Page last updated: 2024-11-06

chloropyramine hydrochloride

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Chloropyramine hydrochloride is an antihistamine that was originally marketed as a treatment for allergies. It is a derivative of pyrilamine, another antihistamine, and works by blocking the action of histamine, a chemical that is released by the body in response to allergens. Chloropyramine hydrochloride is no longer widely used as an antihistamine due to its potential for serious side effects, such as drowsiness, dizziness, and confusion. However, it is still studied as a potential treatment for other conditions, such as cancer and epilepsy. The compound is synthesized by reacting 2-chloro-4-methylaniline with ethyl chloroformate to form the corresponding carbamate. This carbamate is then reacted with N,N-dimethylformamide to produce chloropyramine. Chloropyramine hydrochloride is a white, crystalline solid that is soluble in water. It is a potent antihistamine that works by blocking the histamine receptors in the body. This blocks the action of histamine, which is a chemical that is released by the body in response to allergens. Chloropyramine hydrochloride is no longer widely used as an antihistamine due to its potential for serious side effects, such as drowsiness, dizziness, and confusion. However, it is still studied as a potential treatment for other conditions, such as cancer and epilepsy.'

Cross-References

ID SourceID
PubMed CID80311
CHEMBL ID550011
SCHEMBL ID538104
MeSH IDM0424335

Synonyms (74)

Synonym
AC-12197
MLS001077290
einecs 228-216-2
sinopen
unii-fwa92z14nn
nsc 409949
chloropyramine hcl
g 12144
fwa92z14nn ,
pyridine, 2-((p-chlorobenzyl)(2-(dimethylamino)ethyl)amino)-, monohydrochloride
1,2-ethanediamine, n-((4-chlorophenyl)methyl)-n',n'-dimethyl-n-2-pyridinyl-, monohydrochloride
smr000058807
MLS000028842 ,
n-p-chlorobenzyl-n',n'-dimethyl-n-2-pyridylethylenediamine hydrochloride
PRESTWICK_999
D07679
avapena (tn)
halopyramine hydrochloride
chlorpiramin hydrochloride
alergosan
chloropyribenzamine hydrochloride
chlorpyramine hydrochloride
nsc-409949
nsc409949
nilfan
6170-42-9
1, n-[(4-chlorophenyl)methyl]-n',n'-dimethyl-n-2-pyridinyl-, monohydrochloride
2-[p-chlorobenzyl-(2-dimethylaminoethyl)amino]pyridine hydrochloride
suprastin hydrochloride
sinopen hydrochloride
allergan s hydrochloride
chloropyramine hydrochloride
MLS002222287
CHEMBL550011
HMS1570B15
chlorpyramin hcl
bdbm50015561
chlorpyramin hydrochloride
tox21_113349
dtxsid9048859 ,
dtxcid6028785
pharmakon1600-01506064
nsc759320
nsc-759320
AKOS015961969
FT-0623695
S5670
n-(4-chlorobenzyl)-n'n'-dimethyl-n-(2-pyridyl) ethylenediamine hydrochloride
chloropyramine hydrochloride [who-dd]
chloropyramine hydrochloride [mart.]
