Compounds > N-[3-[[5-bromo-4-[2-(1H-imidazol-5-yl)ethylamino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide
Page last updated: 2024-11-12

N-[3-[[5-bromo-4-[2-(1H-imidazol-5-yl)ethylamino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide

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

Cross-References

ID SourceID
PubMed CID11754511
CHEMBL ID3916849
CHEBI ID91357
SCHEMBL ID3869633
SCHEMBL ID15825412

Synonyms (63)

Synonym
HY-11005
bx-912 ,
bdbm17052
n-{3-[(5-bromo-4-{[2-(1h-imidazol-4-yl)ethyl]amino}pyrimidin-2-yl)amino]phenyl}pyrrolidine-1-carboxamide
cid 11754511
AKOS005266650
BCP9000468
bx912
bx 912
HMS3265I23
HMS3244H17
HMS3244G17
n-[3-[[5-bromo-4-[[2-(1h-imidazol-5-yl)ethyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide
HMS3265I24
HMS3265J24
HMS3265J23
HMS3244G18
702674-56-4
BCPP000309
NCGC00346687-01
n-(3-(4-(2-(1h-imidazol-4-yl)ethylamino)-5-bromopyrimidin-2-ylamino)phenyl)pyrrolidine-1-carboxamide
CS-0079
BRD-K49669041-001-01-9
gtpl8007
n-[3-[[5-bromo-4-[2-(3h-imidazol-4-yl)ethylamino]pyrimidin-2-yl]amino]phenyl]pyrrolidine-1-carboxamide
smr004702813
MLS006011015
SCHEMBL3869633
n-[3-[[5-bromo-4-[2-(1h-imidazol-5-yl)ethylamino]pyrimidin-2-yl]amino]phenyl]pyrrolidine-1-carboxamide
n-(3-((4-((2-(1h-imidazol-4-yl)ethyl)amino)-5-bromopyrimidin-2-yl)amino)phenyl)pyrrolidine-1-carboxamide
pyrrolidine-1-carboxylic acid (3-{5-bromo-4-[2-(1h-imidazol-4-yl)-ethylamino]-pyrimidin-2-ylamino}-phenyl)-amide
SCHEMBL15825412
CHEMBL3916849
n-(3-((4-((2-(1h-imidazol-5-yl)ethyl)amino)-5-bromopyrimidin-2-yl)amino)phenyl)pyrrolidine-1-carboxamide
AC-32073
DTXSID30471901
J-522977
AKOS026750229
EX-A945
CHEBI:91357
HMS3654D11
mfcd10565925
SW220162-1
FT-0700351
S1275
Q27075611
AS-16197
BCP01898
SB19281
HMS3743G13
CCG-269454
nsc-758485
nsc758485
n-(3-((4-((2-(1h-imidazol-4-yl)ethyl)amino)-5-bromopyrimidin-2-yl)amino)phenyl)pyrrolidine-1-carboxamide;bx-912
A866641
n-[3-[[4-[[2-(4-imidazolyl)ethyl]amino]-5-bromo-2-pyrimidinyl]amino]phenyl]pyrrolidine-1-carboxamide
SY280412
1-pyrrolidinecarboxamide, n-(3-((5-bromo-4-((2-(1h-imidazol-4-yl)ethyl)amino)-2-pyrimidinyl)amino)phenyl)-
1-pyrrolidinecarboxamide, n-(3-((5-bromo-4-((2-(1h-imidazol-5-yl)ethyl)amino)-2-pyrimidinyl)amino)phenyl)-
unii-y7rg737fy6
y7rg737fy6 ,
n-(3-((5-bromo-4-((2-(1h-imidazol-5-yl)ethyl)amino)-2-pyrimidinyl)amino)phenyl)-1-pyrrolidinecarboxamide
n-(3-(4-(2-(1h-imidazol-5-yl)ethylamino)-5-bromopyrimidin-2-ylamino)phenyl)pyrrolidine-1-carboxamide

