Page last updated: 2024-11-13

centrinone

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

Description

centrinone: a polo-like kinase 4 inhibitor; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID91801159
CHEMBL ID5185225
SCHEMBL ID18154649
MeSH IDM000607386

Synonyms (30)

Synonym
S7837
CS-4921
2-((2-fluoro-4-((2-fluoro-3-nitrobenzyl)sulfonyl)phenyl)thio)-5-methoxy-n-(5-methyl-1h-pyrazol-3-yl)-6-morpholinopyrimidin-4-amine ,
4j7 ,
2-({2-fluoro-4-[(2-fluoro-3-nitrobenzyl)sulfonyl]phenyl}sulfanyl)-5-methoxy-n-(3-methyl-1h-pyrazol-5-yl)-6-(morpholin-4-yl)pyrimidin-4-amine
HY-18682
centrinone
2-((2-fluoro-4-((2-fluoro-3-nitrobenzyl)sulfonyl)phenyl)thio)-5-methoxy-n-(5-methyl-1h-pyrazol-3-yl)
AKOS027423697
2-[[2-fluoro-4-[[(2-fluoro-3-nitrophenyl)methyl]sulfonyl]phenyl]thio]-5-methoxy-n-(5-methyl-1h-pyrazol-3-yl)-6-(4-morpholinyl)-4-pyrimidinamine
1798871-30-3
EX-A5292
CHEMBL5185225 ,
SCHEMBL18154649
A903323
BCP17384
lcr-263
YWC87130
Q27454747
F85265
MS-30874
2-[2-fluoro-4-[(2-fluoro-3-nitrophenyl)methylsulfonyl]phenyl]sulfanyl-5-methoxy-n-(5-methyl-1h-pyrazol-3-yl)-6-morpholin-4-ylpyrimidin-4-amine
{2-[2-fluoro-4-(2-fluoro-3-nitro-phenylmethanesulfonyl)-phenylsulfanyl]-5-methoxy-6-morpholin-4-yl-pyrimidin-4-yl}-(5-methyl-1h-pyrazol-3-yl)-amine
centrinone (lcr-263)
lcr-263lcr-263
bdbm50591939
2-((2-fluoro-4-((2-fluoro-3-nitrobenzyl)sulfonyl)phenyl)thio)-5-methoxy-n-(3-methyl-1h-pyrazol-5-yl)-6-morpholinopyrimidin-4-amine
AC-36954
2-({2-fluoro-4-[(2-fluoro-3-nitrophenyl)methanesulfonyl]phenyl}sulfanyl)-5-methoxy-n-(3-methyl-1h-pyrazol-5-yl)-6-(morpholin-4-yl)pyrimidin-4-amine
AKOS040741533

Research Excerpts

Treatment

ExcerptReferenceRelevance
"Centrinone treatment caused centrosome depletion in human and other vertebrate cells."( Cell biology. Reversible centriole depletion with an inhibitor of Polo-like kinase 4.
Anzola, JV; Davis, RL; Desai, A; Gahman, TC; Hsia, JE; Kim, SK; Kroll, A; Mitchell, BJ; Mitchell, JW; Motamedi, A; Oegema, K; Seo, CP; Shiau, AK; Wong, YL; Yoon, M, 2015
)
1.14
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (4)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Serine/threonine-protein kinase PLK4Homo sapiens (human)IC50 (µMol)0.00290.00270.46253.1000AID1860388; AID1860515
Aurora kinase AHomo sapiens (human)IC50 (µMol)0.10800.00000.46208.6000AID1860516
Aurora kinase BHomo sapiens (human)IC50 (µMol)0.68000.00030.96349.8000AID1860517
Aurora kinase CHomo sapiens (human)IC50 (µMol)0.49300.00100.41378.6000AID1860518
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (66)

