Page last updated: 2024-12-11

cgp 53716

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

Description

CGP 53716: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID Source	ID
PubMed CID	9864718
CHEMBL ID	20926
SCHEMBL ID	9782
MeSH ID	M0245312

Synonyms (24)

Synonym
n-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide
n-[4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-phenyl]-benzamide
bdbm50240407
n-(4-methyl-3-(4-(pyridin-3-yl)pyrimidin-2-ylamino)phenyl)benzamide
CHEMBL20926 ,
SCHEMBL9782
cgp-53716
cgp53716
n-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide
AKOS032953616
n-(4-methyl-3(4-(pyridine-3-yl)pyrimidin-2-ylamino)phenyl)benzamide
mfcd00945675
152459-94-4
BS-15548
cgp53716;cgp 53716
VCC347042
BCP34642
benzamide, n-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]-
C72889
A921531
CGA45994
cgp 53716
CS-0021956
HY-101837

Research Excerpts

Actions

Excerpt	Reference	Relevance
"CGP 53716 did not inhibit the number of replicating bromodeoxyuridine (BrdU)-incorporating cells in the intima, media, or adventitia during BrdU labeling at 0-96 postoperative h, though it inhibited significantly (P<0.01) the replication of medial and intimal cells from 93 h onward."	( Inhibition of platelet-derived growth factor receptor tyrosine kinase inhibits vascular smooth muscle cell migration and proliferation. Buchdunger, E; Calderon, L; Häyry, P; Lemström, K; Myllärniemi, M, 1997)	1.02

Treatment

Excerpt	Reference	Relevance
"Treatment with CGP 53716, a protein-tyrosine kinase inhibitor selective for PDGF receptor, alone and in combination with suboptimal doses of cyclosporin A, significantly reduced myofibroproliferation and the degree of OB by more than 50%."	( Role of platelet-derived growth factor in obliterative bronchiolitis (chronic rejection) in the rat. Aavik, E; Buchdunger, E; Kallio, EA; Koskinen, PK; Lemström, KB, 1999)	0.64

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

Protein Targets (4)

Inhibition Measurements

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Tyrosine-protein kinase ABL1	Homo sapiens (human)	IC50 (µMol)	6.5491	0.0001	0.7128	10.0000	AID632955; AID743664
Platelet-derived growth factor receptor beta	Mus musculus (house mouse)	IC50 (µMol)	0.1000	0.0018	0.7552	9.5000	AID371451
Breakpoint cluster region protein	Homo sapiens (human)	IC50 (µMol)	0.3981	0.0003	0.6200	10.0000	AID743664
Platelet-derived growth factor receptor alpha	Mus musculus (house mouse)	IC50 (µMol)	0.1000	0.0018	0.8572	9.5000	AID371451
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (141)

