Compounds > ro3280
Page last updated: 2024-11-13

ro3280

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Description

RO3280: inhibits polo-like kinase 1; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID25015677
CHEMBL ID2392553
SCHEMBL ID1559146
MeSH IDM000609847

Synonyms (41)

Synonym
dtxcid7028485
cas-1062243-51-9
NCGC00257406-01
dtxsid4048511 ,
pharmagsid_48511
tox21_303518
bdbm50435735
chembl2392553 ,
S7248
4-(9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5h-pyrimido[4,5-b][1,4]diazepin-2-ylamino)-3-methoxy-n-(1-methyl-piperidin-4-yl)-benzamide
4-(9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5h-pyrimido[4,5-b][1,4]diazepin-2-ylamino)-3-methoxy-n-(1-methylpiperidin-4-yl)benzamide
ro3280
CS-1673
HY-15161
SCHEMBL1559146
4-((9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5h-pyrimido[4,5-b][1,4]diazepin-2-yl)amino)-3-methoxy-n-(1-methylpiperidin-4-yl)benzamide
1062243-51-9
gtpl9403
compound 7 [pmid: 22172702]
4-[(9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-8h-pyrimido[4,5-b][1,4]diazepin-2-yl)amino]-3-methoxy-n-(1-methylpiperidin-4-yl)benzamide
AKOS026750574
4-[(9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5h-pyrimido[4,5-b][1,4]diazepin-2-yl)amino]-3-methoxy-n-(1-methylpiperidin-4-yl)benzamide
79C ,
ro5203280
ro 3280
HMS3653O21
4-[(9-cyclopentyl-7,7-difluoro-6,7,8,9-tetrahydro-5-methyl-6-oxo-5h-pyrimido[4,5-b][1,4]diazepin-2-yl)amino]-3-methoxy-n-(1-methyl-4-piperidinyl)benzamide
NCGC00386371-04
ro3280, >=98% (hplc)
SW219316-1
FT-0744236
BCP07189
EX-A2150
ro-5203280
SB19474
CCG-269974
F84977
nsc-762154
nsc762154
AS-78052
tpki-24

Research Excerpts

Treatment

ExcerptReferenceRelevance
"RO3280 treatment regulated several apoptosis-associated genes."( Molecular targeting of the oncoprotein PLK1 in pediatric acute myeloid leukemia: RO3280, a novel PLK1 inhibitor, induces apoptosis in leukemia cells.
Cao, L; Du, XJ; Fang, F; Feng, X; Hu, SY; Jin, MF; Li, G; Li, YH; Li, YP; Li, ZH; Liu, L; Lu, J; Ni, J; Pan, J; Su, GH; Sun, LC; Tao, YF; Wang, J; Wang, NN; Wu, Y; Xiao, PF; Xu, LX; Xu, YY; Zhao, H; Zhao, WL; Zhou, HT; Zhu, XM, 2015)		1.36

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]