Processvia Protein(s)Taxonomy
positive regulation of centriole replicationSerine/threonine-protein kinase PLK4Homo sapiens (human)
protein phosphorylationSerine/threonine-protein kinase PLK4Homo sapiens (human)
centriole replicationSerine/threonine-protein kinase PLK4Homo sapiens (human)
positive regulation of centriole replicationSerine/threonine-protein kinase PLK4Homo sapiens (human)
cilium assemblySerine/threonine-protein kinase PLK4Homo sapiens (human)
trophoblast giant cell differentiationSerine/threonine-protein kinase PLK4Homo sapiens (human)
de novo centriole assembly involved in multi-ciliated epithelial cell differentiationSerine/threonine-protein kinase PLK4Homo sapiens (human)
protein phosphorylationAurora kinase AHomo sapiens (human)
response to woundingAurora kinase AHomo sapiens (human)
liver regenerationAurora kinase AHomo sapiens (human)
G2/M transition of mitotic cell cycleAurora kinase AHomo sapiens (human)
mitotic cell cycleAurora kinase AHomo sapiens (human)
chromatin remodelingAurora kinase AHomo sapiens (human)
protein phosphorylationAurora kinase AHomo sapiens (human)
apoptotic processAurora kinase AHomo sapiens (human)
spindle organizationAurora kinase AHomo sapiens (human)
spindle assembly involved in female meiosis IAurora kinase AHomo sapiens (human)
mitotic centrosome separationAurora kinase AHomo sapiens (human)
anterior/posterior axis specificationAurora kinase AHomo sapiens (human)
regulation of G2/M transition of mitotic cell cycleAurora kinase AHomo sapiens (human)
negative regulation of gene expressionAurora kinase AHomo sapiens (human)
peptidyl-serine phosphorylationAurora kinase AHomo sapiens (human)
regulation of protein stabilityAurora kinase AHomo sapiens (human)
negative regulation of protein bindingAurora kinase AHomo sapiens (human)
positive regulation of proteasomal ubiquitin-dependent protein catabolic processAurora kinase AHomo sapiens (human)
negative regulation of apoptotic processAurora kinase AHomo sapiens (human)
proteasome-mediated ubiquitin-dependent protein catabolic processAurora kinase AHomo sapiens (human)
positive regulation of mitotic nuclear divisionAurora kinase AHomo sapiens (human)
positive regulation of mitotic cell cycleAurora kinase AHomo sapiens (human)
regulation of centrosome cycleAurora kinase AHomo sapiens (human)
protein autophosphorylationAurora kinase AHomo sapiens (human)
cell divisionAurora kinase AHomo sapiens (human)
centrosome localizationAurora kinase AHomo sapiens (human)
cilium disassemblyAurora kinase AHomo sapiens (human)
protein localization to centrosomeAurora kinase AHomo sapiens (human)
positive regulation of mitochondrial fissionAurora kinase AHomo sapiens (human)
positive regulation of oocyte maturationAurora kinase AHomo sapiens (human)
regulation of signal transduction by p53 class mediatorAurora kinase AHomo sapiens (human)
neuron projection extensionAurora kinase AHomo sapiens (human)
mitotic spindle organizationAurora kinase AHomo sapiens (human)
regulation of cytokinesisAurora kinase AHomo sapiens (human)
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)
protein phosphorylationAurora kinase CHomo sapiens (human)
attachment of spindle microtubules to kinetochoreAurora kinase CHomo sapiens (human)
positive regulation of cytokinesisAurora kinase CHomo sapiens (human)
mitotic spindle midzone assemblyAurora kinase CHomo sapiens (human)
cell divisionAurora kinase CHomo sapiens (human)
meiotic cell cycleAurora kinase CHomo sapiens (human)
regulation of cytokinesisAurora kinase CHomo sapiens (human)
mitotic spindle organizationAurora kinase CHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (13)

Processvia Protein(s)Taxonomy
protein serine/threonine kinase activitySerine/threonine-protein kinase PLK4Homo sapiens (human)
protein bindingSerine/threonine-protein kinase PLK4Homo sapiens (human)
ATP bindingSerine/threonine-protein kinase PLK4Homo sapiens (human)
identical protein bindingSerine/threonine-protein kinase PLK4Homo sapiens (human)
protein serine kinase activitySerine/threonine-protein kinase PLK4Homo sapiens (human)
protein kinase activityAurora kinase AHomo sapiens (human)
protein serine/threonine kinase activityAurora kinase AHomo sapiens (human)
protein serine/threonine/tyrosine kinase activityAurora kinase AHomo sapiens (human)
protein bindingAurora kinase AHomo sapiens (human)
ATP bindingAurora kinase AHomo sapiens (human)
protein kinase bindingAurora kinase AHomo sapiens (human)
ubiquitin protein ligase bindingAurora kinase AHomo sapiens (human)
histone H3S10 kinase activityAurora kinase AHomo sapiens (human)
protein heterodimerization activityAurora kinase AHomo sapiens (human)
protein serine kinase activityAurora kinase AHomo sapiens (human)
molecular function activator activityAurora kinase AHomo sapiens (human)
protein serine/threonine kinase 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)
protein kinase activityAurora kinase CHomo sapiens (human)
protein serine/threonine kinase activityAurora kinase CHomo sapiens (human)
protein serine/threonine/tyrosine kinase activityAurora kinase CHomo sapiens (human)
protein bindingAurora kinase CHomo sapiens (human)
ATP bindingAurora kinase CHomo sapiens (human)
protein serine kinase activityAurora kinase CHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (35)

