Page last updated: 2024-11-13

mpi-0479605

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Description

MPI-0479605: an antineoplastic agent that inhibits mitotic kinase Mps1; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID46909588
CHEMBL ID2047943
SCHEMBL ID2946927
MeSH IDM0573491

Synonyms (37)

Synonym
bdbm50386816
CHEMBL2047943 ,
CS-4665
1246529-32-7
n6-cyclohexyl-n2-(2-methyl-4-morpholinophenyl)-9h-purine-2,6-diamine
c22h29n7o
SCHEMBL2946927
6-n-cyclohexyl-2-n-(2-methyl-4-morpholin-4-ylphenyl)-7h-purine-2,6-diamine
gtpl9399
mpi-0479605
HY-12660
AC-33011
AKOS026750424
EX-A1092
mpi 0479605
FT-0699832
mpi0479605
AKOS027289040
HMS3653P07
n6-cyclohexyl-n2-[2-methyl-4-(morpholin-4-yl)phenyl]-9h-purine-2,6-diamine
mfcd28099811
NCGC00386327-03
OVJBNYKNHXJGSA-UHFFFAOYSA-N
n~-6~-cyclohexyl-n~2~-[2-methyl-4-(morpholin-4-yl)phenyl]-9h-purine-2,6-diamine
SW220076-1
mpi-0479605 hydrochloride
S7488
BCP27897
SB19447
HMS3740O21
CCG-268735
bdbm532282
witj0018d
n6-cyclohexyl-n2-(2-methyl-4-morpholino-phenyl)-9h-purine-2,6-diamine
us11208696, example 1
NCGC00386327-02
WZB52932

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"Efforts to optimize biological activity, novelty, selectivity and oral bioavailability of Mps1 inhibitors, from a purine based lead MPI-0479605, are described in this Letter."( Lead optimization of purine based orally bioavailable Mps1 (TTK) inhibitors.
Bradford, C; Bursavich, M; Carlson, RO; Chan, A; Cimbora, DM; Gerrish, D; Hoarau, C; McKinnon, R; Papac, DI; Patton, S; Reeves, L; Roth, BL; Saunders, M; Shenderovich, M; Slattum, P; Vijay Kumar, D; Williams, BL; Yager, K, 2012
)
0.58
"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]

Protein Targets (11)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
PPM1D proteinHomo sapiens (human)Potency18.55690.00529.466132.9993AID1347411
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency10.68400.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency13.45040.01238.964839.8107AID1645842
Interferon betaHomo sapiens (human)Potency17.28030.00339.158239.8107AID1347411; AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency13.45040.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency13.45040.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency13.45040.01238.964839.8107AID1645842
[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)
Aurora kinase AHomo sapiens (human)IC50 (µMol)10.00000.00000.46208.6000AID671334
Dual specificity protein kinase TTKHomo sapiens (human)IC50 (µMol)0.00290.00180.33662.5000AID1057802; AID1184501; AID1552040; AID671331; AID747736
Serine/threonine-protein kinase PLK1Homo sapiens (human)IC50 (µMol)5.00000.00010.77349.0000AID671336
Aurora kinase BHomo sapiens (human)IC50 (µMol)5.00000.00030.96349.8000AID671335
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (146)

