Page last updated: 2024-10-15

r 1530

Cross-References

ID SourceID
PubMed CID135398512
CHEMBL ID1980391
SCHEMBL ID13751393
SCHEMBL ID3824661
MeSH IDM0553571

Synonyms (40)

Synonym
cid 11610113
KINOME_3737
unii-xqj55r5ppq
pyrazolo(3,4-b)(1,4)benzodiazepine, 5-(2-chlorophenyl)-7-fluoro-1,2-dihydro-8-methoxy-3-methyl-
5-(2-chlorophenyl)-7-fluoro-1,2-dihydro-8-methoxy-3-methylpyrazolo(3,4-b)(1,4)benzodiazepine
xqj55r5ppq ,
rg-1530
CHEMBL1980391 ,
bdbm50426474
r-1530
R1530 ,
HY-13737
CS-1627
882531-87-5
5-(2-chlorophenyl)-1,2-dihydro-7-fluoro-8-methoxy-3-methyl-pyrazolo[3,4-b][1,4]benzodiazepine
UOVCGJXDGOGOCZ-UHFFFAOYSA-N ,
SCHEMBL13751393
SCHEMBL3824661
5-(2-chlorophenyl)-7-fluoro-1,2-dihydro-8-methoxy-3-methylpyrazolo[3,4-b][1,4]benzodiazepine
r-1521
r 1530
AKOS024458398
AKOS030526962
9-(2-chlorophenyl)-12-fluoro-13-methoxy-6-methyl-2,4,5,8-tetraazatricyclo[8.4.0.0?,?]tetradeca-1(14),2,6,8,10,12-hexaene
r1530, >=98% (hplc)
F20797
FT-0768325
EX-A2311
5-(2-chlorophenyl)-7-fluoro-8-methoxy-3-methyl-1,2-dihydrobenzo[e]pyrazolo[4,3-b][1,4]diazepine
mfcd23704870
AS-16578
5-(2-chlorophenyl)-7-fluoro-8-methoxy-3-methyl-1,2-dihydropyrazolo[3,4-b][1,4]benzodiazepine
NCGC00390699-04
Q27293966
5-(2-chlorophenyl)-7-fluoro-8-methoxy-3-methyl-2,10-dihydropyrazolo[3,4-b][1,4]benzodiazepine
compound 2 [pmid: 24900658]
gtpl10361
nsc767953
nsc-767953
AC-36024

Bioavailability

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

Protein Targets (9)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
PPM1D proteinHomo sapiens (human)Potency14.74030.00529.466132.9993AID1347411
Interferon betaHomo sapiens (human)Potency14.74030.00339.158239.8107AID1347411
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Serine/threonine-protein kinase PLK4Homo sapiens (human)IC50 (µMol)0.00700.00270.46253.1000AID1860512
Serine/threonine-protein kinase PLK4Homo sapiens (human)Ki0.01100.00030.95599.3000AID762206
Aurora kinase AHomo sapiens (human)IC50 (µMol)0.05800.00000.46208.6000AID1860511; AID727965
Serine/threonine-protein kinase Chk2Homo sapiens (human)IC50 (µMol)0.02400.00300.34823.5000AID1860510; AID727964
Fibroblast growth factor receptor 1Homo sapiens (human)IC50 (µMol)0.02800.00020.942010.0000AID727967
Cyclin-dependent kinase 4Homo sapiens (human)IC50 (µMol)10.00000.00060.570610.0000AID727966
Cyclin-dependent kinase 2Homo sapiens (human)IC50 (µMol)1.33000.00041.044410.0000AID727968
Vascular endothelial growth factor receptor 2Homo sapiens (human)IC50 (µMol)0.01000.00000.48308.8000AID1860509; AID727969
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (232)

Processvia Protein(s)Taxonomy
positive regulation of centriole replicationSerine/threonine-protein kinase PLK4Homo sapiens (human)
protein phosphorylationSerine/threonine-protein kinase PLK4Homo sapiens (human)
centriole replicationSerine/threonine-protein kinase PLK4Homo sapiens (human)
positive regulation of centriole replicationSerine/threonine-protein kinase PLK4Homo sapiens (human)
cilium assemblySerine/threonine-protein kinase PLK4Homo sapiens (human)
trophoblast giant cell differentiationSerine/threonine-protein kinase PLK4Homo sapiens (human)
de novo centriole assembly involved in multi-ciliated epithelial cell differentiationSerine/threonine-protein kinase PLK4Homo sapiens (human)
protein phosphorylationAurora kinase AHomo sapiens (human)
response to woundingAurora kinase AHomo sapiens (human)
liver regenerationAurora kinase AHomo sapiens (human)
G2/M transition of mitotic cell cycleAurora kinase AHomo sapiens (human)
mitotic cell cycleAurora kinase AHomo sapiens (human)
chromatin remodelingAurora kinase AHomo sapiens (human)
protein phosphorylationAurora kinase AHomo sapiens (human)
apoptotic processAurora kinase AHomo sapiens (human)
spindle organizationAurora kinase AHomo sapiens (human)
spindle assembly involved in female meiosis IAurora kinase AHomo sapiens (human)
mitotic centrosome separationAurora kinase AHomo sapiens (human)
anterior/posterior axis specificationAurora kinase AHomo sapiens (human)
regulation of G2/M transition of mitotic cell cycleAurora kinase AHomo sapiens (human)
negative regulation of gene expressionAurora kinase AHomo sapiens (human)
peptidyl-serine phosphorylationAurora kinase AHomo sapiens (human)
regulation of protein stabilityAurora kinase AHomo sapiens (human)
negative regulation of protein bindingAurora kinase AHomo sapiens (human)
positive regulation of proteasomal ubiquitin-dependent protein catabolic processAurora kinase AHomo sapiens (human)
negative regulation of apoptotic processAurora kinase AHomo sapiens (human)
proteasome-mediated ubiquitin-dependent protein catabolic processAurora kinase AHomo sapiens (human)
positive regulation of mitotic nuclear divisionAurora kinase AHomo sapiens (human)
positive regulation of mitotic cell cycleAurora kinase AHomo sapiens (human)
regulation of centrosome cycleAurora kinase AHomo sapiens (human)
protein autophosphorylationAurora kinase AHomo sapiens (human)
cell divisionAurora kinase AHomo sapiens (human)
centrosome localizationAurora kinase AHomo sapiens (human)
cilium disassemblyAurora kinase AHomo sapiens (human)
protein localization to centrosomeAurora kinase AHomo sapiens (human)
