Page last updated: 2024-10-15

can 508

Description

CAN 508: has antiangiogenic activity; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

CAN-508 : A member of the class of pyrazoles that is 1H-pyrazole substituted by amino, (4-hydroxyphenyl)diazenyl, and amino groups at positions 3, 4 and 5, respectively. It is a CDK9 inhibitor (IC50 = 0.35 muM) with 38-fold selectivity for CDK9/cyclin T over other CDK/cyclin complexes. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID135398514
CHEMBL ID215205
CHEMBL ID1823556
CHEBI ID42356
SCHEMBL ID3310182
SCHEMBL ID922292
SCHEMBL ID12589685
MeSH IDM0569491

Synonyms (53)

Synonym
4-[(e)-(3,5-diamino-1h-pyrazol-4-yl)diazenyl]phenol
F18 ,
bdbm12028
4-[(e)-2-(3,5-diamino-1h-pyrazol-4-yl)diazen-1-yl]phenol
can508
2CLX
4-arylazo-3,5-diamino-1h-pyrazole 31b
cdk9 inhibitor ii
4-(3,5-diamino-1h-pyrazol-4-ylazo)-phenol
AKOS000272941
can-508
DB07731
CHEMBL215205 ,
HMS3229D19
nsc-741614
nsc741614
3,5-diamino-4-(4-hydroxyphenyl)azopyrazole
bdbm50352019
chembl1823556
zg0o47k626 ,
unii-zg0o47k626
phenol, 4-((3,5-diamino-1h-pyrazol-4-yl)azo)-
phenol, 4-(2-(3,5-diamino-1h-pyrazol-4-yl)diazenyl)-
3TNH
140651-18-9
3TN8
SCHEMBL3310182
SCHEMBL922292
SCHEMBL12589685
phenol, 4-[(3,5-diamino-1h-pyrazol-4-yl)azo]-
1649984-48-4
J-007412
4-[(z)-(3,5-diamino-1h-pyrazol-4-yl)diazenyl]phenol
4-[(3,5-diamino-1h-pyrazol-4-yl)diazenyl]phenol
4-[2-(3,5-diamino-1h-pyrazol-4-yl)diazen-1-yl]phenol
Q27096948
can-508;can508;cdk9 inhibitor ii
can 508
HY-100429
phenol, 4-[2-(3,5-diamino-1h-pyrazol-4-yl)diazenyl]-
CS-0018885
NCGC00388443-01
4-((3,5-diamino-1h-pyrazol-4-yl)diazenyl)phenol
DTXSID90901895
noname_1070
MS-23203
4-[(3,5-diamino-1h-pyrazol-4-yl)azo]-phenol
cay10574
(e)-4-((3,5-diamino-1h-pyrazol-4-yl)diazenyl)phenol
bdbm50455463
cay 10574
cay-10574
CHEBI:42356

Bioavailability

ExcerptReference
"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
)
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (4)

RoleDescription
angiogenesis inhibitorAn agent and endogenous substances that antagonize or inhibit the development of new blood vessels.
EC 2.7.11.22 (cyclin-dependent kinase) inhibitorAn EC 2.7.11.* (protein-serine/threonine kinase) inhibitor that interferes with the action of cyclin-dependent kinase (EC 2.7.11.22).
antineoplastic agentA substance that inhibits or prevents the proliferation of neoplasms.
apoptosis inducerAny substance that induces the process of apoptosis (programmed cell death) in multi-celled organisms.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (4)

ClassDescription
pyrazoles
phenolsOrganic aromatic compounds having one or more hydroxy groups attached to a benzene or other arene ring.
aromatic amineAn amino compound in which the amino group is linked directly to an aromatic system.
monoazo compoundCompounds containing single -N=N- group.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (18)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Cyclin-dependent kinase 9Homo sapiens (human)IC50 (µMol)0.74000.74000.74000.7400AID977608
Cyclin-T1Homo sapiens (human)IC50 (µMol)17.40500.00100.55858.0000AID1194742; AID1375009; AID1689408; AID1796840; AID272423
Cyclin-T1Homo sapiens (human)Ki0.35000.00300.27680.7900AID723735
G2/mitotic-specific cyclin-B2Homo sapiens (human)IC50 (µMol)44.00000.00251.817210.0000AID272419
G1/S-specific cyclin-E2Homo sapiens (human)IC50 (µMol)11.75000.00101.739410.0000AID272408; AID272418
G1/S-specific cyclin-E2Homo sapiens (human)Ki13.30000.54000.54000.5400AID272417
Cyclin-dependent kinase 1Homo sapiens (human)IC50 (µMol)28.05380.00041.345210.0000AID1194739; AID1796840; AID1800495; AID272419
Cyclin-dependent kinase 4Homo sapiens (human)IC50 (µMol)23.36150.00060.570610.0000AID1194740; AID1796840; AID1800495; AID272421
G2/mitotic-specific cyclin-B1Homo sapiens (human)IC50 (µMol)32.60620.00131.451810.0000AID1194739; AID1796840; AID272419
Cyclin-A2Homo sapiens (human)IC50 (µMol)31.86880.00041.033910.0000AID1375008; AID1796840; AID272420
Cyclin-A2Homo sapiens (human)Ki69.00000.00100.70075.0000AID723734
Ribosomal protein S6 kinase beta-1Homo sapiens (human)IC50 (µMol)10.00000.00040.904610.0000AID272483
G1/S-specific cyclin-D1Homo sapiens (human)IC50 (µMol)24.98120.00060.54799.5000AID1194740; AID1796840; AID272421
G1/S-specific cyclin-E1Homo sapiens (human)IC50 (µMol)23.63500.00101.040410.0000AID1194735; AID1689407; AID1796840; AID272408; AID272418
G1/S-specific cyclin-E1Homo sapiens (human)Ki13.30000.00050.56331.4850AID272417
Cyclin-dependent kinase 2Homo sapiens (human)IC50 (µMol)24.84120.00041.044410.0000AID1194735; AID1375008; AID1689407; AID1796840; AID1800495; AID272408; AID272418; AID272420
Cyclin-dependent kinase 2Homo sapiens (human)Ki41.15000.00050.64275.0000AID272417; AID723734