chloropyramine hydrochloride [mi]
CCG-213982
MLS006010746
SCHEMBL538104
tox21_113349_1
KS-5156
W-105107
HY-B1305
CS-7974
n-[(4-chlorophenyl)methyl]-n',n'-dimethyl-n-2-pyridinyl-1,2-ethanediamine
n1-(4-chlorobenzyl)-n2,n2-dimethyl-n1-(pyridin-2-yl)ethane-1,2-diamine hydrochloride
OPERA_ID_1968
mfcd00079009
chloropyramine hydrochloride, analytical standard, for drug analysis
SR-01000721869-2
SR-01000721869-3
sr-01000721869
n1-(4-chlorobenzyl)-n2,n2-dimethyl-n1-(pyridin-2-yl)ethane-1,2-diaminehydrochloride
SB17058
Q27278239
n'-[(4-chlorophenyl)methyl]-n,n-dimethyl-n'-pyridin-2-ylethane-1,2-diamine;hydrochloride
AT25066
1,2-ethanediamine, n-((4-chlorophenyl)methyl)-n',n'-dimethyl-n-2-pyridinyl-, monohydrochloride (9ci)
n-p-chlorobenzyl-n',n'-dimethyl-n-(2-pyridyl)ethylenediamine

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

Protein Targets (20)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency35.48130.177814.390939.8107AID2147
acetylcholinesteraseHomo sapiens (human)Potency0.77620.002541.796015,848.9004AID1347398
glp-1 receptor, partialHomo sapiens (human)Potency28.18380.01846.806014.1254AID624417
phosphopantetheinyl transferaseBacillus subtilisPotency5.01190.141337.9142100.0000AID1490
TDP1 proteinHomo sapiens (human)Potency21.70610.000811.382244.6684AID686978; AID686979
GLI family zinc finger 3Homo sapiens (human)Potency10.59090.000714.592883.7951AID1259369; AID1259392
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency11.22020.011212.4002100.0000AID1030
retinoid X nuclear receptor alphaHomo sapiens (human)Potency25.82220.000817.505159.3239AID1159531
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency14.96010.001530.607315,848.9004AID1224841
pregnane X nuclear receptorHomo sapiens (human)Potency29.84930.005428.02631,258.9301AID1346982
estrogen nuclear receptor alphaHomo sapiens (human)Potency4.30940.000229.305416,493.5996AID743069; AID743075
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency26.60110.001019.414170.9645AID743191
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency26.832519.739145.978464.9432AID1159509
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency6.31570.057821.109761.2679AID1159526; AID1159528
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency50.11870.354828.065989.1251AID504847
chromobox protein homolog 1Homo sapiens (human)Potency89.12510.006026.168889.1251AID540317
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency10.12350.000323.4451159.6830AID743065; AID743067
gemininHomo sapiens (human)Potency0.11580.004611.374133.4983AID624297
Cellular tumor antigen p53Homo sapiens (human)Potency4.52200.002319.595674.0614AID651631
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Focal adhesion kinase 1Homo sapiens (human)Kd0.57000.00051.225513.0390AID1142429
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (169)

Processvia Protein(s)Taxonomy
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycle G2/M phase transitionCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
ER overload responseCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
mitophagyCellular tumor antigen p53Homo sapiens (human)
in utero embryonic developmentCellular tumor antigen p53Homo sapiens (human)
somitogenesisCellular tumor antigen p53Homo sapiens (human)
release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
hematopoietic progenitor cell differentiationCellular tumor antigen p53Homo sapiens (human)
T cell proliferation involved in immune responseCellular tumor antigen p53Homo sapiens (human)
B cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
T cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
response to ischemiaCellular tumor antigen p53Homo sapiens (human)
nucleotide-excision repairCellular tumor antigen p53Homo sapiens (human)
double-strand break repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
protein import into nucleusCellular tumor antigen p53Homo sapiens (human)
autophagyCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorCellular tumor antigen p53Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
Ras protein signal transductionCellular tumor antigen p53Homo sapiens (human)
gastrulationCellular tumor antigen p53Homo sapiens (human)
neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
protein localizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA replicationCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
determination of adult lifespanCellular tumor antigen p53Homo sapiens (human)
mRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
rRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
response to salt stressCellular tumor antigen p53Homo sapiens (human)
response to inorganic substanceCellular tumor antigen p53Homo sapiens (human)
response to X-rayCellular tumor antigen p53Homo sapiens (human)
response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
positive regulation of gene expressionCellular tumor antigen p53Homo sapiens (human)
cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
viral processCellular tumor antigen p53Homo sapiens (human)
glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
cerebellum developmentCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell growthCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCellular tumor antigen p53Homo sapiens (human)
negative regulation of telomere maintenance via telomeraseCellular tumor antigen p53Homo sapiens (human)
T cell differentiation in thymusCellular tumor antigen p53Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of tissue remodelingCellular tumor antigen p53Homo sapiens (human)
cellular response to UVCellular tumor antigen p53Homo sapiens (human)
multicellular organism growthCellular tumor antigen p53Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilityCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
entrainment of circadian clock by photoperiodCellular tumor antigen p53Homo sapiens (human)
mitochondrial DNA repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
transcription initiation-coupled chromatin remodelingCellular tumor antigen p53Homo sapiens (human)
negative regulation of proteolysisCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assemblyCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
response to antibioticCellular tumor antigen p53Homo sapiens (human)
fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
circadian behaviorCellular tumor antigen p53Homo sapiens (human)
bone marrow developmentCellular tumor antigen p53Homo sapiens (human)
embryonic organ developmentCellular tumor antigen p53Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationCellular tumor antigen p53Homo sapiens (human)
protein stabilizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of helicase activityCellular tumor antigen p53Homo sapiens (human)
protein tetramerizationCellular tumor antigen p53Homo sapiens (human)
chromosome organizationCellular tumor antigen p53Homo sapiens (human)
neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
hematopoietic stem cell differentiationCellular tumor antigen p53Homo sapiens (human)
negative regulation of glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
type II interferon-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
cardiac septum morphogenesisCellular tumor antigen p53Homo sapiens (human)
positive regulation of programmed necrotic cell deathCellular tumor antigen p53Homo sapiens (human)
protein-containing complex assemblyCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressCellular tumor antigen p53Homo sapiens (human)
thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
necroptotic processCellular tumor antigen p53Homo sapiens (human)
cellular response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
cellular response to xenobiotic stimulusCellular tumor antigen p53Homo sapiens (human)
cellular response to ionizing radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to UV-CCellular tumor antigen p53Homo sapiens (human)
stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
cellular response to actinomycin DCellular tumor antigen p53Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
cellular senescenceCellular tumor antigen p53Homo sapiens (human)
replicative senescenceCellular tumor antigen p53Homo sapiens (human)
oxidative stress-induced premature senescenceCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
oligodendrocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of execution phase of apoptosisCellular tumor antigen p53Homo sapiens (human)
negative regulation of mitophagyCellular tumor antigen p53Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of G1 to G0 transitionCellular tumor antigen p53Homo sapiens (human)
negative regulation of miRNA processingCellular tumor antigen p53Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
negative regulation of pentose-phosphate shuntCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
regulation of fibroblast apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
positive regulation of cellular senescenceCellular tumor antigen p53Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
positive regulation of macrophage chemotaxisFocal adhesion kinase 1Homo sapiens (human)
positive regulation of macrophage proliferationFocal adhesion kinase 1Homo sapiens (human)
angiogenesisFocal adhesion kinase 1Homo sapiens (human)
placenta developmentFocal adhesion kinase 1Homo sapiens (human)
regulation of protein phosphorylationFocal adhesion kinase 1Homo sapiens (human)
positive regulation of protein phosphorylationFocal adhesion kinase 1Homo sapiens (human)
heart morphogenesisFocal adhesion kinase 1Homo sapiens (human)
signal complex assemblyFocal adhesion kinase 1Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayFocal adhesion kinase 1Homo sapiens (human)