positive regulation of mitochondrial fissionAurora kinase AHomo sapiens (human)
positive regulation of oocyte maturationAurora kinase AHomo sapiens (human)
regulation of signal transduction by p53 class mediatorAurora kinase AHomo sapiens (human)
neuron projection extensionAurora kinase AHomo sapiens (human)
mitotic spindle organizationAurora kinase AHomo sapiens (human)
regulation of cytokinesisAurora kinase AHomo sapiens (human)
DNA damage responseSerine/threonine-protein kinase Chk2Homo sapiens (human)
signal transduction in response to DNA damageSerine/threonine-protein kinase Chk2Homo sapiens (human)
DNA damage checkpoint signalingSerine/threonine-protein kinase Chk2Homo sapiens (human)
G2/M transition of mitotic cell cycleSerine/threonine-protein kinase Chk2Homo sapiens (human)
double-strand break repairSerine/threonine-protein kinase Chk2Homo sapiens (human)
regulation of DNA-templated transcriptionSerine/threonine-protein kinase Chk2Homo sapiens (human)
protein phosphorylationSerine/threonine-protein kinase Chk2Homo sapiens (human)
DNA damage responseSerine/threonine-protein kinase Chk2Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestSerine/threonine-protein kinase Chk2Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorSerine/threonine-protein kinase Chk2Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damageSerine/threonine-protein kinase Chk2Homo sapiens (human)
protein catabolic processSerine/threonine-protein kinase Chk2Homo sapiens (human)
mitotic intra-S DNA damage checkpoint signalingSerine/threonine-protein kinase Chk2Homo sapiens (human)
regulation of protein catabolic processSerine/threonine-protein kinase Chk2Homo sapiens (human)
signal transduction in response to DNA damageSerine/threonine-protein kinase Chk2Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorSerine/threonine-protein kinase Chk2Homo sapiens (human)
positive regulation of DNA-templated transcriptionSerine/threonine-protein kinase Chk2Homo sapiens (human)
protein autophosphorylationSerine/threonine-protein kinase Chk2Homo sapiens (human)
protein stabilizationSerine/threonine-protein kinase Chk2Homo sapiens (human)
cell divisionSerine/threonine-protein kinase Chk2Homo sapiens (human)
thymocyte apoptotic processSerine/threonine-protein kinase Chk2Homo sapiens (human)
cellular response to gamma radiationSerine/threonine-protein kinase Chk2Homo sapiens (human)
mitotic spindle assemblySerine/threonine-protein kinase Chk2Homo sapiens (human)
replicative senescenceSerine/threonine-protein kinase Chk2Homo sapiens (human)
regulation of signal transduction by p53 class mediatorSerine/threonine-protein kinase Chk2Homo sapiens (human)
regulation of autophagosome assemblySerine/threonine-protein kinase Chk2Homo sapiens (human)
mitotic DNA damage checkpoint signalingSerine/threonine-protein kinase Chk2Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of cell population proliferationFibroblast growth factor receptor 1Homo sapiens (human)
fibroblast growth factor receptor signaling pathwayFibroblast growth factor receptor 1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIFibroblast growth factor receptor 1Homo sapiens (human)
MAPK cascadeFibroblast growth factor receptor 1Homo sapiens (human)
skeletal system developmentFibroblast growth factor receptor 1Homo sapiens (human)
angiogenesisFibroblast growth factor receptor 1Homo sapiens (human)
ureteric bud developmentFibroblast growth factor receptor 1Homo sapiens (human)
in utero embryonic developmentFibroblast growth factor receptor 1Homo sapiens (human)
organ inductionFibroblast growth factor receptor 1Homo sapiens (human)
neuron migrationFibroblast growth factor receptor 1Homo sapiens (human)
epithelial to mesenchymal transitionFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of mesenchymal cell proliferationFibroblast growth factor receptor 1Homo sapiens (human)
chondrocyte differentiationFibroblast growth factor receptor 1Homo sapiens (human)
protein phosphorylationFibroblast growth factor receptor 1Homo sapiens (human)
sensory perception of soundFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of cell population proliferationFibroblast growth factor receptor 1Homo sapiens (human)
fibroblast growth factor receptor signaling pathwayFibroblast growth factor receptor 1Homo sapiens (human)
mesenchymal cell proliferationFibroblast growth factor receptor 1Homo sapiens (human)
gene expressionFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of phospholipase activityFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of phospholipase C activityFibroblast growth factor receptor 1Homo sapiens (human)
regulation of phosphate transportFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of neuron projection developmentFibroblast growth factor receptor 1Homo sapiens (human)
cell migrationFibroblast growth factor receptor 1Homo sapiens (human)
peptidyl-tyrosine phosphorylationFibroblast growth factor receptor 1Homo sapiens (human)
ventricular zone neuroblast divisionFibroblast growth factor receptor 1Homo sapiens (human)
cell projection assemblyFibroblast growth factor receptor 1Homo sapiens (human)
embryonic limb morphogenesisFibroblast growth factor receptor 1Homo sapiens (human)