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)		0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
ureas
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (10)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Fumarate hydrataseHomo sapiens (human)Potency10.49040.00308.794948.0869AID1347053
PPM1D proteinHomo sapiens (human)Potency5.86820.00529.466132.9993AID1347411
EWS/FLI fusion proteinHomo sapiens (human)Potency3.64400.001310.157742.8575AID1259252; AID1259253; AID1259255; AID1259256
polyproteinZika virusPotency10.49040.00308.794948.0869AID1347053
Interferon betaHomo sapiens (human)Potency5.86820.00339.158239.8107AID1347411
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)IC50 (µMol)0.01200.00251.45139.0000AID1797580
MAP/microtubule affinity-regulating kinase 3Homo sapiens (human)IC50 (µMol)3.33300.00030.66363.3330AID1823773
MAP/microtubule affinity-regulating kinase 4Homo sapiens (human)IC50 (µMol)0.33800.00010.48541.7700AID1823774
Serine/threonine-protein kinase TBK1Homo sapiens (human)IC50 (µMol)2.32700.00220.85656.2200AID1823775
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Aurora kinase AHomo sapiens (human)Kd0.01380.00010.73429.3000AID1342794
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (127)

Processvia Protein(s)Taxonomy
protein phosphorylationAurora kinase AHomo sapiens (human)
response to woundingAurora kinase AHomo sapiens (human)
liver regenerationAurora kinase AHomo sapiens (human)
G2/M transition of mitotic cell cycleAurora kinase AHomo sapiens (human)
mitotic cell cycleAurora kinase AHomo sapiens (human)
chromatin remodelingAurora kinase AHomo sapiens (human)
protein phosphorylationAurora kinase AHomo sapiens (human)
apoptotic processAurora kinase AHomo sapiens (human)
spindle organizationAurora kinase AHomo sapiens (human)
spindle assembly involved in female meiosis IAurora kinase AHomo sapiens (human)
mitotic centrosome separationAurora kinase AHomo sapiens (human)
anterior/posterior axis specificationAurora kinase AHomo sapiens (human)
regulation of G2/M transition of mitotic cell cycleAurora kinase AHomo sapiens (human)
negative regulation of gene expressionAurora kinase AHomo sapiens (human)
peptidyl-serine phosphorylationAurora kinase AHomo sapiens (human)
regulation of protein stabilityAurora kinase AHomo sapiens (human)
negative regulation of protein bindingAurora kinase AHomo sapiens (human)
positive regulation of proteasomal ubiquitin-dependent protein catabolic processAurora kinase AHomo sapiens (human)
negative regulation of apoptotic processAurora kinase AHomo sapiens (human)
proteasome-mediated ubiquitin-dependent protein catabolic processAurora kinase AHomo sapiens (human)
positive regulation of mitotic nuclear divisionAurora kinase AHomo sapiens (human)
positive regulation of mitotic cell cycleAurora kinase AHomo sapiens (human)
regulation of centrosome cycleAurora kinase AHomo sapiens (human)
protein autophosphorylationAurora kinase AHomo sapiens (human)
cell divisionAurora kinase AHomo sapiens (human)
centrosome localizationAurora kinase AHomo sapiens (human)
cilium disassemblyAurora kinase AHomo sapiens (human)
protein localization to centrosomeAurora kinase AHomo sapiens (human)
positive regulation of mitochondrial fissionAurora kinase AHomo sapiens (human)
positive regulation of oocyte maturationAurora kinase AHomo sapiens (human)
regulation of signal transduction by p53 class mediatorAurora kinase AHomo sapiens (human)
neuron projection extensionAurora kinase AHomo sapiens (human)
mitotic spindle organizationAurora kinase AHomo sapiens (human)
regulation of cytokinesisAurora kinase AHomo sapiens (human)
intracellular signal transduction3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
type B pancreatic cell development3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
protein phosphorylation3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
negative regulation of protein kinase activity3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
hyperosmotic response3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
epidermal growth factor receptor signaling pathway3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
insulin receptor signaling pathway3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
positive regulation of phospholipase activity3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
negative regulation of cardiac muscle cell apoptotic process3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
cell migration3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
peptidyl-threonine phosphorylation3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
calcium-mediated signaling3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
actin cytoskeleton organization3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathway3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
T cell costimulation3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
activation of protein kinase B activity3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
cellular response to insulin stimulus3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
negative regulation of toll-like receptor signaling pathway3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
regulation of canonical NF-kappaB signal transduction3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
regulation of mast cell degranulation3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
positive regulation of blood vessel endothelial cell migration3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
positive regulation of angiogenesis3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
protein autophosphorylation3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
insulin-like growth factor receptor signaling pathway3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosol3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