Processvia Protein(s)Taxonomy
XY bodySerine/threonine-protein kinase PLK4Homo sapiens (human)
nucleolusSerine/threonine-protein kinase PLK4Homo sapiens (human)
centrosomeSerine/threonine-protein kinase PLK4Homo sapiens (human)
centrioleSerine/threonine-protein kinase PLK4Homo sapiens (human)
cytosolSerine/threonine-protein kinase PLK4Homo sapiens (human)
cleavage furrowSerine/threonine-protein kinase PLK4Homo sapiens (human)
deuterosomeSerine/threonine-protein kinase PLK4Homo sapiens (human)
procentrioleSerine/threonine-protein kinase PLK4Homo sapiens (human)
procentriole replication complexSerine/threonine-protein kinase PLK4Homo sapiens (human)
nucleusSerine/threonine-protein kinase PLK4Homo sapiens (human)
spindle microtubuleAurora kinase AHomo sapiens (human)
nucleusAurora kinase AHomo sapiens (human)
nucleoplasmAurora kinase AHomo sapiens (human)
centrosomeAurora kinase AHomo sapiens (human)
centrioleAurora kinase AHomo sapiens (human)
spindleAurora kinase AHomo sapiens (human)
cytosolAurora kinase AHomo sapiens (human)
postsynaptic densityAurora kinase AHomo sapiens (human)
microtubule cytoskeletonAurora kinase AHomo sapiens (human)
basolateral plasma membraneAurora kinase AHomo sapiens (human)
midbodyAurora kinase AHomo sapiens (human)
spindle pole centrosomeAurora kinase AHomo sapiens (human)
ciliary basal bodyAurora kinase AHomo sapiens (human)
germinal vesicleAurora kinase AHomo sapiens (human)
axon hillockAurora kinase AHomo sapiens (human)
pronucleusAurora kinase AHomo sapiens (human)
perinuclear region of cytoplasmAurora kinase AHomo sapiens (human)
mitotic spindleAurora kinase AHomo sapiens (human)
meiotic spindleAurora kinase AHomo sapiens (human)
mitotic spindle poleAurora kinase AHomo sapiens (human)
glutamatergic synapseAurora kinase AHomo sapiens (human)
spindle pole centrosomeAurora kinase AHomo sapiens (human)
chromosome passenger complexAurora kinase AHomo sapiens (human)
spindle midzoneAurora kinase AHomo sapiens (human)
kinetochoreAurora kinase AHomo sapiens (human)
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)
condensed chromosomeAurora kinase CHomo sapiens (human)
nucleusAurora kinase CHomo sapiens (human)
cytoplasmAurora kinase CHomo sapiens (human)
spindleAurora kinase CHomo sapiens (human)
midbodyAurora kinase CHomo sapiens (human)
spindle midzoneAurora kinase CHomo sapiens (human)
chromosome passenger complexAurora kinase CHomo sapiens (human)
kinetochoreAurora kinase CHomo sapiens (human)
spindle midzoneAurora kinase CHomo sapiens (human)
spindle pole centrosomeAurora kinase CHomo sapiens (human)
spindle microtubuleAurora kinase CHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (15)

