Page last updated: 2024-11-13

sar131675

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Description

SAR131675: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID71295845
CHEMBL ID4303275
SCHEMBL ID15668398
MeSH IDM0579636

Synonyms (25)

Synonym
sar131675
HY-15458
CS-0970
S2842
1433953-83-3
2-amino-1-ethyl-7-[(3r)-3-hydroxy-4-methoxy-3-methylbut-1-ynyl]-n-methyl-4-oxo-1,8-naphthyridine-3-carboxamide
SCHEMBL15668398
(r)-2-amino-1-ethyl-7-(3-hydroxy-4-methoxy-3-methylbut-1-yn-1-yl)-n-methyl-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxamide
AC-32832
AKOS030231683
HMS3651B17
sar 131675
bdbm50509146
(3s,4as,8as)-n-(1,1-dimethylethyl)decahydro-2-[(2r,3r)-2-hydroxy-3-[(3-hydroxy-2-methylbenzoyl)amino]-4-(phenylthio)butyl]-3-isoquinolinecarboxamidemethanesulf
SW219944-1
sar-131675
EX-A2154
AS-16301
SB19357
CCG-268137
CHEMBL4303275 ,
A925906
(r)-2-amino-1-ethyl-7-(3-hydroxy-4-methoxy-3-methylbut-1-ynyl)-n-methyl-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxamide
C71326
NCGC00386207-01

Research Excerpts

Overview

SAR131675 is a highly selective receptor tyrosine kinase inhibitor to VEGFR3 that reveals the inhibitory effect on proliferation in human lymphatic endothelial cells. It acts as a ligand for VegF-C and VEGF-D to inhibit lymphangiogenesis.