Process	via Protein(s)	Taxonomy
response to oxidative stress	Tyrosine-protein kinase ABL1	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	Tyrosine-protein kinase ABL1	Homo sapiens (human)
negative regulation of ubiquitin-protein transferase activity	Tyrosine-protein kinase ABL1	Homo sapiens (human)
negative regulation of phospholipase C activity	Tyrosine-protein kinase ABL1	Homo sapiens (human)
mitotic cell cycle	Tyrosine-protein kinase ABL1	Homo sapiens (human)
neural tube closure	Tyrosine-protein kinase ABL1	Homo sapiens (human)
B-1 B cell homeostasis	Tyrosine-protein kinase ABL1	Homo sapiens (human)
positive regulation of protein phosphorylation	Tyrosine-protein kinase ABL1	Homo sapiens (human)
B cell proliferation involved in immune response	Tyrosine-protein kinase ABL1	Homo sapiens (human)
transitional one stage B cell differentiation	Tyrosine-protein kinase ABL1	Homo sapiens (human)
mismatch repair	Tyrosine-protein kinase ABL1	Homo sapiens (human)
regulation of DNA-templated transcription	Tyrosine-protein kinase ABL1	Homo sapiens (human)
autophagy	Tyrosine-protein kinase ABL1	Homo sapiens (human)
DNA damage response	Tyrosine-protein kinase ABL1	Homo sapiens (human)
integrin-mediated signaling pathway	Tyrosine-protein kinase ABL1	Homo sapiens (human)
canonical NF-kappaB signal transduction	Tyrosine-protein kinase ABL1	Homo sapiens (human)
associative learning	Tyrosine-protein kinase ABL1	Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage	Tyrosine-protein kinase ABL1	Homo sapiens (human)
response to xenobiotic stimulus	Tyrosine-protein kinase ABL1	Homo sapiens (human)
post-embryonic development	Tyrosine-protein kinase ABL1	Homo sapiens (human)
regulation of autophagy	Tyrosine-protein kinase ABL1	Homo sapiens (human)
positive regulation of endothelial cell migration	Tyrosine-protein kinase ABL1	Homo sapiens (human)
peptidyl-tyrosine phosphorylation	Tyrosine-protein kinase ABL1	Homo sapiens (human)
cerebellum morphogenesis	Tyrosine-protein kinase ABL1	Homo sapiens (human)
negative regulation of cell-cell adhesion	Tyrosine-protein kinase ABL1	Homo sapiens (human)
microspike assembly	Tyrosine-protein kinase ABL1	Homo sapiens (human)
actin cytoskeleton organization	Tyrosine-protein kinase ABL1	Homo sapiens (human)
actin filament polymerization	Tyrosine-protein kinase ABL1	Homo sapiens (human)
regulation of endocytosis	Tyrosine-protein kinase ABL1	Homo sapiens (human)
regulation of cell adhesion	Tyrosine-protein kinase ABL1	Homo sapiens (human)
neuron differentiation	Tyrosine-protein kinase ABL1	Homo sapiens (human)
BMP signaling pathway	Tyrosine-protein kinase ABL1	Homo sapiens (human)
negative regulation of BMP signaling pathway	Tyrosine-protein kinase ABL1	Homo sapiens (human)
regulation of axon extension	Tyrosine-protein kinase ABL1	Homo sapiens (human)
regulation of microtubule polymerization	Tyrosine-protein kinase ABL1	Homo sapiens (human)
regulation of Cdc42 protein signal transduction	Tyrosine-protein kinase ABL1	Homo sapiens (human)
positive regulation of type II interferon production	Tyrosine-protein kinase ABL1	Homo sapiens (human)
positive regulation of interleukin-2 production	Tyrosine-protein kinase ABL1	Homo sapiens (human)
regulation of actin cytoskeleton organization	Tyrosine-protein kinase ABL1	Homo sapiens (human)
positive regulation of osteoblast proliferation	Tyrosine-protein kinase ABL1	Homo sapiens (human)
substrate adhesion-dependent cell spreading	Tyrosine-protein kinase ABL1	Homo sapiens (human)
cellular response to oxidative stress	Tyrosine-protein kinase ABL1	Homo sapiens (human)
response to endoplasmic reticulum stress	Tyrosine-protein kinase ABL1	Homo sapiens (human)
platelet-derived growth factor receptor-beta signaling pathway	Tyrosine-protein kinase ABL1	Homo sapiens (human)
protein modification process	Tyrosine-protein kinase ABL1	Homo sapiens (human)
peptidyl-tyrosine autophosphorylation	Tyrosine-protein kinase ABL1	Homo sapiens (human)
Fc-gamma receptor signaling pathway involved in phagocytosis	Tyrosine-protein kinase ABL1	Homo sapiens (human)
neuropilin signaling pathway	Tyrosine-protein kinase ABL1	Homo sapiens (human)
signal transduction in response to DNA damage	Tyrosine-protein kinase ABL1	Homo sapiens (human)
positive regulation of apoptotic process	Tyrosine-protein kinase ABL1	Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transduction	Tyrosine-protein kinase ABL1	Homo sapiens (human)
positive regulation of neuron apoptotic process	Tyrosine-protein kinase ABL1	Homo sapiens (human)
endothelial cell migration	Tyrosine-protein kinase ABL1	Homo sapiens (human)
regulation of T cell differentiation	Tyrosine-protein kinase ABL1	Homo sapiens (human)
positive regulation of vasoconstriction	Tyrosine-protein kinase ABL1	Homo sapiens (human)
negative regulation of mitotic cell cycle	Tyrosine-protein kinase ABL1	Homo sapiens (human)
positive regulation of mitotic cell cycle	Tyrosine-protein kinase ABL1	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Tyrosine-protein kinase ABL1	Homo sapiens (human)
alpha-beta T cell differentiation	Tyrosine-protein kinase ABL1	Homo sapiens (human)
protein autophosphorylation	Tyrosine-protein kinase ABL1	Homo sapiens (human)
positive regulation of fibroblast proliferation	Tyrosine-protein kinase ABL1	Homo sapiens (human)
spleen development	Tyrosine-protein kinase ABL1	Homo sapiens (human)
thymus development	Tyrosine-protein kinase ABL1	Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylation	Tyrosine-protein kinase ABL1	Homo sapiens (human)
activated T cell proliferation	Tyrosine-protein kinase ABL1	Homo sapiens (human)
T cell receptor signaling pathway	Tyrosine-protein kinase ABL1	Homo sapiens (human)
B cell receptor signaling pathway	Tyrosine-protein kinase ABL1	Homo sapiens (human)
neuromuscular process controlling balance	Tyrosine-protein kinase ABL1	Homo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosol	Tyrosine-protein kinase ABL1	Homo sapiens (human)
positive regulation of oxidoreductase activity	Tyrosine-protein kinase ABL1	Homo sapiens (human)
neuron apoptotic process	Tyrosine-protein kinase ABL1	Homo sapiens (human)
negative regulation of ubiquitin-protein transferase activity	Tyrosine-protein kinase ABL1	Homo sapiens (human)
myoblast proliferation	Tyrosine-protein kinase ABL1	Homo sapiens (human)
positive regulation of stress fiber assembly	Tyrosine-protein kinase ABL1	Homo sapiens (human)
establishment of localization in cell	Tyrosine-protein kinase ABL1	Homo sapiens (human)
regulation of cell cycle	Tyrosine-protein kinase ABL1	Homo sapiens (human)