cellular response to epidermal growth factor stimulus3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
extrinsic apoptotic signaling pathway3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
positive regulation of protein localization to plasma membrane3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
positive regulation of sprouting angiogenesis3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
positive regulation of vascular endothelial cell proliferation3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
negative regulation of endothelial cell apoptotic process3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
peptidyl-serine phosphorylation3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
intracellular signal transduction3-phosphoinositide-dependent protein kinase 1Homo 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)
protein phosphorylationMAP/microtubule affinity-regulating kinase 3Homo sapiens (human)
peptidyl-serine phosphorylationMAP/microtubule affinity-regulating kinase 3Homo sapiens (human)
positive regulation of protein bindingMAP/microtubule affinity-regulating kinase 3Homo sapiens (human)
negative regulation of hippo signalingMAP/microtubule affinity-regulating kinase 3Homo sapiens (human)
peptidyl-serine autophosphorylationMAP/microtubule affinity-regulating kinase 3Homo sapiens (human)
negative regulation of protein localization to nucleusMAP/microtubule affinity-regulating kinase 3Homo sapiens (human)
intracellular signal transductionMAP/microtubule affinity-regulating kinase 3Homo sapiens (human)
microtubule cytoskeleton organizationMAP/microtubule affinity-regulating kinase 4Homo sapiens (human)
positive regulation of cell cycleMAP/microtubule affinity-regulating kinase 4Homo sapiens (human)
microtubule cytoskeleton organizationMAP/microtubule affinity-regulating kinase 4Homo sapiens (human)
microtubule bundle formationMAP/microtubule affinity-regulating kinase 4Homo sapiens (human)
protein phosphorylationMAP/microtubule affinity-regulating kinase 4Homo sapiens (human)
nervous system developmentMAP/microtubule affinity-regulating kinase 4Homo sapiens (human)
positive regulation of programmed cell deathMAP/microtubule affinity-regulating kinase 4Homo sapiens (human)
cilium organizationMAP/microtubule affinity-regulating kinase 4Homo sapiens (human)
positive regulation of cilium assemblyMAP/microtubule affinity-regulating kinase 4Homo sapiens (human)
regulation of centrosome cycleMAP/microtubule affinity-regulating kinase 4Homo sapiens (human)
cell divisionMAP/microtubule affinity-regulating kinase 4Homo sapiens (human)
positive regulation of NLRP3 inflammasome complex assemblyMAP/microtubule affinity-regulating kinase 4Homo sapiens (human)
positive regulation of protein localization to centrosomeMAP/microtubule affinity-regulating kinase 4Homo sapiens (human)
intracellular signal transductionMAP/microtubule affinity-regulating kinase 4Homo sapiens (human)
activation of innate immune responseSerine/threonine-protein kinase TBK1Homo sapiens (human)
cytoplasmic pattern recognition receptor signaling pathwaySerine/threonine-protein kinase TBK1Homo sapiens (human)
protein phosphorylationSerine/threonine-protein kinase TBK1Homo sapiens (human)
inflammatory responseSerine/threonine-protein kinase TBK1Homo sapiens (human)
canonical NF-kappaB signal transductionSerine/threonine-protein kinase TBK1Homo sapiens (human)
response to virusSerine/threonine-protein kinase TBK1Homo sapiens (human)
positive regulation of autophagySerine/threonine-protein kinase TBK1Homo sapiens (human)
negative regulation of gene expressionSerine/threonine-protein kinase TBK1Homo sapiens (human)
positive regulation of macroautophagySerine/threonine-protein kinase TBK1Homo sapiens (human)
peptidyl-serine phosphorylationSerine/threonine-protein kinase TBK1Homo sapiens (human)
peptidyl-threonine phosphorylationSerine/threonine-protein kinase TBK1Homo sapiens (human)
regulation of type I interferon productionSerine/threonine-protein kinase TBK1Homo sapiens (human)
positive regulation of type I interferon productionSerine/threonine-protein kinase TBK1Homo sapiens (human)
positive regulation of interferon-alpha productionSerine/threonine-protein kinase TBK1Homo sapiens (human)
positive regulation of interferon-beta productionSerine/threonine-protein kinase TBK1Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylationSerine/threonine-protein kinase TBK1Homo sapiens (human)
toll-like receptor 4 signaling pathwaySerine/threonine-protein kinase TBK1Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionSerine/threonine-protein kinase TBK1Homo sapiens (human)
dendritic cell proliferationSerine/threonine-protein kinase TBK1Homo sapiens (human)
innate immune responseSerine/threonine-protein kinase TBK1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IISerine/threonine-protein kinase TBK1Homo sapiens (human)
defense response to Gram-positive bacteriumSerine/threonine-protein kinase TBK1Homo sapiens (human)
defense response to virusSerine/threonine-protein kinase TBK1Homo sapiens (human)
type I interferon-mediated signaling pathwaySerine/threonine-protein kinase TBK1Homo sapiens (human)
positive regulation of type I interferon-mediated signaling pathwaySerine/threonine-protein kinase TBK1Homo sapiens (human)
antiviral innate immune responseSerine/threonine-protein kinase TBK1Homo sapiens (human)
cGAS/STING signaling pathwaySerine/threonine-protein kinase TBK1Homo sapiens (human)
negative regulation of TORC1 signalingSerine/threonine-protein kinase TBK1Homo sapiens (human)
positive regulation of TORC1 signalingSerine/threonine-protein kinase TBK1Homo sapiens (human)
positive regulation of xenophagySerine/threonine-protein kinase TBK1Homo sapiens (human)
macroautophagySerine/threonine-protein kinase TBK1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (28)