Cyclin-dependent kinase 7Homo sapiens (human)IC50 (µMol)25.28460.00010.91069.2000AID1194741; AID1796840; AID1800495; AID272422
Cyclin-dependent kinase 9Homo sapiens (human)IC50 (µMol)17.39060.00100.62368.0000AID1194742; AID1375009; AID1689408; AID1796840; AID1800495; AID272423; AID617519
Cyclin-dependent kinase 9Homo sapiens (human)Ki0.35000.00300.24820.7900AID723735
Cyclin-HHomo sapiens (human)IC50 (µMol)28.10620.00051.08239.2000AID1194741; AID1796840; AID272422
Cyclin-A1Homo sapiens (human)IC50 (µMol)69.00000.00051.471510.0000AID272420
Cyclin-A1Homo sapiens (human)Ki69.00000.00400.14800.2500AID723734
G2/mitotic-specific cyclin-B3Homo sapiens (human)IC50 (µMol)44.00000.00251.817210.0000AID272419
Ribosomal protein S6 kinase beta-2Homo sapiens (human)IC50 (µMol)10.00000.00072.503810.0000AID272483
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (186)

Processvia Protein(s)Taxonomy
regulation of cyclin-dependent protein serine/threonine kinase activityCyclin-T1Homo sapiens (human)
transcription by RNA polymerase IICyclin-T1Homo sapiens (human)
response to xenobiotic stimulusCyclin-T1Homo sapiens (human)
positive regulation of transcription elongation by RNA polymerase IICyclin-T1Homo sapiens (human)
positive regulation by host of viral transcriptionCyclin-T1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICyclin-T1Homo sapiens (human)
cell divisionCyclin-T1Homo sapiens (human)
regulation of transcription by RNA polymerase IICyclin-T1Homo sapiens (human)
positive regulation of DNA-templated transcription, elongationCyclin-T1Homo sapiens (human)
in utero embryonic developmentG2/mitotic-specific cyclin-B2Homo sapiens (human)
spindle assembly involved in female meiosis IG2/mitotic-specific cyclin-B2Homo sapiens (human)
G2/MI transition of meiotic cell cycleG2/mitotic-specific cyclin-B2Homo sapiens (human)
regulation of growthG2/mitotic-specific cyclin-B2Homo sapiens (human)
T cell homeostasisG2/mitotic-specific cyclin-B2Homo sapiens (human)
thymus developmentG2/mitotic-specific cyclin-B2Homo sapiens (human)
cell divisionG2/mitotic-specific cyclin-B2Homo sapiens (human)
regulation of cyclin-dependent protein serine/threonine kinase activityG2/mitotic-specific cyclin-B2Homo sapiens (human)
mitotic cell cycle phase transitionG2/mitotic-specific cyclin-B2Homo sapiens (human)
regulation of cyclin-dependent protein serine/threonine kinase activityG1/S-specific cyclin-E2Homo sapiens (human)
G1/S transition of mitotic cell cycleG1/S-specific cyclin-E2Homo sapiens (human)
telomere maintenanceG1/S-specific cyclin-E2Homo sapiens (human)
DNA replication initiationG1/S-specific cyclin-E2Homo sapiens (human)
homologous chromosome pairing at meiosisG1/S-specific cyclin-E2Homo sapiens (human)
regulation of protein localizationG1/S-specific cyclin-E2Homo sapiens (human)
cell divisionG1/S-specific cyclin-E2Homo sapiens (human)
positive regulation of G1/S transition of mitotic cell cycleG1/S-specific cyclin-E2Homo sapiens (human)
G1/S transition of mitotic cell cycleCyclin-dependent kinase 1Homo sapiens (human)
G2/M transition of mitotic cell cycleCyclin-dependent kinase 1Homo sapiens (human)
microtubule cytoskeleton organizationCyclin-dependent kinase 1Homo sapiens (human)
DNA replicationCyclin-dependent kinase 1Homo sapiens (human)
DNA repairCyclin-dependent kinase 1Homo sapiens (human)
chromatin remodelingCyclin-dependent kinase 1Homo sapiens (human)
regulation of transcription by RNA polymerase IICyclin-dependent kinase 1Homo sapiens (human)
protein phosphorylationCyclin-dependent kinase 1Homo sapiens (human)
apoptotic processCyclin-dependent kinase 1Homo sapiens (human)
DNA damage responseCyclin-dependent kinase 1Homo sapiens (human)
mitotic nuclear membrane disassemblyCyclin-dependent kinase 1Homo sapiens (human)
centrosome cycleCyclin-dependent kinase 1Homo sapiens (human)
pronuclear fusionCyclin-dependent kinase 1Homo sapiens (human)
response to xenobiotic stimulusCyclin-dependent kinase 1Homo sapiens (human)
response to toxic substanceCyclin-dependent kinase 1Homo sapiens (human)
positive regulation of gene expressionCyclin-dependent kinase 1Homo sapiens (human)
negative regulation of gene expressionCyclin-dependent kinase 1Homo sapiens (human)
positive regulation of G2/M transition of mitotic cell cycleCyclin-dependent kinase 1Homo sapiens (human)
regulation of Schwann cell differentiationCyclin-dependent kinase 1Homo sapiens (human)
response to amineCyclin-dependent kinase 1Homo sapiens (human)
response to activityCyclin-dependent kinase 1Homo sapiens (human)
cell migrationCyclin-dependent kinase 1Homo sapiens (human)
peptidyl-serine phosphorylationCyclin-dependent kinase 1Homo sapiens (human)
peptidyl-threonine phosphorylationCyclin-dependent kinase 1Homo sapiens (human)
