Page last updated: 2024-11-13

cc-292

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

Description

spebrutinib: inhibits Bruton's tyrosine kinase; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID59174488
CHEMBL ID3301625
SCHEMBL ID626216
MeSH IDM0587919

Synonyms (59)

Synonym
avl-292
cc-292 ,
spebrutinib
bdbm50161162
1202757-89-8
n-(3-(5-fluoro-2-(4-(2-methoxyethoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide
spebrutinib [usan]
spebrutinib [inn]
n-(3-((5-fluoro-2-((4-(2-methoxyethoxy)phenyl)amino)pyrimidin-4-yl)amino)phenyl)acrylamide
btk inhibitor cc-292
spebrutinib [who-dd]
3-(5-fluoro-2-(4-(2-methoxyethoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide
S7173
CHEMBL3301625
CS-1482
HY-18012
n-[3-[[5-fluoro-2-[4-(2-methoxyethoxy)anilino]pyrimidin-4-yl]amino]phenyl]prop-2-enamide
gtpl7837
avl 292
SCHEMBL626216
spebrutinib [usan:inn]
dru6ng543j ,
unii-dru6ng543j
2-propenamide, n-(3-((5-fluoro-2-((4-(2-methoxyethoxy)phenyl)amino)-4-pyrimidinyl)amino)phenyl)-
n-[3-[[5-fluoro-2-[[4-(2-methoxyethoxy)phenyl]amino]-4-pyrimidinyl]amino]phenyl]-2-propenamide
n-(3-{5-fluoro-2-[4-(2-methoxy-ethoxy)-phenylamino]-pyrimidin-4-ylamino}-phenyl)-acrylamide
n-(3-((5-fluoro-2-((4-(2-methoxyethoxyl)phenyl)amino)pyrimidin-4-yl)amino)phenyl)acrylamide
KXBDTLQSDKGAEB-UHFFFAOYSA-N
c22h22fn5o3
avl292
spebrutinib (usan/inn)
D10730
cc 292
AC-32618
AKOS026670200
EX-A255
lmk-435
HMS3653E15
mfcd25976876
NCGC00386306-06
SW219474-1
DB11764
FT-0751022
AKOS032949981
BCP07702
cc-292 (avl-292)
n-{3-[(5-fluoro-2-{[4-(2-methoxyethoxy)phenyl]amino}pyrimidin-4-yl)amino]phenyl}prop-2-enamide
Q27088846
AS-16998
SB14609
HMS3674E05
AMY9065
CCG-268921
spebrutinib (avl-292)
nsc780020
nsc-780020
NCGC00386306-03
n-(3-((5-fluoro-2-((4-(2-methoxyethoxy)phenyl)amino)-4-pyrimidinyl)amino)phenyl)-2-propenamide
DTXSID101026012

Research Excerpts

Pharmacokinetics

This translational pharmacodynamic assay has accompanied CC-292 through each step of drug discovery and development. An analysis was performed to develop a population pharmacokinetic model ofCC-292 and assess the influence of demographics and disease-related covariates.

ExcerptReferenceRelevance
" This translational pharmacodynamic assay has accompanied CC-292 through each step of drug discovery and development."( Inhibition of Btk with CC-292 provides early pharmacodynamic assessment of activity in mice and humans.
Aslanian, S; Chaturvedi, P; Dubrovskiy, A; Evans, EK; Freed, MI; Karp, R; Labenski, MT; Lounsbury, H; Mazdiyasni, H; Nacht, M; Petter, RC; Sheets, M; Singh, J; Tester, R; Westlin, WF; Witowski, SR; Zhu, Z, 2013
)
0.94
" An analysis was performed to develop a population pharmacokinetic model of CC-292 and assess the influence of demographics and disease-related covariates on CC-292 exposure and to assess the exposure-response (overall response rate) relationship in patients with chronic lymphocytic leukemia."( Population Pharmacokinetics and Exposure Response Assessment of CC-292, a Potent BTK Inhibitor, in Patients With Chronic Lymphocytic Leukemia.
Gouedard, O; Li, Y; Mei, J; Palmisano, M; Ramírez-Valle, F; Takeshita, K; Ventura, JI; Xue, Y; Zhou, S, 2017
)
0.92

Compound-Compound Interactions

ExcerptReferenceRelevance
" As CC-292 did not show potent in vitro anti-MM activity, we next evaluated it in combination with the proteasome inhibitor, carfilzomib."( A novel Bruton's tyrosine kinase inhibitor CC-292 in combination with the proteasome inhibitor carfilzomib impacts the bone microenvironment in a multiple myeloma model with resultant antimyeloma activity.
Arastu-Kapur, S; Cirstea, DD; Eda, H; Evans, E; Kirk, CJ; Mishima, Y; Nemani, N; Raje, NS; Santo, L; Scullen, TA; Singh, J; Waterman, PR; Westlin, WF; Yee, AJ, 2014
)
1.22

Bioavailability

The relative bioavailability (Frel) of the CC-292 P22-TAB compared to the P01-CAP reference formulation was 1.

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
" The aim of this study was to evaluate the relative bioavailability of newly developed CC-292 tablet formulation (P22 tablet (P22-TAB) and CC-292 capsule formulation (P22 capsule [P22-CAP]) compared to the current CC-292 capsule formulation (P1 capsule [P01-CAP])."( An open-label, phase 1, randomized, three treatments, three-period, crossover, relative bioavailability study of CC-292, a potent and orally available inhibitor of bruton tyrosine kinase.
Cheng, Y; Li, Y; Liu, L; Xue, Y; Zhou, S, 2022
)
1.15
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (18)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
PPM1D proteinHomo sapiens (human)Potency16.53880.00529.466132.9993AID1347411
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency4.25340.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency3.37860.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency10.68400.00108.379861.1304AID1645840
Interferon betaHomo sapiens (human)Potency13.24870.00339.158239.8107AID1347411; AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency3.37860.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency3.37860.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency3.37860.01238.964839.8107AID1645842
[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 JAK2Homo sapiens (human)IC50 (µMol)0.53370.00010.372210.0000AID1650543
Epidermal growth factor receptorHomo sapiens (human)IC50 (µMol)0.44200.00000.536910.0000AID1469890
Tyrosine-protein kinase LynHomo sapiens (human)IC50 (µMol)4.40000.00020.55945.2000AID1357749
Tyrosine-protein kinase JAK1Homo sapiens (human)IC50 (µMol)1.00000.00030.23787.3000AID1650542
Tyrosine-protein kinase TecHomo sapiens (human)IC50 (µMol)0.00620.00050.06310.4720AID1357748
Cytoplasmic tyrosine-protein kinase BMXHomo sapiens (human)IC50 (µMol)2.66500.00040.23362.6650AID1469888
Tyrosine-protein kinase JAK3Homo sapiens (human)IC50 (µMol)0.46260.00010.41937.9200AID1401308; AID1469889; AID1650544; AID1654023
Tyrosine-protein kinase BTKHomo sapiens (human)IC50 (µMol)0.11630.00010.25577.6000AID1291431; AID1324656; AID1334877; AID1357747; AID1401307; AID1426139; AID1469887; AID1484553; AID1553406; AID1650541; AID1820500; AID1820501; AID1869073; AID1869074; AID1869075; AID1869076; AID1869077
Tyrosine-protein kinase BTKHomo sapiens (human)Ki0.02070.00320.07030.4250AID1469894
Early activation antigen CD69Homo sapiens (human)IC50 (µMol)3.10003.10003.10003.1000AID1820502
Sigma intracellular receptor 2Rattus norvegicus (Norway rat)IC50 (µMol)0.53370.01431.37567.5000AID1650543
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (335)