mitochondrial depolarization	Tyrosine-protein kinase ABL1	Homo sapiens (human)
positive regulation of focal adhesion assembly	Tyrosine-protein kinase ABL1	Homo sapiens (human)
Bergmann glial cell differentiation	Tyrosine-protein kinase ABL1	Homo sapiens (human)
cardiac muscle cell proliferation	Tyrosine-protein kinase ABL1	Homo sapiens (human)
neuroepithelial cell differentiation	Tyrosine-protein kinase ABL1	Homo sapiens (human)
cellular response to hydrogen peroxide	Tyrosine-protein kinase ABL1	Homo sapiens (human)
ERK1 and ERK2 cascade	Tyrosine-protein kinase ABL1	Homo sapiens (human)
negative regulation of ERK1 and ERK2 cascade	Tyrosine-protein kinase ABL1	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	Tyrosine-protein kinase ABL1	Homo sapiens (human)
DNA conformation change	Tyrosine-protein kinase ABL1	Homo sapiens (human)
cellular response to lipopolysaccharide	Tyrosine-protein kinase ABL1	Homo sapiens (human)
cellular response to transforming growth factor beta stimulus	Tyrosine-protein kinase ABL1	Homo sapiens (human)
response to epinephrine	Tyrosine-protein kinase ABL1	Homo sapiens (human)
negative regulation of protein serine/threonine kinase activity	Tyrosine-protein kinase ABL1	Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesis	Tyrosine-protein kinase ABL1	Homo sapiens (human)
cellular senescence	Tyrosine-protein kinase ABL1	Homo sapiens (human)
cell-cell adhesion	Tyrosine-protein kinase ABL1	Homo sapiens (human)
positive regulation of dendrite development	Tyrosine-protein kinase ABL1	Homo sapiens (human)
positive regulation of substrate adhesion-dependent cell spreading	Tyrosine-protein kinase ABL1	Homo sapiens (human)
negative regulation of long-term synaptic potentiation	Tyrosine-protein kinase ABL1	Homo sapiens (human)
regulation of hematopoietic stem cell differentiation	Tyrosine-protein kinase ABL1	Homo sapiens (human)
positive regulation of extracellular matrix organization	Tyrosine-protein kinase ABL1	Homo sapiens (human)
podocyte apoptotic process	Tyrosine-protein kinase ABL1	Homo sapiens (human)
cellular response to dopamine	Tyrosine-protein kinase ABL1	Homo sapiens (human)
positive regulation of establishment of T cell polarity	Tyrosine-protein kinase ABL1	Homo sapiens (human)
DN4 thymocyte differentiation	Tyrosine-protein kinase ABL1	Homo sapiens (human)
protein localization to cytoplasmic microtubule plus-end	Tyrosine-protein kinase ABL1	Homo sapiens (human)
positive regulation of microtubule binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
positive regulation of actin filament binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
regulation of modification of synaptic structure	Tyrosine-protein kinase ABL1	Homo sapiens (human)
positive regulation of blood vessel branching	Tyrosine-protein kinase ABL1	Homo sapiens (human)
activation of protein kinase C activity	Tyrosine-protein kinase ABL1	Homo sapiens (human)
negative regulation of double-strand break repair via homologous recombination	Tyrosine-protein kinase ABL1	Homo sapiens (human)
positive regulation of Wnt signaling pathway, planar cell polarity pathway	Tyrosine-protein kinase ABL1	Homo sapiens (human)
regulation of cell motility	Tyrosine-protein kinase ABL1	Homo sapiens (human)
negative regulation of endothelial cell apoptotic process	Tyrosine-protein kinase ABL1	Homo sapiens (human)
positive regulation of T cell migration	Tyrosine-protein kinase ABL1	Homo sapiens (human)
negative regulation of cellular senescence	Tyrosine-protein kinase ABL1	Homo sapiens (human)
epidermal growth factor receptor signaling pathway	Tyrosine-protein kinase ABL1	Homo sapiens (human)
protein phosphorylation	Tyrosine-protein kinase ABL1	Homo sapiens (human)
negative regulation of cellular extravasation	Breakpoint cluster region protein	Homo sapiens (human)
renal system process	Breakpoint cluster region protein	Homo sapiens (human)
protein phosphorylation	Breakpoint cluster region protein	Homo sapiens (human)
phagocytosis	Breakpoint cluster region protein	Homo sapiens (human)
signal transduction	Breakpoint cluster region protein	Homo sapiens (human)
small GTPase-mediated signal transduction	Breakpoint cluster region protein	Homo sapiens (human)
brain development	Breakpoint cluster region protein	Homo sapiens (human)
actin cytoskeleton organization	Breakpoint cluster region protein	Homo sapiens (human)
keratinocyte differentiation	Breakpoint cluster region protein	Homo sapiens (human)
regulation of Rho protein signal transduction	Breakpoint cluster region protein	Homo sapiens (human)
inner ear morphogenesis	Breakpoint cluster region protein	Homo sapiens (human)
regulation of vascular permeability	Breakpoint cluster region protein	Homo sapiens (human)
neutrophil degranulation	Breakpoint cluster region protein	Homo sapiens (human)
negative regulation of neutrophil degranulation	Breakpoint cluster region protein	Homo sapiens (human)
focal adhesion assembly	Breakpoint cluster region protein	Homo sapiens (human)
homeostasis of number of cells	Breakpoint cluster region protein	Homo sapiens (human)
negative regulation of inflammatory response	Breakpoint cluster region protein	Homo sapiens (human)
positive regulation of phagocytosis	Breakpoint cluster region protein	Homo sapiens (human)
modulation of chemical synaptic transmission	Breakpoint cluster region protein	Homo sapiens (human)
neuromuscular process controlling balance	Breakpoint cluster region protein	Homo sapiens (human)
regulation of small GTPase mediated signal transduction	Breakpoint cluster region protein	Homo sapiens (human)
regulation of cell cycle	Breakpoint cluster region protein	Homo sapiens (human)
definitive hemopoiesis	Breakpoint cluster region protein	Homo sapiens (human)
negative regulation of respiratory burst	Breakpoint cluster region protein	Homo sapiens (human)
negative regulation of blood vessel remodeling	Breakpoint cluster region protein	Homo sapiens (human)
intracellular protein transmembrane transport	Breakpoint cluster region protein	Homo sapiens (human)
cellular response to lipopolysaccharide	Breakpoint cluster region protein	Homo sapiens (human)
activation of GTPase activity	Breakpoint cluster region protein	Homo sapiens (human)
macrophage migration	Breakpoint cluster region protein	Homo sapiens (human)
negative regulation of macrophage migration	Breakpoint cluster region protein	Homo sapiens (human)
negative regulation of reactive oxygen species metabolic process	Breakpoint cluster region protein	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (31)