chromosome condensationCyclin-dependent kinase 1Homo sapiens (human)
epithelial cell differentiationCyclin-dependent kinase 1Homo sapiens (human)
animal organ regenerationCyclin-dependent kinase 1Homo sapiens (human)
protein localization to kinetochoreCyclin-dependent kinase 1Homo sapiens (human)
positive regulation of protein import into nucleusCyclin-dependent kinase 1Homo sapiens (human)
regulation of circadian rhythmCyclin-dependent kinase 1Homo sapiens (human)
negative regulation of apoptotic processCyclin-dependent kinase 1Homo sapiens (human)
response to ethanolCyclin-dependent kinase 1Homo sapiens (human)
positive regulation of DNA replicationCyclin-dependent kinase 1Homo sapiens (human)
regulation of embryonic developmentCyclin-dependent kinase 1Homo sapiens (human)
response to cadmium ionCyclin-dependent kinase 1Homo sapiens (human)
response to copper ionCyclin-dependent kinase 1Homo sapiens (human)
symbiont entry into host cellCyclin-dependent kinase 1Homo sapiens (human)
fibroblast proliferationCyclin-dependent kinase 1Homo sapiens (human)
rhythmic processCyclin-dependent kinase 1Homo sapiens (human)
response to axon injuryCyclin-dependent kinase 1Homo sapiens (human)
cell divisionCyclin-dependent kinase 1Homo sapiens (human)
ventricular cardiac muscle cell developmentCyclin-dependent kinase 1Homo sapiens (human)
positive regulation of cardiac muscle cell proliferationCyclin-dependent kinase 1Homo sapiens (human)
positive regulation of mitotic sister chromatid segregationCyclin-dependent kinase 1Homo sapiens (human)
protein-containing complex assemblyCyclin-dependent kinase 1Homo sapiens (human)
cellular response to hydrogen peroxideCyclin-dependent kinase 1Homo sapiens (human)
ERK1 and ERK2 cascadeCyclin-dependent kinase 1Homo sapiens (human)
cellular response to organic cyclic compoundCyclin-dependent kinase 1Homo sapiens (human)
Golgi disassemblyCyclin-dependent kinase 1Homo sapiens (human)
positive regulation of protein localization to nucleusCyclin-dependent kinase 1Homo sapiens (human)
regulation of attachment of mitotic spindle microtubules to kinetochoreCyclin-dependent kinase 1Homo sapiens (human)
microtubule cytoskeleton organization involved in mitosisCyclin-dependent kinase 1Homo sapiens (human)
positive regulation of mitochondrial ATP synthesis coupled electron transportCyclin-dependent kinase 1Homo sapiens (human)
mitotic G2 DNA damage checkpoint signalingCyclin-dependent kinase 1Homo sapiens (human)
protein deubiquitinationCyclin-dependent kinase 1Homo sapiens (human)
G1/S transition of mitotic cell cycleCyclin-dependent kinase 4Homo sapiens (human)
protein phosphorylationCyclin-dependent kinase 4Homo sapiens (human)
positive regulation of cell population proliferationCyclin-dependent kinase 4Homo sapiens (human)
response to xenobiotic stimulusCyclin-dependent kinase 4Homo sapiens (human)
regulation of gene expressionCyclin-dependent kinase 4Homo sapiens (human)
positive regulation of G2/M transition of mitotic cell cycleCyclin-dependent kinase 4Homo sapiens (human)
positive regulation of fibroblast proliferationCyclin-dependent kinase 4Homo sapiens (human)
cell divisionCyclin-dependent kinase 4Homo sapiens (human)
regulation of cell cycleCyclin-dependent kinase 4Homo sapiens (human)
regulation of transcription initiation by RNA polymerase IICyclin-dependent kinase 4Homo sapiens (human)
regulation of type B pancreatic cell proliferationCyclin-dependent kinase 4Homo sapiens (human)
cellular response to lipopolysaccharideCyclin-dependent kinase 4Homo sapiens (human)
cellular response to interleukin-4Cyclin-dependent kinase 4Homo sapiens (human)
cellular response to phorbol 13-acetate 12-myristateCyclin-dependent kinase 4Homo sapiens (human)
cellular response to ionomycinCyclin-dependent kinase 4Homo sapiens (human)
response to organic substanceCyclin-dependent kinase 4Homo sapiens (human)
regulation of G2/M transition of mitotic cell cycleCyclin-dependent kinase 4Homo sapiens (human)
signal transductionCyclin-dependent kinase 4Homo sapiens (human)
G2/M transition of mitotic cell cycleG2/mitotic-specific cyclin-B1Homo sapiens (human)
in utero embryonic developmentG2/mitotic-specific cyclin-B1Homo sapiens (human)
mitotic spindle organizationG2/mitotic-specific cyclin-B1Homo sapiens (human)
mitotic metaphase chromosome alignmentG2/mitotic-specific cyclin-B1Homo sapiens (human)
positive regulation of G2/M transition of mitotic cell cycleG2/mitotic-specific cyclin-B1Homo sapiens (human)
positive regulation of mitotic cell cycleG2/mitotic-specific cyclin-B1Homo sapiens (human)
positive regulation of fibroblast proliferationG2/mitotic-specific cyclin-B1Homo sapiens (human)
cell divisionG2/mitotic-specific cyclin-B1Homo sapiens (human)