Protein Targets (37)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
acetylcholinesteraseHomo sapiens (human)Potency39.05740.002541.796015,848.9004AID1347395; AID1347397; AID1347398
RAR-related orphan receptor gammaMus musculus (house mouse)Potency12.50450.006038.004119,952.5996AID1159521; AID1159523
SMAD family member 2Homo sapiens (human)Potency50.36260.173734.304761.8120AID1346859; AID1346924
SMAD family member 3Homo sapiens (human)Potency50.36260.173734.304761.8120AID1346859; AID1346924
GLI family zinc finger 3Homo sapiens (human)Potency1.11560.000714.592883.7951AID1259368; AID1259369; AID1259392
AR proteinHomo sapiens (human)Potency4.82440.000221.22318,912.5098AID1259247; AID743035; AID743036; AID743042; AID743053; AID743054; AID743063
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency22.29710.013326.981070.7614AID1346978
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency24.70350.000657.913322,387.1992AID1259377; AID1259378
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency8.26810.001022.650876.6163AID1224838; AID1224839; AID1224893
progesterone receptorHomo sapiens (human)Potency28.07040.000417.946075.1148AID1346795
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency16.93300.01237.983543.2770AID1645841
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency47.62410.000214.376460.0339AID720691; AID720692
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency1.76390.003041.611522,387.1992AID1159552; AID1159553; AID1159555
retinoid X nuclear receptor alphaHomo sapiens (human)Potency7.11390.000817.505159.3239AID1159531
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency9.47610.001530.607315,848.9004AID1224841; AID1224842; AID1224848; AID1224849; AID1259401; AID1259403
farnesoid X nuclear receptorHomo sapiens (human)Potency12.04440.375827.485161.6524AID743217; AID743239
pregnane X nuclear receptorHomo sapiens (human)Potency19.87230.005428.02631,258.9301AID1346982
estrogen nuclear receptor alphaHomo sapiens (human)Potency1.11750.000229.305416,493.5996AID1259244; AID1259248; AID743069; AID743078; AID743079; AID743080; AID743091
cytochrome P450 2D6Homo sapiens (human)Potency23.91850.00108.379861.1304AID1645840
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency14.19410.001024.504861.6448AID743215
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency50.36260.001019.414170.9645AID743191
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency6.34030.023723.228263.5986AID743223
caspase-3Homo sapiens (human)Potency22.29710.013326.981070.7614AID1346978
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency12.53860.001723.839378.1014AID743083
thyroid stimulating hormone receptorHomo sapiens (human)Potency11.39360.001628.015177.1139AID1259385; AID1259395
Caspase-7Cricetulus griseus (Chinese hamster)Potency3.14950.006723.496068.5896AID1346980
caspase-3Cricetulus griseus (Chinese hamster)Potency3.14950.006723.496068.5896AID1346980
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency0.36750.000323.4451159.6830AID743065; AID743066; AID743067
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency49.91690.000627.21521,122.0200AID743202
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency2.80700.001557.789015,848.9004AID1259244
Cellular tumor antigen p53Homo sapiens (human)Potency42.56940.002319.595674.0614AID651631; AID720552
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency2.80700.001551.739315,848.9004AID1259244
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency2.04010.011917.942071.5630AID651632; AID720516
Ataxin-2Homo sapiens (human)Potency1.57850.011912.222168.7989AID651632
[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)
Serine/threonine-protein kinase PLK1Homo sapiens (human)IC50 (µMol)0.00400.00010.77349.0000AID753523
[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)
Bromodomain-containing protein 4Homo sapiens (human)Kd0.21570.00100.36918.9300AID1807750; AID1807751; AID1807752
Bromodomain testis-specific proteinHomo sapiens (human)Kd1.36330.02201.00834.8360AID1807754; AID1807755; AID1807756
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (196)