integrin-mediated signaling pathwayFocal adhesion kinase 1Homo sapiens (human)
axon guidanceFocal adhesion kinase 1Homo sapiens (human)
positive regulation of cell population proliferationFocal adhesion kinase 1Homo sapiens (human)
regulation of cell shapeFocal adhesion kinase 1Homo sapiens (human)
regulation of endothelial cell migrationFocal adhesion kinase 1Homo sapiens (human)
regulation of epithelial cell migrationFocal adhesion kinase 1Homo sapiens (human)
positive regulation of epithelial cell migrationFocal adhesion kinase 1Homo sapiens (human)
positive regulation of epithelial to mesenchymal transitionFocal adhesion kinase 1Homo sapiens (human)
positive regulation of fibroblast migrationFocal adhesion kinase 1Homo sapiens (human)
cell migrationFocal adhesion kinase 1Homo sapiens (human)
peptidyl-tyrosine phosphorylationFocal adhesion kinase 1Homo sapiens (human)
negative regulation of cell-cell adhesionFocal adhesion kinase 1Homo sapiens (human)
establishment of cell polarityFocal adhesion kinase 1Homo sapiens (human)
positive regulation of cell migrationFocal adhesion kinase 1Homo sapiens (human)
regulation of cell adhesion mediated by integrinFocal adhesion kinase 1Homo sapiens (human)
detection of muscle stretchFocal adhesion kinase 1Homo sapiens (human)
netrin-activated signaling pathwayFocal adhesion kinase 1Homo sapiens (human)
Fc-gamma receptor signaling pathway involved in phagocytosisFocal adhesion kinase 1Homo sapiens (human)
regulation of cell population proliferationFocal adhesion kinase 1Homo sapiens (human)
negative regulation of apoptotic processFocal adhesion kinase 1Homo sapiens (human)
regulation of GTPase activityFocal adhesion kinase 1Homo sapiens (human)
regulation of osteoblast differentiationFocal adhesion kinase 1Homo sapiens (human)
positive regulation of protein kinase activityFocal adhesion kinase 1Homo sapiens (human)
protein autophosphorylationFocal adhesion kinase 1Homo sapiens (human)
vascular endothelial growth factor receptor signaling pathwayFocal adhesion kinase 1Homo sapiens (human)
ephrin receptor signaling pathwayFocal adhesion kinase 1Homo sapiens (human)
cell motilityFocal adhesion kinase 1Homo sapiens (human)
regulation of cytoskeleton organizationFocal adhesion kinase 1Homo sapiens (human)
regulation of focal adhesion assemblyFocal adhesion kinase 1Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionFocal adhesion kinase 1Homo sapiens (human)
growth hormone receptor signaling pathwayFocal adhesion kinase 1Homo sapiens (human)
positive regulation of wound healingFocal adhesion kinase 1Homo sapiens (human)
regulation of substrate adhesion-dependent cell spreadingFocal adhesion kinase 1Homo sapiens (human)
positive regulation of ubiquitin-dependent protein catabolic processFocal adhesion kinase 1Homo sapiens (human)
negative regulation of anoikisFocal adhesion kinase 1Homo sapiens (human)
protein phosphorylationFocal adhesion kinase 1Homo sapiens (human)
epidermal growth factor receptor signaling pathwayFocal adhesion kinase 1Homo sapiens (human)
regulation of cell adhesionFocal adhesion kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (44)

Processvia Protein(s)Taxonomy
transcription cis-regulatory region bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
core promoter sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
TFIID-class transcription factor complex bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
protease bindingCellular tumor antigen p53Homo sapiens (human)
p53 bindingCellular tumor antigen p53Homo sapiens (human)
DNA bindingCellular tumor antigen p53Homo sapiens (human)
chromatin bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activityCellular tumor antigen p53Homo sapiens (human)
mRNA 3'-UTR bindingCellular tumor antigen p53Homo sapiens (human)
copper ion bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingCellular tumor antigen p53Homo sapiens (human)
zinc ion bindingCellular tumor antigen p53Homo sapiens (human)
enzyme bindingCellular tumor antigen p53Homo sapiens (human)
receptor tyrosine kinase bindingCellular tumor antigen p53Homo sapiens (human)
ubiquitin protein ligase bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase regulator activityCellular tumor antigen p53Homo sapiens (human)
ATP-dependent DNA/DNA annealing activityCellular tumor antigen p53Homo sapiens (human)
identical protein bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase bindingCellular tumor antigen p53Homo sapiens (human)
protein heterodimerization activityCellular tumor antigen p53Homo sapiens (human)
protein-folding chaperone bindingCellular tumor antigen p53Homo sapiens (human)
protein phosphatase 2A bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCellular tumor antigen p53Homo sapiens (human)
14-3-3 protein bindingCellular tumor antigen p53Homo sapiens (human)
MDM2/MDM4 family protein bindingCellular tumor antigen p53Homo sapiens (human)