Processvia Protein(s)Taxonomy
protein kinase activityAurora kinase AHomo sapiens (human)
protein serine/threonine kinase activityAurora kinase AHomo sapiens (human)
protein serine/threonine/tyrosine kinase activityAurora kinase AHomo sapiens (human)
protein bindingAurora kinase AHomo sapiens (human)
ATP bindingAurora kinase AHomo sapiens (human)
protein kinase bindingAurora kinase AHomo sapiens (human)
ubiquitin protein ligase bindingAurora kinase AHomo sapiens (human)
histone H3S10 kinase activityAurora kinase AHomo sapiens (human)
protein heterodimerization activityAurora kinase AHomo sapiens (human)
protein serine kinase activityAurora kinase AHomo sapiens (human)
molecular function activator activityAurora kinase AHomo sapiens (human)
protein serine/threonine kinase activity3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
3-phosphoinositide-dependent protein kinase activity3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
protein binding3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
ATP binding3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
phospholipase activator activity3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
phospholipase binding3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
protein serine kinase activity3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
protein serine/threonine kinase activityMAP/microtubule affinity-regulating kinase 3Homo sapiens (human)
protein bindingMAP/microtubule affinity-regulating kinase 3Homo sapiens (human)
ATP bindingMAP/microtubule affinity-regulating kinase 3Homo sapiens (human)
tau protein bindingMAP/microtubule affinity-regulating kinase 3Homo sapiens (human)
tau-protein kinase activityMAP/microtubule affinity-regulating kinase 3Homo sapiens (human)
protein serine kinase activityMAP/microtubule affinity-regulating kinase 3Homo sapiens (human)
protein serine/threonine kinase activityMAP/microtubule affinity-regulating kinase 4Homo sapiens (human)
protein bindingMAP/microtubule affinity-regulating kinase 4Homo sapiens (human)
ATP bindingMAP/microtubule affinity-regulating kinase 4Homo sapiens (human)
microtubule bindingMAP/microtubule affinity-regulating kinase 4Homo sapiens (human)
cytoskeletal anchor activityMAP/microtubule affinity-regulating kinase 4Homo sapiens (human)
gamma-tubulin bindingMAP/microtubule affinity-regulating kinase 4Homo sapiens (human)
ubiquitin bindingMAP/microtubule affinity-regulating kinase 4Homo sapiens (human)
tau protein bindingMAP/microtubule affinity-regulating kinase 4Homo sapiens (human)
tau-protein kinase activityMAP/microtubule affinity-regulating kinase 4Homo sapiens (human)
protein serine kinase activityMAP/microtubule affinity-regulating kinase 4Homo sapiens (human)
nucleic acid bindingSerine/threonine-protein kinase TBK1Homo sapiens (human)
protein kinase activitySerine/threonine-protein kinase TBK1Homo sapiens (human)
protein serine/threonine kinase activitySerine/threonine-protein kinase TBK1Homo sapiens (human)
protein bindingSerine/threonine-protein kinase TBK1Homo sapiens (human)
ATP bindingSerine/threonine-protein kinase TBK1Homo sapiens (human)
protein phosphatase bindingSerine/threonine-protein kinase TBK1Homo sapiens (human)
identical protein bindingSerine/threonine-protein kinase TBK1Homo sapiens (human)
phosphoprotein bindingSerine/threonine-protein kinase TBK1Homo sapiens (human)
protein serine kinase activitySerine/threonine-protein kinase TBK1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (38)