midbrain developmentFibroblast growth factor receptor 1Homo sapiens (human)
neuron projection developmentFibroblast growth factor receptor 1Homo sapiens (human)
fibroblast growth factor receptor signaling pathway involved in orbitofrontal cortex developmentFibroblast growth factor receptor 1Homo sapiens (human)
inner ear morphogenesisFibroblast growth factor receptor 1Homo sapiens (human)
outer ear morphogenesisFibroblast growth factor receptor 1Homo sapiens (human)
middle ear morphogenesisFibroblast growth factor receptor 1Homo sapiens (human)
chordate embryonic developmentFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of MAP kinase activityFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of MAPK cascadeFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of blood vessel endothelial cell migrationFibroblast growth factor receptor 1Homo sapiens (human)
cellular response to fibroblast growth factor stimulusFibroblast growth factor receptor 1Homo sapiens (human)
regulation of cell differentiationFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of neuron differentiationFibroblast growth factor receptor 1Homo sapiens (human)
protein autophosphorylationFibroblast growth factor receptor 1Homo sapiens (human)
phosphatidylinositol-mediated signalingFibroblast growth factor receptor 1Homo sapiens (human)
paraxial mesoderm developmentFibroblast growth factor receptor 1Homo sapiens (human)
regulation of lateral mesodermal cell fate specificationFibroblast growth factor receptor 1Homo sapiens (human)
cell maturationFibroblast growth factor receptor 1Homo sapiens (human)
skeletal system morphogenesisFibroblast growth factor receptor 1Homo sapiens (human)
stem cell differentiationFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionFibroblast growth factor receptor 1Homo sapiens (human)
calcium ion homeostasisFibroblast growth factor receptor 1Homo sapiens (human)
cardiac muscle cell proliferationFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of cardiac muscle cell proliferationFibroblast growth factor receptor 1Homo sapiens (human)
auditory receptor cell developmentFibroblast growth factor receptor 1Homo sapiens (human)
branching involved in salivary gland morphogenesisFibroblast growth factor receptor 1Homo sapiens (human)
lung-associated mesenchyme developmentFibroblast growth factor receptor 1Homo sapiens (human)
regulation of branching involved in salivary gland morphogenesis by mesenchymal-epithelial signalingFibroblast growth factor receptor 1Homo sapiens (human)
vitamin D3 metabolic processFibroblast growth factor receptor 1Homo sapiens (human)
diphosphate metabolic processFibroblast growth factor receptor 1Homo sapiens (human)
cementum mineralizationFibroblast growth factor receptor 1Homo sapiens (human)
stem cell proliferationFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of MAPKKK cascade by fibroblast growth factor receptor signaling pathwayFibroblast growth factor receptor 1Homo sapiens (human)
negative regulation of fibroblast growth factor productionFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of mitotic cell cycle DNA replicationFibroblast growth factor receptor 1Homo sapiens (human)
response to sodium phosphateFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of vascular endothelial cell proliferationFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of stem cell proliferationFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of parathyroid hormone secretionFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of endothelial cell chemotaxisFibroblast growth factor receptor 1Homo sapiens (human)
regulation of extrinsic apoptotic signaling pathway in absence of ligandFibroblast growth factor receptor 1Homo sapiens (human)
multicellular organism developmentFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of cell differentiationFibroblast growth factor receptor 1Homo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayFibroblast growth factor receptor 1Homo sapiens (human)
positive regulation of kinase activityFibroblast growth factor receptor 1Homo sapiens (human)
G1/S transition of mitotic cell cycleCyclin-dependent kinase 4Homo sapiens (human)
protein phosphorylationCyclin-dependent kinase 4Homo sapiens (human)
positive regulation of cell population proliferationCyclin-dependent kinase 4Homo sapiens (human)
response to xenobiotic stimulusCyclin-dependent kinase 4Homo sapiens (human)
regulation of gene expressionCyclin-dependent kinase 4Homo sapiens (human)
positive regulation of G2/M transition of mitotic cell cycleCyclin-dependent kinase 4Homo sapiens (human)
positive regulation of fibroblast proliferationCyclin-dependent kinase 4Homo sapiens (human)
cell divisionCyclin-dependent kinase 4Homo sapiens (human)
regulation of cell cycleCyclin-dependent kinase 4Homo sapiens (human)
regulation of transcription initiation by RNA polymerase IICyclin-dependent kinase 4Homo sapiens (human)
regulation of type B pancreatic cell proliferationCyclin-dependent kinase 4Homo sapiens (human)
cellular response to lipopolysaccharideCyclin-dependent kinase 4Homo sapiens (human)