Process	via Protein(s)	Taxonomy
supercoiled DNA binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
magnesium ion binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
four-way junction DNA binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
bubble DNA binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
phosphotyrosine residue binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
DNA binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
transcription coactivator activity	Tyrosine-protein kinase ABL1	Homo sapiens (human)
actin monomer binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
nicotinate-nucleotide adenylyltransferase activity	Tyrosine-protein kinase ABL1	Homo sapiens (human)
protein kinase activity	Tyrosine-protein kinase ABL1	Homo sapiens (human)
protein tyrosine kinase activity	Tyrosine-protein kinase ABL1	Homo sapiens (human)
non-membrane spanning protein tyrosine kinase activity	Tyrosine-protein kinase ABL1	Homo sapiens (human)
protein kinase C binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
protein binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
ATP binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
kinase activity	Tyrosine-protein kinase ABL1	Homo sapiens (human)
SH3 domain binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
syntaxin binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
manganese ion binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
neuropilin binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
SH2 domain binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
ephrin receptor binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
actin filament binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
mitogen-activated protein kinase binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
proline-rich region binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
delta-catenin binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
sequence-specific double-stranded DNA binding	Tyrosine-protein kinase ABL1	Homo sapiens (human)
protein serine/threonine kinase activity	Breakpoint cluster region protein	Homo sapiens (human)
protein tyrosine kinase activity	Breakpoint cluster region protein	Homo sapiens (human)
guanyl-nucleotide exchange factor activity	Breakpoint cluster region protein	Homo sapiens (human)
GTPase activator activity	Breakpoint cluster region protein	Homo sapiens (human)
protein binding	Breakpoint cluster region protein	Homo sapiens (human)
ATP binding	Breakpoint cluster region protein	Homo sapiens (human)
protein serine kinase activity	Breakpoint cluster region protein	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (24)