positive regulation of attachment of spindle microtubules to kinetochoreG2/mitotic-specific cyclin-B1Homo sapiens (human)
regulation of mitotic cell cycle spindle assembly checkpointG2/mitotic-specific cyclin-B1Homo sapiens (human)
positive regulation of mitochondrial ATP synthesis coupled electron transportG2/mitotic-specific cyclin-B1Homo sapiens (human)
regulation of cyclin-dependent protein serine/threonine kinase activityG2/mitotic-specific cyclin-B1Homo sapiens (human)
mitotic cell cycle phase transitionG2/mitotic-specific cyclin-B1Homo sapiens (human)
G1/S transition of mitotic cell cycleCyclin-A2Homo sapiens (human)
G2/M transition of mitotic cell cycleCyclin-A2Homo sapiens (human)
regulation of DNA replicationCyclin-A2Homo sapiens (human)
DNA-templated transcriptionCyclin-A2Homo sapiens (human)
Ras protein signal transductionCyclin-A2Homo sapiens (human)
animal organ regenerationCyclin-A2Homo sapiens (human)
response to glucagonCyclin-A2Homo sapiens (human)
cellular response to platelet-derived growth factor stimulusCyclin-A2Homo sapiens (human)
post-translational protein modificationCyclin-A2Homo sapiens (human)
cellular response to leptin stimulusCyclin-A2Homo sapiens (human)
cell cycle G1/S phase transitionCyclin-A2Homo sapiens (human)
positive regulation of DNA-templated transcriptionCyclin-A2Homo sapiens (human)
positive regulation of fibroblast proliferationCyclin-A2Homo sapiens (human)
cell divisionCyclin-A2Homo sapiens (human)
cellular response to cocaineCyclin-A2Homo sapiens (human)
cellular response to luteinizing hormone stimulusCyclin-A2Homo sapiens (human)
cellular response to estradiol stimulusCyclin-A2Homo sapiens (human)
cellular response to hypoxiaCyclin-A2Homo sapiens (human)
cellular response to nitric oxideCyclin-A2Homo sapiens (human)
cochlea developmentCyclin-A2Homo sapiens (human)
cellular response to insulin-like growth factor stimulusCyclin-A2Homo sapiens (human)
positive regulation of DNA biosynthetic processCyclin-A2Homo sapiens (human)
regulation of cyclin-dependent protein serine/threonine kinase activityCyclin-A2Homo sapiens (human)
mitotic cell cycle phase transitionCyclin-A2Homo sapiens (human)
G1/S transition of mitotic cell cycleRibosomal protein S6 kinase beta-1Homo sapiens (human)
behavioral fear responseRibosomal protein S6 kinase beta-1Homo sapiens (human)
skeletal muscle contractionRibosomal protein S6 kinase beta-1Homo sapiens (human)
apoptotic processRibosomal protein S6 kinase beta-1Homo sapiens (human)
signal transductionRibosomal protein S6 kinase beta-1Homo sapiens (human)
germ cell developmentRibosomal protein S6 kinase beta-1Homo sapiens (human)
long-term memoryRibosomal protein S6 kinase beta-1Homo sapiens (human)
response to xenobiotic stimulusRibosomal protein S6 kinase beta-1Homo sapiens (human)
response to mechanical stimulusRibosomal protein S6 kinase beta-1Homo sapiens (human)
response to toxic substanceRibosomal protein S6 kinase beta-1Homo sapiens (human)
response to glucoseRibosomal protein S6 kinase beta-1Homo sapiens (human)
skeletal muscle atrophyRibosomal protein S6 kinase beta-1Homo sapiens (human)
response to electrical stimulus involved in regulation of muscle adaptationRibosomal protein S6 kinase beta-1Homo sapiens (human)
positive regulation of smooth muscle cell migrationRibosomal protein S6 kinase beta-1Homo sapiens (human)
cell migrationRibosomal protein S6 kinase beta-1Homo sapiens (human)
peptidyl-serine phosphorylationRibosomal protein S6 kinase beta-1Homo sapiens (human)
response to nutrient levelsRibosomal protein S6 kinase beta-1Homo sapiens (human)
cellular response to nutrientRibosomal protein S6 kinase beta-1Homo sapiens (human)
TOR signalingRibosomal protein S6 kinase beta-1Homo sapiens (human)
response to lipopolysaccharideRibosomal protein S6 kinase beta-1Homo sapiens (human)
response to testosteroneRibosomal protein S6 kinase beta-1Homo sapiens (human)
response to glucagonRibosomal protein S6 kinase beta-1Homo sapiens (human)
response to tumor necrosis factorRibosomal protein S6 kinase beta-1Homo sapiens (human)
negative regulation of apoptotic processRibosomal protein S6 kinase beta-1Homo sapiens (human)
response to L-leucineRibosomal protein S6 kinase beta-1Homo sapiens (human)
long-chain fatty acid import into cellRibosomal protein S6 kinase beta-1Homo sapiens (human)
response to ethanolRibosomal protein S6 kinase beta-1Homo sapiens (human)
positive regulation of translationRibosomal protein S6 kinase beta-1Homo sapiens (human)
positive regulation of mitotic cell cycleRibosomal protein S6 kinase beta-1Homo sapiens (human)
positive regulation of translational initiationRibosomal protein S6 kinase beta-1Homo sapiens (human)
regulation of glucose importRibosomal protein S6 kinase beta-1Homo sapiens (human)