Processvia Protein(s)Taxonomy
regulation of transcription by RNA polymerase IIBromodomain-containing protein 4Homo sapiens (human)
positive regulation of G2/M transition of mitotic cell cycleBromodomain-containing protein 4Homo sapiens (human)
positive regulation of transcription elongation by RNA polymerase IIBromodomain-containing protein 4Homo sapiens (human)
chromatin organizationBromodomain-containing protein 4Homo sapiens (human)
DNA damage responseBromodomain-containing protein 4Homo sapiens (human)
positive regulation of transcription elongation by RNA polymerase IIBromodomain-containing protein 4Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionBromodomain-containing protein 4Homo sapiens (human)
positive regulation of DNA-templated transcriptionBromodomain-containing protein 4Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIBromodomain-containing protein 4Homo sapiens (human)
regulation of inflammatory responseBromodomain-containing protein 4Homo sapiens (human)
positive regulation of T-helper 17 cell lineage commitmentBromodomain-containing protein 4Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycle G2/M phase transitionCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
ER overload responseCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
mitophagyCellular tumor antigen p53Homo sapiens (human)
in utero embryonic developmentCellular tumor antigen p53Homo sapiens (human)
somitogenesisCellular tumor antigen p53Homo sapiens (human)
release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
hematopoietic progenitor cell differentiationCellular tumor antigen p53Homo sapiens (human)
T cell proliferation involved in immune responseCellular tumor antigen p53Homo sapiens (human)
B cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
T cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
response to ischemiaCellular tumor antigen p53Homo sapiens (human)
nucleotide-excision repairCellular tumor antigen p53Homo sapiens (human)
double-strand break repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
protein import into nucleusCellular tumor antigen p53Homo sapiens (human)
autophagyCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorCellular tumor antigen p53Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
Ras protein signal transductionCellular tumor antigen p53Homo sapiens (human)
gastrulationCellular tumor antigen p53Homo sapiens (human)
neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
protein localizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA replicationCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
determination of adult lifespanCellular tumor antigen p53Homo sapiens (human)
mRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
rRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
response to salt stressCellular tumor antigen p53Homo sapiens (human)
response to inorganic substanceCellular tumor antigen p53Homo sapiens (human)
response to X-rayCellular tumor antigen p53Homo sapiens (human)
response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
positive regulation of gene expressionCellular tumor antigen p53Homo sapiens (human)
cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
viral processCellular tumor antigen p53Homo sapiens (human)
glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
cerebellum developmentCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell growthCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCellular tumor antigen p53Homo sapiens (human)
negative regulation of telomere maintenance via telomeraseCellular tumor antigen p53Homo sapiens (human)
T cell differentiation in thymusCellular tumor antigen p53Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of tissue remodelingCellular tumor antigen p53Homo sapiens (human)
cellular response to UVCellular tumor antigen p53Homo sapiens (human)
multicellular organism growthCellular tumor antigen p53Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilityCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
entrainment of circadian clock by photoperiodCellular tumor antigen p53Homo sapiens (human)
mitochondrial DNA repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
transcription initiation-coupled chromatin remodelingCellular tumor antigen p53Homo sapiens (human)
negative regulation of proteolysisCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assemblyCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
response to antibioticCellular tumor antigen p53Homo sapiens (human)
fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
circadian behaviorCellular tumor antigen p53Homo sapiens (human)
bone marrow developmentCellular tumor antigen p53Homo sapiens (human)
embryonic organ developmentCellular tumor antigen p53Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationCellular tumor antigen p53Homo sapiens (human)
protein stabilizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of helicase activityCellular tumor antigen p53Homo sapiens (human)
protein tetramerizationCellular tumor antigen p53Homo sapiens (human)
chromosome organizationCellular tumor antigen p53Homo sapiens (human)
neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
hematopoietic stem cell differentiationCellular tumor antigen p53Homo sapiens (human)
negative regulation of glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
type II interferon-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
cardiac septum morphogenesisCellular tumor antigen p53Homo sapiens (human)
positive regulation of programmed necrotic cell deathCellular tumor antigen p53Homo sapiens (human)
protein-containing complex assemblyCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressCellular tumor antigen p53Homo sapiens (human)
thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
necroptotic processCellular tumor antigen p53Homo sapiens (human)
cellular response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
cellular response to xenobiotic stimulusCellular tumor antigen p53Homo sapiens (human)
cellular response to ionizing radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to UV-CCellular tumor antigen p53Homo sapiens (human)
stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
cellular response to actinomycin DCellular tumor antigen p53Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
cellular senescenceCellular tumor antigen p53Homo sapiens (human)
replicative senescenceCellular tumor antigen p53Homo sapiens (human)
oxidative stress-induced premature senescenceCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
oligodendrocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of execution phase of apoptosisCellular tumor antigen p53Homo sapiens (human)
negative regulation of mitophagyCellular tumor antigen p53Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of G1 to G0 transitionCellular tumor antigen p53Homo sapiens (human)
negative regulation of miRNA processingCellular tumor antigen p53Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
negative regulation of pentose-phosphate shuntCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
regulation of fibroblast apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
positive regulation of cellular senescenceCellular tumor antigen p53Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo 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)
positive regulation of gene expressionBromodomain testis-specific proteinHomo sapiens (human)
chromatin remodelingBromodomain testis-specific proteinHomo sapiens (human)
regulation of DNA-templated transcriptionBromodomain testis-specific proteinHomo sapiens (human)
mRNA processingBromodomain testis-specific proteinHomo sapiens (human)
male meiotic nuclear divisionBromodomain testis-specific proteinHomo sapiens (human)
male meiosis IBromodomain testis-specific proteinHomo sapiens (human)
RNA splicingBromodomain testis-specific proteinHomo sapiens (human)
sperm DNA condensationBromodomain testis-specific proteinHomo sapiens (human)
regulation of RNA splicingBromodomain testis-specific proteinHomo sapiens (human)
positive regulation of DNA-templated transcriptionBromodomain testis-specific proteinHomo sapiens (human)
cell population proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of B cell proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
nuclear DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
signal transduction in response to DNA damageATPase family AAA domain-containing protein 5Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
isotype switchingATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of isotype switching to IgG isotypesATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloadingATPase family AAA domain-containing protein 5Homo sapiens (human)
regulation of mitotic cell cycle phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of cell cycle G2/M phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (55)