ExcerptReferenceRelevance
"SAR131675 is a highly selective receptor tyrosine kinase inhibitor to VEGFR3 that reveals the inhibitory effect on proliferation in human lymphatic endothelial cells."( SAR131675 Receptor Tyrosine Kinase Inhibitor Induces Apoptosis through Bcl- 2/Bax/Cyto c Mitochondrial Pathway in Human Umbilical Vein Endothelial Cells.
Aghaei, M; Babaei, Z; Panjehpour, M; Parsian, H, 2022
)
2.89
"SAR131675 is a selective vascular endothelial cell growth factor receptor-3 (VEGFR-3)-tyrosine kinase inhibitor that acts as a ligand for VEGF-C and VEGF-D to inhibit lymphangiogenesis."( Inhibition of lymphatic proliferation by the selective VEGFR-3 inhibitor SAR131675 ameliorates diabetic nephropathy in db/db mice.
Choi, BS; Chung, S; Hong, YA; Hwang, SD; Kim, EN; Kim, MY; Kim, Y; Kim, YS; Lim, JH; Park, CW; Song, JH, 2019
)
1.47
"SAR131675 is a potent and selective VEGFR-3 inhibitor. "( SAR131675, a potent and selective VEGFR-3-TK inhibitor with antilymphangiogenic, antitumoral, and antimetastatic activities.
Alam, A; Barron, P; Blanc, I; Bonnin, J; Bono, F; Dol, F; Duclos, O; Gaujarengues, F; Gueguen-Dorbes, G; Hérault, JP; Laplace, MC; Morin, G; Savi, P; Schaeffer, P, 2012
)
3.26
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (8)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
GVesicular stomatitis virusPotency26.83700.01238.964839.8107AID1645842
Interferon betaHomo sapiens (human)Potency26.83700.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency26.83700.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency26.83700.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency26.83700.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Vascular endothelial growth factor receptor 3Homo sapiens (human)GI500.05900.05000.05450.0590AID1540762
Vascular endothelial growth factor receptor 3Homo sapiens (human)IC50 (µMol)0.00120.00010.22644.9000AID1540765
Vascular endothelial growth factor receptor 2Homo sapiens (human)GI504.60000.00300.83054.6000AID1540761
Vascular endothelial growth factor receptor 2Homo sapiens (human)IC50 (µMol)0.06700.00000.48308.8000AID1540763
Receptor-type tyrosine-protein kinase FLT3Homo sapiens (human)GI5018.00000.00000.64579.3000AID1540766
Receptor-type tyrosine-protein kinase FLT3Homo sapiens (human)IC50 (µMol)0.29000.00010.32759.5480AID1540764
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (132)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
vascular endothelial growth factor receptor signaling pathwayVascular endothelial growth factor receptor 3Homo sapiens (human)
positive regulation of protein phosphorylationVascular endothelial growth factor receptor 3Homo sapiens (human)
positive regulation of endothelial cell proliferationVascular endothelial growth factor receptor 3Homo sapiens (human)
vasculature developmentVascular endothelial growth factor receptor 3Homo sapiens (human)
lymph vessel developmentVascular endothelial growth factor receptor 3Homo sapiens (human)
lymphangiogenesisVascular endothelial growth factor receptor 3Homo sapiens (human)
sprouting angiogenesisVascular endothelial growth factor receptor 3Homo sapiens (human)
respiratory system processVascular endothelial growth factor receptor 3Homo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayVascular endothelial growth factor receptor 3Homo sapiens (human)
positive regulation of cell population proliferationVascular endothelial growth factor receptor 3Homo sapiens (human)
positive regulation of vascular endothelial growth factor productionVascular endothelial growth factor receptor 3Homo sapiens (human)
positive regulation of endothelial cell migrationVascular endothelial growth factor receptor 3Homo sapiens (human)
peptidyl-tyrosine phosphorylationVascular endothelial growth factor receptor 3Homo sapiens (human)
cellular response to vascular endothelial growth factor stimulusVascular endothelial growth factor receptor 3Homo sapiens (human)
vascular endothelial growth factor signaling pathwayVascular endothelial growth factor receptor 3Homo sapiens (human)
negative regulation of apoptotic processVascular endothelial growth factor receptor 3Homo sapiens (human)
positive regulation of MAPK cascadeVascular endothelial growth factor receptor 3Homo sapiens (human)
positive regulation of JNK cascadeVascular endothelial growth factor receptor 3Homo sapiens (human)
protein autophosphorylationVascular endothelial growth factor receptor 3Homo sapiens (human)
vascular endothelial growth factor receptor signaling pathwayVascular endothelial growth factor receptor 3Homo sapiens (human)
lung alveolus developmentVascular endothelial growth factor receptor 3Homo sapiens (human)
blood vessel morphogenesisVascular endothelial growth factor receptor 3Homo sapiens (human)
regulation of blood vessel remodelingVascular endothelial growth factor receptor 3Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeVascular endothelial growth factor receptor 3Homo sapiens (human)
positive regulation of protein kinase C signalingVascular endothelial growth factor receptor 3Homo sapiens (human)
positive regulation of cell migrationVascular endothelial growth factor receptor 3Homo sapiens (human)
positive regulation of kinase activityVascular endothelial growth factor receptor 3Homo sapiens (human)
multicellular organism developmentVascular endothelial growth factor receptor 3Homo sapiens (human)
regulation of MAPK cascadeVascular endothelial growth factor receptor 3Homo sapiens (human)
angiogenesisVascular endothelial growth factor receptor 3Homo 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)
hemopoiesisReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
leukocyte homeostasisReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
myeloid progenitor cell differentiationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
pro-B cell differentiationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
positive regulation of cell population proliferationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
response to organonitrogen compoundReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
peptidyl-tyrosine phosphorylationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
cytokine-mediated signaling pathwayReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
B cell differentiationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
animal organ regenerationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
common myeloid progenitor cell proliferationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
vascular endothelial growth factor signaling pathwayReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
positive regulation of tyrosine phosphorylation of STAT proteinReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
regulation of apoptotic processReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
positive regulation of MAP kinase activityReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
positive regulation of MAPK cascadeReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
lymphocyte proliferationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
protein autophosphorylationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
cellular response to cytokine stimulusReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
cellular response to glucocorticoid stimulusReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
dendritic cell differentiationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
positive regulation of kinase activityReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
multicellular organism developmentReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (34)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
transmembrane receptor protein tyrosine kinase activityVascular endothelial growth factor receptor 3Homo sapiens (human)
vascular endothelial growth factor receptor activityVascular endothelial growth factor receptor 3Homo sapiens (human)
protein bindingVascular endothelial growth factor receptor 3Homo sapiens (human)
ATP bindingVascular endothelial growth factor receptor 3Homo sapiens (human)
growth factor bindingVascular endothelial growth factor receptor 3Homo sapiens (human)
protein phosphatase bindingVascular endothelial growth factor receptor 3Homo sapiens (human)
protein homodimerization activityVascular endothelial growth factor receptor 3Homo 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)
protein tyrosine kinase activityReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
transmembrane receptor protein tyrosine kinase activityReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
cytokine receptor activityReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
vascular endothelial growth factor receptor activityReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
protein bindingReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
ATP bindingReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
nuclear glucocorticoid receptor bindingReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
protein-containing complex bindingReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
phosphatidylinositol 3-kinase activator activityReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
growth factor bindingReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (31)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular regionVascular endothelial growth factor receptor 3Homo sapiens (human)
nucleoplasmVascular endothelial growth factor receptor 3Homo sapiens (human)
cytosolVascular endothelial growth factor receptor 3Homo sapiens (human)
plasma membraneVascular endothelial growth factor receptor 3Homo sapiens (human)
receptor complexVascular endothelial growth factor receptor 3Homo sapiens (human)
plasma membraneVascular endothelial growth factor receptor 3Homo 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)
endoplasmic reticulumReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
endoplasmic reticulum lumenReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
plasma membraneReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
endosome membraneReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
receptor complexReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
plasma membraneReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (39)