Processvia Protein(s)Taxonomy
positive regulation of platelet aggregationTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of platelet activationTyrosine-protein kinase JAK2Homo sapiens (human)
response to antibioticTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of SMAD protein signal transductionTyrosine-protein kinase JAK2Homo sapiens (human)
microglial cell activationTyrosine-protein kinase JAK2Homo sapiens (human)
adaptive immune responseTyrosine-protein kinase JAK2Homo sapiens (human)
chromatin remodelingTyrosine-protein kinase JAK2Homo sapiens (human)
transcription by RNA polymerase IITyrosine-protein kinase JAK2Homo sapiens (human)
protein phosphorylationTyrosine-protein kinase JAK2Homo sapiens (human)
apoptotic processTyrosine-protein kinase JAK2Homo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processTyrosine-protein kinase JAK2Homo sapiens (human)
immune responseTyrosine-protein kinase JAK2Homo sapiens (human)
signal transductionTyrosine-protein kinase JAK2Homo sapiens (human)
enzyme-linked receptor protein signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
G protein-coupled receptor signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationTyrosine-protein kinase JAK2Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STATTyrosine-protein kinase JAK2Homo sapiens (human)
tyrosine phosphorylation of STAT proteinTyrosine-protein kinase JAK2Homo sapiens (human)
mesoderm developmentTyrosine-protein kinase JAK2Homo sapiens (human)
negative regulation of cell population proliferationTyrosine-protein kinase JAK2Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to oxidative stressTyrosine-protein kinase JAK2Homo sapiens (human)
negative regulation of cardiac muscle cell apoptotic processTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of cell-substrate adhesionTyrosine-protein kinase JAK2Homo sapiens (human)
response to amineTyrosine-protein kinase JAK2Homo sapiens (human)
peptidyl-tyrosine phosphorylationTyrosine-protein kinase JAK2Homo sapiens (human)
cytokine-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
negative regulation of cell-cell adhesionTyrosine-protein kinase JAK2Homo sapiens (human)
actin filament polymerizationTyrosine-protein kinase JAK2Homo sapiens (human)
cell differentiationTyrosine-protein kinase JAK2Homo sapiens (human)
erythrocyte differentiationTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of cell migrationTyrosine-protein kinase JAK2Homo sapiens (human)
axon regenerationTyrosine-protein kinase JAK2Homo sapiens (human)
intracellular mineralocorticoid receptor signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of insulin secretionTyrosine-protein kinase JAK2Homo sapiens (human)
response to lipopolysaccharideTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of type II interferon productionTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of interleukin-1 beta productionTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of interleukin-17 productionTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of tumor necrosis factor productionTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of natural killer cell proliferationTyrosine-protein kinase JAK2Homo sapiens (human)
response to hydroperoxideTyrosine-protein kinase JAK2Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
symbiont-induced defense-related programmed cell deathTyrosine-protein kinase JAK2Homo sapiens (human)
response to tumor necrosis factorTyrosine-protein kinase JAK2Homo sapiens (human)
post-embryonic hemopoiesisTyrosine-protein kinase JAK2Homo sapiens (human)
intracellular signal transductionTyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-12-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
cellular response to interleukin-3Tyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-5-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
collagen-activated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-3-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
granulocyte-macrophage colony-stimulating factor signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of T cell proliferationTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of protein import into nucleusTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of tyrosine phosphorylation of STAT proteinTyrosine-protein kinase JAK2Homo sapiens (human)
activation of Janus kinase activityTyrosine-protein kinase JAK2Homo sapiens (human)
negative regulation of DNA bindingTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of MAPK cascadeTyrosine-protein kinase JAK2Homo sapiens (human)
negative regulation of neuron apoptotic processTyrosine-protein kinase JAK2Homo sapiens (human)
post-translational protein modificationTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of MHC class II biosynthetic processTyrosine-protein kinase JAK2Homo sapiens (human)
regulation of nitric oxide biosynthetic processTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of nitric oxide biosynthetic processTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of cell differentiationTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of transcription by RNA polymerase IITyrosine-protein kinase JAK2Homo sapiens (human)
regulation of receptor signaling pathway via JAK-STATTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of receptor signaling pathway via JAK-STATTyrosine-protein kinase JAK2Homo sapiens (human)
protein autophosphorylationTyrosine-protein kinase JAK2Homo sapiens (human)
platelet-derived growth factor receptor signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
regulation of inflammatory responseTyrosine-protein kinase JAK2Homo sapiens (human)
modulation of chemical synaptic transmissionTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of NK T cell proliferationTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of nitric-oxide synthase biosynthetic processTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionTyrosine-protein kinase JAK2Homo sapiens (human)
type II interferon-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
growth hormone receptor signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
growth hormone receptor signaling pathway via JAK-STATTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of growth hormone receptor signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
mammary gland epithelium developmentTyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-6-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of leukocyte proliferationTyrosine-protein kinase JAK2Homo sapiens (human)
response to interleukin-12Tyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-35-mediated signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
cellular response to lipopolysaccharideTyrosine-protein kinase JAK2Homo sapiens (human)
cellular response to dexamethasone stimulusTyrosine-protein kinase JAK2Homo sapiens (human)
extrinsic apoptotic signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
cellular response to virusTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of cold-induced thermogenesisTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of growth factor dependent skeletal muscle satellite cell proliferationTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of epithelial cell apoptotic processTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferationTyrosine-protein kinase JAK2Homo sapiens (human)
regulation of postsynapse to nucleus signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of signaling receptor activityTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of T-helper 17 type immune responseTyrosine-protein kinase JAK2Homo sapiens (human)
positive regulation of apoptotic signaling pathwayTyrosine-protein kinase JAK2Homo sapiens (human)
regulation of apoptotic processTyrosine-protein kinase JAK2Homo sapiens (human)
cell surface receptor signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
epidermal growth factor receptor signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cell population proliferationEpidermal growth factor receptorHomo sapiens (human)
MAPK cascadeEpidermal growth factor receptorHomo sapiens (human)
ossificationEpidermal growth factor receptorHomo sapiens (human)
embryonic placenta developmentEpidermal growth factor receptorHomo sapiens (human)
positive regulation of protein phosphorylationEpidermal growth factor receptorHomo sapiens (human)
hair follicle developmentEpidermal growth factor receptorHomo sapiens (human)
translationEpidermal growth factor receptorHomo sapiens (human)
signal transductionEpidermal growth factor receptorHomo sapiens (human)
epidermal growth factor receptor signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
activation of phospholipase C activityEpidermal growth factor receptorHomo sapiens (human)
salivary gland morphogenesisEpidermal growth factor receptorHomo sapiens (human)
midgut developmentEpidermal growth factor receptorHomo sapiens (human)
learning or memoryEpidermal growth factor receptorHomo sapiens (human)
circadian rhythmEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cell population proliferationEpidermal growth factor receptorHomo sapiens (human)
diterpenoid metabolic processEpidermal growth factor receptorHomo sapiens (human)
peptidyl-tyrosine phosphorylationEpidermal growth factor receptorHomo sapiens (human)
cerebral cortex cell migrationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cell growthEpidermal growth factor receptorHomo sapiens (human)
lung developmentEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cell migrationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of superoxide anion generationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationEpidermal growth factor receptorHomo sapiens (human)
response to cobalaminEpidermal growth factor receptorHomo sapiens (human)
response to hydroxyisoflavoneEpidermal growth factor receptorHomo sapiens (human)
cellular response to reactive oxygen speciesEpidermal growth factor receptorHomo sapiens (human)
peptidyl-tyrosine autophosphorylationEpidermal growth factor receptorHomo sapiens (human)
ERBB2-EGFR signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
negative regulation of epidermal growth factor receptor signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
negative regulation of protein catabolic processEpidermal growth factor receptorHomo sapiens (human)
vasodilationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of phosphorylationEpidermal growth factor receptorHomo sapiens (human)
ovulation cycleEpidermal growth factor receptorHomo sapiens (human)
hydrogen peroxide metabolic processEpidermal growth factor receptorHomo sapiens (human)
