Compounds > hh-gv678
Page last updated: 2024-11-13

hh-gv678

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Description

flumatinib: an antineoplastic agent and tyrosine kinase inhibitor [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID46848036
CHEMBL ID3545413
SCHEMBL ID4883843
MeSH IDM0551557

Synonyms (42)

Synonym
895519-90-1
flumatinib
4-(4-methylpiperazin-1-ylmethyl)-n-(6-methyl-5-(4-pyridin-3-ylpyrimidin-2-ylamino)pyridin-3-yl)-3-trifluoromethylbenzamide
hh-gv-678
hh-gv678
hhgv678
r4009y24ai ,
unii-r4009y24ai
flumatinib [who-dd]
4-(4-methyl-piperazin-1-ylmethyl)-n-(6-methyl-5-(4-pyridin-3-yl-pyrimidin-2-ylamino)-pyridin-3-yl)-3-trifluoromethyl-benzamide
flumbatinib [inn]
flumbatinib
benzamide, 4-((4-methyl-1-piperazinyl)methyl)-n-(6-methyl-5-((4-(3-pyridinyl)-2-pyrimidinyl)amino)-3-pyridinyl)-3-(trifluoromethyl)-
SCHEMBL4883843
hhgv-678
CHEMBL3545413
HY-13904
CS-5550
DTXSID60237779
AKOS030526971
NCGC00378614-01
DB11904
4-[(4-methylpiperazin-1-yl)methyl]-n-[6-methyl-5-[(4-pyridin-3-ylpyrimidin-2-yl)amino]pyridin-3-yl]-3-(trifluoromethyl)benzamide
gtpl9913
flumatinib (pseudo inn)
hansoh xinfu
EX-A3572
BCP23797
n-(6-methyl-5-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)pyridin-3-yl)-4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)benzamide
895519-90-1 (free base)
flumatinib free base
FT-0739882
SB17192
Q27287759
nsc-830368
nsc830368
F85380
MS-30208
VKB51990
bdbm50529313
benzamide, 4-[(4-methyl-1-piperazinyl)methyl]-n-[6-methyl-5-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-3-pyridinyl]-3-(trifluoromethyl)-
bjcjyeyyygbrof-uhfffaoysa-n

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" One subject withdrew due to a treatment-emergent adverse event."( Effect of high-fat diet on the pharmacokinetics and safety of flumatinib in healthy Chinese subjects.
Guo, C; He, QN; Huang, J; Kuang, Y; Pei, Q; Song, HL; Wu, ST; Yang, GP; Yang, S; Yang, XY; Ye, L, 2020)		0.56
"Among the subjects, oral administration of 400 mg of flumatinib was safe and well tolerated."( Effect of high-fat diet on the pharmacokinetics and safety of flumatinib in healthy Chinese subjects.
Guo, C; He, QN; Huang, J; Kuang, Y; Pei, Q; Song, HL; Wu, ST; Yang, GP; Yang, S; Yang, XY; Ye, L, 2020)		0.56

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)		0.51

Dosage Studied

ExcerptRelevanceReference
" The validated method was successfully applied to clinical pharmacokinetic studies of flumatinib mesylate in CML patients following oral administration at all dosage regimens."( Simultaneous determination of flumatinib and its two major metabolites in plasma of chronic myelogenous leukemia patients by liquid chromatography-tandem mass spectrometry.
Chen, X; Liu, K; Yang, Y; Zhong, D, 2012)		0.38
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (12)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
PPM1D proteinHomo sapiens (human)Potency52.30040.00529.466132.9993AID1347411
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency1.69330.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency4.77240.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency10.68400.00108.379861.1304AID1645840
Interferon betaHomo sapiens (human)Potency40.41840.00339.158239.8107AID1347411; AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency4.77240.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency4.77240.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency4.77240.01238.964839.8107AID1645842
[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)
Tyrosine-protein kinase ABL1Homo sapiens (human)IC50 (µMol)0.05090.00010.712810.0000AID1611401; AID1611402; AID1611403; AID1611405; AID1611406; AID1611407; AID1611408; AID1854088
Platelet-derived growth factor receptor betaHomo sapiens (human)IC50 (µMol)0.30760.00060.80078.5000AID1854089
Mast/stem cell growth factor receptor KitHomo sapiens (human)IC50 (µMol)0.66550.00070.470810.0000AID1854090
Breakpoint cluster region proteinHomo sapiens (human)IC50 (µMol)0.05090.00030.620010.0000AID1611401; AID1611402; AID1611403; AID1611405; AID1611406; AID1611407; AID1611408; AID1854088
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (278)

Processvia Protein(s)Taxonomy
response to oxidative stressTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationTyrosine-protein kinase ABL1Homo sapiens (human)
negative regulation of ubiquitin-protein transferase activityTyrosine-protein kinase ABL1Homo sapiens (human)
negative regulation of phospholipase C activityTyrosine-protein kinase ABL1Homo sapiens (human)
mitotic cell cycleTyrosine-protein kinase ABL1Homo sapiens (human)
neural tube closureTyrosine-protein kinase ABL1Homo sapiens (human)
B-1 B cell homeostasisTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of protein phosphorylationTyrosine-protein kinase ABL1Homo sapiens (human)
B cell proliferation involved in immune responseTyrosine-protein kinase ABL1Homo sapiens (human)
transitional one stage B cell differentiationTyrosine-protein kinase ABL1Homo sapiens (human)
mismatch repairTyrosine-protein kinase ABL1Homo sapiens (human)
regulation of DNA-templated transcriptionTyrosine-protein kinase ABL1Homo sapiens (human)
autophagyTyrosine-protein kinase ABL1Homo sapiens (human)
DNA damage responseTyrosine-protein kinase ABL1Homo sapiens (human)
integrin-mediated signaling pathwayTyrosine-protein kinase ABL1Homo sapiens (human)
canonical NF-kappaB signal transductionTyrosine-protein kinase ABL1Homo sapiens (human)
associative learningTyrosine-protein kinase ABL1Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damageTyrosine-protein kinase ABL1Homo sapiens (human)
response to xenobiotic stimulusTyrosine-protein kinase ABL1Homo sapiens (human)
post-embryonic developmentTyrosine-protein kinase ABL1Homo sapiens (human)
regulation of autophagyTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of endothelial cell migrationTyrosine-protein kinase ABL1Homo sapiens (human)
peptidyl-tyrosine phosphorylationTyrosine-protein kinase ABL1Homo sapiens (human)
cerebellum morphogenesisTyrosine-protein kinase ABL1Homo sapiens (human)
negative regulation of cell-cell adhesionTyrosine-protein kinase ABL1Homo sapiens (human)
microspike assemblyTyrosine-protein kinase ABL1Homo sapiens (human)