Processvia Protein(s)Taxonomy
spindle microtubuleAurora kinase AHomo sapiens (human)
nucleusAurora kinase AHomo sapiens (human)
nucleoplasmAurora kinase AHomo sapiens (human)
centrosomeAurora kinase AHomo sapiens (human)
centrioleAurora kinase AHomo sapiens (human)
spindleAurora kinase AHomo sapiens (human)
cytosolAurora kinase AHomo sapiens (human)
postsynaptic densityAurora kinase AHomo sapiens (human)
microtubule cytoskeletonAurora kinase AHomo sapiens (human)
basolateral plasma membraneAurora kinase AHomo sapiens (human)
midbodyAurora kinase AHomo sapiens (human)
spindle pole centrosomeAurora kinase AHomo sapiens (human)
ciliary basal bodyAurora kinase AHomo sapiens (human)
germinal vesicleAurora kinase AHomo sapiens (human)
axon hillockAurora kinase AHomo sapiens (human)
pronucleusAurora kinase AHomo sapiens (human)
perinuclear region of cytoplasmAurora kinase AHomo sapiens (human)
mitotic spindleAurora kinase AHomo sapiens (human)
meiotic spindleAurora kinase AHomo sapiens (human)
mitotic spindle poleAurora kinase AHomo sapiens (human)
glutamatergic synapseAurora kinase AHomo sapiens (human)
spindle pole centrosomeAurora kinase AHomo sapiens (human)
chromosome passenger complexAurora kinase AHomo sapiens (human)
spindle midzoneAurora kinase AHomo sapiens (human)
kinetochoreAurora kinase AHomo sapiens (human)
nucleus3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
cytoplasm3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
cytosol3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
plasma membrane3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
focal adhesion3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
postsynaptic density3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
cytoplasmic vesicle3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
cell projection3-phosphoinositide-dependent protein kinase 1Homo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
cytoplasmMAP/microtubule affinity-regulating kinase 3Homo sapiens (human)
cytosolMAP/microtubule affinity-regulating kinase 3Homo sapiens (human)
plasma membraneMAP/microtubule affinity-regulating kinase 3Homo sapiens (human)
dendriteMAP/microtubule affinity-regulating kinase 3Homo sapiens (human)
extracellular exosomeMAP/microtubule affinity-regulating kinase 3Homo sapiens (human)
plasma membraneMAP/microtubule affinity-regulating kinase 3Homo sapiens (human)
cytoplasmMAP/microtubule affinity-regulating kinase 3Homo sapiens (human)
microtubule organizing centerMAP/microtubule affinity-regulating kinase 4Homo sapiens (human)
cytoplasmMAP/microtubule affinity-regulating kinase 4Homo sapiens (human)
centrosomeMAP/microtubule affinity-regulating kinase 4Homo sapiens (human)
microtubule organizing centerMAP/microtubule affinity-regulating kinase 4Homo sapiens (human)
cytosolMAP/microtubule affinity-regulating kinase 4Homo sapiens (human)
microtubule cytoskeletonMAP/microtubule affinity-regulating kinase 4Homo sapiens (human)
dendriteMAP/microtubule affinity-regulating kinase 4Homo sapiens (human)
midbodyMAP/microtubule affinity-regulating kinase 4Homo sapiens (human)
neuron projectionMAP/microtubule affinity-regulating kinase 4Homo sapiens (human)
gamma-tubulin complexMAP/microtubule affinity-regulating kinase 4Homo sapiens (human)
ciliary basal bodyMAP/microtubule affinity-regulating kinase 4Homo sapiens (human)
cytoplasmMAP/microtubule affinity-regulating kinase 4Homo sapiens (human)
cytoplasmSerine/threonine-protein kinase TBK1Homo sapiens (human)
cytosolSerine/threonine-protein kinase TBK1Homo sapiens (human)
nucleoplasmSerine/threonine-protein kinase TBK1Homo sapiens (human)
cytoplasmSerine/threonine-protein kinase TBK1Homo sapiens (human)
cytosolSerine/threonine-protein kinase TBK1Homo sapiens (human)
intracellular membrane-bounded organelleSerine/threonine-protein kinase TBK1Homo sapiens (human)
serine/threonine protein kinase complexSerine/threonine-protein kinase TBK1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (42)