negative regulation of apoptotic processEpidermal growth factor receptorHomo sapiens (human)
positive regulation of MAP kinase activityEpidermal growth factor receptorHomo sapiens (human)
tongue developmentEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cyclin-dependent protein serine/threonine kinase activityEpidermal growth factor receptorHomo sapiens (human)
positive regulation of DNA repairEpidermal growth factor receptorHomo sapiens (human)
positive regulation of DNA replicationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of bone resorptionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of DNA-templated transcriptionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of vasoconstrictionEpidermal growth factor receptorHomo sapiens (human)
negative regulation of mitotic cell cycleEpidermal growth factor receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIEpidermal growth factor receptorHomo sapiens (human)
regulation of JNK cascadeEpidermal growth factor receptorHomo sapiens (human)
symbiont entry into host cellEpidermal growth factor receptorHomo sapiens (human)
protein autophosphorylationEpidermal growth factor receptorHomo sapiens (human)
astrocyte activationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of fibroblast proliferationEpidermal growth factor receptorHomo sapiens (human)
digestive tract morphogenesisEpidermal growth factor receptorHomo sapiens (human)
positive regulation of smooth muscle cell proliferationEpidermal growth factor receptorHomo sapiens (human)
neuron projection morphogenesisEpidermal growth factor receptorHomo sapiens (human)
epithelial cell proliferationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of epithelial cell proliferationEpidermal growth factor receptorHomo sapiens (human)
regulation of peptidyl-tyrosine phosphorylationEpidermal growth factor receptorHomo sapiens (human)
protein insertion into membraneEpidermal growth factor receptorHomo sapiens (human)
response to calcium ionEpidermal growth factor receptorHomo sapiens (human)
regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of synaptic transmission, glutamatergicEpidermal growth factor receptorHomo sapiens (human)
positive regulation of glial cell proliferationEpidermal growth factor receptorHomo sapiens (human)
morphogenesis of an epithelial foldEpidermal growth factor receptorHomo sapiens (human)
eyelid development in camera-type eyeEpidermal growth factor receptorHomo sapiens (human)
response to UV-AEpidermal growth factor receptorHomo sapiens (human)
positive regulation of mucus secretionEpidermal growth factor receptorHomo sapiens (human)
regulation of ERK1 and ERK2 cascadeEpidermal growth factor receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeEpidermal growth factor receptorHomo sapiens (human)
cellular response to amino acid stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to mechanical stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to cadmium ionEpidermal growth factor receptorHomo sapiens (human)
cellular response to epidermal growth factor stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to estradiol stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to xenobiotic stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to dexamethasone stimulusEpidermal growth factor receptorHomo sapiens (human)
positive regulation of canonical Wnt signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
liver regenerationEpidermal growth factor receptorHomo sapiens (human)
cell-cell adhesionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of protein kinase C activityEpidermal growth factor receptorHomo sapiens (human)
positive regulation of G1/S transition of mitotic cell cycleEpidermal growth factor receptorHomo sapiens (human)
positive regulation of non-canonical NF-kappaB signal transductionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of prolactin secretionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of miRNA transcriptionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of protein localization to plasma membraneEpidermal growth factor receptorHomo sapiens (human)
negative regulation of cardiocyte differentiationEpidermal growth factor receptorHomo sapiens (human)
neurogenesisEpidermal growth factor receptorHomo sapiens (human)
multicellular organism developmentEpidermal growth factor receptorHomo sapiens (human)
positive regulation of kinase activityEpidermal growth factor receptorHomo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayEpidermal growth factor receptorHomo 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)
DNA damage checkpoint signalingTyrosine-protein kinase LynHomo sapiens (human)
B cell homeostasisTyrosine-protein kinase LynHomo sapiens (human)
regulation of cytokine productionTyrosine-protein kinase LynHomo sapiens (human)
regulation of protein phosphorylationTyrosine-protein kinase LynHomo sapiens (human)
negative regulation of protein phosphorylationTyrosine-protein kinase LynHomo sapiens (human)
positive regulation of protein phosphorylationTyrosine-protein kinase LynHomo sapiens (human)
stimulatory C-type lectin receptor signaling pathwayTyrosine-protein kinase LynHomo sapiens (human)
hematopoietic progenitor cell differentiationTyrosine-protein kinase LynHomo sapiens (human)
adaptive immune responseTyrosine-protein kinase LynHomo sapiens (human)
Fc receptor mediated stimulatory signaling pathwayTyrosine-protein kinase LynHomo sapiens (human)
tolerance induction to self antigenTyrosine-protein kinase LynHomo sapiens (human)
histamine secretion by mast cellTyrosine-protein kinase LynHomo sapiens (human)
platelet degranulationTyrosine-protein kinase LynHomo sapiens (human)
negative regulation of myeloid leukocyte differentiationTyrosine-protein kinase LynHomo sapiens (human)
immune response-regulating cell surface receptor signaling pathwayTyrosine-protein kinase LynHomo sapiens (human)
Fc receptor mediated inhibitory signaling pathwayTyrosine-protein kinase LynHomo sapiens (human)
negative regulation of inflammatory response to antigenic stimulusTyrosine-protein kinase LynHomo sapiens (human)
regulation of B cell apoptotic processTyrosine-protein kinase LynHomo sapiens (human)
protein phosphorylationTyrosine-protein kinase LynHomo sapiens (human)
DNA damage responseTyrosine-protein kinase LynHomo sapiens (human)
response to sterol depletionTyrosine-protein kinase LynHomo sapiens (human)
signal transductionTyrosine-protein kinase LynHomo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayTyrosine-protein kinase LynHomo sapiens (human)
positive regulation of cell population proliferationTyrosine-protein kinase LynHomo sapiens (human)
negative regulation of cell population proliferationTyrosine-protein kinase LynHomo sapiens (human)
response to xenobiotic stimulusTyrosine-protein kinase LynHomo sapiens (human)
response to toxic substanceTyrosine-protein kinase LynHomo sapiens (human)
response to hormoneTyrosine-protein kinase LynHomo sapiens (human)
response to carbohydrateTyrosine-protein kinase LynHomo sapiens (human)
positive regulation of neuron projection developmentTyrosine-protein kinase LynHomo sapiens (human)
oligodendrocyte developmentTyrosine-protein kinase LynHomo sapiens (human)
response to organic cyclic compoundTyrosine-protein kinase LynHomo sapiens (human)
fatty acid transportTyrosine-protein kinase LynHomo sapiens (human)
peptidyl-tyrosine phosphorylationTyrosine-protein kinase LynHomo sapiens (human)
erythrocyte differentiationTyrosine-protein kinase LynHomo sapiens (human)
eosinophil differentiationTyrosine-protein kinase LynHomo sapiens (human)
positive regulation of cell migrationTyrosine-protein kinase LynHomo sapiens (human)
negative regulation of B cell proliferationTyrosine-protein kinase LynHomo sapiens (human)
T cell costimulationTyrosine-protein kinase LynHomo sapiens (human)
lipopolysaccharide-mediated signaling pathwayTyrosine-protein kinase LynHomo sapiens (human)
response to insulinTyrosine-protein kinase LynHomo sapiens (human)
regulation of mast cell activationTyrosine-protein kinase LynHomo sapiens (human)
regulation of cell adhesion mediated by integrinTyrosine-protein kinase LynHomo sapiens (human)
negative regulation of toll-like receptor 2 signaling pathwayTyrosine-protein kinase LynHomo sapiens (human)
toll-like receptor 4 signaling pathwayTyrosine-protein kinase LynHomo sapiens (human)
negative regulation of toll-like receptor 4 signaling pathwayTyrosine-protein kinase LynHomo sapiens (human)
cellular response to heatTyrosine-protein kinase LynHomo sapiens (human)
interleukin-5-mediated signaling pathwayTyrosine-protein kinase LynHomo sapiens (human)
Fc-epsilon receptor signaling pathwayTyrosine-protein kinase LynHomo sapiens (human)
Fc-gamma receptor signaling pathway involved in phagocytosisTyrosine-protein kinase LynHomo sapiens (human)
C-X-C chemokine receptor CXCR4 signaling pathwayTyrosine-protein kinase LynHomo sapiens (human)
positive regulation of tyrosine phosphorylation of STAT proteinTyrosine-protein kinase LynHomo sapiens (human)
response to amino acidTyrosine-protein kinase LynHomo sapiens (human)
regulation of mast cell degranulationTyrosine-protein kinase LynHomo sapiens (human)
negative regulation of MAP kinase activityTyrosine-protein kinase LynHomo sapiens (human)
positive regulation of MAPK cascadeTyrosine-protein kinase LynHomo sapiens (human)
regulation of erythrocyte differentiationTyrosine-protein kinase LynHomo sapiens (human)
protein autophosphorylationTyrosine-protein kinase LynHomo sapiens (human)
ephrin receptor signaling pathwayTyrosine-protein kinase LynHomo sapiens (human)
response to axon injuryTyrosine-protein kinase LynHomo sapiens (human)
negative regulation of immune responseTyrosine-protein kinase LynHomo sapiens (human)
B cell receptor signaling pathwayTyrosine-protein kinase LynHomo sapiens (human)
regulation of B cell receptor signaling pathwayTyrosine-protein kinase LynHomo sapiens (human)
leukocyte migrationTyrosine-protein kinase LynHomo sapiens (human)
regulation of release of sequestered calcium ion into cytosolTyrosine-protein kinase LynHomo sapiens (human)
positive regulation of glial cell proliferationTyrosine-protein kinase LynHomo sapiens (human)
positive regulation of Fc receptor mediated stimulatory signaling pathwayTyrosine-protein kinase LynHomo sapiens (human)
growth hormone receptor signaling pathway via JAK-STATTyrosine-protein kinase LynHomo sapiens (human)
regulation of ERK1 and ERK2 cascadeTyrosine-protein kinase LynHomo sapiens (human)
negative regulation of ERK1 and ERK2 cascadeTyrosine-protein kinase LynHomo sapiens (human)
positive regulation of oligodendrocyte progenitor proliferationTyrosine-protein kinase LynHomo sapiens (human)
