-methoxyanilino)quinazolines as potent apoptosis inducers. Structure-activity relationship of the quinazoline ring.
AID1469203Selectivity index, ratio of IC50 for HLF to IC50 for human A549 cells2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents.
AID1380403Inhibition of porcine brain tubulin polymerization measured every 60 secs for 90 mins by DAPI dye based fluorescence assay2018Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10
Synthesis and evaluation of new 2-chloro-4-aminopyrimidine and 2,6-dimethyl-4-aminopyrimidine derivatives as tubulin polymerization inhibitors.
AID1469211Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents.
AID414606Induction of apoptosis in human T47D cells assessed as S phase DNA content at 5 nM after 24 hrs by using propidium iodide staining by flow cytometry2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration.
AID1771040Half life in mouse liver microsomes at 1 ug/ml measured up to 60 mins in presence of NADPH by LC-MS/MS analysis
AID414615Induction of apoptosis in human T47D cells assessed as sub-diploid DNA content at 5 nM after 24 hrs by using propidium iodide staining by flow cytometry2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration.
AID375807Induction of apoptosis in human T47D cells assessed as caspase activation after 48 hrs by HTS assay2009Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
Discovery of 4-anilino-N-methylthieno[3,2-d]pyrimidines and 4-anilino-N-methylthieno[2,3-d]pyrimidines as potent apoptosis inducers.
AID1771039Intrinsic clearance in rat liver microsomes at 1 ug/ml measured up to 60 mins in presence of NADPH by LC-MS/MS analysis
AID1469212Antiproliferative activity against human MGC803 cells after 48 hrs by MTT assay2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents.
AID414625AUC (0 to infinity) in C57BL/6 mouse plasma at 2.5 mg/kg, iv2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration.
AID1709290Inhibition of VEGFR2 in human U251 cells preincubated for 60 mins followed by VEGF stimulation and measured after 10 mins by ELISA2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.
AID1625809Inhibition of porcine brain tubulin polymerization at 10 uM preincubated for 5 mins followed by GTP addition measured every 2 mins by spectrophotometry2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
Design, Synthesis, and Evaluation of in Vitro and in Vivo Anticancer Activity of 4-Substituted Coumarins: A Novel Class of Potent Tubulin Polymerization Inhibitors.
AID1771028Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay
AID1709288Potency index, ratio IC50 for erlotinib to IC50 for test compound for antiangiogenic activity in Leghorn chicken fertilized egg chorioallantoic membrane2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.
AID414622Antitumor activity against human MX1 cells xenografted in Crl:Nu/Nu-nuBR mouse assessed as tumor growth inhibition at 7.5 mg/kg, iv administered once weekly for 3 weeks2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration.
AID1771035Antiproliferative activity against human MDA-MB-231/TxR cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay
AID1469217Growth inhibition of human A549/CDDP cells after 48 hrs by MTT assay2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Synthesis and Biological Evaluation of Selenium-Containing 4-Anilinoquinazoline Derivatives as Novel Antimitotic Agents.
AID1709296Potency index, ratio of IC50 for erlotinib to IC50 for test compound for inhibition of PDGFRbeta in human SH-SY5Y cells2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.
AID1625733Toxicity in mouse xenografted with human H460 cells assessed as body weight loss at 2.5 to 5 mg/kg, iv qd administered every 2 days measured daily during compound dosing2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
Design, Synthesis, and Evaluation of in Vitro and in Vivo Anticancer Activity of 4-Substituted Coumarins: A Novel Class of Potent Tubulin Polymerization Inhibitors.
AID1625716Solubility of the compound in 2.5% ethanol/2.5% Tween-80 at 1 mg2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
Design, Synthesis, and Evaluation of in Vitro and in Vivo Anticancer Activity of 4-Substituted Coumarins: A Novel Class of Potent Tubulin Polymerization Inhibitors.
AID473424Induction of apoptosis in human H1299 cells assessed as caspase activation2010Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7
Discovery of N-methyl-4-(4-methoxyanilino)quinazolines as potent apoptosis inducers. Structure-activity relationship of the quinazoline ring.
AID414616Induction of apoptosis in human T47D cells assessed as sub-diploid DNA content at 5 nM after 48 hrs by using propidium iodide staining by flow cytometry2009Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration.
AID1709300Cytotoxicity against human HeLa cells assessed as reduction in cell viability by Sulforhodamine B assay2021Bioorganic & medicinal chemistry, 04-01, Volume: 35Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.
AID1380401Antiproliferative activity against human HepG2 cells incubated for 48 hrs by MTT assay2018Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10
Synthesis and evaluation of new 2-chloro-4-aminopyrimidine and 2,6-dimethyl-4-aminopyrimidine derivatives as tubulin polymerization inhibitors.
AID1399022Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay2018Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
Evaluation of 4-phenylamino-substituted naphthalene-1,2-diones as tubulin polymerization inhibitors.
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.
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.
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.
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.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (23)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's3 (13.04)29.6817
2010's12 (52.17)24.3611
2020's8 (34.78)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 22.21

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

MetricThis Compound (vs All)
Research Demand Index22.21 (24.57)
Research Supply Index3.30 (2.92)
Research Growth Index4.92 (4.65)
Search Engine Demand Index21.17 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (22.21)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials3 (13.04%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other20 (86.96%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]