Page last updated: 2024-11-13

aki603

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

Description

AKI603: an aurora-A kinase inhibitor with antineoplastic activity; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID72194397
CHEMBL ID3237164
MeSH IDM000604861

Synonyms (14)

Synonym
CHEMBL3237164 ,
bdbm50004228
n4-(5-methyl-1h-pyrazol-3-yl)-6-(4-methylpiperazin-1-yl)-n2-(4-nitrophenyl)pyrimidine-2,4-diamine
SB17137
1432515-73-5
aki-603
aki603
6-(4-methylpiperazin-1-yl)-4-n-(5-methyl-1h-pyrazol-3-yl)-2-n-(4-nitrophenyl)pyrimidine-2,4-diamine
MS-27048
HY-123159
CS-0081580
EN300-21614951
AKOS040759009
Z2327390334

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" The method has been successfully used to the bioavailability study of AKI603 administered to rats intravenously (2."( Determination of a novel Aurora-A (AurA) kinase AKI603 by UPLC-MS/MS and its application to a bioavailability study in rat.
Bi, H; Chen, J; Gou, X; Huang, L; Huang, M; Jiang, F; Li, Z; Lu, G; Wen, D; Zhao, Z; Zhong, G, 2016
)
0.92
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Aurora kinase AHomo sapiens (human)IC50 (µMol)0.01200.00000.46208.6000AID1126527
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (33)

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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (11)

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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (24)

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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (16)

Assay IDTitleYearJournalArticle
AID1126536Antiproliferative activity against human SKBR3 cells assessed as cell viability after 72 hrs by CCK8 assay2014European journal of medicinal chemistry, May-06, Volume: 78Design, synthesis and bioevaluation of N-trisubstituted pyrimidine derivatives as potent aurora A kinase inhibitors.
AID1126537Antiproliferative activity against human A549 cells assessed as cell viability after 72 hrs by CCK8 assay2014European journal of medicinal chemistry, May-06, Volume: 78Design, synthesis and bioevaluation of N-trisubstituted pyrimidine derivatives as potent aurora A kinase inhibitors.
AID1126527Inhibition of Aurora A (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition measured after 60 mins2014European journal of medicinal chemistry, May-06, Volume: 78Design, synthesis and bioevaluation of N-trisubstituted pyrimidine derivatives as potent aurora A kinase inhibitors.
AID1126532Antiproliferative activity against human U937 cells assessed as cell viability after 72 hrs by CCK8 assay2014European journal of medicinal chemistry, May-06, Volume: 78Design, synthesis and bioevaluation of N-trisubstituted pyrimidine derivatives as potent aurora A kinase inhibitors.
AID1126538Antiproliferative activity against human A431 cells assessed as cell viability after 72 hrs by CCK8 assay2014European journal of medicinal chemistry, May-06, Volume: 78Design, synthesis and bioevaluation of N-trisubstituted pyrimidine derivatives as potent aurora A kinase inhibitors.
AID1126533Antiproliferative activity against human MOLT4 cells assessed as cell viability after 72 hrs by CCK8 assay2014European journal of medicinal chemistry, May-06, Volume: 78Design, synthesis and bioevaluation of N-trisubstituted pyrimidine derivatives as potent aurora A kinase inhibitors.
AID1126521Antiproliferative activity against human PANC1 cells assessed as cell viability after 72 hrs by CCK8 assay2014European journal of medicinal chemistry, May-06, Volume: 78Design, synthesis and bioevaluation of N-trisubstituted pyrimidine derivatives as potent aurora A kinase inhibitors.
AID1126530Antiproliferative activity against human HL60 cells assessed as cell viability after 72 hrs by CCK8 assay2014European journal of medicinal chemistry, May-06, Volume: 78Design, synthesis and bioevaluation of N-trisubstituted pyrimidine derivatives as potent aurora A kinase inhibitors.
AID1126542Antiproliferative activity against human NCI-N87 cells assessed as cell viability after 72 hrs by CCK8 assay2014European journal of medicinal chemistry, May-06, Volume: 78Design, synthesis and bioevaluation of N-trisubstituted pyrimidine derivatives as potent aurora A kinase inhibitors.
AID1126531Antiproliferative activity against human K562 cells assessed as cell viability after 72 hrs by CCK8 assay2014European journal of medicinal chemistry, May-06, Volume: 78Design, synthesis and bioevaluation of N-trisubstituted pyrimidine derivatives as potent aurora A kinase inhibitors.
AID1126541Antiproliferative activity against human HeLa cells assessed as cell viability after 72 hrs by CCK8 assay2014European journal of medicinal chemistry, May-06, Volume: 78Design, synthesis and bioevaluation of N-trisubstituted pyrimidine derivatives as potent aurora A kinase inhibitors.
AID1126535Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 72 hrs by CCK8 assay2014European journal of medicinal chemistry, May-06, Volume: 78Design, synthesis and bioevaluation of N-trisubstituted pyrimidine derivatives as potent aurora A kinase inhibitors.
AID1126534Antiproliferative activity against human MCF7 cells assessed as cell viability after 72 hrs by CCK8 assay2014European journal of medicinal chemistry, May-06, Volume: 78Design, synthesis and bioevaluation of N-trisubstituted pyrimidine derivatives as potent aurora A kinase inhibitors.
AID1126543Antiproliferative activity against human HCT116 cells assessed as cell viability after 72 hrs by CCK8 assay2014European journal of medicinal chemistry, May-06, Volume: 78Design, synthesis and bioevaluation of N-trisubstituted pyrimidine derivatives as potent aurora A kinase inhibitors.
AID1126540Antiproliferative activity against human PC3 cells assessed as cell viability after 72 hrs by CCK8 assay2014European journal of medicinal chemistry, May-06, Volume: 78Design, synthesis and bioevaluation of N-trisubstituted pyrimidine derivatives as potent aurora A kinase inhibitors.
AID1126539Antiproliferative activity against human DU145 cells assessed as cell viability after 72 hrs by CCK8 assay2014European journal of medicinal chemistry, May-06, Volume: 78Design, synthesis and bioevaluation of N-trisubstituted pyrimidine derivatives as potent aurora A kinase inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

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 (100.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

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%
Other5 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]