actin cytoskeleton organizationTyrosine-protein kinase ABL1Homo sapiens (human)
actin filament polymerizationTyrosine-protein kinase ABL1Homo sapiens (human)
regulation of endocytosisTyrosine-protein kinase ABL1Homo sapiens (human)
regulation of cell adhesionTyrosine-protein kinase ABL1Homo sapiens (human)
neuron differentiationTyrosine-protein kinase ABL1Homo sapiens (human)
BMP signaling pathwayTyrosine-protein kinase ABL1Homo sapiens (human)
negative regulation of BMP signaling pathwayTyrosine-protein kinase ABL1Homo sapiens (human)
regulation of axon extensionTyrosine-protein kinase ABL1Homo sapiens (human)
regulation of microtubule polymerizationTyrosine-protein kinase ABL1Homo sapiens (human)
regulation of Cdc42 protein signal transductionTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of type II interferon productionTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of interleukin-2 productionTyrosine-protein kinase ABL1Homo sapiens (human)
regulation of actin cytoskeleton organizationTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of osteoblast proliferationTyrosine-protein kinase ABL1Homo sapiens (human)
substrate adhesion-dependent cell spreadingTyrosine-protein kinase ABL1Homo sapiens (human)
cellular response to oxidative stressTyrosine-protein kinase ABL1Homo sapiens (human)
response to endoplasmic reticulum stressTyrosine-protein kinase ABL1Homo sapiens (human)
platelet-derived growth factor receptor-beta signaling pathwayTyrosine-protein kinase ABL1Homo sapiens (human)
protein modification processTyrosine-protein kinase ABL1Homo sapiens (human)
peptidyl-tyrosine autophosphorylationTyrosine-protein kinase ABL1Homo sapiens (human)
Fc-gamma receptor signaling pathway involved in phagocytosisTyrosine-protein kinase ABL1Homo sapiens (human)
neuropilin signaling pathwayTyrosine-protein kinase ABL1Homo sapiens (human)
signal transduction in response to DNA damageTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of apoptotic processTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of neuron apoptotic processTyrosine-protein kinase ABL1Homo sapiens (human)
endothelial cell migrationTyrosine-protein kinase ABL1Homo sapiens (human)
regulation of T cell differentiationTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of vasoconstrictionTyrosine-protein kinase ABL1Homo sapiens (human)
negative regulation of mitotic cell cycleTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of mitotic cell cycleTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IITyrosine-protein kinase ABL1Homo sapiens (human)
alpha-beta T cell differentiationTyrosine-protein kinase ABL1Homo sapiens (human)
protein autophosphorylationTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of fibroblast proliferationTyrosine-protein kinase ABL1Homo sapiens (human)
spleen developmentTyrosine-protein kinase ABL1Homo sapiens (human)
thymus developmentTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationTyrosine-protein kinase ABL1Homo sapiens (human)
activated T cell proliferationTyrosine-protein kinase ABL1Homo sapiens (human)
T cell receptor signaling pathwayTyrosine-protein kinase ABL1Homo sapiens (human)
B cell receptor signaling pathwayTyrosine-protein kinase ABL1Homo sapiens (human)
neuromuscular process controlling balanceTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosolTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of oxidoreductase activityTyrosine-protein kinase ABL1Homo sapiens (human)
neuron apoptotic processTyrosine-protein kinase ABL1Homo sapiens (human)
negative regulation of ubiquitin-protein transferase activityTyrosine-protein kinase ABL1Homo sapiens (human)
myoblast proliferationTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of stress fiber assemblyTyrosine-protein kinase ABL1Homo sapiens (human)
establishment of localization in cellTyrosine-protein kinase ABL1Homo sapiens (human)
regulation of cell cycleTyrosine-protein kinase ABL1Homo sapiens (human)
mitochondrial depolarizationTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of focal adhesion assemblyTyrosine-protein kinase ABL1Homo sapiens (human)
Bergmann glial cell differentiationTyrosine-protein kinase ABL1Homo sapiens (human)
cardiac muscle cell proliferationTyrosine-protein kinase ABL1Homo sapiens (human)
neuroepithelial cell differentiationTyrosine-protein kinase ABL1Homo sapiens (human)
cellular response to hydrogen peroxideTyrosine-protein kinase ABL1Homo sapiens (human)
ERK1 and ERK2 cascadeTyrosine-protein kinase ABL1Homo sapiens (human)
negative regulation of ERK1 and ERK2 cascadeTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeTyrosine-protein kinase ABL1Homo sapiens (human)
DNA conformation changeTyrosine-protein kinase ABL1Homo sapiens (human)
cellular response to lipopolysaccharideTyrosine-protein kinase ABL1Homo sapiens (human)
cellular response to transforming growth factor beta stimulusTyrosine-protein kinase ABL1Homo sapiens (human)
response to epinephrineTyrosine-protein kinase ABL1Homo sapiens (human)
negative regulation of protein serine/threonine kinase activityTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesisTyrosine-protein kinase ABL1Homo sapiens (human)
cellular senescenceTyrosine-protein kinase ABL1Homo sapiens (human)
cell-cell adhesionTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of dendrite developmentTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of substrate adhesion-dependent cell spreadingTyrosine-protein kinase ABL1Homo sapiens (human)
negative regulation of long-term synaptic potentiationTyrosine-protein kinase ABL1Homo sapiens (human)
regulation of hematopoietic stem cell differentiationTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of extracellular matrix organizationTyrosine-protein kinase ABL1Homo sapiens (human)
podocyte apoptotic processTyrosine-protein kinase ABL1Homo sapiens (human)
cellular response to dopamineTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of establishment of T cell polarityTyrosine-protein kinase ABL1Homo sapiens (human)
DN4 thymocyte differentiationTyrosine-protein kinase ABL1Homo sapiens (human)