negative regulation of mast cell proliferationTyrosine-protein kinase LynHomo sapiens (human)
positive regulation of mast cell proliferationTyrosine-protein kinase LynHomo sapiens (human)
cellular response to retinoic acidTyrosine-protein kinase LynHomo sapiens (human)
regulation of monocyte chemotaxisTyrosine-protein kinase LynHomo sapiens (human)
regulation of platelet aggregationTyrosine-protein kinase LynHomo sapiens (human)
dendritic cell differentiationTyrosine-protein kinase LynHomo sapiens (human)
negative regulation of intracellular signal transductionTyrosine-protein kinase LynHomo sapiens (human)
positive regulation of aspartic-type endopeptidase activity involved in amyloid precursor protein catabolic processTyrosine-protein kinase LynHomo sapiens (human)
positive regulation of dendritic cell apoptotic processTyrosine-protein kinase LynHomo sapiens (human)
neuron projection developmentTyrosine-protein kinase LynHomo sapiens (human)
innate immune responseTyrosine-protein kinase LynHomo sapiens (human)
response to antibioticTyrosine-protein kinase JAK1Homo sapiens (human)
protein phosphorylationTyrosine-protein kinase JAK1Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STATTyrosine-protein kinase JAK1Homo sapiens (human)
cytokine-mediated signaling pathwayTyrosine-protein kinase JAK1Homo sapiens (human)
positive regulation of homotypic cell-cell adhesionTyrosine-protein kinase JAK1Homo sapiens (human)
interleukin-15-mediated signaling pathwayTyrosine-protein kinase JAK1Homo sapiens (human)
interleukin-4-mediated signaling pathwayTyrosine-protein kinase JAK1Homo sapiens (human)
interleukin-2-mediated signaling pathwayTyrosine-protein kinase JAK1Homo sapiens (human)
interleukin-9-mediated signaling pathwayTyrosine-protein kinase JAK1Homo sapiens (human)
interleukin-11-mediated signaling pathwayTyrosine-protein kinase JAK1Homo sapiens (human)
type III interferon-mediated signaling pathwayTyrosine-protein kinase JAK1Homo sapiens (human)
type II interferon-mediated signaling pathwayTyrosine-protein kinase JAK1Homo sapiens (human)
type I interferon-mediated signaling pathwayTyrosine-protein kinase JAK1Homo sapiens (human)
interleukin-6-mediated signaling pathwayTyrosine-protein kinase JAK1Homo sapiens (human)
T-helper 17 cell lineage commitmentTyrosine-protein kinase JAK1Homo sapiens (human)
cellular response to virusTyrosine-protein kinase JAK1Homo sapiens (human)
interleukin-10-mediated signaling pathwayTyrosine-protein kinase JAK1Homo sapiens (human)
protein localization to cell-cell junctionTyrosine-protein kinase JAK1Homo sapiens (human)
positive regulation of protein localization to nucleusTyrosine-protein kinase JAK1Homo sapiens (human)
positive regulation of sprouting angiogenesisTyrosine-protein kinase JAK1Homo sapiens (human)
intracellular signal transductionTyrosine-protein kinase JAK1Homo sapiens (human)
tyrosine phosphorylation of STAT proteinTyrosine-protein kinase JAK1Homo sapiens (human)
cell differentiationTyrosine-protein kinase JAK1Homo sapiens (human)
growth hormone receptor signaling pathway via JAK-STATTyrosine-protein kinase JAK1Homo sapiens (human)
protein phosphorylationTyrosine-protein kinase TecHomo sapiens (human)
integrin-mediated signaling pathwayTyrosine-protein kinase TecHomo sapiens (human)
regulation of platelet activationTyrosine-protein kinase TecHomo sapiens (human)
intracellular signal transductionTyrosine-protein kinase TecHomo sapiens (human)
tissue regenerationTyrosine-protein kinase TecHomo sapiens (human)
B cell receptor signaling pathwayTyrosine-protein kinase TecHomo sapiens (human)
adaptive immune responseTyrosine-protein kinase TecHomo sapiens (human)
T cell receptor signaling pathwayTyrosine-protein kinase TecHomo sapiens (human)
protein phosphorylationCytoplasmic tyrosine-protein kinase BMXHomo sapiens (human)
phosphatidylinositol biosynthetic processCytoplasmic tyrosine-protein kinase BMXHomo sapiens (human)
apoptotic processCytoplasmic tyrosine-protein kinase BMXHomo sapiens (human)
cell adhesionCytoplasmic tyrosine-protein kinase BMXHomo sapiens (human)
signal transductionCytoplasmic tyrosine-protein kinase BMXHomo sapiens (human)
mesoderm developmentCytoplasmic tyrosine-protein kinase BMXHomo sapiens (human)
intracellular signal transductionCytoplasmic tyrosine-protein kinase BMXHomo sapiens (human)
protein autophosphorylationCytoplasmic tyrosine-protein kinase BMXHomo sapiens (human)
B cell receptor signaling pathwayCytoplasmic tyrosine-protein kinase BMXHomo sapiens (human)
adaptive immune responseCytoplasmic tyrosine-protein kinase BMXHomo sapiens (human)
adaptive immune responseTyrosine-protein kinase JAK3Homo sapiens (human)
negative regulation of dendritic cell cytokine productionTyrosine-protein kinase JAK3Homo sapiens (human)
protein phosphorylationTyrosine-protein kinase JAK3Homo sapiens (human)
enzyme-linked receptor protein signaling pathwayTyrosine-protein kinase JAK3Homo sapiens (human)
tyrosine phosphorylation of STAT proteinTyrosine-protein kinase JAK3Homo sapiens (human)
peptidyl-tyrosine phosphorylationTyrosine-protein kinase JAK3Homo sapiens (human)
B cell differentiationTyrosine-protein kinase JAK3Homo sapiens (human)
negative regulation of interleukin-10 productionTyrosine-protein kinase JAK3Homo sapiens (human)
negative regulation of interleukin-12 productionTyrosine-protein kinase JAK3Homo sapiens (human)
intracellular signal transductionTyrosine-protein kinase JAK3Homo sapiens (human)
interleukin-15-mediated signaling pathwayTyrosine-protein kinase JAK3Homo sapiens (human)
interleukin-4-mediated signaling pathwayTyrosine-protein kinase JAK3Homo sapiens (human)
interleukin-2-mediated signaling pathwayTyrosine-protein kinase JAK3Homo sapiens (human)
interleukin-9-mediated signaling pathwayTyrosine-protein kinase JAK3Homo sapiens (human)
T cell homeostasisTyrosine-protein kinase JAK3Homo sapiens (human)
innate immune responseTyrosine-protein kinase JAK3Homo sapiens (human)
negative regulation of FasL productionTyrosine-protein kinase JAK3Homo sapiens (human)
negative regulation of T-helper 1 cell differentiationTyrosine-protein kinase JAK3Homo sapiens (human)
regulation of receptor signaling pathway via JAK-STATTyrosine-protein kinase JAK3Homo sapiens (human)
negative regulation of T cell activationTyrosine-protein kinase JAK3Homo sapiens (human)
growth hormone receptor signaling pathway via JAK-STATTyrosine-protein kinase JAK3Homo sapiens (human)
regulation of T cell apoptotic processTyrosine-protein kinase JAK3Homo sapiens (human)
negative regulation of thymocyte apoptotic processTyrosine-protein kinase JAK3Homo sapiens (human)
response to interleukin-2Tyrosine-protein kinase JAK3Homo sapiens (human)
response to interleukin-4Tyrosine-protein kinase JAK3Homo sapiens (human)
response to interleukin-15Tyrosine-protein kinase JAK3Homo sapiens (human)
response to interleukin-9Tyrosine-protein kinase JAK3Homo sapiens (human)
regulation of apoptotic processTyrosine-protein kinase JAK3Homo sapiens (human)
cell differentiationTyrosine-protein kinase JAK3Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STATTyrosine-protein kinase JAK3Homo sapiens (human)
cytokine-mediated signaling pathwayTyrosine-protein kinase JAK3Homo sapiens (human)
neutrophil homeostasisTyrosine-protein kinase BTKHomo sapiens (human)
positive regulation of type III hypersensitivityTyrosine-protein kinase BTKHomo sapiens (human)
positive regulation of type I hypersensitivityTyrosine-protein kinase BTKHomo sapiens (human)
adaptive immune responseTyrosine-protein kinase BTKHomo sapiens (human)
B cell affinity maturationTyrosine-protein kinase BTKHomo sapiens (human)
histamine secretion by mast cellTyrosine-protein kinase BTKHomo sapiens (human)
positive regulation of immunoglobulin productionTyrosine-protein kinase BTKHomo sapiens (human)
regulation of B cell cytokine productionTyrosine-protein kinase BTKHomo sapiens (human)
MyD88-dependent toll-like receptor signaling pathwayTyrosine-protein kinase BTKHomo sapiens (human)
regulation of B cell apoptotic processTyrosine-protein kinase BTKHomo sapiens (human)
protein phosphorylationTyrosine-protein kinase BTKHomo sapiens (human)
mesoderm developmentTyrosine-protein kinase BTKHomo sapiens (human)
peptidyl-tyrosine phosphorylationTyrosine-protein kinase BTKHomo sapiens (human)
calcium-mediated signalingTyrosine-protein kinase BTKHomo sapiens (human)
proteoglycan catabolic processTyrosine-protein kinase BTKHomo sapiens (human)
negative regulation of B cell proliferationTyrosine-protein kinase BTKHomo sapiens (human)
positive regulation of B cell proliferationTyrosine-protein kinase BTKHomo sapiens (human)
response to lipopolysaccharideTyrosine-protein kinase BTKHomo sapiens (human)
negative regulation of interleukin-10 productionTyrosine-protein kinase BTKHomo sapiens (human)
positive regulation of interleukin-6 productionTyrosine-protein kinase BTKHomo sapiens (human)
positive regulation of tumor necrosis factor productionTyrosine-protein kinase BTKHomo sapiens (human)
cellular response to reactive oxygen speciesTyrosine-protein kinase BTKHomo sapiens (human)
intracellular signal transductionTyrosine-protein kinase BTKHomo sapiens (human)
Fc-epsilon receptor signaling pathwayTyrosine-protein kinase BTKHomo sapiens (human)
B cell activationTyrosine-protein kinase BTKHomo sapiens (human)
innate immune responseTyrosine-protein kinase BTKHomo sapiens (human)
positive regulation of B cell differentiationTyrosine-protein kinase BTKHomo sapiens (human)
cell maturationTyrosine-protein kinase BTKHomo sapiens (human)
positive regulation of phagocytosisTyrosine-protein kinase BTKHomo sapiens (human)
B cell receptor signaling pathwayTyrosine-protein kinase BTKHomo sapiens (human)
positive regulation of NF-kappaB transcription factor activityTyrosine-protein kinase BTKHomo sapiens (human)
monocyte proliferationTyrosine-protein kinase BTKHomo sapiens (human)
cellular response to molecule of fungal originTyrosine-protein kinase BTKHomo sapiens (human)
apoptotic signaling pathwayTyrosine-protein kinase BTKHomo sapiens (human)
cellular response to interleukin-7Tyrosine-protein kinase BTKHomo sapiens (human)
positive regulation of interleukin-17A productionTyrosine-protein kinase BTKHomo sapiens (human)
positive regulation of NLRP3 inflammasome complex assemblyTyrosine-protein kinase BTKHomo sapiens (human)
positive regulation of synoviocyte proliferationTyrosine-protein kinase BTKHomo sapiens (human)
eosinophil homeostasisTyrosine-protein kinase BTKHomo sapiens (human)
T cell receptor signaling pathwayTyrosine-protein kinase BTKHomo sapiens (human)
cellular response to xenobiotic stimulusEarly activation antigen CD69Homo 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 (71)