disordered domain specific bindingCellular tumor antigen p53Homo sapiens (human)
general transcription initiation factor bindingCellular tumor antigen p53Homo sapiens (human)
molecular function activator activityCellular tumor antigen p53Homo sapiens (human)
promoter-specific chromatin bindingCellular tumor antigen p53Homo sapiens (human)
actin bindingFocal adhesion kinase 1Homo sapiens (human)
protein tyrosine kinase activityFocal adhesion kinase 1Homo sapiens (human)
non-membrane spanning protein tyrosine kinase activityFocal adhesion kinase 1Homo sapiens (human)
protein tyrosine phosphatase activityFocal adhesion kinase 1Homo sapiens (human)
integrin bindingFocal adhesion kinase 1Homo sapiens (human)
protein bindingFocal adhesion kinase 1Homo sapiens (human)
ATP bindingFocal adhesion kinase 1Homo sapiens (human)
JUN kinase bindingFocal adhesion kinase 1Homo sapiens (human)
protein kinase bindingFocal adhesion kinase 1Homo sapiens (human)
protein phosphatase bindingFocal adhesion kinase 1Homo sapiens (human)
SH2 domain bindingFocal adhesion kinase 1Homo sapiens (human)
molecular function activator activityFocal adhesion kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (28)

Processvia Protein(s)Taxonomy
nuclear bodyCellular tumor antigen p53Homo sapiens (human)
nucleusCellular tumor antigen p53Homo sapiens (human)
nucleoplasmCellular tumor antigen p53Homo sapiens (human)
replication forkCellular tumor antigen p53Homo sapiens (human)
nucleolusCellular tumor antigen p53Homo sapiens (human)
cytoplasmCellular tumor antigen p53Homo sapiens (human)
mitochondrionCellular tumor antigen p53Homo sapiens (human)
mitochondrial matrixCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulumCellular tumor antigen p53Homo sapiens (human)
centrosomeCellular tumor antigen p53Homo sapiens (human)
cytosolCellular tumor antigen p53Homo sapiens (human)
nuclear matrixCellular tumor antigen p53Homo sapiens (human)
PML bodyCellular tumor antigen p53Homo sapiens (human)
transcription repressor complexCellular tumor antigen p53Homo sapiens (human)
site of double-strand breakCellular tumor antigen p53Homo sapiens (human)
germ cell nucleusCellular tumor antigen p53Homo sapiens (human)
chromatinCellular tumor antigen p53Homo sapiens (human)
transcription regulator complexCellular tumor antigen p53Homo sapiens (human)
protein-containing complexCellular tumor antigen p53Homo sapiens (human)
stress fiberFocal adhesion kinase 1Homo sapiens (human)
nucleusFocal adhesion kinase 1Homo sapiens (human)
cytoplasmFocal adhesion kinase 1Homo sapiens (human)
centrosomeFocal adhesion kinase 1Homo sapiens (human)
cytosolFocal adhesion kinase 1Homo sapiens (human)
cytoskeletonFocal adhesion kinase 1Homo sapiens (human)
plasma membraneFocal adhesion kinase 1Homo sapiens (human)
focal adhesionFocal adhesion kinase 1Homo sapiens (human)
cell cortexFocal adhesion kinase 1Homo sapiens (human)
ciliary basal bodyFocal adhesion kinase 1Homo sapiens (human)
intracellular membrane-bounded organelleFocal adhesion kinase 1Homo sapiens (human)
perinuclear region of cytoplasmFocal adhesion kinase 1Homo sapiens (human)
plasma membraneFocal adhesion kinase 1Homo sapiens (human)
focal adhesionFocal adhesion kinase 1Homo sapiens (human)
dendritic spineFocal adhesion kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (103)

Assay IDTitleYearJournalArticle
AID420148Antiproliferative activity against human MCF10A cells after 48 hrs by BrdU incorporation assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420169Inhibition of VEGFR3 phosphorylation in human BT474 cells assessed as partial dephosphorylation at Tyr1063/1068 activation loop at 1 uM after 24 hrs by Western blotting2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420143Cytotoxicity against human MCF10A cells assessed as cell viability at 0.1 to 10 uM by MTS assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420149Antiproliferative activity against human MCF7 cells expressing VEGFR3 after 48 hrs by BrdU incorporation assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420138Cytotoxicity against human MIAPaCa2 cells after 72 hrs by MTS assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420141Cytotoxicity against human HT-29 cells after 72 hrs by MTS assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420199Inhibition of VEGFR3 phosphorylation in human MCF7 cells expressing VEGFR3 assessed as complete dephosphorylation at Tyr1063/1068 activation loop at 10 uM by Western blotting2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420176Inhibition of FAK phosphorylation in human BT474 cells assessed as decrease in total phosphorylation at 10 uM after 24 hrs by immunoprecipitation technique2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420161Induction of apoptosis in human MCF7 cells expressing VEGFR3 assessed as procaspase 8 activation after 48 hrs2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420137Cytotoxicity