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)
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)
spindle organizationDual specificity protein kinase TTKHomo sapiens (human)
mitotic spindle organizationDual specificity protein kinase TTKHomo sapiens (human)
positive regulation of cell population proliferationDual specificity protein kinase TTKHomo sapiens (human)
female meiosis chromosome segregationDual specificity protein kinase TTKHomo sapiens (human)
protein localization to meiotic spindle midzoneDual specificity protein kinase TTKHomo sapiens (human)
chromosome segregationDual specificity protein kinase TTKHomo sapiens (human)
peptidyl-serine phosphorylationDual specificity protein kinase TTKHomo sapiens (human)
protein localization to kinetochoreDual specificity protein kinase TTKHomo sapiens (human)
mitotic spindle assembly checkpoint signalingDual specificity protein kinase TTKHomo sapiens (human)
meiotic spindle assembly checkpoint signalingDual specificity protein kinase TTKHomo sapiens (human)
establishment of protein localizationSerine/threonine-protein kinase PLK1Homo sapiens (human)
mitotic sister chromatid segregationSerine/threonine-protein kinase PLK1Homo sapiens (human)
G2/M transition of mitotic cell cycleSerine/threonine-protein kinase PLK1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IISerine/threonine-protein kinase PLK1Homo sapiens (human)
establishment of mitotic spindle orientationSerine/threonine-protein kinase PLK1Homo sapiens (human)
mitotic cell cycleSerine/threonine-protein kinase PLK1Homo sapiens (human)
mitotic cytokinesisSerine/threonine-protein kinase PLK1Homo sapiens (human)
microtubule bundle formationSerine/threonine-protein kinase PLK1Homo sapiens (human)
double-strand break repairSerine/threonine-protein kinase PLK1Homo sapiens (human)
protein phosphorylationSerine/threonine-protein kinase PLK1Homo sapiens (human)
mitotic spindle organizationSerine/threonine-protein kinase PLK1Homo sapiens (human)
sister chromatid cohesionSerine/threonine-protein kinase PLK1Homo sapiens (human)
mitotic chromosome condensationSerine/threonine-protein kinase PLK1Homo sapiens (human)
mitotic nuclear membrane disassemblySerine/threonine-protein kinase PLK1Homo sapiens (human)
metaphase/anaphase transition of mitotic cell cycleSerine/threonine-protein kinase PLK1Homo sapiens (human)
mitotic spindle assembly checkpoint signalingSerine/threonine-protein kinase PLK1Homo sapiens (human)
mitotic G2 DNA damage checkpoint signalingSerine/threonine-protein kinase PLK1Homo sapiens (human)
centrosome cycleSerine/threonine-protein kinase PLK1Homo sapiens (human)
regulation of mitotic cell cycleSerine/threonine-protein kinase PLK1Homo sapiens (human)
positive regulation of peptidyl-threonine phosphorylationSerine/threonine-protein kinase PLK1Homo sapiens (human)
female meiosis chromosome segregationSerine/threonine-protein kinase PLK1Homo sapiens (human)
protein ubiquitinationSerine/threonine-protein kinase PLK1Homo sapiens (human)
peptidyl-serine phosphorylationSerine/threonine-protein kinase PLK1Homo sapiens (human)
regulation of mitotic metaphase/anaphase transitionSerine/threonine-protein kinase PLK1Homo sapiens (human)
protein destabilizationSerine/threonine-protein kinase PLK1Homo sapiens (human)
positive regulation of proteasomal ubiquitin-dependent protein catabolic processSerine/threonine-protein kinase PLK1Homo sapiens (human)
regulation of cytokinesisSerine/threonine-protein kinase PLK1Homo sapiens (human)
negative regulation of apoptotic processSerine/threonine-protein kinase PLK1Homo sapiens (human)
regulation of protein bindingSerine/threonine-protein kinase PLK1Homo sapiens (human)
homologous chromosome segregationSerine/threonine-protein kinase PLK1Homo sapiens (human)
negative regulation of cyclin-dependent protein serine/threonine kinase activitySerine/threonine-protein kinase PLK1Homo sapiens (human)
positive regulation of proteolysisSerine/threonine-protein kinase PLK1Homo sapiens (human)
Golgi inheritanceSerine/threonine-protein kinase PLK1Homo sapiens (human)
nuclear membrane disassemblySerine/threonine-protein kinase PLK1Homo sapiens (human)
positive regulation of ubiquitin-protein transferase activitySerine/threonine-protein kinase PLK1Homo sapiens (human)
regulation of cell cycleSerine/threonine-protein kinase PLK1Homo sapiens (human)
synaptonemal complex disassemblySerine/threonine-protein kinase PLK1Homo sapiens (human)
protein localization to chromatinSerine/threonine-protein kinase PLK1Homo sapiens (human)
protein localization to nuclear envelopeSerine/threonine-protein kinase PLK1Homo sapiens (human)
double-strand break repair via alternative nonhomologous end joiningSerine/threonine-protein kinase PLK1Homo sapiens (human)
positive regulation of protein localization to nucleusSerine/threonine-protein kinase PLK1Homo sapiens (human)
regulation of mitotic spindle assemblySerine/threonine-protein kinase PLK1Homo sapiens (human)
regulation of mitotic cell cycle phase transitionSerine/threonine-protein kinase PLK1Homo sapiens (human)
positive regulation of ubiquitin protein ligase activitySerine/threonine-protein kinase PLK1Homo sapiens (human)
regulation of protein localization to cell cortexSerine/threonine-protein kinase PLK1Homo sapiens (human)
regulation of anaphase-promoting complex-dependent catabolic processSerine/threonine-protein kinase PLK1Homo sapiens (human)
negative regulation of double-strand break repair via homologous recombinationSerine/threonine-protein kinase PLK1Homo 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)
negative regulation of transcription by RNA polymerase IIAurora kinase BHomo sapiens (human)
mitotic cell cycleAurora kinase BHomo sapiens (human)
mitotic cytokinesisAurora kinase BHomo sapiens (human)
negative regulation of B cell apoptotic processAurora kinase BHomo sapiens (human)
protein phosphorylationAurora kinase BHomo sapiens (human)
spindle organizationAurora kinase BHomo sapiens (human)
attachment of spindle microtubules to kinetochoreAurora kinase BHomo sapiens (human)
abscissionAurora kinase BHomo sapiens (human)
negative regulation of protein bindingAurora kinase BHomo sapiens (human)
positive regulation of telomere maintenance via telomeraseAurora kinase BHomo sapiens (human)
negative regulation of cytokinesisAurora kinase BHomo sapiens (human)
positive regulation of cytokinesisAurora kinase BHomo sapiens (human)
protein localization to kinetochoreAurora kinase BHomo sapiens (human)
cellular response to UVAurora kinase BHomo sapiens (human)
cleavage furrow formationAurora kinase BHomo sapiens (human)
post-translational protein modificationAurora kinase BHomo sapiens (human)
cell cycle G2/M phase transitionAurora kinase BHomo sapiens (human)
mitotic cytokinesis checkpoint signalingAurora kinase BHomo sapiens (human)
negative regulation of innate immune responseAurora kinase BHomo sapiens (human)
protein autophosphorylationAurora kinase BHomo sapiens (human)
mitotic spindle midzone assemblyAurora kinase BHomo sapiens (human)
positive regulation of telomerase activityAurora kinase BHomo sapiens (human)
regulation of chromosome segregationAurora kinase BHomo sapiens (human)
positive regulation of mitotic sister chromatid segregationAurora kinase BHomo sapiens (human)
positive regulation of mitotic cell cycle spindle assembly checkpointAurora kinase BHomo sapiens (human)
mitotic spindle assemblyAurora kinase BHomo sapiens (human)
negative regulation of cGAS/STING signaling pathwayAurora kinase BHomo sapiens (human)
regulation of signal transduction by p53 class mediatorAurora kinase BHomo sapiens (human)
positive regulation of mitotic sister chromatid separationAurora kinase BHomo sapiens (human)
positive regulation of attachment of mitotic spindle microtubules to kinetochoreAurora kinase BHomo sapiens (human)
positive regulation of mitotic cytokinesisAurora kinase BHomo sapiens (human)
positive regulation of telomere cappingAurora kinase BHomo sapiens (human)
positive regulation of lateral attachment of mitotic spindle microtubules to kinetochoreAurora kinase BHomo sapiens (human)
mitotic spindle organizationAurora kinase BHomo sapiens (human)
regulation of cytokinesisAurora kinase BHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (34)