Process	via Protein(s)	Taxonomy
ruffle	Tyrosine-protein kinase ABL1	Homo sapiens (human)
nucleus	Tyrosine-protein kinase ABL1	Homo sapiens (human)
nucleoplasm	Tyrosine-protein kinase ABL1	Homo sapiens (human)
nucleolus	Tyrosine-protein kinase ABL1	Homo sapiens (human)
cytoplasm	Tyrosine-protein kinase ABL1	Homo sapiens (human)
mitochondrion	Tyrosine-protein kinase ABL1	Homo sapiens (human)
cytosol	Tyrosine-protein kinase ABL1	Homo sapiens (human)
actin cytoskeleton	Tyrosine-protein kinase ABL1	Homo sapiens (human)
nuclear body	Tyrosine-protein kinase ABL1	Homo sapiens (human)
dendrite	Tyrosine-protein kinase ABL1	Homo sapiens (human)
growth cone	Tyrosine-protein kinase ABL1	Homo sapiens (human)
nuclear membrane	Tyrosine-protein kinase ABL1	Homo sapiens (human)
neuronal cell body	Tyrosine-protein kinase ABL1	Homo sapiens (human)
perinuclear region of cytoplasm	Tyrosine-protein kinase ABL1	Homo sapiens (human)
postsynapse	Tyrosine-protein kinase ABL1	Homo sapiens (human)
protein-containing complex	Tyrosine-protein kinase ABL1	Homo sapiens (human)
plasma membrane	Tyrosine-protein kinase ABL1	Homo sapiens (human)
cytosol	Breakpoint cluster region protein	Homo sapiens (human)
plasma membrane	Breakpoint cluster region protein	Homo sapiens (human)
postsynaptic density	Breakpoint cluster region protein	Homo sapiens (human)
membrane	Breakpoint cluster region protein	Homo sapiens (human)
axon	Breakpoint cluster region protein	Homo sapiens (human)
dendritic spine	Breakpoint cluster region protein	Homo sapiens (human)
extracellular exosome	Breakpoint cluster region protein	Homo sapiens (human)
protein-containing complex	Breakpoint cluster region protein	Homo sapiens (human)
Schaffer collateral - CA1 synapse	Breakpoint cluster region protein	Homo sapiens (human)
glutamatergic synapse	Breakpoint cluster region protein	Homo sapiens (human)
membrane	Breakpoint cluster region protein	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (4)