cellular response to interleukin-4Cyclin-dependent kinase 4Homo sapiens (human)
cellular response to phorbol 13-acetate 12-myristateCyclin-dependent kinase 4Homo sapiens (human)
cellular response to ionomycinCyclin-dependent kinase 4Homo sapiens (human)
response to organic substanceCyclin-dependent kinase 4Homo sapiens (human)
regulation of G2/M transition of mitotic cell cycleCyclin-dependent kinase 4Homo sapiens (human)
signal transductionCyclin-dependent kinase 4Homo sapiens (human)
G1/S transition of mitotic cell cycleCyclin-dependent kinase 2Homo sapiens (human)
G2/M transition of mitotic cell cycleCyclin-dependent kinase 2Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICyclin-dependent kinase 2Homo sapiens (human)
DNA replicationCyclin-dependent kinase 2Homo sapiens (human)
DNA repairCyclin-dependent kinase 2Homo sapiens (human)
chromatin remodelingCyclin-dependent kinase 2Homo sapiens (human)
DNA-templated transcriptionCyclin-dependent kinase 2Homo sapiens (human)
protein phosphorylationCyclin-dependent kinase 2Homo sapiens (human)
potassium ion transportCyclin-dependent kinase 2Homo sapiens (human)
centriole replicationCyclin-dependent kinase 2Homo sapiens (human)
Ras protein signal transductionCyclin-dependent kinase 2Homo sapiens (human)
regulation of mitotic cell cycleCyclin-dependent kinase 2Homo sapiens (human)
positive regulation of cell population proliferationCyclin-dependent kinase 2Homo sapiens (human)
peptidyl-serine phosphorylationCyclin-dependent kinase 2Homo sapiens (human)
positive regulation of heterochromatin formationCyclin-dependent kinase 2Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCyclin-dependent kinase 2Homo sapiens (human)
positive regulation of DNA-templated DNA replication initiationCyclin-dependent kinase 2Homo sapiens (human)
telomere maintenance in response to DNA damageCyclin-dependent kinase 2Homo sapiens (human)
post-translational protein modificationCyclin-dependent kinase 2Homo sapiens (human)
positive regulation of DNA replicationCyclin-dependent kinase 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionCyclin-dependent kinase 2Homo sapiens (human)
centrosome duplicationCyclin-dependent kinase 2Homo sapiens (human)
cell divisionCyclin-dependent kinase 2Homo sapiens (human)
meiotic cell cycleCyclin-dependent kinase 2Homo sapiens (human)
cellular response to nitric oxideCyclin-dependent kinase 2Homo sapiens (human)
cellular senescenceCyclin-dependent kinase 2Homo sapiens (human)
regulation of anaphase-promoting complex-dependent catabolic processCyclin-dependent kinase 2Homo sapiens (human)
regulation of G2/M transition of mitotic cell cycleCyclin-dependent kinase 2Homo sapiens (human)
signal transductionCyclin-dependent kinase 2Homo sapiens (human)
regulation of gene expressionCyclin-dependent kinase 2Homo sapiens (human)
response to organic substanceCyclin-dependent kinase 2Homo sapiens (human)
branching involved in blood vessel morphogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of macroautophagyVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of mitochondrial depolarizationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of mitochondrial fissionVascular endothelial growth factor receptor 2Homo sapiens (human)
angiogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
ovarian follicle developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
vasculogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of protein phosphorylationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of endothelial cell proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
lymph vessel developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
cell migration involved in sprouting angiogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of mesenchymal cell proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
epithelial cell maturationVascular endothelial growth factor receptor 2Homo sapiens (human)
endocardium developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
endothelium developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of cell population proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
regulation of cell shapeVascular endothelial growth factor receptor 2Homo sapiens (human)
mesenchymal cell proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of endothelial cell migrationVascular endothelial growth factor receptor 2Homo sapiens (human)
negative regulation of gene expressionVascular endothelial growth factor receptor 2Homo sapiens (human)
peptidyl-tyrosine phosphorylationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of cell migrationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of BMP signaling pathwayVascular endothelial growth factor receptor 2Homo sapiens (human)
embryonic hemopoiesisVascular endothelial growth factor receptor 2Homo sapiens (human)
cellular response to vascular endothelial growth factor stimulusVascular endothelial growth factor receptor 2Homo sapiens (human)
vascular endothelial growth factor receptor-2 signaling pathwayVascular endothelial growth factor receptor 2Homo sapiens (human)
peptidyl-tyrosine autophosphorylationVascular endothelial growth factor receptor 2Homo sapiens (human)