protein localization to cytoplasmic microtubule plus-endTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of microtubule bindingTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of actin filament bindingTyrosine-protein kinase ABL1Homo sapiens (human)
regulation of modification of synaptic structureTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of blood vessel branchingTyrosine-protein kinase ABL1Homo sapiens (human)
activation of protein kinase C activityTyrosine-protein kinase ABL1Homo sapiens (human)
negative regulation of double-strand break repair via homologous recombinationTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of Wnt signaling pathway, planar cell polarity pathwayTyrosine-protein kinase ABL1Homo sapiens (human)
regulation of cell motilityTyrosine-protein kinase ABL1Homo sapiens (human)
negative regulation of endothelial cell apoptotic processTyrosine-protein kinase ABL1Homo sapiens (human)
positive regulation of T cell migrationTyrosine-protein kinase ABL1Homo sapiens (human)
negative regulation of cellular senescenceTyrosine-protein kinase ABL1Homo sapiens (human)
epidermal growth factor receptor signaling pathwayTyrosine-protein kinase ABL1Homo sapiens (human)
protein phosphorylationTyrosine-protein kinase ABL1Homo 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 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)
signal transductionPlatelet-derived growth factor receptor betaHomo sapiens (human)
G protein-coupled receptor signaling pathwayPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of cell population proliferationPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of phospholipase C activityPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of smooth muscle cell migrationPlatelet-derived growth factor receptor betaHomo sapiens (human)
peptidyl-tyrosine phosphorylationPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of cell migrationPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of phosphoprotein phosphatase activityPlatelet-derived growth factor receptor betaHomo sapiens (human)
regulation of actin cytoskeleton organizationPlatelet-derived growth factor receptor betaHomo sapiens (human)
cell migration involved in vasculogenesisPlatelet-derived growth factor receptor betaHomo sapiens (human)
platelet-derived growth factor receptor-beta signaling pathwayPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of metanephric mesenchymal cell migration by platelet-derived growth factor receptor-beta signaling pathwayPlatelet-derived growth factor receptor betaHomo sapiens (human)
aorta morphogenesisPlatelet-derived growth factor receptor betaHomo sapiens (human)
cellular response to platelet-derived growth factor stimulusPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of cell proliferation by VEGF-activated platelet derived growth factor receptor signaling pathwayPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of MAP kinase activityPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of mitotic nuclear divisionPlatelet-derived growth factor receptor betaHomo sapiens (human)
phosphatidylinositol metabolic processPlatelet-derived growth factor receptor betaHomo sapiens (human)
protein autophosphorylationPlatelet-derived growth factor receptor betaHomo sapiens (human)
platelet-derived growth factor receptor signaling pathwayPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of smooth muscle cell proliferationPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of calcium-mediated signalingPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of chemotaxisPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionPlatelet-derived growth factor receptor betaHomo sapiens (human)
cardiac myofibril assemblyPlatelet-derived growth factor receptor betaHomo sapiens (human)
cell chemotaxisPlatelet-derived growth factor receptor betaHomo sapiens (human)
cell migration involved in coronary angiogenesisPlatelet-derived growth factor receptor betaHomo sapiens (human)
retina vasculature development in camera-type eyePlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadePlatelet-derived growth factor receptor betaHomo sapiens (human)
smooth muscle cell chemotaxisPlatelet-derived growth factor receptor betaHomo sapiens (human)
metanephric glomerular mesangial cell proliferation involved in metanephros developmentPlatelet-derived growth factor receptor betaHomo sapiens (human)
metanephric glomerular capillary formationPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of calcium ion importPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of reactive oxygen species metabolic processPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of DNA biosynthetic processPlatelet-derived growth factor receptor betaHomo sapiens (human)
positive regulation of kinase activityPlatelet-derived growth factor receptor betaHomo sapiens (human)
angiogenesisPlatelet-derived growth factor receptor betaHomo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayPlatelet-derived growth factor receptor betaHomo sapiens (human)
multicellular organism developmentPlatelet-derived growth factor receptor betaHomo sapiens (human)
ovarian follicle developmentMast/stem cell growth factor receptor KitHomo sapiens (human)
myeloid progenitor cell differentiationMast/stem cell growth factor receptor KitHomo sapiens (human)
lymphoid progenitor cell differentiationMast/stem cell growth factor receptor KitHomo sapiens (human)
immature B cell differentiationMast/stem cell growth factor receptor KitHomo sapiens (human)
mast cell chemotaxisMast/stem cell growth factor receptor KitHomo sapiens (human)
positive regulation of dendritic cell cytokine productionMast/stem cell growth factor receptor KitHomo sapiens (human)
glycosphingolipid metabolic processMast/stem cell growth factor receptor KitHomo sapiens (human)
inflammatory responseMast/stem cell growth factor receptor KitHomo sapiens (human)
signal transductionMast/stem cell growth factor receptor KitHomo sapiens (human)
spermatogenesisMast/stem cell growth factor receptor KitHomo sapiens (human)
spermatid developmentMast/stem cell growth factor receptor KitHomo sapiens (human)
germ cell migrationMast/stem cell growth factor receptor KitHomo sapiens (human)
regulation of cell shapeMast/stem cell growth factor receptor KitHomo sapiens (human)