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)
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 activityDual specificity protein kinase TTKHomo sapiens (human)
protein bindingDual specificity protein kinase TTKHomo sapiens (human)
ATP bindingDual specificity protein kinase TTKHomo sapiens (human)
identical protein bindingDual specificity protein kinase TTKHomo sapiens (human)
kinetochore bindingDual specificity protein kinase TTKHomo sapiens (human)
protein serine kinase activityDual specificity protein kinase TTKHomo sapiens (human)
protein serine/threonine/tyrosine kinase activityDual specificity protein kinase TTKHomo sapiens (human)
protein serine/threonine kinase activityDual specificity protein kinase TTKHomo sapiens (human)
magnesium ion bindingSerine/threonine-protein kinase PLK1Homo sapiens (human)
protein kinase activitySerine/threonine-protein kinase PLK1Homo sapiens (human)
protein serine/threonine kinase activitySerine/threonine-protein kinase PLK1Homo sapiens (human)
protein bindingSerine/threonine-protein kinase PLK1Homo sapiens (human)
ATP bindingSerine/threonine-protein kinase PLK1Homo sapiens (human)
microtubule bindingSerine/threonine-protein kinase PLK1Homo sapiens (human)
anaphase-promoting complex bindingSerine/threonine-protein kinase PLK1Homo sapiens (human)
protein kinase bindingSerine/threonine-protein kinase PLK1Homo sapiens (human)
identical protein bindingSerine/threonine-protein kinase PLK1Homo sapiens (human)
protein serine kinase activitySerine/threonine-protein kinase PLK1Homo 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)
protein serine/threonine kinase activityAurora kinase BHomo sapiens (human)
protein serine/threonine kinase activityAurora kinase BHomo sapiens (human)
protein serine/threonine/tyrosine kinase activityAurora kinase BHomo sapiens (human)
protein bindingAurora kinase BHomo sapiens (human)
ATP bindingAurora kinase BHomo sapiens (human)
kinase bindingAurora kinase BHomo sapiens (human)
protein serine kinase activityAurora kinase BHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (51)