vascular endothelial growth factor signaling pathwayVascular endothelial growth factor receptor 2Homo sapiens (human)
surfactant homeostasisVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of MAPK cascadeVascular endothelial growth factor receptor 2Homo sapiens (human)
negative regulation of neuron apoptotic processVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of blood vessel endothelial cell migrationVascular endothelial growth factor receptor 2Homo sapiens (human)
cell fate commitmentVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of angiogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
protein autophosphorylationVascular endothelial growth factor receptor 2Homo sapiens (human)
vascular endothelial growth factor receptor signaling pathwayVascular endothelial growth factor receptor 2Homo sapiens (human)
lung alveolus developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
post-embryonic camera-type eye morphogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
epithelial cell proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of positive chemotaxisVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of nitric-oxide synthase biosynthetic processVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of focal adhesion assemblyVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionVascular endothelial growth factor receptor 2Homo sapiens (human)
calcium ion homeostasisVascular endothelial growth factor receptor 2Homo sapiens (human)
blood vessel endothelial cell differentiationVascular endothelial growth factor receptor 2Homo sapiens (human)
vascular wound healingVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeVascular endothelial growth factor receptor 2Homo sapiens (human)
semaphorin-plexin signaling pathwayVascular endothelial growth factor receptor 2Homo sapiens (human)
stem cell proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
regulation of hematopoietic progenitor cell differentiationVascular endothelial growth factor receptor 2Homo sapiens (human)
regulation of bone developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
cellular response to hydrogen sulfideVascular endothelial growth factor receptor 2Homo sapiens (human)
negative regulation of endothelial cell apoptotic processVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of stem cell proliferationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of endothelial cell chemotaxisVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of vasculogenesisVascular endothelial growth factor receptor 2Homo sapiens (human)
regulation of MAPK cascadeVascular endothelial growth factor receptor 2Homo sapiens (human)
multicellular organism developmentVascular endothelial growth factor receptor 2Homo sapiens (human)
cell migrationVascular endothelial growth factor receptor 2Homo sapiens (human)
endothelial cell differentiationVascular endothelial growth factor receptor 2Homo sapiens (human)
positive regulation of kinase activityVascular endothelial growth factor receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (39)

Processvia Protein(s)Taxonomy
protein serine/threonine kinase activitySerine/threonine-protein kinase PLK4Homo sapiens (human)
protein bindingSerine/threonine-protein kinase PLK4Homo sapiens (human)
ATP bindingSerine/threonine-protein kinase PLK4Homo sapiens (human)
identical protein bindingSerine/threonine-protein kinase PLK4Homo sapiens (human)
protein serine kinase activitySerine/threonine-protein kinase PLK4Homo sapiens (human)
protein kinase activityAurora kinase AHomo sapiens (human)
protein serine/threonine kinase activityAurora kinase AHomo sapiens (human)
protein serine/threonine/tyrosine kinase activityAurora kinase AHomo sapiens (human)
protein bindingAurora kinase AHomo sapiens (human)
ATP bindingAurora kinase AHomo sapiens (human)
protein kinase bindingAurora kinase AHomo sapiens (human)
ubiquitin protein ligase bindingAurora kinase AHomo sapiens (human)
histone H3S10 kinase activityAurora kinase AHomo sapiens (human)
protein heterodimerization activityAurora kinase AHomo sapiens (human)
protein serine kinase activityAurora kinase AHomo sapiens (human)
molecular function activator activityAurora kinase AHomo sapiens (human)
protein serine/threonine kinase activitySerine/threonine-protein kinase Chk2Homo sapiens (human)
protein bindingSerine/threonine-protein kinase Chk2Homo sapiens (human)
ATP bindingSerine/threonine-protein kinase Chk2Homo sapiens (human)
protein kinase bindingSerine/threonine-protein kinase Chk2Homo sapiens (human)
ubiquitin protein ligase bindingSerine/threonine-protein kinase Chk2Homo sapiens (human)
identical protein bindingSerine/threonine-protein kinase Chk2Homo sapiens (human)
protein homodimerization activitySerine/threonine-protein kinase Chk2Homo sapiens (human)
metal ion bindingSerine/threonine-protein kinase Chk2Homo sapiens (human)
protein serine kinase activitySerine/threonine-protein kinase Chk2Homo sapiens (human)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
protein tyrosine kinase activityFibroblast growth factor receptor 1Homo sapiens (human)
fibroblast growth factor receptor activityFibroblast growth factor receptor 1Homo sapiens (human)