visual learningMast/stem cell growth factor receptor KitHomo sapiens (human)
male gonad developmentMast/stem cell growth factor receptor KitHomo sapiens (human)
positive regulation of phospholipase C activityMast/stem cell growth factor receptor KitHomo sapiens (human)
cytokine-mediated signaling pathwayMast/stem cell growth factor receptor KitHomo sapiens (human)
stem cell population maintenanceMast/stem cell growth factor receptor KitHomo sapiens (human)
lamellipodium assemblyMast/stem cell growth factor receptor KitHomo sapiens (human)
actin cytoskeleton organizationMast/stem cell growth factor receptor KitHomo sapiens (human)
hemopoiesisMast/stem cell growth factor receptor KitHomo sapiens (human)
T cell differentiationMast/stem cell growth factor receptor KitHomo sapiens (human)
erythrocyte differentiationMast/stem cell growth factor receptor KitHomo sapiens (human)
melanocyte differentiationMast/stem cell growth factor receptor KitHomo sapiens (human)
positive regulation of pseudopodium assemblyMast/stem cell growth factor receptor KitHomo sapiens (human)
positive regulation of mast cell cytokine productionMast/stem cell growth factor receptor KitHomo sapiens (human)
somatic stem cell population maintenanceMast/stem cell growth factor receptor KitHomo sapiens (human)
embryonic hemopoiesisMast/stem cell growth factor receptor KitHomo sapiens (human)
ectopic germ cell programmed cell deathMast/stem cell growth factor receptor KitHomo sapiens (human)
intracellular signal transductionMast/stem cell growth factor receptor KitHomo sapiens (human)
hematopoietic stem cell migrationMast/stem cell growth factor receptor KitHomo sapiens (human)
megakaryocyte developmentMast/stem cell growth factor receptor KitHomo sapiens (human)
Fc receptor signaling pathwayMast/stem cell growth factor receptor KitHomo sapiens (human)
Kit signaling pathwayMast/stem cell growth factor receptor KitHomo sapiens (human)
erythropoietin-mediated signaling pathwayMast/stem cell growth factor receptor KitHomo sapiens (human)
regulation of cell population proliferationMast/stem cell growth factor receptor KitHomo sapiens (human)
positive regulation of tyrosine phosphorylation of STAT proteinMast/stem cell growth factor receptor KitHomo sapiens (human)
negative regulation of programmed cell deathMast/stem cell growth factor receptor KitHomo sapiens (human)
mast cell degranulationMast/stem cell growth factor receptor KitHomo sapiens (human)
positive regulation of MAPK cascadeMast/stem cell growth factor receptor KitHomo sapiens (human)
pigmentationMast/stem cell growth factor receptor KitHomo sapiens (human)
tongue developmentMast/stem cell growth factor receptor KitHomo sapiens (human)
positive regulation of Notch signaling pathwayMast/stem cell growth factor receptor KitHomo sapiens (human)
positive regulation of receptor signaling pathway via JAK-STATMast/stem cell growth factor receptor KitHomo sapiens (human)
response to cadmium ionMast/stem cell growth factor receptor KitHomo sapiens (human)
protein autophosphorylationMast/stem cell growth factor receptor KitHomo sapiens (human)
positive regulation of long-term neuronal synaptic plasticityMast/stem cell growth factor receptor KitHomo sapiens (human)
digestive tract developmentMast/stem cell growth factor receptor KitHomo sapiens (human)
stem cell differentiationMast/stem cell growth factor receptor KitHomo sapiens (human)
epithelial cell proliferationMast/stem cell growth factor receptor KitHomo sapiens (human)
detection of mechanical stimulus involved in sensory perception of soundMast/stem cell growth factor receptor KitHomo sapiens (human)
positive regulation of DNA-binding transcription factor activityMast/stem cell growth factor receptor KitHomo sapiens (human)
negative regulation of developmental processMast/stem cell growth factor receptor KitHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionMast/stem cell growth factor receptor KitHomo sapiens (human)
cell chemotaxisMast/stem cell growth factor receptor KitHomo sapiens (human)
mast cell differentiationMast/stem cell growth factor receptor KitHomo sapiens (human)
mast cell proliferationMast/stem cell growth factor receptor KitHomo sapiens (human)
positive regulation of mast cell proliferationMast/stem cell growth factor receptor KitHomo sapiens (human)
melanocyte migrationMast/stem cell growth factor receptor KitHomo sapiens (human)
melanocyte adhesionMast/stem cell growth factor receptor KitHomo sapiens (human)
positive regulation of pyloric antrum smooth muscle contractionMast/stem cell growth factor receptor KitHomo sapiens (human)
regulation of bile acid metabolic processMast/stem cell growth factor receptor KitHomo sapiens (human)
positive regulation of colon smooth muscle contractionMast/stem cell growth factor receptor KitHomo sapiens (human)
positive regulation of small intestine smooth muscle contractionMast/stem cell growth factor receptor KitHomo sapiens (human)
positive regulation of vascular associated smooth muscle cell differentiationMast/stem cell growth factor receptor KitHomo sapiens (human)
negative regulation of reproductive processMast/stem cell growth factor receptor KitHomo sapiens (human)
positive regulation of cell migrationMast/stem cell growth factor receptor KitHomo sapiens (human)
positive regulation of MAP kinase activityMast/stem cell growth factor receptor KitHomo sapiens (human)
multicellular organism developmentMast/stem cell growth factor receptor KitHomo sapiens (human)
B cell differentiationMast/stem cell growth factor receptor KitHomo sapiens (human)
hematopoietic progenitor cell differentiationMast/stem cell growth factor receptor KitHomo sapiens (human)
negative regulation of cellular extravasationBreakpoint cluster region proteinHomo sapiens (human)
renal system processBreakpoint cluster region proteinHomo sapiens (human)
protein phosphorylationBreakpoint cluster region proteinHomo sapiens (human)
phagocytosisBreakpoint cluster region proteinHomo sapiens (human)
signal transductionBreakpoint cluster region proteinHomo sapiens (human)
small GTPase-mediated signal transductionBreakpoint cluster region proteinHomo sapiens (human)