against human T47D cells after 72 hrs by MTS assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420171Inhibition of SRC phosphorylation2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420162Induction of apoptosis in human BT474 cells assessed as PARP degradation after 48 hrs2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420177Antitumor activity against human BT474 cells xenografted in nude-foxn1nu mouse assessed as reduction in tumor growth at 10 mg/kg, ip qd administered day after injection of cells after 14 days relative to control2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420136Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTS assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420170Inhibition of VEGFR3 phosphorylation in human BT474 cells assessed as complete dephosphorylation at Tyr1063/1068 activation loop at 10 uM by Western blotting2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420172Inhibition of EGFR phosphorylation2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420142Cytotoxicity against human BT474 cells assessed as reduction in viability at 1 uM after 48 hrs by MTS assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420188Cytotoxicity against human MCF7 cells expressing VEGFR3 assessed as cell viability at 10 uM after 48 hrs by MTS assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420200Inhibition of VEGFR3 phosphorylation in human MCF7 cells expressing VEGFR3 assessed as partial dephosphorylation at Tyr1063/1068 activation loop at 1 to 10 uM by Western blotting2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420155Antiproliferative activity against human BT474 cells 10uM after 12 hrs at by BrdU incorporation assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420175Inhibition of FAK phosphorylation in human BT474 cells assessed as partial dephosphorylation at 1 uM after 24 hrs by Western blotting2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420147Cytotoxicity against human BT474 cells assessed as cell viability at 100 uM by MTS assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420135Cytotoxicity against human BT474 cells after 72 hrs by MTS assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID1142436Inhibition of FAK/VEGFR-3 interaction in human MIAPaCa2 cells transfected with retroviral expression vector pMSCV-LucSh assessed as reduction in VEGFR3 pan-phosphorylated tyrosine level after 24 hrs by immunoprecipitation assay2014European journal of medicinal chemistry, Jun-10, Volume: 80Design, synthesis, and biological evaluation of novel FAK scaffold inhibitors targeting the FAK-VEGFR3 protein-protein interaction.
AID420194Inhibition of VEGFR3 phosphorylation in human BT474 cells assessed as partial dephosphorylation at Tyr1063/1068 activation loop at 1 to 10 uM by Western blotting2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420356Inhibition of FAK phosphorylation in human MCF7 cells expressing VEGFR3 cells assessed as decrease in total phosphorylation at 10 uM after 24 hrs by immunoprecipitation technique2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420355Inhibition of VEGFR3 phosphorylation in human MCF7 cells expressing VEGFR3 assessed as complete dephosphorylation at Tyr1063/1068 activation loop after 24 hrs by Western blotting2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420186Cytotoxicity against human MCF7 cells assessed as cell viability at 1 uM after 48 hrs by MTS assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420202Inhibition of VEGFR3 phosphorylation in human MCF7 cells expressing VEGFR3 assessed as partial dephosphorylation at Tyr1063/1068 activation loop after 24 hrs by Western blotting2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420182Cytotoxicity against human COLO205 cells assessed as cell viability after 72 hrs by MTS assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420154Antiproliferative activity against human MCF7 cells 10 uM after 12 hrs by BrdU incorporation assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420174Inhibition of IGF1R phosphorylation2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420187Cytotoxicity against human MCF7 cells expressing VEGFR3 assessed as cell viability at 1 uM after 48 hrs by MTS assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420163Induction of apoptosis in human MCF7 cells assessed as PARP degradation after 48 hrs2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID1142443Inhibition of FAK/VEGFR-3 interaction in human MIAPaCa2 cells transfected with retroviral expression vector pMSCV-LucSh assessed as reduction in VEGFR3 pan-phosphorylated tyrosine level after 24 hrs by densitometric analysis2014European journal of medicinal chemistry, Jun-10, Volume: 80Design, synthesis, and biological evaluation of novel FAK scaffold inhibitors targeting the FAK-VEGFR3 protein-protein interaction.