Processvia Protein(s)Taxonomy
transcription cis-regulatory region bindingBromodomain-containing protein 4Homo sapiens (human)
p53 bindingBromodomain-containing protein 4Homo sapiens (human)
chromatin bindingBromodomain-containing protein 4Homo sapiens (human)
transcription coregulator activityBromodomain-containing protein 4Homo sapiens (human)
transcription coactivator activityBromodomain-containing protein 4Homo sapiens (human)
protein bindingBromodomain-containing protein 4Homo sapiens (human)
RNA polymerase II CTD heptapeptide repeat kinase activityBromodomain-containing protein 4Homo sapiens (human)
enzyme bindingBromodomain-containing protein 4Homo sapiens (human)
lysine-acetylated histone bindingBromodomain-containing protein 4Homo sapiens (human)
RNA polymerase II C-terminal domain bindingBromodomain-containing protein 4Homo sapiens (human)
P-TEFb complex bindingBromodomain-containing protein 4Homo sapiens (human)
histone reader activityBromodomain-containing protein 4Homo sapiens (human)
transcription cis-regulatory region bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
core promoter sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
TFIID-class transcription factor complex bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
protease bindingCellular tumor antigen p53Homo sapiens (human)
p53 bindingCellular tumor antigen p53Homo sapiens (human)
DNA bindingCellular tumor antigen p53Homo sapiens (human)
chromatin bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activityCellular tumor antigen p53Homo sapiens (human)
mRNA 3'-UTR bindingCellular tumor antigen p53Homo sapiens (human)
copper ion bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingCellular tumor antigen p53Homo sapiens (human)
zinc ion bindingCellular tumor antigen p53Homo sapiens (human)
enzyme bindingCellular tumor antigen p53Homo sapiens (human)
receptor tyrosine kinase bindingCellular tumor antigen p53Homo sapiens (human)
ubiquitin protein ligase bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase regulator activityCellular tumor antigen p53Homo sapiens (human)
ATP-dependent DNA/DNA annealing activityCellular tumor antigen p53Homo sapiens (human)
identical protein bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase bindingCellular tumor antigen p53Homo sapiens (human)
protein heterodimerization activityCellular tumor antigen p53Homo sapiens (human)
protein-folding chaperone bindingCellular tumor antigen p53Homo sapiens (human)
protein phosphatase 2A bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCellular tumor antigen p53Homo sapiens (human)
14-3-3 protein bindingCellular tumor antigen p53Homo sapiens (human)
MDM2/MDM4 family protein bindingCellular tumor antigen p53Homo sapiens (human)
disordered domain specific bindingCellular tumor antigen p53Homo sapiens (human)
general transcription initiation factor bindingCellular tumor antigen p53Homo sapiens (human)
molecular function activator activityCellular tumor antigen p53Homo sapiens (human)
promoter-specific chromatin bindingCellular tumor antigen p53Homo 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)
transcription coactivator activityBromodomain testis-specific proteinHomo sapiens (human)
histone bindingBromodomain testis-specific proteinHomo sapiens (human)
lysine-acetylated histone bindingBromodomain testis-specific proteinHomo sapiens (human)
histone reader activityBromodomain testis-specific proteinHomo sapiens (human)
protein bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP hydrolysis activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloader activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (40)

Processvia Protein(s)Taxonomy
condensed nuclear chromosomeBromodomain-containing protein 4Homo sapiens (human)
nucleusBromodomain-containing protein 4Homo sapiens (human)
nucleoplasmBromodomain-containing protein 4Homo sapiens (human)
nuclear bodyCellular tumor antigen p53Homo sapiens (human)
nucleusCellular tumor antigen p53Homo sapiens (human)
nucleoplasmCellular tumor antigen p53Homo sapiens (human)
replication forkCellular tumor antigen p53Homo sapiens (human)
nucleolusCellular tumor antigen p53Homo sapiens (human)
cytoplasmCellular tumor antigen p53Homo sapiens (human)
mitochondrionCellular tumor antigen p53Homo sapiens (human)
mitochondrial matrixCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulumCellular tumor antigen p53Homo sapiens (human)
centrosomeCellular tumor antigen p53Homo sapiens (human)
cytosolCellular tumor antigen p53Homo sapiens (human)
nuclear matrixCellular tumor antigen p53Homo sapiens (human)
PML bodyCellular tumor antigen p53Homo sapiens (human)
transcription repressor complexCellular tumor antigen p53Homo sapiens (human)
site of double-strand breakCellular tumor antigen p53Homo sapiens (human)
germ cell nucleusCellular tumor antigen p53Homo sapiens (human)
chromatinCellular tumor antigen p53Homo sapiens (human)
transcription regulator complexCellular tumor antigen p53Homo sapiens (human)
protein-containing complexCellular tumor antigen p53Homo sapiens (human)
plasma membraneGlutamate receptor 2Rattus norvegicus (Norway rat)
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)
nucleusBromodomain testis-specific proteinHomo sapiens (human)
Elg1 RFC-like complexATPase family AAA domain-containing protein 5Homo sapiens (human)
nucleusATPase family AAA domain-containing protein 5Homo sapiens (human)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (30)