brain developmentBreakpoint cluster region proteinHomo sapiens (human)
actin cytoskeleton organizationBreakpoint cluster region proteinHomo sapiens (human)
keratinocyte differentiationBreakpoint cluster region proteinHomo sapiens (human)
regulation of Rho protein signal transductionBreakpoint cluster region proteinHomo sapiens (human)
inner ear morphogenesisBreakpoint cluster region proteinHomo sapiens (human)
regulation of vascular permeabilityBreakpoint cluster region proteinHomo sapiens (human)
neutrophil degranulationBreakpoint cluster region proteinHomo sapiens (human)
negative regulation of neutrophil degranulationBreakpoint cluster region proteinHomo sapiens (human)
focal adhesion assemblyBreakpoint cluster region proteinHomo sapiens (human)
homeostasis of number of cellsBreakpoint cluster region proteinHomo sapiens (human)
negative regulation of inflammatory responseBreakpoint cluster region proteinHomo sapiens (human)
positive regulation of phagocytosisBreakpoint cluster region proteinHomo sapiens (human)
modulation of chemical synaptic transmissionBreakpoint cluster region proteinHomo sapiens (human)
neuromuscular process controlling balanceBreakpoint cluster region proteinHomo sapiens (human)
regulation of small GTPase mediated signal transductionBreakpoint cluster region proteinHomo sapiens (human)
regulation of cell cycleBreakpoint cluster region proteinHomo sapiens (human)
definitive hemopoiesisBreakpoint cluster region proteinHomo sapiens (human)
negative regulation of respiratory burstBreakpoint cluster region proteinHomo sapiens (human)
negative regulation of blood vessel remodelingBreakpoint cluster region proteinHomo sapiens (human)
intracellular protein transmembrane transportBreakpoint cluster region proteinHomo sapiens (human)
cellular response to lipopolysaccharideBreakpoint cluster region proteinHomo sapiens (human)
activation of GTPase activityBreakpoint cluster region proteinHomo sapiens (human)
macrophage migrationBreakpoint cluster region proteinHomo sapiens (human)
negative regulation of macrophage migrationBreakpoint cluster region proteinHomo sapiens (human)
negative regulation of reactive oxygen species metabolic processBreakpoint cluster region proteinHomo 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 (62)

Processvia Protein(s)Taxonomy
supercoiled DNA bindingTyrosine-protein kinase ABL1Homo sapiens (human)
magnesium ion bindingTyrosine-protein kinase ABL1Homo sapiens (human)
four-way junction DNA bindingTyrosine-protein kinase ABL1Homo sapiens (human)
bubble DNA bindingTyrosine-protein kinase ABL1Homo sapiens (human)
phosphotyrosine residue bindingTyrosine-protein kinase ABL1Homo sapiens (human)
DNA bindingTyrosine-protein kinase ABL1Homo sapiens (human)
transcription coactivator activityTyrosine-protein kinase ABL1Homo sapiens (human)
actin monomer bindingTyrosine-protein kinase ABL1Homo sapiens (human)
nicotinate-nucleotide adenylyltransferase activityTyrosine-protein kinase ABL1Homo sapiens (human)
protein kinase activityTyrosine-protein kinase ABL1Homo sapiens (human)
protein tyrosine kinase activityTyrosine-protein kinase ABL1Homo sapiens (human)
non-membrane spanning protein tyrosine kinase activityTyrosine-protein kinase ABL1Homo sapiens (human)
protein kinase C bindingTyrosine-protein kinase ABL1Homo sapiens (human)
protein bindingTyrosine-protein kinase ABL1Homo sapiens (human)
ATP bindingTyrosine-protein kinase ABL1Homo sapiens (human)
kinase activityTyrosine-protein kinase ABL1Homo sapiens (human)
SH3 domain bindingTyrosine-protein kinase ABL1Homo sapiens (human)
syntaxin bindingTyrosine-protein kinase ABL1Homo sapiens (human)
manganese ion bindingTyrosine-protein kinase ABL1Homo sapiens (human)
neuropilin bindingTyrosine-protein kinase ABL1Homo sapiens (human)
SH2 domain bindingTyrosine-protein kinase ABL1Homo sapiens (human)
ephrin receptor bindingTyrosine-protein kinase ABL1Homo sapiens (human)
actin filament bindingTyrosine-protein kinase ABL1Homo sapiens (human)
mitogen-activated protein kinase bindingTyrosine-protein kinase ABL1Homo sapiens (human)
proline-rich region bindingTyrosine-protein kinase ABL1Homo sapiens (human)
delta-catenin bindingTyrosine-protein kinase ABL1Homo sapiens (human)
sequence-specific double-stranded DNA bindingTyrosine-protein kinase ABL1Homo 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)
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)
protein kinase activityPlatelet-derived growth factor receptor betaHomo sapiens (human)
protein tyrosine kinase activityPlatelet-derived growth factor receptor betaHomo sapiens (human)
platelet activating factor receptor activityPlatelet-derived growth factor receptor betaHomo sapiens (human)
platelet-derived growth factor receptor activityPlatelet-derived growth factor receptor betaHomo sapiens (human)
platelet-derived growth factor beta-receptor activityPlatelet-derived growth factor receptor betaHomo sapiens (human)
signaling receptor bindingPlatelet-derived growth factor receptor betaHomo sapiens (human)
platelet-derived growth factor receptor bindingPlatelet-derived growth factor receptor betaHomo sapiens (human)
protein bindingPlatelet-derived growth factor receptor betaHomo sapiens (human)
ATP bindingPlatelet-derived growth factor receptor betaHomo sapiens (human)
enzyme bindingPlatelet-derived growth factor receptor betaHomo sapiens (human)
protein kinase bindingPlatelet-derived growth factor receptor betaHomo sapiens (human)
vascular endothelial growth factor bindingPlatelet-derived growth factor receptor betaHomo sapiens (human)
platelet-derived growth factor bindingPlatelet-derived growth factor receptor betaHomo sapiens (human)
protease bindingMast/stem cell growth factor receptor KitHomo sapiens (human)
protein tyrosine kinase activityMast/stem cell growth factor receptor KitHomo sapiens (human)
transmembrane receptor protein tyrosine kinase activityMast/stem cell growth factor receptor KitHomo sapiens (human)
stem cell factor receptor activityMast/stem cell growth factor receptor KitHomo sapiens (human)
protein bindingMast/stem cell growth factor receptor KitHomo sapiens (human)
ATP bindingMast/stem cell growth factor receptor KitHomo sapiens (human)