protein bindingFibroblast growth factor receptor 1Homo sapiens (human)
ATP bindingFibroblast growth factor receptor 1Homo sapiens (human)
heparin bindingFibroblast growth factor receptor 1Homo sapiens (human)
fibroblast growth factor bindingFibroblast growth factor receptor 1Homo sapiens (human)
SH2 domain bindingFibroblast growth factor receptor 1Homo sapiens (human)
identical protein bindingFibroblast growth factor receptor 1Homo sapiens (human)
protein homodimerization activityFibroblast growth factor receptor 1Homo sapiens (human)
receptor-receptor interactionFibroblast growth factor receptor 1Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase activityCyclin-dependent kinase 4Homo sapiens (human)
protein bindingCyclin-dependent kinase 4Homo sapiens (human)
ATP bindingCyclin-dependent kinase 4Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase regulator activityCyclin-dependent kinase 4Homo sapiens (human)
cyclin bindingCyclin-dependent kinase 4Homo sapiens (human)
protein serine kinase activityCyclin-dependent kinase 4Homo sapiens (human)
histone kinase activityCyclin-dependent kinase 2Homo sapiens (human)
magnesium ion bindingCyclin-dependent kinase 2Homo sapiens (human)
protein serine/threonine kinase activityCyclin-dependent kinase 2Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase activityCyclin-dependent kinase 2Homo sapiens (human)
protein bindingCyclin-dependent kinase 2Homo sapiens (human)
ATP bindingCyclin-dependent kinase 2Homo sapiens (human)
protein domain specific bindingCyclin-dependent kinase 2Homo sapiens (human)
cyclin bindingCyclin-dependent kinase 2Homo sapiens (human)
cyclin-dependent protein kinase activityCyclin-dependent kinase 2Homo sapiens (human)
protein serine kinase activityCyclin-dependent kinase 2Homo sapiens (human)
protein tyrosine kinase activityVascular endothelial growth factor receptor 2Homo sapiens (human)
transmembrane receptor protein tyrosine kinase activityVascular endothelial growth factor receptor 2Homo sapiens (human)
vascular endothelial growth factor receptor activityVascular endothelial growth factor receptor 2Homo sapiens (human)
integrin bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
protein bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
ATP bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
coreceptor activityVascular endothelial growth factor receptor 2Homo sapiens (human)
growth factor bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
vascular endothelial growth factor bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
identical protein bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
cadherin bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
Hsp90 protein bindingVascular endothelial growth factor receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (66)

Processvia Protein(s)Taxonomy
XY bodySerine/threonine-protein kinase PLK4Homo sapiens (human)
nucleolusSerine/threonine-protein kinase PLK4Homo sapiens (human)
centrosomeSerine/threonine-protein kinase PLK4Homo sapiens (human)
centrioleSerine/threonine-protein kinase PLK4Homo sapiens (human)
cytosolSerine/threonine-protein kinase PLK4Homo sapiens (human)
cleavage furrowSerine/threonine-protein kinase PLK4Homo sapiens (human)
deuterosomeSerine/threonine-protein kinase PLK4Homo sapiens (human)
procentrioleSerine/threonine-protein kinase PLK4Homo sapiens (human)
procentriole replication complexSerine/threonine-protein kinase PLK4Homo sapiens (human)
nucleusSerine/threonine-protein kinase PLK4Homo sapiens (human)
spindle microtubuleAurora kinase AHomo sapiens (human)
nucleusAurora kinase AHomo sapiens (human)
nucleoplasmAurora kinase AHomo sapiens (human)
centrosomeAurora kinase AHomo sapiens (human)
centrioleAurora kinase AHomo sapiens (human)
spindleAurora kinase AHomo sapiens (human)
cytosolAurora kinase AHomo sapiens (human)
postsynaptic densityAurora kinase AHomo sapiens (human)
microtubule cytoskeletonAurora kinase AHomo sapiens (human)
basolateral plasma membraneAurora kinase AHomo sapiens (human)
midbodyAurora kinase AHomo sapiens (human)
spindle pole centrosomeAurora kinase AHomo sapiens (human)
ciliary basal bodyAurora kinase AHomo sapiens (human)
germinal vesicleAurora kinase AHomo sapiens (human)
axon hillockAurora kinase AHomo sapiens (human)
pronucleusAurora kinase AHomo sapiens (human)
perinuclear region of cytoplasmAurora kinase AHomo sapiens (human)
mitotic spindleAurora kinase AHomo sapiens (human)
meiotic spindleAurora kinase AHomo sapiens (human)
mitotic spindle poleAurora kinase AHomo sapiens (human)
glutamatergic synapseAurora kinase AHomo sapiens (human)
spindle pole centrosomeAurora kinase AHomo sapiens (human)
chromosome passenger complexAurora kinase AHomo sapiens (human)
spindle midzoneAurora kinase AHomo sapiens (human)
kinetochoreAurora kinase AHomo sapiens (human)
chromosome, telomeric regionSerine/threonine-protein kinase Chk2Homo sapiens (human)
nucleoplasmSerine/threonine-protein kinase Chk2Homo sapiens (human)
Golgi apparatusSerine/threonine-protein kinase Chk2Homo sapiens (human)
PML bodySerine/threonine-protein kinase Chk2Homo sapiens (human)
cytoplasmSerine/threonine-protein kinase Chk2Homo sapiens (human)