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.
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.
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.
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.
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.
AID1807756Binding affinity to recombinant human N-terminal hexaHis-tagged BRDT expressed in Escherichia coli BL21 (DE3) cells by ITC analysis2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors.
AID1807758Inhibition of cell growth in HEK293T cells incubated for 72 hrs by CellTiter-blue reagent based assay2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors.
AID1807763Inhibition of PLK1 in HEK293T cells assessed as increase in p21 levels at 0.0001 to 10 uM incubated for 6 hrs by immunoblotting analysis2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors.
AID1807750Binding affinity to recombinant human N-terminal hexaHis-tagged BRD4 expressed in Escherichia coli BL21 (DE3) cells by MST assay2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors.
AID1807761Inhibition of PLK1 in human MM1.S cells assessed as increase in p21 levels incubated for 6 hrs by immunoblotting analysis2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors.
AID1807753Binding affinity to recombinant human N-terminal hexaHis-tagged BRDT expressed in Escherichia coli BL21 (DE3) cells assessed as change in melting temperature by DSF assay2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors.
AID1807755Binding affinity to recombinant human N-terminal hexaHis-tagged BRDT expressed in Escherichia coli BL21 (DE3) cells by qPCR assay2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors.
AID1807757Inhibition of cell growth in human MM1.S cells incubated for 72 hrs by CellTiter-blue reagent based assay2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors.
AID753522Inhibition of PLK1 (21 to 351) (unknown origin) assessed as half life of dissociation rate using FAM-mTOR peptide as substrate2013Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12
Discovery of TAK-960: an orally available small molecule inhibitor of polo-like kinase 1 (PLK1).
AID753517Volume of distribution at steady state in rat at 1 mg/kg, iv and 5 mg/kg, po2013Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12
Discovery of TAK-960: an orally available small molecule inhibitor of polo-like kinase 1 (PLK1).
AID1807760Inhibition of PLK1 in human MM1.S cells assessed as reduction in c-Myc levels incubated for 6 hrs by immunoblotting analysis2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors.
AID1807752Binding affinity to recombinant human N-terminal hexaHis-tagged BRD4 expressed in Escherichia coli BL21 (DE3) cells by ITC analysis2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors.
AID753516Oral bioavailability in rat at 5 mg/kg2013Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12
Discovery of TAK-960: an orally available small molecule inhibitor of polo-like kinase 1 (PLK1).
AID753519Clearance in rat at 1 mg/kg, iv and 5 mg/kg, po2013Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12
Discovery of TAK-960: an orally available small molecule inhibitor of polo-like kinase 1 (PLK1).
AID753521Antiproliferative activity against human HT-29 cells after 72 hrs by Cell Titer-Glo Assay2013Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12
Discovery of TAK-960: an orally available small molecule inhibitor of polo-like kinase 1 (PLK1).
AID753518Half life in rat at 1 mg/kg, iv and 5 mg/kg, po2013Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12
Discovery of TAK-960: an orally available small molecule inhibitor of polo-like kinase 1 (PLK1).
AID1807749Binding affinity to recombinant human N-terminal hexaHis-tagged BRD4 expressed in Escherichia coli BL21 (DE3) cells assessed as change in melting temperature by DSF assay2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors.
AID1807754Binding affinity to recombinant human N-terminal hexaHis-tagged BRDT expressed in Escherichia coli BL21 (DE3) cells by MST assay2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors.
AID753520Ratio of efflux ratio in pig LLC cells expressing MDR to efflux ratio in wild type pig LLC cells2013Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12
Discovery of TAK-960: an orally available small molecule inhibitor of polo-like kinase 1 (PLK1).
AID753523Inhibition of PLK1 (unknown origin) using biotin-AGAGTVPESIHSFIGDGLV as substrate by TR-FRET assay2013Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12
Discovery of TAK-960: an orally available small molecule inhibitor of polo-like kinase 1 (PLK1).
AID1807751Binding affinity to recombinant human N-terminal hexaHis-tagged BRD4 expressed in Escherichia coli BL21 (DE3) cells by qPCR assay2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors.
AID1807759Inhibition of PLK1 in HEK293T cells assessed as reduction in phosphorylation of TCTP at S46 residue at 30 to 100 nM incubated for 6 hrs by immunoblotting analysis2021Journal of medicinal chemistry, 11-11, Volume: 64, Issue:21
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors.
AID1345608Human FER tyrosine kinase (Fer family)2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
Identification of novel, potent and selective inhibitors of Polo-like kinase 1.
AID1345775Human polo like kinase 1 (Polo-like kinase (PLK) family)2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
Identification of novel, potent and selective inhibitors of Polo-like kinase 1.
AID1345801Human TTK protein kinase (TTK family)2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
Identification of novel, potent and selective inhibitors of Polo-like 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's0 (0.00)29.6817
2010's6 (60.00)24.3611
2020's4 (40.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 17.29