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)
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)
cytoplasmDual specificity protein kinase TTKHomo sapiens (human)
spindleDual specificity protein kinase TTKHomo sapiens (human)
membraneDual specificity protein kinase TTKHomo sapiens (human)
kinetochoreDual specificity protein kinase TTKHomo sapiens (human)
nucleusDual specificity protein kinase TTKHomo sapiens (human)
spindle microtubuleSerine/threonine-protein kinase PLK1Homo sapiens (human)
kinetochoreSerine/threonine-protein kinase PLK1Homo sapiens (human)
synaptonemal complexSerine/threonine-protein kinase PLK1Homo sapiens (human)
spindle poleSerine/threonine-protein kinase PLK1Homo sapiens (human)
nucleusSerine/threonine-protein kinase PLK1Homo sapiens (human)
nucleoplasmSerine/threonine-protein kinase PLK1Homo sapiens (human)
centrosomeSerine/threonine-protein kinase PLK1Homo sapiens (human)
centrioleSerine/threonine-protein kinase PLK1Homo sapiens (human)
spindleSerine/threonine-protein kinase PLK1Homo sapiens (human)
cytosolSerine/threonine-protein kinase PLK1Homo sapiens (human)
microtubule cytoskeletonSerine/threonine-protein kinase PLK1Homo sapiens (human)
midbodySerine/threonine-protein kinase PLK1Homo sapiens (human)
centriolar satelliteSerine/threonine-protein kinase PLK1Homo sapiens (human)
spindle midzoneSerine/threonine-protein kinase PLK1Homo sapiens (human)
mitotic spindle poleSerine/threonine-protein kinase PLK1Homo sapiens (human)
chromatinSerine/threonine-protein kinase PLK1Homo sapiens (human)
outer kinetochoreSerine/threonine-protein kinase PLK1Homo sapiens (human)
nucleusSerine/threonine-protein kinase PLK1Homo sapiens (human)
centrosomeSerine/threonine-protein kinase PLK1Homo sapiens (human)
cytoplasmSerine/threonine-protein kinase PLK1Homo sapiens (human)
spindle poleSerine/threonine-protein kinase PLK1Homo sapiens (human)
kinetochoreSerine/threonine-protein kinase PLK1Homo 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)
kinetochoreAurora kinase BHomo sapiens (human)
condensed chromosome, centromeric regionAurora kinase BHomo sapiens (human)
nucleusAurora kinase BHomo sapiens (human)
nucleoplasmAurora kinase BHomo sapiens (human)
spindleAurora kinase BHomo sapiens (human)
cytosolAurora kinase BHomo sapiens (human)
chromocenterAurora kinase BHomo sapiens (human)
microtubule cytoskeletonAurora kinase BHomo sapiens (human)
midbodyAurora kinase BHomo sapiens (human)
chromosome passenger complexAurora kinase BHomo sapiens (human)
mitotic spindle poleAurora kinase BHomo sapiens (human)
mitotic spindle midzoneAurora kinase BHomo sapiens (human)
kinetochoreAurora kinase BHomo sapiens (human)
spindle pole centrosomeAurora kinase BHomo sapiens (human)
spindle microtubuleAurora kinase BHomo sapiens (human)
spindle midzoneAurora kinase BHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (26)