negative regulation of insulin receptor signaling pathwayRibosomal protein S6 kinase beta-1Homo sapiens (human)
phosphatidylinositol-mediated signalingRibosomal protein S6 kinase beta-1Homo sapiens (human)
positive regulation of skeletal muscle tissue growthRibosomal protein S6 kinase beta-1Homo sapiens (human)
positive regulation of smooth muscle cell proliferationRibosomal protein S6 kinase beta-1Homo sapiens (human)
modulation of chemical synaptic transmissionRibosomal protein S6 kinase beta-1Homo sapiens (human)
cellular response to type II interferonRibosomal protein S6 kinase beta-1Homo sapiens (human)
cellular response to growth factor stimulusRibosomal protein S6 kinase beta-1Homo sapiens (human)
cellular response to dexamethasone stimulusRibosomal protein S6 kinase beta-1Homo sapiens (human)
positive regulation of TORC1 signalingRibosomal protein S6 kinase beta-1Homo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathwayRibosomal protein S6 kinase beta-1Homo sapiens (human)
cellular response to insulin stimulusRibosomal protein S6 kinase beta-1Homo sapiens (human)
G1/S transition of mitotic cell cycleG1/S-specific cyclin-D1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIG1/S-specific cyclin-D1Homo sapiens (human)
re-entry into mitotic cell cycleG1/S-specific cyclin-D1Homo sapiens (human)
positive regulation of protein phosphorylationG1/S-specific cyclin-D1Homo sapiens (human)
DNA damage responseG1/S-specific cyclin-D1Homo sapiens (human)
lactationG1/S-specific cyclin-D1Homo sapiens (human)
response to xenobiotic stimulusG1/S-specific cyclin-D1Homo sapiens (human)
positive regulation of G2/M transition of mitotic cell cycleG1/S-specific cyclin-D1Homo sapiens (human)
Wnt signaling pathwayG1/S-specific cyclin-D1Homo sapiens (human)
neuron differentiationG1/S-specific cyclin-D1Homo sapiens (human)
negative regulation of epithelial cell differentiationG1/S-specific cyclin-D1Homo sapiens (human)
endoplasmic reticulum unfolded protein responseG1/S-specific cyclin-D1Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingG1/S-specific cyclin-D1Homo sapiens (human)
mammary gland epithelial cell proliferationG1/S-specific cyclin-D1Homo sapiens (human)
positive regulation of mammary gland epithelial cell proliferationG1/S-specific cyclin-D1Homo sapiens (human)
negative regulation of neuron apoptotic processG1/S-specific cyclin-D1Homo sapiens (human)
response to leptinG1/S-specific cyclin-D1Homo sapiens (human)
fat cell differentiationG1/S-specific cyclin-D1Homo sapiens (human)
positive regulation of cyclin-dependent protein serine/threonine kinase activityG1/S-specific cyclin-D1Homo sapiens (human)
cell divisionG1/S-specific cyclin-D1Homo sapiens (human)
mammary gland alveolus developmentG1/S-specific cyclin-D1Homo sapiens (human)
response to UV-AG1/S-specific cyclin-D1Homo sapiens (human)
liver regenerationG1/S-specific cyclin-D1Homo sapiens (human)
positive regulation of G1/S transition of mitotic cell cycleG1/S-specific cyclin-D1Homo sapiens (human)
regulation of cyclin-dependent protein serine/threonine kinase activityG1/S-specific cyclin-D1Homo sapiens (human)
protein phosphorylationG1/S-specific cyclin-E1Homo sapiens (human)
G1/S transition of mitotic cell cycleG1/S-specific cyclin-E1Homo sapiens (human)
negative regulation of transcription by RNA polymerase IIG1/S-specific cyclin-E1Homo sapiens (human)
telomere maintenanceG1/S-specific cyclin-E1Homo sapiens (human)
DNA replication initiationG1/S-specific cyclin-E1Homo sapiens (human)
homologous chromosome pairing at meiosisG1/S-specific cyclin-E1Homo sapiens (human)
Wnt signaling pathwayG1/S-specific cyclin-E1Homo sapiens (human)
regulation of protein localizationG1/S-specific cyclin-E1Homo sapiens (human)
cell divisionG1/S-specific cyclin-E1Homo sapiens (human)
positive regulation of mesenchymal stem cell proliferationG1/S-specific cyclin-E1Homo sapiens (human)
regulation of cyclin-dependent protein serine/threonine kinase activityG1/S-specific cyclin-E1Homo sapiens (human)
positive regulation of G1/S transition of mitotic cell cycleG1/S-specific cyclin-E1Homo sapiens (human)
G1/S transition of mitotic cell cycleCyclin-dependent kinase 2Homo sapiens (human)
G2/M transition of mitotic cell cycleCyclin-dependent kinase 2Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICyclin-dependent kinase 2Homo sapiens (human)
DNA replicationCyclin-dependent kinase 2Homo sapiens (human)
DNA repairCyclin-dependent kinase 2Homo sapiens (human)
chromatin remodelingCyclin-dependent kinase 2Homo sapiens (human)
DNA-templated transcriptionCyclin-dependent kinase 2Homo sapiens (human)
protein phosphorylationCyclin-dependent kinase 2Homo sapiens (human)
potassium ion transportCyclin-dependent kinase 2Homo sapiens (human)