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 Index17.29 (24.57)
Research Supply Index2.48 (2.92)
Research Growth Index4.59 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (17.29)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (10.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other9 (90.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
volasertib
BI 6727: a polo-like kinase inhibitor with broad antitumor activity; structure in first source		2.3110
bi 2536
[no description available]		2.3110
gsk 461364
GSK 461364: an antineoplastic agent that inhibits polo-like kinase 1		2.8220(trifluoromethyl)benzenes
xmd 8-92
XMD8-92 : A dimethylpyrimido[4,5-b][1,4]benzodiazepin-6-one carrying at C-2 on the pyrimidine ring a [2-ethoxy-4-(4-hydroxypiperidin-1-yl)phenyl]amino substituent. It is an inhibitor of the BMK1 kinase pathway.		2.3110pyrimidobenzodiazepineprotein kinase inhibitor
lrrk2-in1
LRRK2-IN1: inhibits leucine-rich repeat kinase 2; structure in first source		2.3110aromatic amine;
aromatic ether;
N-acylpiperidine;
N-alkylpiperazine;
pyrimidobenzodiazepine;
secondary amino compound;
tertiary amino compound		antineoplastic agent;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor
jq1 compound
[no description available]		2.3110carboxylic ester;
organochlorine compound;
tert-butyl ester;
thienotriazolodiazepine		angiogenesis inhibitor;
anti-inflammatory agent;
antineoplastic agent;
apoptosis inducer;
bromodomain-containing protein 4 inhibitor;
cardioprotective agent;
ferroptosis inducer
tak-960
4-((9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido(4,5-b)(1,4)diazepin-2-yl)amino)-2-fluoro-5-methoxy-N-(1-methylpiperidin-4-yl)benzamide: a polo-like kinase 1 inhibitor; structure in first source		3.4711
ConditionIndicatedRelationship StrengthStudiesTrials
Experimental Neoplasms
[description not available]		02.0710
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.		02.5420
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
Breast Cancer
[description not available]		07.2110
Breast Neoplasms
Tumors or cancer of the human BREAST.		02.2110
Acute Myelogenous Leukemia
[description not available]		02.1110
Leukemia, Myeloid, Acute
Clonal expansion of myeloid blasts in bone marrow, blood, and other tissue. Myeloid leukemias develop from changes in cells that normally produce NEUTROPHILS; BASOPHILS; EOSINOPHILS; and MONOCYTES.		02.1110
Nasopharyngeal Carcinoma
A carcinoma that originates in the EPITHELIUM of the NASOPHARYNX and includes four subtypes: keratinizing squamous cell, non-keratinizing, basaloid squamous cell, and PAPILLARY ADENOCARCINOMA. It is most prevalent in Southeast Asian populations and is associated with EPSTEIN-BARR VIRUS INFECTIONS. Somatic mutations associated with this cancer have been identified in NPCR, BAP1, UBAP1, ERBB2, ERBB3, MLL2, PIK3CA, KRAS, NRAS, and ARID1A genes.		02.0810
Carcinoma, Anaplastic
[description not available]		02.0810
Cancer of Nasopharynx
[description not available]		02.0810
Carcinoma
A malignant neoplasm made up of epithelial cells tending to infiltrate the surrounding tissues and give rise to metastases. It is a histological type of neoplasm and not a synonym for cancer.		02.0810
Nasopharyngeal Neoplasms
Tumors or cancer of the NASOPHARYNX.		02.0810