Assay IDTitleYearJournalArticle
AID1860388Inhibition of recombinant human PLK4 incubated for 60 mins by Lanthascreen Eu kinase binding assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis, and biological evaluation of novel pyrazolo [3,4-d]pyrimidine derivatives as potent PLK4 inhibitors for the treatment of TRIM37-amplified breast cancer.
AID1860521Selectivity index, ratio of IC50 for inhibition of Aurora B (unknown origin) to IC50 for inhibition of PLK4 (unknown origin)2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis, and biological evaluation of novel pyrazolo [3,4-d]pyrimidine derivatives as potent PLK4 inhibitors for the treatment of TRIM37-amplified breast cancer.
AID1860518Inhibition of Aurora C (unknown origin) by Z'-LYTE kinase assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis, and biological evaluation of novel pyrazolo [3,4-d]pyrimidine derivatives as potent PLK4 inhibitors for the treatment of TRIM37-amplified breast cancer.
AID1860393Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 5 days by MTT assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis, and biological evaluation of novel pyrazolo [3,4-d]pyrimidine derivatives as potent PLK4 inhibitors for the treatment of TRIM37-amplified breast cancer.
AID1860456Antiproliferative activity against TRIM37 amplified human BT-474 cells assessed as inhibition of cell proliferation at 150 nM incubated for 4 to 8 days by passsaging based LUNA-II automated cell counter2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis, and biological evaluation of novel pyrazolo [3,4-d]pyrimidine derivatives as potent PLK4 inhibitors for the treatment of TRIM37-amplified breast cancer.
AID1860515Inhibition of PLK4 (unknown origin) by Lanthascreen Eu Kinase binding assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis, and biological evaluation of novel pyrazolo [3,4-d]pyrimidine derivatives as potent PLK4 inhibitors for the treatment of TRIM37-amplified breast cancer.
AID1860454Antiproliferative activity against TRIM37 non-amplified human K562 cells assessed as inhibition of cell proliferation at 150 nM incubated for 4 to 8 days by passsaging based LUNA-II automated cell counter2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis, and biological evaluation of novel pyrazolo [3,4-d]pyrimidine derivatives as potent PLK4 inhibitors for the treatment of TRIM37-amplified breast cancer.
AID1860391Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 5 days by MTT assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis, and biological evaluation of novel pyrazolo [3,4-d]pyrimidine derivatives as potent PLK4 inhibitors for the treatment of TRIM37-amplified breast cancer.
AID1860453Antiproliferative activity against TRIM37 non-amplified human MDA-MB-231 cells assessed as inhibition of cell proliferation at 150 nM incubated for 4 to 8 days by passsaging based LUNA-II automated cell counter2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis, and biological evaluation of novel pyrazolo [3,4-d]pyrimidine derivatives as potent PLK4 inhibitors for the treatment of TRIM37-amplified breast cancer.
AID1860455Antiproliferative activity against TRIM37 amplified human MCF7 cells assessed as inhibition of cell proliferation at 150 nM incubated for 4 to 8 days by passsaging based LUNA-II automated cell counter2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis, and biological evaluation of novel pyrazolo [3,4-d]pyrimidine derivatives as potent PLK4 inhibitors for the treatment of TRIM37-amplified breast cancer.
AID1860517Inhibition of Aurora B (unknown origin) by Z'-LYTE kinase assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis, and biological evaluation of novel pyrazolo [3,4-d]pyrimidine derivatives as potent PLK4 inhibitors for the treatment of TRIM37-amplified breast cancer.
AID1860392Antiproliferative activity against human BT-474 cells assessed as cell growth inhibition incubated for 5 days by MTT assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis, and biological evaluation of novel pyrazolo [3,4-d]pyrimidine derivatives as potent PLK4 inhibitors for the treatment of TRIM37-amplified breast cancer.
AID1860383Antiproliferative activity against human MCF7 cells assessed as reduction in colony formation incubated for 14 days by cresyl-violet staining based assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis, and biological evaluation of novel pyrazolo [3,4-d]pyrimidine derivatives as potent PLK4 inhibitors for the treatment of TRIM37-amplified breast cancer.
AID1860522Selectivity index, ratio of IC50 for inhibition of Aurora C (unknown origin) to IC50 for inhibition of PLK4 (unknown origin)2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis, and biological evaluation of novel pyrazolo [3,4-d]pyrimidine derivatives as potent PLK4 inhibitors for the treatment of TRIM37-amplified breast cancer.
AID1860516Inhibition of Aurora A (unknown origin) by Z'-LYTE kinase assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis, and biological evaluation of novel pyrazolo [3,4-d]pyrimidine derivatives as potent PLK4 inhibitors for the treatment of TRIM37-amplified breast cancer.
[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's0 (0.00)29.6817
2010's5 (50.00)24.3611
2020's5 (50.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 29.43

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 Index29.43 (24.57)
Research Supply Index2.40 (2.92)
Research Growth Index4.64 (4.65)
Search Engine Demand Index34.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (29.43)

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]