cytokine bindingMast/stem cell growth factor receptor KitHomo sapiens (human)
SH2 domain bindingMast/stem cell growth factor receptor KitHomo sapiens (human)
protein homodimerization activityMast/stem cell growth factor receptor KitHomo sapiens (human)
metal ion bindingMast/stem cell growth factor receptor KitHomo sapiens (human)
growth factor bindingMast/stem cell growth factor receptor KitHomo sapiens (human)
protein serine/threonine kinase activityBreakpoint cluster region proteinHomo sapiens (human)
protein tyrosine kinase activityBreakpoint cluster region proteinHomo sapiens (human)
guanyl-nucleotide exchange factor activityBreakpoint cluster region proteinHomo sapiens (human)
GTPase activator activityBreakpoint cluster region proteinHomo sapiens (human)
protein bindingBreakpoint cluster region proteinHomo sapiens (human)
ATP bindingBreakpoint cluster region proteinHomo sapiens (human)
protein serine kinase activityBreakpoint cluster region proteinHomo 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 (48)

Processvia Protein(s)Taxonomy
ruffleTyrosine-protein kinase ABL1Homo sapiens (human)
nucleusTyrosine-protein kinase ABL1Homo sapiens (human)
nucleoplasmTyrosine-protein kinase ABL1Homo sapiens (human)
nucleolusTyrosine-protein kinase ABL1Homo sapiens (human)
cytoplasmTyrosine-protein kinase ABL1Homo sapiens (human)
mitochondrionTyrosine-protein kinase ABL1Homo sapiens (human)
cytosolTyrosine-protein kinase ABL1Homo sapiens (human)
actin cytoskeletonTyrosine-protein kinase ABL1Homo sapiens (human)
nuclear bodyTyrosine-protein kinase ABL1Homo sapiens (human)
dendriteTyrosine-protein kinase ABL1Homo sapiens (human)
growth coneTyrosine-protein kinase ABL1Homo sapiens (human)
nuclear membraneTyrosine-protein kinase ABL1Homo sapiens (human)
neuronal cell bodyTyrosine-protein kinase ABL1Homo sapiens (human)
perinuclear region of cytoplasmTyrosine-protein kinase ABL1Homo sapiens (human)
postsynapseTyrosine-protein kinase ABL1Homo sapiens (human)
protein-containing complexTyrosine-protein kinase ABL1Homo sapiens (human)
plasma membraneTyrosine-protein kinase ABL1Homo sapiens (human)
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)
nucleusPlatelet-derived growth factor receptor betaHomo sapiens (human)
cytoplasmPlatelet-derived growth factor receptor betaHomo sapiens (human)
Golgi apparatusPlatelet-derived growth factor receptor betaHomo sapiens (human)
plasma membranePlatelet-derived growth factor receptor betaHomo sapiens (human)
focal adhesionPlatelet-derived growth factor receptor betaHomo sapiens (human)
membranePlatelet-derived growth factor receptor betaHomo sapiens (human)
apical plasma membranePlatelet-derived growth factor receptor betaHomo sapiens (human)
cytoplasmic vesiclePlatelet-derived growth factor receptor betaHomo sapiens (human)
lysosomal lumenPlatelet-derived growth factor receptor betaHomo sapiens (human)
intracellular membrane-bounded organellePlatelet-derived growth factor receptor betaHomo sapiens (human)
plasma membranePlatelet-derived growth factor receptor betaHomo sapiens (human)
receptor complexPlatelet-derived growth factor receptor betaHomo sapiens (human)
fibrillar centerMast/stem cell growth factor receptor KitHomo sapiens (human)
acrosomal vesicleMast/stem cell growth factor receptor KitHomo sapiens (human)
extracellular spaceMast/stem cell growth factor receptor KitHomo sapiens (human)
plasma membraneMast/stem cell growth factor receptor KitHomo sapiens (human)
cell-cell junctionMast/stem cell growth factor receptor KitHomo sapiens (human)
external side of plasma membraneMast/stem cell growth factor receptor KitHomo sapiens (human)
cytoplasmic side of plasma membraneMast/stem cell growth factor receptor KitHomo sapiens (human)
plasma membraneMast/stem cell growth factor receptor KitHomo sapiens (human)
receptor complexMast/stem cell growth factor receptor KitHomo sapiens (human)
cytosolBreakpoint cluster region proteinHomo sapiens (human)
plasma membraneBreakpoint cluster region proteinHomo sapiens (human)
postsynaptic densityBreakpoint cluster region proteinHomo sapiens (human)
membraneBreakpoint cluster region proteinHomo sapiens (human)
axonBreakpoint cluster region proteinHomo sapiens (human)
dendritic spineBreakpoint cluster region proteinHomo sapiens (human)
extracellular exosomeBreakpoint cluster region proteinHomo sapiens (human)
protein-containing complexBreakpoint cluster region proteinHomo sapiens (human)
Schaffer collateral - CA1 synapseBreakpoint cluster region proteinHomo sapiens (human)
glutamatergic synapseBreakpoint cluster region proteinHomo sapiens (human)
membraneBreakpoint cluster region proteinHomo 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 (23)

Assay IDTitleYearJournalArticle
AID1854090Inhibition of c-Kit (unknown origin)2022European journal of medicinal chemistry, Aug-05, Volume: 238The progress of small-molecules and degraders against BCR-ABL for the treatment of CML.
AID1611411Inhibition of BCR/Abl P230 mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay2019Bioorganic & medicinal chemistry letters, 12-15, Volume: 29, Issue:24
Structure-based analysis and biological characterization of imatinib derivatives reveal insights towards the inhibition of wild-type BCR-ABL and its mutants.
AID1611403Inhibition of BCR/Abl Y253F mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay2019Bioorganic & medicinal chemistry letters, 12-15, Volume: 29, Issue:24
Structure-based analysis and biological characterization of imatinib derivatives reveal insights towards the inhibition of wild-type BCR-ABL and its mutants.
AID1611407Inhibition of BCR/Abl F317I mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay2019Bioorganic & medicinal chemistry letters, 12-15, Volume: 29, Issue:24
Structure-based analysis and biological characterization of imatinib derivatives reveal insights towards the inhibition of wild-type BCR-ABL and its mutants.
AID1611402Inhibition of BCR/Abl Q252H mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay2019Bioorganic & medicinal chemistry letters, 12-15, Volume: 29, Issue:24
Structure-based analysis and biological characterization of imatinib derivatives reveal insights towards the inhibition of wild-type BCR-ABL and its mutants.