centriole replicationCyclin-dependent kinase 2Homo sapiens (human)
Ras protein signal transductionCyclin-dependent kinase 2Homo sapiens (human)
regulation of mitotic cell cycleCyclin-dependent kinase 2Homo sapiens (human)
positive regulation of cell population proliferationCyclin-dependent kinase 2Homo sapiens (human)
peptidyl-serine phosphorylationCyclin-dependent kinase 2Homo sapiens (human)
positive regulation of heterochromatin formationCyclin-dependent kinase 2Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCyclin-dependent kinase 2Homo sapiens (human)
positive regulation of DNA-templated DNA replication initiationCyclin-dependent kinase 2Homo sapiens (human)
telomere maintenance in response to DNA damageCyclin-dependent kinase 2Homo sapiens (human)
post-translational protein modificationCyclin-dependent kinase 2Homo sapiens (human)
positive regulation of DNA replicationCyclin-dependent kinase 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionCyclin-dependent kinase 2Homo sapiens (human)
centrosome duplicationCyclin-dependent kinase 2Homo sapiens (human)
cell divisionCyclin-dependent kinase 2Homo sapiens (human)
meiotic cell cycleCyclin-dependent kinase 2Homo sapiens (human)
cellular response to nitric oxideCyclin-dependent kinase 2Homo sapiens (human)
cellular senescenceCyclin-dependent kinase 2Homo sapiens (human)
regulation of anaphase-promoting complex-dependent catabolic processCyclin-dependent kinase 2Homo sapiens (human)
regulation of G2/M transition of mitotic cell cycleCyclin-dependent kinase 2Homo sapiens (human)
signal transductionCyclin-dependent kinase 2Homo sapiens (human)
regulation of gene expressionCyclin-dependent kinase 2Homo sapiens (human)
response to organic substanceCyclin-dependent kinase 2Homo sapiens (human)
DNA repairCyclin-dependent kinase 7Homo sapiens (human)
transcription by RNA polymerase IICyclin-dependent kinase 7Homo sapiens (human)
transcription initiation at RNA polymerase II promoterCyclin-dependent kinase 7Homo sapiens (human)
snRNA transcription by RNA polymerase IICyclin-dependent kinase 7Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICyclin-dependent kinase 7Homo sapiens (human)
protein stabilizationCyclin-dependent kinase 7Homo sapiens (human)
cell divisionCyclin-dependent kinase 7Homo sapiens (human)
regulation of cell cycleCyclin-dependent kinase 7Homo sapiens (human)
regulation of G1/S transition of mitotic cell cycleCyclin-dependent kinase 7Homo sapiens (human)
protein phosphorylationCyclin-dependent kinase 7Homo sapiens (human)
regulation of mitotic cell cycleCyclin-dependent kinase 9Homo sapiens (human)
protein phosphorylationCyclin-dependent kinase 9Homo sapiens (human)
DNA repairCyclin-dependent kinase 9Homo sapiens (human)
regulation of DNA repairCyclin-dependent kinase 9Homo sapiens (human)
transcription by RNA polymerase IICyclin-dependent kinase 9Homo sapiens (human)
transcription initiation at RNA polymerase II promoterCyclin-dependent kinase 9Homo sapiens (human)
transcription elongation by RNA polymerase IICyclin-dependent kinase 9Homo sapiens (human)
cell population proliferationCyclin-dependent kinase 9Homo sapiens (human)
replication fork processingCyclin-dependent kinase 9Homo sapiens (human)
regulation of mRNA 3'-end processingCyclin-dependent kinase 9Homo sapiens (human)
positive regulation of transcription elongation by RNA polymerase IICyclin-dependent kinase 9Homo sapiens (human)
positive regulation by host of viral transcriptionCyclin-dependent kinase 9Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICyclin-dependent kinase 9Homo sapiens (human)
regulation of muscle cell differentiationCyclin-dependent kinase 9Homo sapiens (human)
nucleus localizationCyclin-dependent kinase 9Homo sapiens (human)
regulation of cell cycleCyclin-dependent kinase 9Homo sapiens (human)
cellular response to cytokine stimulusCyclin-dependent kinase 9Homo sapiens (human)
negative regulation of protein localization to chromatinCyclin-dependent kinase 9Homo sapiens (human)
positive regulation of protein localization to chromatinCyclin-dependent kinase 9Homo sapiens (human)
transcription elongation-coupled chromatin remodelingCyclin-dependent kinase 9Homo sapiens (human)
protein phosphorylationCyclin-dependent kinase 9Homo sapiens (human)
regulation of transcription by RNA polymerase IICyclin-HHomo sapiens (human)
transcription initiation at RNA polymerase II promoterCyclin-HHomo sapiens (human)
protein stabilizationCyclin-HHomo sapiens (human)
regulation of G1/S transition of mitotic cell cycleCyclin-HHomo sapiens (human)
regulation of cyclin-dependent protein serine/threonine kinase activityCyclin-HHomo sapiens (human)
male meiosis ICyclin-A1Homo sapiens (human)
spermatogenesisCyclin-A1Homo sapiens (human)