nucleusSerine/threonine-protein kinase Chk2Homo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
extracellular regionFibroblast growth factor receptor 1Homo sapiens (human)
nucleusFibroblast growth factor receptor 1Homo sapiens (human)
cytosolFibroblast growth factor receptor 1Homo sapiens (human)
plasma membraneFibroblast growth factor receptor 1Homo sapiens (human)
membraneFibroblast growth factor receptor 1Homo sapiens (human)
cytoplasmic vesicleFibroblast growth factor receptor 1Homo sapiens (human)
receptor complexFibroblast growth factor receptor 1Homo sapiens (human)
plasma membraneFibroblast growth factor receptor 1Homo sapiens (human)
nucleusCyclin-dependent kinase 4Homo sapiens (human)
nucleoplasmCyclin-dependent kinase 4Homo sapiens (human)
nucleolusCyclin-dependent kinase 4Homo sapiens (human)
cytosolCyclin-dependent kinase 4Homo sapiens (human)
bicellular tight junctionCyclin-dependent kinase 4Homo sapiens (human)
nuclear membraneCyclin-dependent kinase 4Homo sapiens (human)
cyclin D1-CDK4 complexCyclin-dependent kinase 4Homo sapiens (human)
cyclin D2-CDK4 complexCyclin-dependent kinase 4Homo sapiens (human)
cyclin D3-CDK4 complexCyclin-dependent kinase 4Homo sapiens (human)
cyclin-dependent protein kinase holoenzyme complexCyclin-dependent kinase 4Homo sapiens (human)
chromatinCyclin-dependent kinase 4Homo sapiens (human)
transcription regulator complexCyclin-dependent kinase 4Homo sapiens (human)
nucleusCyclin-dependent kinase 4Homo sapiens (human)
cytoplasmCyclin-dependent kinase 4Homo sapiens (human)
chromosome, telomeric regionCyclin-dependent kinase 2Homo sapiens (human)
condensed chromosomeCyclin-dependent kinase 2Homo sapiens (human)
X chromosomeCyclin-dependent kinase 2Homo sapiens (human)
Y chromosomeCyclin-dependent kinase 2Homo sapiens (human)
male germ cell nucleusCyclin-dependent kinase 2Homo sapiens (human)
nucleusCyclin-dependent kinase 2Homo sapiens (human)
nuclear envelopeCyclin-dependent kinase 2Homo sapiens (human)
nucleoplasmCyclin-dependent kinase 2Homo sapiens (human)
cytoplasmCyclin-dependent kinase 2Homo sapiens (human)
endosomeCyclin-dependent kinase 2Homo sapiens (human)
centrosomeCyclin-dependent kinase 2Homo sapiens (human)
cytosolCyclin-dependent kinase 2Homo sapiens (human)
Cajal bodyCyclin-dependent kinase 2Homo sapiens (human)
cyclin A1-CDK2 complexCyclin-dependent kinase 2Homo sapiens (human)
cyclin A2-CDK2 complexCyclin-dependent kinase 2Homo sapiens (human)
cyclin E1-CDK2 complexCyclin-dependent kinase 2Homo sapiens (human)
cyclin E2-CDK2 complexCyclin-dependent kinase 2Homo sapiens (human)
cyclin-dependent protein kinase holoenzyme complexCyclin-dependent kinase 2Homo sapiens (human)
transcription regulator complexCyclin-dependent kinase 2Homo sapiens (human)
cytoplasmCyclin-dependent kinase 2Homo sapiens (human)
nucleusCyclin-dependent kinase 2Homo sapiens (human)
extracellular regionVascular endothelial growth factor receptor 2Homo sapiens (human)
nucleusVascular endothelial growth factor receptor 2Homo sapiens (human)
endosomeVascular endothelial growth factor receptor 2Homo sapiens (human)
early endosomeVascular endothelial growth factor receptor 2Homo sapiens (human)
endoplasmic reticulumVascular endothelial growth factor receptor 2Homo sapiens (human)
Golgi apparatusVascular endothelial growth factor receptor 2Homo sapiens (human)
plasma membraneVascular endothelial growth factor receptor 2Homo sapiens (human)
external side of plasma membraneVascular endothelial growth factor receptor 2Homo sapiens (human)
cell junctionVascular endothelial growth factor receptor 2Homo sapiens (human)
membrane raftVascular endothelial growth factor receptor 2Homo sapiens (human)
anchoring junctionVascular endothelial growth factor receptor 2Homo sapiens (human)
sorting endosomeVascular endothelial growth factor receptor 2Homo sapiens (human)
plasma membraneVascular endothelial growth factor receptor 2Homo sapiens (human)
receptor complexVascular endothelial growth factor receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (59)

Assay IDTitleYearJournalArticle
AID493040Navigating the Kinome2011Nature chemical biology, Apr, Volume: 7, Issue:4
Navigating the kinome.
AID727933Antitumor activity against human MDA-MB-231 cells xenografted in mouse assessed as tumor regression at 25 mg/kg, po qd up to 32 days2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727950Total clearance in monkey at 1 mg/kg, iv2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727930Antitumor activity against human A549 cells xenografted in mouse assessed as tumor growth inhibition at 1.56 mg/kg, po qd up to 32 days2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727961Antiproliferative activity against human lung cancer cells by MTT assay2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727948Volume of distribution at steady state in monkey at 1 mg/kg, iv2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID1860512Inhibition of PLK4 (unknown origin)2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis, and biological evaluation of novel pyrazolo [3,4-d]pyrimidine derivatives as potent PLK4 inhibitors for the treatment of TRIM37-amplified breast cancer.