Processvia Protein(s)Taxonomy
protein kinase activityTyrosine-protein kinase JAK2Homo sapiens (human)
protein tyrosine kinase activityTyrosine-protein kinase JAK2Homo sapiens (human)
non-membrane spanning protein tyrosine kinase activityTyrosine-protein kinase JAK2Homo sapiens (human)
signaling receptor bindingTyrosine-protein kinase JAK2Homo sapiens (human)
growth hormone receptor bindingTyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-12 receptor bindingTyrosine-protein kinase JAK2Homo sapiens (human)
protein bindingTyrosine-protein kinase JAK2Homo sapiens (human)
ATP bindingTyrosine-protein kinase JAK2Homo sapiens (human)
protein kinase bindingTyrosine-protein kinase JAK2Homo sapiens (human)
heme bindingTyrosine-protein kinase JAK2Homo sapiens (human)
type 1 angiotensin receptor bindingTyrosine-protein kinase JAK2Homo sapiens (human)
acetylcholine receptor bindingTyrosine-protein kinase JAK2Homo sapiens (human)
histone H3Y41 kinase activityTyrosine-protein kinase JAK2Homo sapiens (human)
SH2 domain bindingTyrosine-protein kinase JAK2Homo sapiens (human)
histone bindingTyrosine-protein kinase JAK2Homo sapiens (human)
identical protein bindingTyrosine-protein kinase JAK2Homo sapiens (human)
phosphatidylinositol 3-kinase bindingTyrosine-protein kinase JAK2Homo sapiens (human)
insulin receptor substrate bindingTyrosine-protein kinase JAK2Homo sapiens (human)
metal ion bindingTyrosine-protein kinase JAK2Homo sapiens (human)
peptide hormone receptor bindingTyrosine-protein kinase JAK2Homo sapiens (human)
epidermal growth factor receptor activityEpidermal growth factor receptorHomo sapiens (human)
virus receptor activityEpidermal growth factor receptorHomo sapiens (human)
chromatin bindingEpidermal growth factor receptorHomo sapiens (human)
double-stranded DNA bindingEpidermal growth factor receptorHomo sapiens (human)
MAP kinase kinase kinase activityEpidermal growth factor receptorHomo sapiens (human)
protein tyrosine kinase activityEpidermal growth factor receptorHomo sapiens (human)
transmembrane receptor protein tyrosine kinase activityEpidermal growth factor receptorHomo sapiens (human)
transmembrane signaling receptor activityEpidermal growth factor receptorHomo sapiens (human)
epidermal growth factor receptor activityEpidermal growth factor receptorHomo sapiens (human)
integrin bindingEpidermal growth factor receptorHomo sapiens (human)
protein bindingEpidermal growth factor receptorHomo sapiens (human)
calmodulin bindingEpidermal growth factor receptorHomo sapiens (human)
ATP bindingEpidermal growth factor receptorHomo sapiens (human)
enzyme bindingEpidermal growth factor receptorHomo sapiens (human)
kinase bindingEpidermal growth factor receptorHomo sapiens (human)
protein kinase bindingEpidermal growth factor receptorHomo sapiens (human)
protein phosphatase bindingEpidermal growth factor receptorHomo sapiens (human)
protein tyrosine kinase activator activityEpidermal growth factor receptorHomo sapiens (human)
transmembrane receptor protein tyrosine kinase activator activityEpidermal growth factor receptorHomo sapiens (human)
ubiquitin protein ligase bindingEpidermal growth factor receptorHomo sapiens (human)
identical protein bindingEpidermal growth factor receptorHomo sapiens (human)
cadherin bindingEpidermal growth factor receptorHomo sapiens (human)
actin filament bindingEpidermal growth factor receptorHomo sapiens (human)
ATPase bindingEpidermal growth factor receptorHomo sapiens (human)
epidermal growth factor bindingEpidermal growth factor receptorHomo 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 tyrosine kinase activityTyrosine-protein kinase LynHomo sapiens (human)
non-membrane spanning protein tyrosine kinase activityTyrosine-protein kinase LynHomo sapiens (human)
platelet-derived growth factor receptor bindingTyrosine-protein kinase LynHomo sapiens (human)
integrin bindingTyrosine-protein kinase LynHomo sapiens (human)
protein bindingTyrosine-protein kinase LynHomo sapiens (human)
ATP bindingTyrosine-protein kinase LynHomo sapiens (human)
kinase activityTyrosine-protein kinase LynHomo sapiens (human)
SH3 domain bindingTyrosine-protein kinase LynHomo sapiens (human)
ubiquitin protein ligase bindingTyrosine-protein kinase LynHomo sapiens (human)
gamma-tubulin bindingTyrosine-protein kinase LynHomo sapiens (human)
glycosphingolipid bindingTyrosine-protein kinase LynHomo sapiens (human)
transmembrane transporter bindingTyrosine-protein kinase LynHomo sapiens (human)
ephrin receptor bindingTyrosine-protein kinase LynHomo sapiens (human)
phosphoprotein bindingTyrosine-protein kinase LynHomo sapiens (human)
scaffold protein bindingTyrosine-protein kinase LynHomo sapiens (human)
phosphorylation-dependent protein bindingTyrosine-protein kinase LynHomo sapiens (human)
phosphatidylinositol 3-kinase activator activityTyrosine-protein kinase LynHomo sapiens (human)
signaling receptor bindingTyrosine-protein kinase LynHomo sapiens (human)
protein tyrosine kinase activityTyrosine-protein kinase JAK1Homo sapiens (human)
non-membrane spanning protein tyrosine kinase activityTyrosine-protein kinase JAK1Homo sapiens (human)
growth hormone receptor bindingTyrosine-protein kinase JAK1Homo sapiens (human)
protein bindingTyrosine-protein kinase JAK1Homo sapiens (human)
ATP bindingTyrosine-protein kinase JAK1Homo sapiens (human)
protein phosphatase bindingTyrosine-protein kinase JAK1Homo sapiens (human)
ubiquitin protein ligase bindingTyrosine-protein kinase JAK1Homo sapiens (human)
CCR5 chemokine receptor bindingTyrosine-protein kinase JAK1Homo sapiens (human)
metal ion bindingTyrosine-protein kinase JAK1Homo sapiens (human)
non-membrane spanning protein tyrosine kinase activityTyrosine-protein kinase TecHomo sapiens (human)
protein bindingTyrosine-protein kinase TecHomo sapiens (human)
ATP bindingTyrosine-protein kinase TecHomo sapiens (human)
phospholipid bindingTyrosine-protein kinase TecHomo sapiens (human)
metal ion bindingTyrosine-protein kinase TecHomo sapiens (human)
protein tyrosine kinase activityCytoplasmic tyrosine-protein kinase BMXHomo sapiens (human)
non-membrane spanning protein tyrosine kinase activityCytoplasmic tyrosine-protein kinase BMXHomo sapiens (human)
protein bindingCytoplasmic tyrosine-protein kinase BMXHomo sapiens (human)
ATP bindingCytoplasmic tyrosine-protein kinase BMXHomo sapiens (human)
metal ion bindingCytoplasmic tyrosine-protein kinase BMXHomo sapiens (human)
protein tyrosine kinase activityTyrosine-protein kinase JAK3Homo sapiens (human)
protein bindingTyrosine-protein kinase JAK3Homo sapiens (human)
ATP bindingTyrosine-protein kinase JAK3Homo sapiens (human)
protein phosphatase bindingTyrosine-protein kinase JAK3Homo sapiens (human)
growth hormone receptor bindingTyrosine-protein kinase JAK3Homo sapiens (human)
non-membrane spanning protein tyrosine kinase activityTyrosine-protein kinase JAK3Homo sapiens (human)
protein tyrosine kinase activityTyrosine-protein kinase BTKHomo sapiens (human)
non-membrane spanning protein tyrosine kinase activityTyrosine-protein kinase BTKHomo sapiens (human)
protein bindingTyrosine-protein kinase BTKHomo sapiens (human)
ATP bindingTyrosine-protein kinase BTKHomo sapiens (human)
phosphatidylinositol-3,4,5-trisphosphate bindingTyrosine-protein kinase BTKHomo sapiens (human)
phospholipase activator activityTyrosine-protein kinase BTKHomo sapiens (human)
identical protein bindingTyrosine-protein kinase BTKHomo sapiens (human)
phospholipase bindingTyrosine-protein kinase BTKHomo sapiens (human)
metal ion bindingTyrosine-protein kinase BTKHomo sapiens (human)
transmembrane signaling receptor activityEarly activation antigen CD69Homo sapiens (human)
protein bindingEarly activation antigen CD69Homo sapiens (human)
carbohydrate bindingEarly activation antigen CD69Homo sapiens (human)
identical protein bindingEarly activation antigen CD69Homo 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 (60)