cell divisionCyclin-A1Homo sapiens (human)
regulation of cyclin-dependent protein serine/threonine kinase activityCyclin-A1Homo sapiens (human)
mitotic cell cycle phase transitionCyclin-A1Homo sapiens (human)
cell divisionG2/mitotic-specific cyclin-B3Homo sapiens (human)
meiotic cell cycleG2/mitotic-specific cyclin-B3Homo sapiens (human)
regulation of cyclin-dependent protein serine/threonine kinase activityG2/mitotic-specific cyclin-B3Homo sapiens (human)
mitotic cell cycle phase transitionG2/mitotic-specific cyclin-B3Homo sapiens (human)
translationRibosomal protein S6 kinase beta-2Homo sapiens (human)
signal transductionRibosomal protein S6 kinase beta-2Homo sapiens (human)
TOR signalingRibosomal protein S6 kinase beta-2Homo sapiens (human)
positive regulation of translational initiationRibosomal protein S6 kinase beta-2Homo sapiens (human)
negative regulation of insulin receptor signaling pathwayRibosomal protein S6 kinase beta-2Homo sapiens (human)
peptidyl-serine phosphorylationRibosomal protein S6 kinase beta-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (43)

Processvia Protein(s)Taxonomy
transcription cis-regulatory region bindingCyclin-T1Homo sapiens (human)
DNA bindingCyclin-T1Homo sapiens (human)
chromatin bindingCyclin-T1Homo sapiens (human)
protein bindingCyclin-T1Homo sapiens (human)
protein kinase bindingCyclin-T1Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase activator activityCyclin-T1Homo sapiens (human)
RNA polymerase bindingCyclin-T1Homo sapiens (human)
7SK snRNA bindingCyclin-T1Homo sapiens (human)
DNA-binding transcription factor bindingCyclin-T1Homo sapiens (human)
molecular condensate scaffold activityCyclin-T1Homo sapiens (human)
protein bindingG2/mitotic-specific cyclin-B2Homo sapiens (human)
cadherin bindingG2/mitotic-specific cyclin-B2Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase regulator activityG2/mitotic-specific cyclin-B2Homo sapiens (human)
protein bindingG1/S-specific cyclin-E2Homo sapiens (human)
protein kinase bindingG1/S-specific cyclin-E2Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase regulator activityG1/S-specific cyclin-E2Homo sapiens (human)
virus receptor activityCyclin-dependent kinase 1Homo sapiens (human)
chromatin bindingCyclin-dependent kinase 1Homo sapiens (human)
protein kinase activityCyclin-dependent kinase 1Homo sapiens (human)
protein serine/threonine kinase activityCyclin-dependent kinase 1Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase activityCyclin-dependent kinase 1Homo sapiens (human)
protein bindingCyclin-dependent kinase 1Homo sapiens (human)
ATP bindingCyclin-dependent kinase 1Homo sapiens (human)
RNA polymerase II CTD heptapeptide repeat kinase activityCyclin-dependent kinase 1Homo sapiens (human)
kinase activityCyclin-dependent kinase 1Homo sapiens (human)
cyclin bindingCyclin-dependent kinase 1Homo sapiens (human)
Hsp70 protein bindingCyclin-dependent kinase 1Homo sapiens (human)
histone kinase activityCyclin-dependent kinase 1Homo sapiens (human)
cyclin-dependent protein kinase activityCyclin-dependent kinase 1Homo sapiens (human)
protein serine kinase activityCyclin-dependent kinase 1Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase activityCyclin-dependent kinase 4Homo sapiens (human)
protein bindingCyclin-dependent kinase 4Homo sapiens (human)
ATP bindingCyclin-dependent kinase 4Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase regulator activityCyclin-dependent kinase 4Homo sapiens (human)
cyclin bindingCyclin-dependent kinase 4Homo sapiens (human)
protein serine kinase activityCyclin-dependent kinase 4Homo sapiens (human)
patched bindingG2/mitotic-specific cyclin-B1Homo sapiens (human)
protein bindingG2/mitotic-specific cyclin-B1Homo sapiens (human)
protein kinase bindingG2/mitotic-specific cyclin-B1Homo sapiens (human)
ubiquitin-like protein ligase bindingG2/mitotic-specific cyclin-B1Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase activator activityG2/mitotic-specific cyclin-B1Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase regulator activityG2/mitotic-specific cyclin-B1Homo sapiens (human)
protein bindingCyclin-A2Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase regulator activityCyclin-A2Homo sapiens (human)
protein kinase bindingCyclin-A2Homo sapiens (human)
protein domain specific bindingCyclin-A2Homo sapiens (human)
protein kinase activityRibosomal protein S6 kinase beta-1Homo sapiens (human)
protein serine/threonine kinase activityRibosomal protein S6 kinase beta-1Homo sapiens (human)
ribosomal protein S6 kinase activityRibosomal protein S6 kinase beta-1Homo sapiens (human)
protein serine/threonine/tyrosine kinase activityRibosomal protein S6 kinase beta-1Homo sapiens (human)