Assay IDTitleYearJournalArticle
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.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC 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.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1823773Displacement of tracer K9 from NLuc fused MARK3 (unknown origin) expressed in HEK293 cells by NanoBRET assay2022Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
Identification of Pyrimidine-Based Lead Compounds for Understudied Kinases Implicated in Driving Neurodegeneration.
AID1823774Displacement of tracer K5 from NLuc fused MARK4 (unknown origin) expressed in HEK293 cells by NanoBRET assay2022Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
Identification of Pyrimidine-Based Lead Compounds for Understudied Kinases Implicated in Driving Neurodegeneration.
AID1823815Effective permeability in PBS at 7.4 incubated for 5 hrs by PAMPA analysis2022Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
Identification of Pyrimidine-Based Lead Compounds for Understudied Kinases Implicated in Driving Neurodegeneration.
AID1823814Kinetic solubility of compound in PBS at pH 7.4 incubated for 24 hrs by chemiluminscent nitrogen detection method2022Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
Identification of Pyrimidine-Based Lead Compounds for Understudied Kinases Implicated in Driving Neurodegeneration.
AID1823775Displacement of tracer K5 from NLuc fused TBK1 (unknown origin) expressed in HEK293 cells by NanoBRET assay2022Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
Identification of Pyrimidine-Based Lead Compounds for Understudied Kinases Implicated in Driving Neurodegeneration.
AID1823817Inhibition of wild-type human full length TBK1 (M1 to L729 residues) expressed in mammalian expression system at 10 uM by Kinomescan method relative to control2022Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
Identification of Pyrimidine-Based Lead Compounds for Understudied Kinases Implicated in Driving Neurodegeneration.
AID1797580PDK1-mediated AKT2 Activation Assay (cAKT2 33P-SPA) from Article 10.1074/jbc.M501367200: \\Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1.\\2005The Journal of biological chemistry, May-20, Volume: 280, Issue:20
Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1.
AID1345633Human glycogen synthase kinase 3 beta (GSK subfamily)2005The Journal of biological chemistry, May-20, Volume: 280, Issue:20
Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1.
AID1345506Human kinase insert domain receptor (Type IV RTKs: VEGF (vascular endothelial growth factor) receptor family)2005The Journal of biological chemistry, May-20, Volume: 280, Issue:20
Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1.
AID1345650Human checkpoint kinase 1 (CHK1 subfamily)2005The Journal of biological chemistry, May-20, Volume: 280, Issue:20
Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1.
AID1345388Human 3-phosphoinositide dependent protein kinase 1 (PDK1 family)2005The Journal of biological chemistry, May-20, Volume: 280, Issue:20
Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1.
AID1345612Human cyclin dependent kinase 2 (CDK1 subfamily)2005The Journal of biological chemistry, May-20, Volume: 280, Issue:20
Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (10)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (10.00)29.6817
2010's2 (20.00)24.3611
2020's7 (70.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.98

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

MetricThis Compound (vs All)
Research Demand Index12.98 (24.57)
Research Supply Index2.40 (2.92)
Research Growth Index5.38 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.98)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other10 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
dasatinib
N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)-1,3-thiazole-5-carboxamide: a dasatinib prodrug; structure in first source. dasatinib (anhydrous) : An aminopyrimidine that is 2-methylpyrimidine which is substituted at position 4 by the primary amino group of 2-amino-1,3-thiazole-5-carboxylic acid and at position 6 by a 4-(2-hydroxyethyl)piperazin-1-yl group, and in which the carboxylic acid group has been formally condensed with 2-chloro-6-methylaniline to afford the corresponding amide. A multi-targeted kinase inhibitor, it is used, particularly as the monohydrate, for the treatment of chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia. Note that the name 'dasatinib' is used to refer to the monohydrate (USAN) as well as to anhydrous dasatinib (INN).		2.41101,3-thiazoles;
aminopyrimidine;
monocarboxylic acid amide;
N-(2-hydroxyethyl)piperazine;
N-arylpiperazine;
organochlorine compound;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor
bx795
BX795: structure in first source		2.0210ureas
mrt67307
MRT67307: IKK (IκB(inhibitor of NF-κB (nuclear factor κB)) kinase) family inhibitor; structure in first source		2.4110aromatic amine
ConditionIndicatedRelationship StrengthStudiesTrials
Cancer of Lung
[description not available]		02.0210
B16 Melanoma
[description not available]		02.0210
Lung Neoplasms
Tumors or cancer of the LUNG.		02.0210
Congenital Zika Syndrome
[description not available]		02.2510
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.2510
Zika Virus Infection
A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.		02.2510
Degenerative Diseases, Central Nervous System
[description not available]		02.4110
Neurodegenerative Diseases
Hereditary and sporadic conditions which are characterized by progressive nervous system dysfunction. These disorders are often associated with atrophy of the affected central or peripheral nervous system structures.		02.4110