Processvia Protein(s)Taxonomy
extrinsic component of plasma membraneTyrosine-protein kinase JAK2Homo sapiens (human)
extrinsic component of cytoplasmic side of plasma membraneTyrosine-protein kinase JAK2Homo sapiens (human)
nucleusTyrosine-protein kinase JAK2Homo sapiens (human)
nucleoplasmTyrosine-protein kinase JAK2Homo sapiens (human)
cytoplasmTyrosine-protein kinase JAK2Homo sapiens (human)
cytosolTyrosine-protein kinase JAK2Homo sapiens (human)
cytoskeletonTyrosine-protein kinase JAK2Homo sapiens (human)
plasma membraneTyrosine-protein kinase JAK2Homo sapiens (human)
caveolaTyrosine-protein kinase JAK2Homo sapiens (human)
focal adhesionTyrosine-protein kinase JAK2Homo sapiens (human)
granulocyte macrophage colony-stimulating factor receptor complexTyrosine-protein kinase JAK2Homo sapiens (human)
endosome lumenTyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-12 receptor complexTyrosine-protein kinase JAK2Homo sapiens (human)
membrane raftTyrosine-protein kinase JAK2Homo sapiens (human)
interleukin-23 receptor complexTyrosine-protein kinase JAK2Homo sapiens (human)
postsynapseTyrosine-protein kinase JAK2Homo sapiens (human)
glutamatergic synapseTyrosine-protein kinase JAK2Homo sapiens (human)
euchromatinTyrosine-protein kinase JAK2Homo sapiens (human)
cytosolTyrosine-protein kinase JAK2Homo sapiens (human)
endosomeEpidermal growth factor receptorHomo sapiens (human)
plasma membraneEpidermal growth factor receptorHomo sapiens (human)
ruffle membraneEpidermal growth factor receptorHomo sapiens (human)
Golgi membraneEpidermal growth factor receptorHomo sapiens (human)
extracellular spaceEpidermal growth factor receptorHomo sapiens (human)
nucleusEpidermal growth factor receptorHomo sapiens (human)
cytoplasmEpidermal growth factor receptorHomo sapiens (human)
endosomeEpidermal growth factor receptorHomo sapiens (human)
endoplasmic reticulum membraneEpidermal growth factor receptorHomo sapiens (human)
plasma membraneEpidermal growth factor receptorHomo sapiens (human)
focal adhesionEpidermal growth factor receptorHomo sapiens (human)
cell surfaceEpidermal growth factor receptorHomo sapiens (human)
endosome membraneEpidermal growth factor receptorHomo sapiens (human)
membraneEpidermal growth factor receptorHomo sapiens (human)
basolateral plasma membraneEpidermal growth factor receptorHomo sapiens (human)
apical plasma membraneEpidermal growth factor receptorHomo sapiens (human)
cell junctionEpidermal growth factor receptorHomo sapiens (human)
clathrin-coated endocytic vesicle membraneEpidermal growth factor receptorHomo sapiens (human)
early endosome membraneEpidermal growth factor receptorHomo sapiens (human)
nuclear membraneEpidermal growth factor receptorHomo sapiens (human)
membrane raftEpidermal growth factor receptorHomo sapiens (human)
perinuclear region of cytoplasmEpidermal growth factor receptorHomo sapiens (human)
multivesicular body, internal vesicle lumenEpidermal growth factor receptorHomo sapiens (human)
intracellular vesicleEpidermal growth factor receptorHomo sapiens (human)
protein-containing complexEpidermal growth factor receptorHomo sapiens (human)
receptor complexEpidermal growth factor receptorHomo sapiens (human)
Shc-EGFR complexEpidermal growth factor receptorHomo sapiens (human)
basal plasma membraneEpidermal growth factor receptorHomo 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)
plasma membraneTyrosine-protein kinase LynHomo sapiens (human)
cytoplasmic side of plasma membraneTyrosine-protein kinase LynHomo sapiens (human)
nucleusTyrosine-protein kinase LynHomo sapiens (human)
cytoplasmTyrosine-protein kinase LynHomo sapiens (human)
lysosomal membraneTyrosine-protein kinase LynHomo sapiens (human)
Golgi apparatusTyrosine-protein kinase LynHomo sapiens (human)
cytosolTyrosine-protein kinase LynHomo sapiens (human)
plasma membraneTyrosine-protein kinase LynHomo sapiens (human)
adherens junctionTyrosine-protein kinase LynHomo sapiens (human)
mitochondrial cristaTyrosine-protein kinase LynHomo sapiens (human)
endocytic vesicle membraneTyrosine-protein kinase LynHomo sapiens (human)
intracellular membrane-bounded organelleTyrosine-protein kinase LynHomo sapiens (human)
membrane raftTyrosine-protein kinase LynHomo sapiens (human)
perinuclear region of cytoplasmTyrosine-protein kinase LynHomo sapiens (human)
extracellular exosomeTyrosine-protein kinase LynHomo sapiens (human)
glutamatergic synapseTyrosine-protein kinase LynHomo sapiens (human)
postsynaptic specialization, intracellular componentTyrosine-protein kinase LynHomo sapiens (human)
integrin alpha2-beta1 complexTyrosine-protein kinase LynHomo sapiens (human)
cytoplasmTyrosine-protein kinase JAK1Homo sapiens (human)
plasma membraneTyrosine-protein kinase JAK1Homo sapiens (human)
cytoplasmic side of plasma membraneTyrosine-protein kinase JAK1Homo sapiens (human)
extrinsic component of cytoplasmic side of plasma membraneTyrosine-protein kinase JAK1Homo sapiens (human)
nucleusTyrosine-protein kinase JAK1Homo sapiens (human)
cytoplasmTyrosine-protein kinase JAK1Homo sapiens (human)
endosomeTyrosine-protein kinase JAK1Homo sapiens (human)
cytosolTyrosine-protein kinase JAK1Homo sapiens (human)
cytoskeletonTyrosine-protein kinase JAK1Homo sapiens (human)
focal adhesionTyrosine-protein kinase JAK1Homo sapiens (human)
cytosolTyrosine-protein kinase JAK1Homo sapiens (human)
cytosolTyrosine-protein kinase TecHomo sapiens (human)
cytoskeletonTyrosine-protein kinase TecHomo sapiens (human)
plasma membraneTyrosine-protein kinase TecHomo sapiens (human)
plasma membraneTyrosine-protein kinase TecHomo sapiens (human)
nucleoplasmCytoplasmic tyrosine-protein kinase BMXHomo sapiens (human)
cytosolCytoplasmic tyrosine-protein kinase BMXHomo sapiens (human)
plasma membraneCytoplasmic tyrosine-protein kinase BMXHomo sapiens (human)
ruffle membraneCytoplasmic tyrosine-protein kinase BMXHomo sapiens (human)
plasma membraneCytoplasmic tyrosine-protein kinase BMXHomo sapiens (human)
extrinsic component of plasma membraneTyrosine-protein kinase JAK3Homo sapiens (human)
extrinsic component of cytoplasmic side of plasma membraneTyrosine-protein kinase JAK3Homo sapiens (human)
endosomeTyrosine-protein kinase JAK3Homo sapiens (human)
cytosolTyrosine-protein kinase JAK3Homo sapiens (human)
cytoskeletonTyrosine-protein kinase JAK3Homo sapiens (human)
plasma membraneTyrosine-protein kinase JAK3Homo sapiens (human)
cytosolTyrosine-protein kinase JAK3Homo sapiens (human)
nucleusTyrosine-protein kinase BTKHomo sapiens (human)
cytoplasmTyrosine-protein kinase BTKHomo sapiens (human)
cytosolTyrosine-protein kinase BTKHomo sapiens (human)
plasma membraneTyrosine-protein kinase BTKHomo sapiens (human)
cytoplasmic vesicleTyrosine-protein kinase BTKHomo sapiens (human)
membrane raftTyrosine-protein kinase BTKHomo sapiens (human)
perinuclear region of cytoplasmTyrosine-protein kinase BTKHomo sapiens (human)
plasma membraneTyrosine-protein kinase BTKHomo sapiens (human)
plasma membraneEarly activation antigen CD69Homo sapiens (human)
protein-containing complexEarly activation antigen CD69Homo sapiens (human)
external side of plasma membraneEarly activation antigen CD69Homo 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 (128)