Assay ID	Title	Year	Journal	Article
AID632955	Inhibition of Abl using DAIpYAAPFAKKK phosphopeptide as substrate by MALDI-MS analysis	2011	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23	Synthesis and docking study of 2-phenylaminopyrimidine Abl tyrosine kinase inhibitors.
AID743664	Inhibition of BCR-ABL kinase (unknown origin)	2013	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 23, Issue:8	BCR-ABL tyrosine kinase inhibitor pharmacophore model derived from a series of phenylaminopyrimidine-based (PAP) derivatives.
AID632954	Inhibition of Abl at 10 uM using DAIpYAAPFAKKK phosphopeptide as substrate by MALDI-MS analysis	2011	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23	Synthesis and docking study of 2-phenylaminopyrimidine Abl tyrosine kinase inhibitors.
AID371451	Inhibition of PDGFR autophosphorylation in mouse Swiss 3T3 fibroblast by immunoblotting	2008	European journal of medicinal chemistry, Jul, Volume: 43, Issue:7	Inhibition of PDGFR tyrosine kinase activity by a series of novel N-(3-(4-(pyridin-3-yl)-1H-imidazol-2-ylamino)phenyl)amides: a SAR study on the bioisosterism of pyrimidine and imidazole.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (13)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	8 (61.54)	18.2507
2000's	3 (23.08)	29.6817
2010's	2 (15.38)	24.3611
2020's	0 (0.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	15 (100.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one: specific inhibitor of phosphatidylinositol 3-kinase; structure in first source	1.99	1	chromones; morpholines; organochlorine compound	autophagy inhibitor; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor; geroprotector
imatinib [no description available]	2.75	3	aromatic amine; benzamides; N-methylpiperazine; pyridines; pyrimidines	antineoplastic agent; apoptosis inducer; tyrosine kinase inhibitor
tetradecanoylphorbol acetate Tetradecanoylphorbol Acetate: A phorbol ester found in CROTON OIL with very effective tumor promoting activity. It stimulates the synthesis of both DNA and RNA.. phorbol ester : Esters of phorbol, originally found in croton oil (from Croton tiglium, of the family Euphorbiaceae). A number of phorbol esters possess activity as tumour promoters and activate the mechanisms associated with cell growth. Some of these are used in experiments as activators of protein kinase C.. phorbol 13-acetate 12-myristate : A phorbol ester that is phorbol in which the hydroxy groups at the cyclopropane ring juction (position 13) and the adjacent carbon (position 12) have been converted into the corresponding acetate and myristate esters. It is a major active constituent of the seed oil of Croton tiglium. It has been used as a tumour promoting agent for skin carcinogenesis in rodents and is associated with increased cell proliferation of malignant cells. However its function is controversial since a decrease in cell proliferation has also been observed in several cancer cell types.	1.98	1	acetate ester; diester; phorbol ester; tertiary alpha-hydroxy ketone; tetradecanoate ester	antineoplastic agent; apoptosis inducer; carcinogenic agent; mitogen; plant metabolite; protein kinase C agonist; reactive oxygen species generator
vatalanib [no description available]	2.92	1	monochlorobenzenes; phthalazines; pyridines; secondary amino compound	angiogenesis inhibitor; antineoplastic agent; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor; vascular endothelial growth factor receptor antagonist
genistein [no description available]	2.92	1	7-hydroxyisoflavones	antineoplastic agent; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; geroprotector; human urinary metabolite; phytoestrogen; plant metabolite; tyrosine kinase inhibitor
vx680 [no description available]	2.08	1	N-arylpiperazine
pha 680626 [no description available]	2.08	1
epidermal growth factor Epidermal Growth Factor: A 6-kDa polypeptide growth factor initially discovered in mouse submaxillary glands. Human epidermal growth factor was originally isolated from urine based on its ability to inhibit gastric secretion and called urogastrone. Epidermal growth factor exerts a wide variety of biological effects including the promotion of proliferation and differentiation of mesenchymal and EPITHELIAL CELLS. It is synthesized as a transmembrane protein which can be cleaved to release a soluble active form.	2.39	2
cyclosporine Cyclosporine: A cyclic undecapeptide from an extract of soil fungi. It is a powerful immunosupressant with a specific action on T-lymphocytes. It is used for the prophylaxis of graft rejection in organ and tissue transplantation. (From Martindale, The Extra Pharmacopoeia, 30th ed).	2.4	2