Assay IDTitleYearJournalArticle
AID1540783Inhibition of rhVEGF-A-induced of VEGFR2 phosphorylation at Tyr1175 residue in HUVEC at 0.1 uM incubated for 2 hrs by Western blot analysis2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Identification of a Unique Resorcylic Acid Lactone Derivative That Targets Both Lymphangiogenesis and Angiogenesis.
AID1540766Inhibition of TEL-fused FLT3 (unknown origin) expressed in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by Cell-titer-Glo assay2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Identification of a Unique Resorcylic Acid Lactone Derivative That Targets Both Lymphangiogenesis and Angiogenesis.
AID1779542Anticancer activity against human MDA-MB-231 cells assessed as cell viability incubated for 48 hrs by MTT assay
AID1540764Inhibition of human FLT3 using EAIYAAPFAKKK substrate and [gamma-33P]-ATP by radiometric biochemical kinase assay2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Identification of a Unique Resorcylic Acid Lactone Derivative That Targets Both Lymphangiogenesis and Angiogenesis.
AID1779536Antimetastatic activity against human MDA-MB-231 cells injected into vein of BALB/c mouse lung metastatic model assessed as less lung metastatic nodules at 25 mg/kg, po once a day measured on day 21
AID1779613Toxicity in BALB/c mouse xenografted with MDA-MB-231 cells assessed as creatinine level in blood at 300 mg/kg, po
AID1779533Toxicity in BALB/c mouse xenografted with MDA-MB-231 cells assessed as LDH level in blood at 300 mg/kg, po
AID1779534Toxicity in BALB/c mouse xenografted with MDA-MB-231 cells assessed as AST level in blood at 300 mg/kg, po
AID1779619Toxicity in BALB/c mouse xenografted with MDA-MB-231 cells assessed as change in kidney at 300 mg/kg, po by hematoxylin and eosin staining based analysis
AID1540791Anti-angiogenesis activity in truncated-FOSB transfected HUVEC cells model of pseudomyogenic-hemangioendothelioma assessed as inhibition of tube formation up to 5 uM2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Identification of a Unique Resorcylic Acid Lactone Derivative That Targets Both Lymphangiogenesis and Angiogenesis.
AID1540767Growth inhibition of mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by Cell-titer-Glo assay2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Identification of a Unique Resorcylic Acid Lactone Derivative That Targets Both Lymphangiogenesis and Angiogenesis.
AID1779556Selectivity ratio of IC50 for human VEGFR2 to IC50 for human VEGFR3
AID1779535Toxicity in BALB/c mouse xenografted with MDA-MB-231 cells assessed as ALT level in blood at 300 mg/kg, po
AID1540763Inhibition of human VEGFR2 using poly[Glu:Tyr] (4:1) substrate and [gamma-33P]-ATP by radiometric biochemical kinase assay2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Identification of a Unique Resorcylic Acid Lactone Derivative That Targets Both Lymphangiogenesis and Angiogenesis.
AID1779616Toxicity in BALB/c mouse xenografted with MDA-MB-231 cells assessed as change in liver at 300 mg/kg, po by hematoxylin and eosin staining based analysis
AID1540786Anti-angiogenesis activity in HUVEC assessed as inhibition of VEGF-A-induced tube formation at 0.1 uM incubated for 6 hrs by tube formation assay2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Identification of a Unique Resorcylic Acid Lactone Derivative That Targets Both Lymphangiogenesis and Angiogenesis.
AID1540761Inhibition of TEL-fused VEGFR2 (unknown origin) expressed in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by Cell-titer-Glo assay2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Identification of a Unique Resorcylic Acid Lactone Derivative That Targets Both Lymphangiogenesis and Angiogenesis.
AID1779611Toxicity in BALB/c mouse xenografted with MDA-MB-231 cells assessed as effect on body weight at 50 mg/kg, po
AID1540787Anti-lymphangiogenic activity in C57BL/6 mouse assessed as suppression of suture-induced corneal lymphangiogenesis at 200 nM administered topically every 12 hrs for 7 days by immunohistochemical analysis2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Identification of a Unique Resorcylic Acid Lactone Derivative That Targets Both Lymphangiogenesis and Angiogenesis.
AID1540784Inhibition of rhVEGF-A-induced of VEGFR2 phosphorylation at Tyr1175 residue in HUVEC at 0.1 uM by ELISA2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Identification of a Unique Resorcylic Acid Lactone Derivative That Targets Both Lymphangiogenesis and Angiogenesis.