AID727957Antiangiogenic activity in HUVEC assessed as inhibition of PDGF-induced cell proliferation2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727929Toxicity in human MDA-MB-231 cells xenografted mouse assessed as changes in body weight and gross observation at 25 to 50 mg/kg, po qd up to 32 days2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727940Oral bioavailability in rat at 50 mg/kg2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727926Toxicity in human A549 cells xenografted mouse assessed as changes in body weight and gross observation at 25 to 50 mg/kg, po qd up to 32 days2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727939Tmax in monkey at 10 mg/kg, po2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727934Antitumor activity against human MDA-MB-231 cells xenografted in mouse assessed as tumor regression at 50 mg/kg, po qd up to 32 days2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727955Terminal half life in mouse at 5 mg/kg, iv2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727943Tmax in rat at 50 mg/kg, po2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID1860509Inhibition of VEGFR2 (unknown origin)2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis, and biological evaluation of novel pyrazolo [3,4-d]pyrimidine derivatives as potent PLK4 inhibitors for the treatment of TRIM37-amplified breast cancer.
AID727931Antitumor activity against human HCT116 cells xenografted in mouse assessed as tumor growth inhibition at 1.56 mg/kg, po qd up to 32 days2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID1860511Inhibition of Aurora A (unknown origin)2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis, and biological evaluation of novel pyrazolo [3,4-d]pyrimidine derivatives as potent PLK4 inhibitors for the treatment of TRIM37-amplified breast cancer.
AID727927Toxicity in human HCT116 cells xenografted mouse assessed as changes in body weight and gross observation at 25 to 50 mg/kg, po qd up to 32 days2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727947Tmax in mouse at 25 mg/kg, po2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727941Cmax in rat at 50 mg/kg, po2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727954Volume of distribution at steady state in mouse at 5 mg/kg, iv2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727928Toxicity in human LoVo cells xenografted mouse assessed as changes in body weight and gross observation at 25 to 50 mg/kg, po qd up to 32 days2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727958Antiproliferative activity against human melanoma cells by MTT assay2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727935Antitumor activity against human MDA-MB-231 cells xenografted in mouse assessed as tumor growth inhibition at 50 mg/kg, po qd up to 32 days2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727952Terminal half life in rat at 5 mg/kg, iv2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID1860510Inhibition of CHK2 (unknown origin)2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis, and biological evaluation of novel pyrazolo [3,4-d]pyrimidine derivatives as potent PLK4 inhibitors for the treatment of TRIM37-amplified breast cancer.
AID727959Antiproliferative activity against human oral epidermoid cancer cells by MTT assay2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727932Antitumor activity against human LoVo cells xenografted in mouse assessed as tumor growth inhibition at 25 to 50 mg/kg, po qd up to 32 days2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727967Inhibition of FGFR1 (unknown origin)2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727963Antiproliferative activity against human colon cancer cells by MTT assay2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727922Antitumor activity against human A549 cells xenografted in mouse assessed as increase in mouse survival at 25 to 50 mg/kg, po qd up to 32 days2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727937Cmax in monkey at 10 mg/kg, po2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727945AUC (0 to 24 hrs) in mouse at 25 mg/kg, po2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727965Inhibition of aurora-A (unknown origin)2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727946Cmax in mouse at 25 mg/kg, po2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727964Inhibition of CHK2 (unknown origin)2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727960Antiproliferative activity against human prostate cancer cells by MTT assay2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727936Oral bioavailability in monkey at 10 mg/kg2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727968Inhibition of CDK2 (unknown origin)2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727970Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced cell proliferation2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727923Antitumor activity against human HCT116 cells xenografted in mouse assessed as increase in mouse survival at 25 to 50 mg/kg, po qd up to 32 days2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727944Oral bioavailability in mouse at 25 mg/kg2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727938AUC (0 to 24 hrs) in monkey at 10 mg/kg, po2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727971Antiangiogenic activity in HUVEC assessed as inhibition of bFGF-induced cell proliferation2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727951Volume of distribution at steady state in rat at 5 mg/kg, iv2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727924Antitumor activity against human LoVo cells xenografted in mouse assessed as increase in mouse survival at 25 to 50 mg/kg, po qd up to 32 days2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727925Antitumor activity against human MDA-MB-231 cells xenografted in mouse assessed as increase in mouse survival at 25 to 50 mg/kg, po qd up to 32 days2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727956Total clearance in mouse at 5 mg/kg, iv2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727962Antiproliferative activity against human breast cancer cells by MTT assay2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727942AUC (0 to 24 hrs) in rat at 50 mg/kg, po2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727949Terminal half life in monkey at 1 mg/kg, iv2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727969Inhibition of KDR (unknown origin)2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID727966Inhibition of CDK4 (unknown origin)2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID762206Inhibition of human PLK42013Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15
The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents.
AID727953Total clearance in rat at 5 mg/kg, iv2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's4 (66.67)24.3611
2020's2 (33.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

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%
Other6 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]