Condition	Relationship Strength	Studies
Bronchiolitis, Exudative [description not available]	2.41	2
Cytomegalic Inclusion Disease [description not available]	2.02	1
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	2.02	1
Bronchiolitis Obliterans Inflammation of the BRONCHIOLES leading to an obstructive lung disease. Bronchioles are characterized by fibrous granulation tissue with bronchial exudates in the lumens. Clinical features include a nonproductive cough and DYSPNEA.	2.41	2
Cytomegalovirus Infections Infection with CYTOMEGALOVIRUS, characterized by enlarged cells bearing intranuclear inclusions. Infection may be in almost any organ, but the salivary glands are the most common site in children, as are the lungs in adults.	2.02	1
Carcinoma, Epidermoid [description not available]	1.98	1
Carcinoma, Squamous Cell A carcinoma derived from stratified SQUAMOUS EPITHELIAL CELLS. It may also occur in sites where glandular or columnar epithelium is normally present. (From Stedman, 25th ed)	1.98	1
Cell Transformation, Neoplastic Cell changes manifested by escape from control mechanisms, increased growth potential, alterations in the cell surface, karyotypic abnormalities, morphological and biochemical deviations from the norm, and other attributes conferring the ability to invade, metastasize, and kill.	1.99	1
Arteriosclerosis Thickening and loss of elasticity of the walls of ARTERIES of all sizes. There are many forms classified by the types of lesions and arteries involved, such as ATHEROSCLEROSIS with fatty lesions in the ARTERIAL INTIMA of medium and large muscular arteries.	2	1
Chronic Illness [description not available]	2	1
Chronic Disease Diseases which have one or more of the following characteristics: they are permanent, leave residual disability, are caused by nonreversible pathological alteration, require special training of the patient for rehabilitation, or may be expected to require a long period of supervision, observation, or care (Dictionary of Health Services Management, 2d ed). For epidemiological studies chronic disease often includes HEART DISEASES; STROKE; CANCER; and diabetes (DIABETES MELLITUS, TYPE 2).	2	1
Choroid Neovascularization [description not available]	2.92	1

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