AID1779561Inhibition of cell migration in VEGF-C-induced human dermal lymphatic endothelial cells assessed as cell migration at 100 nM incubated for 24 hrs by inverted microscopy based by scratch wound healing assay
AID1779609Antitumor activity against human MDA-MB-231 cells xenografted in BALB/c mouse assessed as reduction in tumor volume at 25 mg/kg, po
AID1540780Anti-lymphangiogenic activity in HDLEC assessed as reduction in growth factor cocktail-induced lymphatic sprouting at 10 uM incubated for 4 days by Hoechst 33342 and phalloidin staining based microfluidic platform assay relative to control2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Identification of a Unique Resorcylic Acid Lactone Derivative That Targets Both Lymphangiogenesis and Angiogenesis.
AID1540789Toxicity in C57BL/6 mouse assessed as induction of clinically detectable corneal-epitheliopathy at 200 nM administered topically every 12 hrs for 7 days by immunohistochemical analysis2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Identification of a Unique Resorcylic Acid Lactone Derivative That Targets Both Lymphangiogenesis and Angiogenesis.
AID1779562Antimigratory activity against VEGF-C-induced human dermal lymphatic endothelial cells assessed as cell migration at 100 nM incubated for 12 hrs by inverted microscopy based by transwell assay
AID1540765Inhibition of human VEGFR3 using poly[Glu:Tyr] (4:1) substrate and [gamma-33P]-ATP by radiometric biochemical kinase assay2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Identification of a Unique Resorcylic Acid Lactone Derivative That Targets Both Lymphangiogenesis and Angiogenesis.
AID1779559Antiproliferative activity against VEGF-D-induced human dermal lymphatic endothelial cells assessed as cell viability incubated for 48 hrs by CCK-8 assay
AID1779620Toxicity in BALB/c mouse xenografted with MDA-MB-231 cells assessed as change in liver at 25 mg/kg, po by hematoxylin and eosin staining based analysis
AID1779558Antiproliferative activity against VEGF-C-induced human dermal lymphatic endothelial cells assessed as cell viability incubated for 48 hrs by CCK-8 assay
AID1779560Anti-lymphangiogenic activity against human dermal lymphatic endothelial cells assessed as inhibition of VEGF-C-mediated tube formation at 100 nM incubated for 12 hrs by inverted microscopy
AID1779543Anticancer activity against human MDA-MB-436 cells assessed as cell viability incubated for 48 hrs by MTT assay
AID1779541Inhibition of VEGFR3 (unknown origin) at 1 uM incubated for 1 hr by ELISA relative to control
AID1779615Toxicity in BALB/c mouse xenografted with MDA-MB-231 cells assessed as change in heart at 300 mg/kg, po by hematoxylin and eosin staining based analysis
AID1540785Anti-angiogenesis activity in HUVEC assessed as inhibition of VEGF-A-induced cell migration at 0.1 uM incubated for 12 hrs by wound healing assay2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Identification of a Unique Resorcylic Acid Lactone Derivative That Targets Both Lymphangiogenesis and Angiogenesis.
AID1779614Toxicity in BALB/c mouse xenografted with MDA-MB-231 cells assessed as uric acid level in blood at 300 mg/kg, po
AID1779557Selectivity ratio of IC50 for human VEGFR1 to IC50 for human VEGFR3
AID1540762Inhibition of TEL-fused VEGFR3 (unknown origin) expressed in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by Cell-titer-Glo assay2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Identification of a Unique Resorcylic Acid Lactone Derivative That Targets Both Lymphangiogenesis and Angiogenesis.
AID1779617Toxicity in BALB/c mouse xenografted with MDA-MB-231 cells assessed as change in spleen at 300 mg/kg, po by hematoxylin and eosin staining based analysis
AID1779618Toxicity in BALB/c mouse xenografted with MDA-MB-231 cells assessed as change in lung at 300 mg/kg, po by hematoxylin and eosin staining based analysis
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (9)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's6 (66.67)24.3611
2020's3 (33.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 21.55

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 Index21.55 (24.57)
Research Supply Index2.30 (2.92)
Research Growth Index4.56 (4.65)
Search Engine Demand Index18.60 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (21.55)

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%
Other9 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]