Assay IDTitleYearJournalArticle
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.
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.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID671335Inhibition of Aur B2012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Lead optimization of purine based orally bioavailable Mps1 (TTK) inhibitors.
AID747736Inhibition of human MPS1 expressed in Escherichia coli2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Indazole-based potent and cell-active Mps1 kinase inhibitors: rational design from pan-kinase inhibitor anthrapyrazolone (SP600125).
AID670210Antitumor activity against human HCT116 xenografted in mouse assessed as tumor growth inhibition at 150 mg/kg, ip administered one dose every 4 days 6 times2012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Lead optimization of purine based orally bioavailable Mps1 (TTK) inhibitors.
AID671337Kinetic solubility of the compound at pH 7.42012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Lead optimization of purine based orally bioavailable Mps1 (TTK) inhibitors.
AID670208Oral bioavailability in CD-1 mouse at 10 mg/kg2012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Lead optimization of purine based orally bioavailable Mps1 (TTK) inhibitors.
AID671332Cytotoxicity against human HCT116 cells2012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Lead optimization of purine based orally bioavailable Mps1 (TTK) inhibitors.
AID671331Inhibition of Mps12012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Lead optimization of purine based orally bioavailable Mps1 (TTK) inhibitors.
AID1552040Inhibition of MPS1 (519 to 808 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) after 18 hrs2019European journal of medicinal chemistry, Aug-01, Volume: 175Molecular design and anticancer activities of small-molecule monopolar spindle 1 inhibitors: A Medicinal chemistry perspective.
AID671333Cell cycle arrest in human HCT116 cells assessed as G2 checkpoint inhibition by Hoescht 33342 staining method2012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Lead optimization of purine based orally bioavailable Mps1 (TTK) inhibitors.
AID1057802Inhibition of full-length Mps1 kinase (unknown origin)2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Novel Mps1 kinase inhibitors: from purine to pyrrolopyrimidine and quinazoline leads.
AID1184501Inhibition of GST-fused full length human TTK compound pre-incubated for 15 mins prior ATP addition by MBP-based assay2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Discovery of inhibitors of the mitotic kinase TTK based on N-(3-(3-sulfamoylphenyl)-1H-indazol-5-yl)-acetamides and carboxamides.
AID1057801Cytotoxicity against human HCT116 cells2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Novel Mps1 kinase inhibitors: from purine to pyrrolopyrimidine and quinazoline leads.
AID1203305Antitumor activity against human HCT116 cells xenografted in nude mouse assessed as tumor growth inhibition at 30 mg/kg, po qd administered for 21 days measured on day 22 relative to vehicle-treated control2015Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
The Discovery of Orally Bioavailable Tyrosine Threonine Kinase (TTK) Inhibitors: 3-(4-(heterocyclyl)phenyl)-1H-indazole-5-carboxamides as Anticancer Agents.
AID671334Inhibition of Aur A2012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Lead optimization of purine based orally bioavailable Mps1 (TTK) inhibitors.
AID747739Antiproliferative activity against human A549 cells after 72 hrs by WST8 assay2013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
Indazole-based potent and cell-active Mps1 kinase inhibitors: rational design from pan-kinase inhibitor anthrapyrazolone (SP600125).
AID670209Antitumor activity against human HCT116 xenografted in mouse assessed as tumor growth inhibition at 150 mg/kg, ip administered one dose everyday 15 times2012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Lead optimization of purine based orally bioavailable Mps1 (TTK) inhibitors.
AID671336Inhibition of PLK12012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Lead optimization of purine based orally bioavailable Mps1 (TTK) inhibitors.
AID671338Apparent permeability of the compound by PAMPA2012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Lead optimization of purine based orally bioavailable Mps1 (TTK) inhibitors.
AID671339Metabolic stability in mouse liver microsomes assessed as compound remaining at 1 uM after 40 mins by mass spectrometry2012Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
Lead optimization of purine based orally bioavailable Mps1 (TTK) inhibitors.
AID1345801Human TTK protein kinase (TTK family)2011Molecular cancer therapeutics, Dec, Volume: 10, Issue:12
Characterization of the cellular and antitumor effects of MPI-0479605, a small-molecule inhibitor of the mitotic kinase Mps1.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (11)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's8 (72.73)24.3611
2020's3 (27.27)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 17.21

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 Index17.21 (24.57)
Research Supply Index2.48 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (17.21)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (9.09%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other10 (90.91%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]