Assay IDTitleYearJournalArticle
AID1324655Antiproliferative activity against human Ramos cells after 48 hrs by CCK-8 assay2016ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
Discovery of Novel Bruton's Tyrosine Kinase (BTK) Inhibitors Bearing a
AID1869077Inhibition of BTK T474I mutant (unknown origin) expressed in baculovirus infected Trichoplusia ni pro cells incubated for 30 mins in presence of ATP by Microfluidic chip based mobility shift assay2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Medicinal Chemistry Strategies for the Development of Bruton's Tyrosine Kinase Inhibitors against Resistance.
AID1820501Inhibition of BTK phosphorylation in human whole blood assessed as reduction in BTK phosphorylation incubated for 30 mins2022Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
Discovery and Preclinical Characterization of BIIB091, a Reversible, Selective BTK Inhibitor for the Treatment of Multiple Sclerosis.
AID1468817Selectivity ratio of IC50 for recombinant human full length His-tagged STK16 to IC50 for recombinant human full length His-tagged BTK2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development.
AID1469889Inhibition of recombinant human N-terminal GST-tagged JAK3 (781 to end residues) expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr)4:1 as substrate pretreated for 60 mins followed by substrate addition after 1 hr by ADP-Glo luminescen
AID1468808Inhibition of recombinant human cytoplasmic GST-tagged LTK expressed in baculovirus at 1 uM by Z'-LYTE assay2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development.
AID1650542Inhibition of recombinant human N-terminal GST-tagged JAK1 (850 to 1154 residues) expressed in baculovirus expression system using Ulight-Poly GT as substrate incubated for 2 hrs by Lanthascreen TR-FRET assay2020Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2
Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors.
AID1809419Inhibition of Btk (unknown origin) assessed as ratio of Kinact/Ki2021Journal of medicinal chemistry, 09-09, Volume: 64, Issue:17
Discovery of the Bruton's Tyrosine Kinase Inhibitor Clinical Candidate TAK-020 (
AID1324661Induction of apoptosis in human Ramos cells assessed as late apoptotic cells at 10 uM after 48 hrs by annexin V/FITC propidium iodide staining based flow cytometry relative to control2016ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
Discovery of Novel Bruton's Tyrosine Kinase (BTK) Inhibitors Bearing a
AID1484561Induction of apoptosis in human Ramos cells assessed as early apoptotic cells at 10 uM after 48 hrs by annexin V-FITC/propidium iodide staining-based flow cytometric analysis relative to control2017European journal of medicinal chemistry, Jul-28, Volume: 135Design and synthesis of sulfonamide-substituted diphenylpyrimidines (SFA-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B-cell lymphoblastic leukemia.
AID1869074Inhibition of His-tagged full-length recombinant wild-type human BTK (Ala2 to Ser659 residues) expressed in baculovirus infected insect cells incubated for 30 mins in presence of ATP by Microfluidic chip based mobility shift assay2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Medicinal Chemistry Strategies for the Development of Bruton's Tyrosine Kinase Inhibitors against Resistance.
AID1553424Cytotoxicity against human BJ cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay2019Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
Design, synthesis and biological evaluation of novel dithiocarbamate-substituted diphenylaminopyrimidine derivatives as BTK inhibitors.
AID1426144Induction of apoptosis in human Ramos cells assessed as viable cells at 10 uM after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 94.3%)2017European journal of medicinal chemistry, Jan-27, Volume: 126Structural optimization of diphenylpyrimidine derivatives (DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B leukemia cell lines.
AID1469895Ratio of Kinact to Ki for full length recombinant human N-terminal His tagged BKT expressed in baculovirus infected Sf9 insect cells
AID1334888Cell cycle arrest in human Ramos cells assessed as accumulation at S phase at 10 uM measured after 48 hrs by propidium iodide based flow cytometry (Rvb = 55.07 %)2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Design and synthesis of phosphoryl-substituted diphenylpyrimidines (Pho-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors: Targeted treatment of B lymphoblastic leukemia cell lines.
AID1426145Induction of apoptosis in human Ramos cells assessed as early apoptotic cells at 10 uM after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 1.7%)2017European journal of medicinal chemistry, Jan-27, Volume: 126Structural optimization of diphenylpyrimidine derivatives (DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B leukemia cell lines.
AID1553423Cytotoxicity against human HELF cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay2019Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
Design, synthesis and biological evaluation of novel dithiocarbamate-substituted diphenylaminopyrimidine derivatives as BTK inhibitors.
AID1401319Induction of apoptosis in human Ramos cells assessed as early apoptotic cells at 10 uM after 72 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 0.0%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma.
AID1650556Metabolic stability in human liver microsomes assessed as compound remaining at 0.2 uM incubated for 60 mins by UPLC-MS/MS analysis2020Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2
Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors.
AID1468806Inhibition of recombinant human catalytic GST-tagged JAK3 expressed in baculovirus at 1 uM by Z'-LYTE assay2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development.
AID1334877Inhibition of human recombinant full-length N-terminal His-tagged BTK expressed in baculovirus infected Sf9 insect cells measured after 60 mins by ADP-Glo kinase assay2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Design and synthesis of phosphoryl-substituted diphenylpyrimidines (Pho-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors: Targeted treatment of B lymphoblastic leukemia cell lines.
AID1869073Inhibition of BTK T474M mutant (unknown origin) expressed in baculovirus infected Trichoplusia ni pro cells incubated for 30 mins in presence of ATP by Microfluidic chip based mobility shift assay2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Medicinal Chemistry Strategies for the Development of Bruton's Tyrosine Kinase Inhibitors against Resistance.
AID1650554Metabolic stability in human liver microsomes assessed as half life at 0.2 uM incubated for 60 mins by UPLC-MS/MS analysis2020Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2
Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors.
AID1553414Cytotoxicity against human HepG2 cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay2019Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
Design, synthesis and biological evaluation of novel dithiocarbamate-substituted diphenylaminopyrimidine derivatives as BTK inhibitors.
AID1324656Inhibition of recombinant human N-terminal His-tagged BTK expressed in baculovirus infected sf9 cells using poly(4:1 Glu,Tyr) as substrate by ADP-Glo kinase assay2016ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
Discovery of Novel Bruton's Tyrosine Kinase (BTK) Inhibitors Bearing a
AID1401320Induction of apoptosis in human Ramos cells assessed as viable cells at 10 uM after 72 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 98.7%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma.
AID1468807Inhibition of recombinant human cytoplasmic GST-tagged EGFR expressed in baculovirus at 1 uM by Z'-LYTE assay2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development.
AID1484562Induction of apoptosis in human Ramos cells assessed as late apoptotic cells at 10 uM after 48 hrs by annexin V-FITC/propidium iodide staining-based flow cytometric analysis relative to control2017European journal of medicinal chemistry, Jul-28, Volume: 135Design and synthesis of sulfonamide-substituted diphenylpyrimidines (SFA-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B-cell lymphoblastic leukemia.
AID1650550Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay2020Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2
Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors.
AID1650541Inhibition of recombinant human His-tagged full length BTK expressed in baculovirus expression system using Ulight-Poly GT as substrate incubated for 2 hrs by Lanthascreen TR-FRET assay2020Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2
Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors.
AID1468805Inhibition of recombinant human full length His-tagged BLK expressed in baculovirus at 1 uM by Z'-LYTE assay2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development.
AID1401311Antiproliferative activity against human NAMALWA cells after 72 hrs by CCK-8 assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma.
AID1334900Induction of apoptosis in human Ramos cells assessed as necrotic cells at 10 uM measured after 48 hrs by Annexin V-FITC/propidium iodide based flow cytometry (Rvb = 0.2 %)2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Design and synthesis of phosphoryl-substituted diphenylpyrimidines (Pho-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors: Targeted treatment of B lymphoblastic leukemia cell lines.
AID1650544Inhibition of recombinant human N-terminal His-tagged JAK3 (795 to 1124 residues) expressed in baculovirus expression system using Ulight-Poly GT as substrate incubated for 2 hrs by Lanthascreen TR-FRET assay2020Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2
Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors.
AID1469888Inhibition of full length recombinant human N-terminal GST-tagged BMX expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr)4:1 as substrate pretreated for 60 mins followed by substrate addition after 1 hr by ADP-Glo luminescence assay
AID1553407Antiproliferative activity against human Ramos cells assessed as reduction in cell growth incubated for 48 hrs by MTS assay2019Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
Design, synthesis and biological evaluation of novel dithiocarbamate-substituted diphenylaminopyrimidine derivatives as BTK inhibitors.
AID1553419Cytotoxicity against human A549 cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay2019Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
Design, synthesis and biological evaluation of novel dithiocarbamate-substituted diphenylaminopyrimidine derivatives as BTK inhibitors.
AID1468804Inhibition of human full length GST-tagged TXK expressed in baculovirus at 1 uM by Z'-LYTE assay2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development.
AID1650549Antiproliferative activity against human Raji cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay2020Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2
Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors.
AID1334897Induction of apoptosis in human Ramos cells assessed as viable cells at 10 uM measured after 48 hrs by Annexin V-FITC/propidium iodide based flow cytometry relative to control2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Design and synthesis of phosphoryl-substituted diphenylpyrimidines (Pho-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors: Targeted treatment of B lymphoblastic leukemia cell lines.
AID1468815Selectivity ratio of IC50 for human full length GST-tagged TXK to IC50 for recombinant human full length His-tagged BTK2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development.
AID1426158Cell cycle arrest in human Ramos cells assessed as accumulation at G2/M phase at 10 uM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 1.58%)2017European journal of medicinal chemistry, Jan-27, Volume: 126Structural optimization of diphenylpyrimidine derivatives (DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B leukemia cell lines.
AID1553409Cytotoxicity against human K562 cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay2019Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
Design, synthesis and biological evaluation of novel dithiocarbamate-substituted diphenylaminopyrimidine derivatives as BTK inhibitors.
AID1553408Antiproliferative activity against human Raji cells assessed as reduction in cell growth incubated for 48 hrs by MTS assay2019Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
Design, synthesis and biological evaluation of novel dithiocarbamate-substituted diphenylaminopyrimidine derivatives as BTK inhibitors.
AID1650551Antiproliferative activity against human HEL cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay2020Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2
Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors.
AID1469887Inhibition of full length recombinant human N-terminal His tagged BKT expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr)4:1 as substrate pretreated for 60 mins followed by substrate addition after 1 hr by ADP-Glo luminescence assay
AID1468809Inhibition of recombinant human cytoplasmic GST-tagged ERBB4 expressed in baculovirus at 1 uM by Z'-LYTE assay2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development.
AID1484560Induction of apoptosis in human Ramos cells assessed as viable cells at 10 uM after 48 hrs by annexin V-FITC/propidium iodide staining-based flow cytometric analysis relative to control2017European journal of medicinal chemistry, Jul-28, Volume: 135Design and synthesis of sulfonamide-substituted diphenylpyrimidines (SFA-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B-cell lymphoblastic leukemia.
AID1820500Inhibition of human BTK using fluorescein-labeled polyGAT peptide as substrate incubated for 30 mins by FRET assay2022Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
Discovery and Preclinical Characterization of BIIB091, a Reversible, Selective BTK Inhibitor for the Treatment of Multiple Sclerosis.
AID1468811Selectivity ratio of IC50 for cytoplasmic recombinant human full length His-tagged BMX to IC50 for recombinant human full length His-tagged BTK2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development.
AID1553417Cytotoxicity against human PC3 cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay2019Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
Design, synthesis and biological evaluation of novel dithiocarbamate-substituted diphenylaminopyrimidine derivatives as BTK inhibitors.
AID1553406Inhibition of human recombinant full length BTK expressed in baculovirus in Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate incubated for 1 hr by ADP-Glo assay2019Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
Design, synthesis and biological evaluation of novel dithiocarbamate-substituted diphenylaminopyrimidine derivatives as BTK inhibitors.
AID1468802Inhibition of recombinant human full length His-tagged BTK expressed in baculovirus at 1 uM by Z'-LYTE assay2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development.
AID1401318Induction of apoptosis in human Ramos cells assessed as late apoptotic cells at 10 uM after 72 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 0.5%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma.
AID1553421Cytotoxicity against human NCI-H3122 cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay2019Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
Design, synthesis and biological evaluation of novel dithiocarbamate-substituted diphenylaminopyrimidine derivatives as BTK inhibitors.
AID1869076Inhibition of BTK C481R mutant (unknown origin) expressed in baculovirus infected Trichoplusia ni pro cells incubated for 30 mins in presence of ATP by Microfluidic chip based mobility shift assay2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Medicinal Chemistry Strategies for the Development of Bruton's Tyrosine Kinase Inhibitors against Resistance.
AID1426141Antiproliferative activity against human Ramos cells after 48 hrs by CCK-8 assay2017European journal of medicinal chemistry, Jan-27, Volume: 126Structural optimization of diphenylpyrimidine derivatives (DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B leukemia cell lines.
AID1553432Antitumor activity in human Ramos cells xenografted in NOD/SCID mouse assessed as reduction in tumor growth at 30 mg/kg/day, ip administered daily for 14 days2019Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
Design, synthesis and biological evaluation of novel dithiocarbamate-substituted diphenylaminopyrimidine derivatives as BTK inhibitors.
AID1468814Selectivity ratio of IC50 for recombinant human cytoplasmic full length His-tagged TEC to IC50 for recombinant human full length His-tagged BTK2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development.
AID1484563Induction of apoptosis in human Ramos cells assessed as necrotic cells at 10 uM after 48 hrs by annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 0.2%)2017European journal of medicinal chemistry, Jul-28, Volume: 135Design and synthesis of sulfonamide-substituted diphenylpyrimidines (SFA-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B-cell lymphoblastic leukemia.
AID1334886Cell cycle arrest in human Ramos cells assessed as accumulation at G0/G1 phase at 10 uM measured after 48 hrs by propidium iodide based flow cytometry (Rvb = 39.95 %)2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Design and synthesis of phosphoryl-substituted diphenylpyrimidines (Pho-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors: Targeted treatment of B lymphoblastic leukemia cell lines.
AID1468810Inhibition of recombinant human cytoplasmic full length His-tagged TEC expressed in baculovirus at 1 uM by Z'-LYTE assay2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development.
AID1553413Cytotoxicity against human MCF7 cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay2019Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
Design, synthesis and biological evaluation of novel dithiocarbamate-substituted diphenylaminopyrimidine derivatives as BTK inhibitors.