AID1611405Inhibition of BCR/Abl V299L mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay2019Bioorganic & medicinal chemistry letters, 12-15, Volume: 29, Issue:24
Structure-based analysis and biological characterization of imatinib derivatives reveal insights towards the inhibition of wild-type BCR-ABL and its mutants.
AID1611404Inhibition of BCR/Abl E255K mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay2019Bioorganic & medicinal chemistry letters, 12-15, Volume: 29, Issue:24
Structure-based analysis and biological characterization of imatinib derivatives reveal insights towards the inhibition of wild-type BCR-ABL and its mutants.
AID1611406Inhibition of BCR/Abl F317L mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay2019Bioorganic & medicinal chemistry letters, 12-15, Volume: 29, Issue:24
Structure-based analysis and biological characterization of imatinib derivatives reveal insights towards the inhibition of wild-type BCR-ABL and its mutants.
AID1854088Inhibition of BCR-ABL phosphorylation in human K562 cells incubated for 3 hrs by Western blot analysis2022European journal of medicinal chemistry, Aug-05, Volume: 238The progress of small-molecules and degraders against BCR-ABL for the treatment of CML.
AID1611408Inhibition of BCR/Abl M351T mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay2019Bioorganic & medicinal chemistry letters, 12-15, Volume: 29, Issue:24
Structure-based analysis and biological characterization of imatinib derivatives reveal insights towards the inhibition of wild-type BCR-ABL and its mutants.
AID1611410Inhibition of BCR/Abl P190 mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay2019Bioorganic & medicinal chemistry letters, 12-15, Volume: 29, Issue:24
Structure-based analysis and biological characterization of imatinib derivatives reveal insights towards the inhibition of wild-type BCR-ABL and its mutants.
AID1611409Inhibition of BCR/Abl H396P mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay2019Bioorganic & medicinal chemistry letters, 12-15, Volume: 29, Issue:24
Structure-based analysis and biological characterization of imatinib derivatives reveal insights towards the inhibition of wild-type BCR-ABL and its mutants.
AID1854089Inhibition of PDGFRbeta (unknown origin)2022European journal of medicinal chemistry, Aug-05, Volume: 238The progress of small-molecules and degraders against BCR-ABL for the treatment of CML.
AID1611401Inhibition of wild type BCR/Abl (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay2019Bioorganic & medicinal chemistry letters, 12-15, Volume: 29, Issue:24
Structure-based analysis and biological characterization of imatinib derivatives reveal insights towards the inhibition of wild-type BCR-ABL and its mutants.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
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.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
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.
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.
AID1345606Human ABL proto-oncogene 1, non-receptor tyrosine kinase (Abl family)2010Leukemia, Oct, Volume: 24, Issue:10
HH-GV-678, a novel selective inhibitor of Bcr-Abl, outperforms imatinib and effectively overrides imatinib resistance.
AID1345590Human platelet derived growth factor receptor beta (Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family)2010Leukemia, Oct, Volume: 24, Issue:10
HH-GV-678, a novel selective inhibitor of Bcr-Abl, outperforms imatinib and effectively overrides imatinib resistance.
AID1345555Human KIT proto-oncogene receptor tyrosine kinase (Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family)2010Leukemia, Oct, Volume: 24, Issue:10
HH-GV-678, a novel selective inhibitor of Bcr-Abl, outperforms imatinib and effectively overrides imatinib resistance.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (17)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (5.88)29.6817
2010's7 (41.18)24.3611
2020's9 (52.94)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.11

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.11 (24.57)
Research Supply Index2.94 (2.92)
Research Growth Index5.06 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.11)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (5.88%)5.53%
Reviews1 (5.88%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other15 (88.24%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
imatinib
[no description available]		3.7820aromatic amine;
benzamides;
N-methylpiperazine;
pyridines;
pyrimidines		antineoplastic agent;
apoptosis inducer;
tyrosine kinase inhibitor
pyrroles
1H-pyrrole : A tautomer of pyrrole that has the double bonds at positions 2 and 4.. pyrrole : A five-membered monocyclic heteroarene comprising one NH and four CH units which forms the parent compound of the pyrrole group of compounds. Its five-membered ring structure has three tautomers. A 'closed class'.. azole : Any monocyclic heteroarene consisting of a five-membered ring containing nitrogen. Azoles can also contain one or more other non-carbon atoms, such as nitrogen, sulfur or oxygen.		2.110pyrrole;
secondary amine
alpha-aminopyridine
alpha-aminopyridine: RN given refers to parent cpd; structure in Merck Index, 9th ed, #485. aminopyridine : Compounds containing a pyridine skeleton substituted by one or more amine groups.		6.21111
erythromycin
Erythromycin: A bacteriostatic antibiotic macrolide produced by Streptomyces erythreus. Erythromycin A is considered its major active component. In sensitive organisms, it inhibits protein synthesis by binding to 50S ribosomal subunits. This binding process inhibits peptidyl transferase activity and interferes with translocation of amino acids during translation and assembly of proteins.. erythromycin : Any of several wide-spectrum macrolide antibiotics obtained from actinomycete Saccharopolyspora erythraea (formerly known as Streptomyces erythraeus).. erythromycin A : An erythromycin that consists of erythronolide A having 2,6-dideoxy-3-C-methyl-3-O-methyl-alpha-L-ribo-hexopyranosyl and 3,4,6-trideoxy-3-(dimethylamino)-beta-D-xylo-hexopyranosyl residues attahced at positions 4 and 6 respectively.		2.2510cyclic ketone;
erythromycin
voriconazole