AID1142433Cytotoxicity against human MCF7 cells overexpressing VEGFR-3/FAK assessed as inhibition of colony formation at >10 uM after 14 days by 1,9-dimethyl-methylene blue staining-based assay2014European journal of medicinal chemistry, Jun-10, Volume: 80Design, synthesis, and biological evaluation of novel FAK scaffold inhibitors targeting the FAK-VEGFR3 protein-protein interaction.
AID420146Cytotoxicity against human MCF10A cells assessed as cell viability at 100 uM by MTS assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420160Induction of apoptosis in human MCF7 cells assessed as procaspase 8 activation after 48 hrs2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420191Induction of apoptosis in human MCF7 cells expressing VEGFR3 after 48 hrs by TUNEL assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420197Inhibition of VEGFR3 phosphorylation in human BT474 cells assessed as complete dephosphorylation at Tyr1063/1068 activation loop after 24 hrs by Western blotting2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420140Cytotoxicity against human C8161 cells after 72 hrs by MTS assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420157Induction of apoptosis in human MCF7 cells at 10 uM after 48 hrs by TUNEL assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID1142429Binding affinity to biotinylated human FAK FAT domain by biolayer interoferometry2014European journal of medicinal chemistry, Jun-10, Volume: 80Design, synthesis, and biological evaluation of novel FAK scaffold inhibitors targeting the FAK-VEGFR3 protein-protein interaction.
AID420168Disruption of FAK-VEGFR3 binding in human BT474 cells at 10 uM after 24 hrs by immunoprecipitation technique2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420164Induction of apoptosis in human MCF7 cells expressing VEGFR3 assessed as PARP degradation after 48 hrs2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID1142435Inhibition of FAK/VEGFR-3 interaction in human MIAPaCa2 cells transfected with retroviral expression vector pMSCV-LucSh assessed as decrease in levels of VEGFR3 and phosphorylated tyrosine residues associated with FAK protein after 24 hrs by immunoprecipi2014European journal of medicinal chemistry, Jun-10, Volume: 80Design, synthesis, and biological evaluation of novel FAK scaffold inhibitors targeting the FAK-VEGFR3 protein-protein interaction.
AID420145Cytotoxicity against human MCF7 cells expressing VEGFR3 assessed as cell viability after 48 hrs by MTS assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420167Decrease in colocalization of FAK-VEGFR3 complex in human MCF7 cells expressing VEGFR3 at 10 uM after 24 hrs by confocal microscopy2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420196Inhibition of VEGFR3 phosphorylation in human BT474 cells assessed as partial dephosphorylation at Tyr1063/1068 activation loop after 24 hrs by Western blotting2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420183Cytotoxicity against human Saos2 cells after 72 hrs by MTS assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420139Cytotoxicity against human PANC1 cells after 72 hrs by MTS assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID1142442Inhibition of FAK/VEGFR-3 interaction in human MIAPaCa2 cells transfected with retroviral expression vector pMSCV-LucSh assessed as decrease in levels of VEGFR3 and phosphorylated tyrosine residues associated with FAK protein after 24 hrs by densitometric2014European journal of medicinal chemistry, Jun-10, Volume: 80Design, synthesis, and biological evaluation of novel FAK scaffold inhibitors targeting the FAK-VEGFR3 protein-protein interaction.