AID1484554Antiproliferative activity against human Ramos cells over expressing BTK after 48 hrs by CCK-8 assay2017European journal of medicinal chemistry, Jul-28, Volume: 135Design and synthesis of sulfonamide-substituted diphenylpyrimidines (SFA-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B-cell lymphoblastic leukemia.
AID1357749Inhibition of LYN (unknown origin)2018European journal of medicinal chemistry, May-10, Volume: 151The development of Bruton's tyrosine kinase (BTK) inhibitors from 2012 to 2017: A mini-review.
AID1334878Antiproliferative activity against human Ramos cells measured after 48 hrs by CCK-8 assay2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Design and synthesis of phosphoryl-substituted diphenylpyrimidines (Pho-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors: Targeted treatment of B lymphoblastic leukemia cell lines.
AID1820499Inhibition of human BTK assessed as ratio of Kinact/Kt using fluorescein-labeled polyGAT peptide as substrate incubated for 30 mins by FRET assay2022Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
Discovery and Preclinical Characterization of BIIB091, a Reversible, Selective BTK Inhibitor for the Treatment of Multiple Sclerosis.
AID1553411Cytotoxicity against human Jurkat cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay2019Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
Design, synthesis and biological evaluation of novel dithiocarbamate-substituted diphenylaminopyrimidine derivatives as BTK inhibitors.
AID1650555Metabolic stability in human liver microsomes assessed as intrinsic clearance at 0.2 uM incubated for 60 mins by UPLC-MS/MS analysis2020Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2
Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors.
AID1426146Induction of apoptosis in human Ramos cells assessed as late apoptotic cells at 10 uM after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 3%)2017European journal of medicinal chemistry, Jan-27, Volume: 126Structural optimization of diphenylpyrimidine derivatives (DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B leukemia cell lines.
AID1650552Antiproliferative activity against human JeKo1 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay2020Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2
Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors.
AID1324660Induction of apoptosis in human Ramos cells assessed as early apoptotic cells at 10 uM after 48 hrs by annexin V/FITC propidium iodide staining based flow cytometry relative to control2016ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
Discovery of Novel Bruton's Tyrosine Kinase (BTK) Inhibitors Bearing a
AID1426157Cell cycle arrest in human Ramos cells assessed as accumulation at S phase at 10 uM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 42.23%)2017European journal of medicinal chemistry, Jan-27, Volume: 126Structural optimization of diphenylpyrimidine derivatives (DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B leukemia cell lines.
AID1401307Inhibition of recombinant full-length N-terminal His-tagged human BTK expressed in baculovirus infected Sf9 insect cells using Poly(4:1 Glu,Tyr) peptide substrate incubated for 60 mins by ADP-Glo luminescence assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma.
AID1553420Cytotoxicity against human H1299 cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay2019Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
Design, synthesis and biological evaluation of novel dithiocarbamate-substituted diphenylaminopyrimidine derivatives as BTK inhibitors.
AID1553410Cytotoxicity against human KARPAS299 cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay2019Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
Design, synthesis and biological evaluation of novel dithiocarbamate-substituted diphenylaminopyrimidine derivatives as BTK inhibitors.
AID1553418Cytotoxicity against human HT-29 cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay2019Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
Design, synthesis and biological evaluation of novel dithiocarbamate-substituted diphenylaminopyrimidine derivatives as BTK inhibitors.
AID1401309Antiproliferative activity against human Ramos cells after 72 hrs by CCK-8 assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma.
AID1291431Inhibition of BTK (unknown origin)2016Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8
Approaching the active conformation of 1,3-diaminopyrimidine based covalent inhibitors of Bruton's tyrosine kinase for treatment of Rheumatoid arthritis.
AID1334879Antiproliferative activity against human Raji cells measured after 48 hrs by CCK-8 assay2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Design and synthesis of phosphoryl-substituted diphenylpyrimidines (Pho-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors: Targeted treatment of B lymphoblastic leukemia cell lines.
AID1401310Antiproliferative activity against human Raji cells after 72 hrs by CCK-8 assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma.
AID1426147Induction of apoptosis in human Ramos cells assessed as necrotic cells at 10 uM after 48 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 1%)2017European journal of medicinal chemistry, Jan-27, Volume: 126Structural optimization of diphenylpyrimidine derivatives (DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B leukemia cell lines.
AID1401330Induction of apoptosis in human Ramos cells assessed as total apoptosis rate at 10 uM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry relative to control2018European journal of medicinal chemistry, Jan-01, Volume: 143Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma.
AID1357747Inhibition of BTK (unknown origin)2018European journal of medicinal chemistry, May-10, Volume: 151The development of Bruton's tyrosine kinase (BTK) inhibitors from 2012 to 2017: A mini-review.
AID1820502Inhibition of CD69 in human whole blood preincubated for 30 mins followed by anti-human IgD stimulation and measured after 18 to 22 hrs by flow cytometry2022Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
Discovery and Preclinical Characterization of BIIB091, a Reversible, Selective BTK Inhibitor for the Treatment of Multiple Sclerosis.
AID1553436Inhibition of BTK in anti-IgM-stimulated human Ramos cells assessed as reduction in Erk phosphorylation at 10 uM incubated for 4 hrs followed by anti-IgM stimulation for 30 mins by Western blot analysis2019Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
Design, synthesis and biological evaluation of novel dithiocarbamate-substituted diphenylaminopyrimidine derivatives as BTK inhibitors.
AID1484555Antiproliferative activity against human Raji cells over expressing BTK after 48 hrs by CCK-8 assay2017European journal of medicinal chemistry, Jul-28, Volume: 135Design and synthesis of sulfonamide-substituted diphenylpyrimidines (SFA-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B-cell lymphoblastic leukemia.
AID1869075Inhibition of BTK C481S mutant (unknown origin) expressed in baculovirus infected Sf9 insect cells incubated for 30 mins in presence of ATP by Microfluidic chip based mobility shift assay2022Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
Medicinal Chemistry Strategies for the Development of Bruton's Tyrosine Kinase Inhibitors against Resistance.
AID1324663Cell cycle arrest in human Ramos cells assessed as accumulation at G0/G1 phase at 10 uM by propidium iodide staining based flow cytometry (Rvb = 56.19%)2016ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
Discovery of Novel Bruton's Tyrosine Kinase (BTK) Inhibitors Bearing a
AID1484553Inhibition of human recombinant full-length N-terminal His-tagged BTK expressed in baculovirus infected Sf9 insect cells after 60 mins by ADP-Glo kinase assay2017European journal of medicinal chemistry, Jul-28, Volume: 135Design and synthesis of sulfonamide-substituted diphenylpyrimidines (SFA-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B-cell lymphoblastic leukemia.
AID1469893Reversible inhibition of full length recombinant human N-terminal His tagged BKT expressed in baculovirus infected Sf9 insect cells assessed as inactivation rate using poly (Glu,Tyr)4:1 as substrate pretreated for 2 to 60 mins followed by substrate additi
AID1553437Inhibition of BTK in anti-IgM-stimulated human Ramos cells assessed as reduction in Akt phosphorylation at 10 uM incubated for 4 hrs followed by anti-IgM stimulation for 30 mins by Western blot analysis2019Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
Design, synthesis and biological evaluation of novel dithiocarbamate-substituted diphenylaminopyrimidine derivatives as BTK inhibitors.
AID1334898Induction of apoptosis in human Ramos cells assessed as late apoptotic cells at 10 uM measured after 48 hrs by Annexin V-FITC/propidium iodide based flow cytometry relative to control2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Design and synthesis of phosphoryl-substituted diphenylpyrimidines (Pho-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors: Targeted treatment of B lymphoblastic leukemia cell lines.
AID1401308Inhibition of recombinant N-terminal GST-tagged human JAK3 (781 to end residues) expressed in baculovirus infected Sf9 insect cells using Poly(4:1 Glu,Tyr) peptide substrate incubated for 60 mins by ADP-Glo luminescence assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma.
AID1553422Cytotoxicity against human HEF cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay2019Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
Design, synthesis and biological evaluation of novel dithiocarbamate-substituted diphenylaminopyrimidine derivatives as BTK inhibitors.
AID1553415Cytotoxicity against human 786-O cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay2019Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
Design, synthesis and biological evaluation of novel dithiocarbamate-substituted diphenylaminopyrimidine derivatives as BTK inhibitors.
AID1324662Induction of apoptosis in human Ramos cells assessed as necrotic cells at 10 uM after 48 hrs by annexin V/FITC propidium iodide staining based flow cytometry relative to control2016ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
Discovery of Novel Bruton's Tyrosine Kinase (BTK) Inhibitors Bearing a
AID1357748Inhibition of TEC (unknown origin)2018European journal of medicinal chemistry, May-10, Volume: 151The development of Bruton's tyrosine kinase (BTK) inhibitors from 2012 to 2017: A mini-review.
AID1553416Cytotoxicity against human HeLa cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay2019Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
Design, synthesis and biological evaluation of novel dithiocarbamate-substituted diphenylaminopyrimidine derivatives as BTK inhibitors.
AID1426156Cell cycle arrest in human Ramos cells assessed as accumulation at G0/G1 phase at 10 uM after 48 hrs by propidium iodide staining based flow cytometry (Rvb = 56.19%)2017European journal of medicinal chemistry, Jan-27, Volume: 126Structural optimization of diphenylpyrimidine derivatives (DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B leukemia cell lines.
AID1553412Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay2019Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
Design, synthesis and biological evaluation of novel dithiocarbamate-substituted diphenylaminopyrimidine derivatives as BTK inhibitors.
AID1324665Cell cycle arrest in human Ramos cells assessed as accumulation at G2/M phase at 10 uM by propidium iodide staining based flow cytometry (Rvb = 1.58%)2016ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
Discovery of Novel Bruton's Tyrosine Kinase (BTK) Inhibitors Bearing a
AID1650545Inhibition of recombinant human N-terminal GST-tagged TYK2 (871 to 1187 residues) expressed in baculovirus expression system using Ulight-Poly GT as substrate incubated for 2 hrs by Lanthascreen TR-FRET assay2020Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2
Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors.
AID1468816Selectivity ratio of IC50 for recombinant human catalytic GST-tagged JAK3 to IC50 for recombinant human full length His-tagged BTK2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development.
AID1468764Inhibition of recombinant human cytoplasmic His-tagged ERBB2 expressed in baculovirus at 1 uM by Z'-LYTE assay2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development.
AID1426142Antiproliferative activity against human Raji cells after 48 hrs by CCK-8 assay2017European journal of medicinal chemistry, Jan-27, Volume: 126Structural optimization of diphenylpyrimidine derivatives (DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B leukemia cell lines.
AID1469890Inhibition of recombinant human N-terminal GST-tagged wild-type EGFR (695 to end residues) expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr)4:1 as substrate pretreated for 60 mins followed by substrate addition after 1 hr by ADP-Glo
AID1650543Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using Ulight-Poly GT as substrate incubated for 2 hrs by Lanthascreen TR-FRET assay2020Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2
Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors.
AID1553425Cytotoxicity against human MCF10A cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay2019Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
Design, synthesis and biological evaluation of novel dithiocarbamate-substituted diphenylaminopyrimidine derivatives as BTK inhibitors.
AID1291432Antiproliferative activity against B cells (unknown origin)2016Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8
Approaching the active conformation of 1,3-diaminopyrimidine based covalent inhibitors of Bruton's tyrosine kinase for treatment of Rheumatoid arthritis.
AID1553435Inhibition of BTK in anti-IgM-stimulated human Ramos cells assessed as reduction in autophosphorylation at Y223 residue at 10 uM incubated for 4 hrs followed by anti-IgM stimulation for 30 mins by Western blot analysis2019Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18
Design, synthesis and biological evaluation of novel dithiocarbamate-substituted diphenylaminopyrimidine derivatives as BTK inhibitors.
AID1334890Cell cycle arrest in human Ramos cells assessed as accumulation at G2/M phase at 10 uM measured after 48 hrs by propidium iodide based flow cytometry (Rvb = 4.98 %)2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Design and synthesis of phosphoryl-substituted diphenylpyrimidines (Pho-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors: Targeted treatment of B lymphoblastic leukemia cell lines.
AID1468803Inhibition of cytoplasmic recombinant human full length His-tagged BMX expressed in baculovirus at 1 uM by Z'-LYTE assay2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development.
AID1654023Inhibition of recombinant human N-terminal GST-tagged JAK3 (781 to end residues) expressed in baculovirus infected Sf9 cells using poly (Glu,Tyr) 4:1 as substrate incubated for 60 mins in presence of ATP by ADP-Glo kinase assay2020Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2
Synthesis and biological activity of thieno[3,2-d]pyrimidines as potent JAK3 inhibitors for the treatment of idiopathic pulmonary fibrosis.
AID1334899Induction of apoptosis in human Ramos cells assessed as early apoptotic cells at 10 uM measured after 48 hrs by Annexin V-FITC/propidium iodide based flow cytometry relative to control2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Design and synthesis of phosphoryl-substituted diphenylpyrimidines (Pho-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors: Targeted treatment of B lymphoblastic leukemia cell lines.
AID1401317Induction of apoptosis in human Ramos cells assessed as necrotic cells at 10 uM after 72 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 0.7%)2018European journal of medicinal chemistry, Jan-01, Volume: 143Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma.
AID1324658Antiproliferative activity against human Raji cells after 48 hrs by CCK-8 assay2016ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
Discovery of Novel Bruton's Tyrosine Kinase (BTK) Inhibitors Bearing a
AID1469894Reversible inhibition of full length recombinant human N-terminal His tagged BKT expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr)4:1 as substrate pretreated for 2 to 60 mins followed by substrate addition after 1 hr by ADP-Glo lumin
AID1426139Inhibition of N-terminal His-tagged full length human recombinant BTK expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) peptide substrate incubated for 60 mins by ADP-Glo luminescence assay2017European journal of medicinal chemistry, Jan-27, Volume: 126Structural optimization of diphenylpyrimidine derivatives (DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B leukemia cell lines.
AID1324664Cell cycle arrest in human Ramos cells assessed as accumulation at S phase at 10 uM by propidium iodide staining based flow cytometry (Rvb = 42.23%)2016ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
Discovery of Novel Bruton's Tyrosine Kinase (BTK) Inhibitors Bearing a
AID1324659Induction of apoptosis in human Ramos cells assessed as viable cells at 10 uM after 48 hrs by annexin V-FITC/propidium iodide staining based flow cytometry relative to control2016ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
Discovery of Novel Bruton's Tyrosine Kinase (BTK) Inhibitors Bearing a
AID1650553Antiproliferative activity against human OCI-LY10 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay2020Bioorganic & medicinal chemistry, 01-15, Volume: 28, Issue:2
Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors.
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.
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.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (33)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's19 (57.58)24.3611
2020's14 (42.42)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 22.61

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index22.61 (24.57)
Research Supply Index3.66 (2.92)
Research Growth Index4.63 (4.65)
Search Engine Demand Index23.28 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (22.61)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials5 (15.15%)5.53%
Reviews2 (6.06%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other26 (78.79%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]