Voriconazole: A triazole antifungal agent that specifically inhibits STEROL 14-ALPHA-DEMETHYLASE and CYTOCHROME P-450 CYP3A.. voriconazole : A triazole-based antifungal agent used for the treatment of esophageal candidiasis, invasive pulmonary aspergillosis, and serious fungal infections caused by Scedosporium apiospermum and Fusarium spp. It is an inhibitor of cytochrome P450 2C9 (CYP2C9) and CYP3A4.		2.2510conazole antifungal drug;
difluorobenzene;
pyrimidines;
tertiary alcohol;
triazole antifungal drug		P450 inhibitor
imatinib mesylate
imatinib methanesulfonate : A methanesulfonate (mesylate) salt that is the monomesylate salt of imatinib. Used for treatment of chronic myelogenous leukemia and gastrointestinal stromal tumours.		4.1250methanesulfonate saltanticoronaviral agent;
antineoplastic agent;
apoptosis inducer;
tyrosine kinase inhibitor
berbamine
[no description available]		3.5110bisbenzylisoquinoline alkaloid;
isoquinolines
homoharringtonine
Homoharringtonine: Semisynthetic derivative of harringtonine that acts as a protein synthesis inhibitor and induces APOPTOSIS in tumor cells. It is used in the treatment of MYELOID LEUKEMIA, CHRONIC.. omacetaxine mepesuccinate : A cephalotaxine-derived alkaloid ester obtained from Cephalotaxus harringtonia; used for the treatment of chronic or accelerated phase chronic myeloid leukaemia.		3.5110alkaloid ester;
enol ether;
organic heteropentacyclic compound;
tertiary alcohol		anticoronaviral agent;
antineoplastic agent;
apoptosis inducer;
protein synthesis inhibitor
s 1033
[no description available]		3.7820(trifluoromethyl)benzenes;
imidazoles;
pyridines;
pyrimidines;
secondary amino compound;
secondary carboxamide		anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor
dasatinib
N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)-1,3-thiazole-5-carboxamide: a dasatinib prodrug; structure in first source. dasatinib (anhydrous) : An aminopyrimidine that is 2-methylpyrimidine which is substituted at position 4 by the primary amino group of 2-amino-1,3-thiazole-5-carboxylic acid and at position 6 by a 4-(2-hydroxyethyl)piperazin-1-yl group, and in which the carboxylic acid group has been formally condensed with 2-chloro-6-methylaniline to afford the corresponding amide. A multi-targeted kinase inhibitor, it is used, particularly as the monohydrate, for the treatment of chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia. Note that the name 'dasatinib' is used to refer to the monohydrate (USAN) as well as to anhydrous dasatinib (INN).		3.51101,3-thiazoles;
aminopyrimidine;
monocarboxylic acid amide;
N-(2-hydroxyethyl)piperazine;
N-arylpiperazine;
organochlorine compound;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor
diosmetin
[no description available]		3.51103'-hydroxyflavonoid;
monomethoxyflavone;
trihydroxyflavone		angiogenesis inhibitor;
anti-inflammatory agent;
antineoplastic agent;
antioxidant;
apoptosis inducer;
bone density conservation agent;
cardioprotective agent;
plant metabolite;
tropomyosin-related kinase B receptor agonist;
vasodilator agent
bosutinib
4-((2,4-dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methyl-1-piperazinyl)propoxy)-3-quinolinecarbonitrile: a Src kinase inhibitor; structure in first source		3.5110aminoquinoline;
aromatic ether;
dichlorobenzene;
N-methylpiperazine;
nitrile;
tertiary amino compound		antineoplastic agent;
tyrosine kinase inhibitor
su 11248
[no description available]		2.110monocarboxylic acid amide;
pyrroles		angiogenesis inhibitor;
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
immunomodulator;
neuroprotective agent;
vascular endothelial growth factor receptor antagonist
vx680
[no description available]		3.5110N-arylpiperazine
gambogic acid
gambogic acid: RN given refers to (1R-(1alpha,1(Z),3abeta,5alpha,11beta,14aS*))-isomer		3.5110pyranoxanthonesmetabolite
inno-406
[no description available]		3.5110biaryl
kw 2449
KW 2449: has both multikinase inhibitory activity and antineoplastic activity; structure in first source		3.5110
ponatinib
[no description available]		3.5110(trifluoromethyl)benzenes;
acetylenic compound;
benzamides;
imidazopyridazine;
N-methylpiperazine		antineoplastic agent;
tyrosine kinase inhibitor
dcc-2036
rebastinib: an inhibitor of Tie2 tyrosine kinase receptor and antineoplastic agent		3.5110organofluorine compound;
phenylureas;
pyrazoles;
pyridinecarboxamide;
quinolines		tyrosine kinase inhibitor
cyclosporine
Cyclosporine: A cyclic undecapeptide from an extract of soil fungi. It is a powerful immunosupressant with a specific action on T-lymphocytes. It is used for the prophylaxis of graft rejection in organ and tissue transplantation. (From Martindale, The Extra Pharmacopoeia, 30th ed).		2.2510
at 9283
[no description available]		3.5110
ConditionIndicatedRelationship StrengthStudiesTrials
Experimental Leukemia
[description not available]		02.0510
Granulocytic Leukemia, Chronic
[description not available]		05.2160
Leukemia, Myelogenous, Chronic, BCR-ABL Positive
Clonal hematopoetic disorder caused by an acquired genetic defect in PLURIPOTENT STEM CELLS. It starts in MYELOID CELLS of the bone marrow, invades the blood and then other organs. The condition progresses from a stable, more indolent, chronic phase (LEUKEMIA, MYELOID, CHRONIC PHASE) lasting up to 7 years, to an advanced phase composed of an accelerated phase (LEUKEMIA, MYELOID, ACCELERATED PHASE) and BLAST CRISIS.		17.2160
Congenital Zika Syndrome
[description not available]		02.2510
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.2510
Zika Virus Infection
A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.		02.2510
Acute Lymphoid Leukemia
[description not available]		02.3110
Precursor Cell Lymphoblastic Leukemia-Lymphoma
A neoplasm characterized by abnormalities of the lymphoid cell precursors leading to excessive lymphoblasts in the marrow and other organs. It is the most common cancer in children and accounts for the vast majority of all childhood leukemias.		14.3110
Gastrointestinal Stromal Neoplasm
[description not available]		02.110
Gastrointestinal Stromal Tumors
All tumors in the GASTROINTESTINAL TRACT arising from mesenchymal cells (MESODERM) except those of smooth muscle cells (LEIOMYOMA) or Schwann cells (SCHWANNOMA).		02.110
Sensitivity and Specificity
Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)		02.0710