AID420201Inhibition of VEGFR3 phosphorylation in human MCF7 cells expressing VEGFR3 assessed as complete dephosphorylation at Tyr1063/1068 activation loop at 1 to 10 uM by Western blotting2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420150Antiproliferative activity against human MCF7 cells after 48 hrs by BrdU incorporation assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID1142434Cytotoxicity against human MIAPaCa2 cells transfected with retroviral expression vector pMSCV-LucSh assessed as inhibition of colony formation at >10 uM after 14 days by 1,9-dimethyl-methylene blue staining-based assay2014European journal of medicinal chemistry, Jun-10, Volume: 80Design, synthesis, and biological evaluation of novel FAK scaffold inhibitors targeting the FAK-VEGFR3 protein-protein interaction.
AID420173Inhibition of PDGFR phosphorylation2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420185Cytotoxicity against human BT474 cells assessed as induction of cytostatic effect at 10 uM2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420166Decrease in colocalization of FAK-VEGFR3 complex in human BT474 cells at 10 uM after 24 hrs by confocal microscopy2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420190Antiproliferative activity against human MCF7 cells expressing VEGFR3 at 0.1 to 10 uM by BrdU incorporation assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420198Inhibition of VEGFR3 phosphorylation in human MCF7 cells expressing VEGFR3 cells assessed as partial dephosphorylation at Tyr1063/1068 activation loop at 1 uM after 24 hrs by Western blotting2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420144Cytotoxicity against human BT474 cells assessed as cell viability at 0.1 to 10 uM by MTS assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420195Inhibition of VEGFR3 phosphorylation in human BT474 cells assessed as complete dephosphorylation at Tyr1063/1068 activation loop at 1 to 10 uM by Western blotting2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420152Cytotoxicity against human MCF7 cells assessed as cell viability at 10 uM after 48 hrs by MTS assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420156Induction of apoptosis in human BT474 cells at 10 uM by TUNEL assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420165Decrease in colocalization of FAK-paxillin complex in human BT474 cells at 10 uM after 24 hrs by confocal microscopy2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420184Cytotoxicity against human A375 cells after 72 hrs by MTS assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420151Antiproliferative activity against human BT474 cells after 48 hrs by BrdU incorporation assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420193Relocalization of FAK-VEGFR3 complex from cytoplasm to nucleus in human BT474 cells at 10 uM after 24 hrs by confocal microscopy2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420179Antitumor activity against human MCF7 cells expressing VEGFR3 xenografted in nude-foxn1nu mouse assessed as reduction in tumor growth at 30 mg/kg after 21 days relative to control2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420153Antiproliferative activity against human MCF7 cells expressing VEGFR3 at 10 uM after 12 hrs by BrdU incorporation assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420159Induction of apoptosis in human BT474 cells assessed as procaspase 8 activation after 48 hrs2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420178Antitumor activity against human MCF7 cells expressing VEGFR3 xenografted in nude-foxn1nu mouse assessed as reduction in tumor growth at 60 mg/kg, ip qd administered day after injection of cells after 21 days relative to control2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420158Induction of apoptosis in human MCF7 cells expressing VEGFR3 at 10 uM after 48 hrs by TUNEL assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420192Relocalization of FAK-paxillin complex from cytoplasm to nucleus in human BT474 cells at 10 uM after 24 hrs by confocal microscopy2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
AID420189Antiproliferative activity against human MCF7 cells at 10 uM after 48 hrs by BrdU incorporation assay2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Small molecule chloropyramine hydrochloride (C4) targets the binding site of focal adhesion kinase and vascular endothelial growth factor receptor 3 and suppresses breast cancer growth in vivo.
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AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
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AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
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AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
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AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
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Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (12)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's2 (16.67)29.6817
2010's8 (66.67)24.3611
2020's2 (16.67)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 56.72

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 very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index56.72 (24.57)
Research Supply Index2.56 (2.92)
Research Growth Index4.46 (4.65)
Search Engine Demand Index85.94 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (56.72)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other12 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]