protein bindingRibosomal protein S6 kinase beta-1Homo sapiens (human)
ATP bindingRibosomal protein S6 kinase beta-1Homo sapiens (human)
PDZ domain bindingRibosomal protein S6 kinase beta-1Homo sapiens (human)
peptide bindingRibosomal protein S6 kinase beta-1Homo sapiens (human)
identical protein bindingRibosomal protein S6 kinase beta-1Homo sapiens (human)
protein phosphatase 2A bindingRibosomal protein S6 kinase beta-1Homo sapiens (human)
protein serine kinase activityRibosomal protein S6 kinase beta-1Homo sapiens (human)
transcription corepressor activityG1/S-specific cyclin-D1Homo sapiens (human)
protein kinase activityG1/S-specific cyclin-D1Homo sapiens (human)
protein bindingG1/S-specific cyclin-D1Homo sapiens (human)
enzyme bindingG1/S-specific cyclin-D1Homo sapiens (human)
protein kinase bindingG1/S-specific cyclin-D1Homo sapiens (human)
histone deacetylase bindingG1/S-specific cyclin-D1Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase activator activityG1/S-specific cyclin-D1Homo sapiens (human)
proline-rich region bindingG1/S-specific cyclin-D1Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase regulator activityG1/S-specific cyclin-D1Homo sapiens (human)
protein bindingG1/S-specific cyclin-E1Homo sapiens (human)
kinase activityG1/S-specific cyclin-E1Homo sapiens (human)
protein kinase bindingG1/S-specific cyclin-E1Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase regulator activityG1/S-specific cyclin-E1Homo sapiens (human)
histone kinase activityCyclin-dependent kinase 2Homo sapiens (human)
magnesium ion bindingCyclin-dependent kinase 2Homo sapiens (human)
protein serine/threonine kinase activityCyclin-dependent kinase 2Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase activityCyclin-dependent kinase 2Homo sapiens (human)
protein bindingCyclin-dependent kinase 2Homo sapiens (human)
ATP bindingCyclin-dependent kinase 2Homo sapiens (human)
protein domain specific bindingCyclin-dependent kinase 2Homo sapiens (human)
cyclin bindingCyclin-dependent kinase 2Homo sapiens (human)
cyclin-dependent protein kinase activityCyclin-dependent kinase 2Homo sapiens (human)
protein serine kinase activityCyclin-dependent kinase 2Homo sapiens (human)
protein kinase activityCyclin-dependent kinase 7Homo sapiens (human)
protein serine/threonine kinase activityCyclin-dependent kinase 7Homo sapiens (human)
protein bindingCyclin-dependent kinase 7Homo sapiens (human)
ATP bindingCyclin-dependent kinase 7Homo sapiens (human)
ATP-dependent activity, acting on DNACyclin-dependent kinase 7Homo sapiens (human)
RNA polymerase II CTD heptapeptide repeat kinase activityCyclin-dependent kinase 7Homo sapiens (human)
protein serine kinase activityCyclin-dependent kinase 7Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase activityCyclin-dependent kinase 7Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCyclin-dependent kinase 9Homo sapiens (human)
transcription coactivator bindingCyclin-dependent kinase 9Homo sapiens (human)
DNA bindingCyclin-dependent kinase 9Homo sapiens (human)
chromatin bindingCyclin-dependent kinase 9Homo sapiens (human)
transcription elongation factor activityCyclin-dependent kinase 9Homo sapiens (human)
protein kinase activityCyclin-dependent kinase 9Homo sapiens (human)
protein serine/threonine kinase activityCyclin-dependent kinase 9Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase activityCyclin-dependent kinase 9Homo sapiens (human)
protein bindingCyclin-dependent kinase 9Homo sapiens (human)
ATP bindingCyclin-dependent kinase 9Homo sapiens (human)
RNA polymerase II CTD heptapeptide repeat kinase activityCyclin-dependent kinase 9Homo sapiens (human)
kinase activityCyclin-dependent kinase 9Homo sapiens (human)
protein kinase bindingCyclin-dependent kinase 9Homo sapiens (human)
7SK snRNA bindingCyclin-dependent kinase 9Homo sapiens (human)
protein serine kinase activityCyclin-dependent kinase 9Homo sapiens (human)
RNA polymerase II general transcription initiation factor activityCyclin-HHomo sapiens (human)
protein bindingCyclin-HHomo sapiens (human)
cyclin-dependent protein serine/threonine kinase regulator activityCyclin-HHomo sapiens (human)
protein bindingCyclin-A1Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase regulator activityCyclin-A1Homo sapiens (human)
protein bindingG2/mitotic-specific cyclin-B3Homo sapiens (human)
cyclin-dependent protein serine/threonine kinase regulator activityG2/mitotic-specific cyclin-B3Homo sapiens (human)
protein kinase activityRibosomal protein S6 kinase beta-2Homo sapiens (human)
protein serine/threonine kinase activityRibosomal protein S6 kinase beta-2Homo sapiens (human)
ribosomal protein S6 kinase activityRibosomal protein S6 kinase beta-2Homo sapiens (human)
ATP bindingRibosomal protein S6 kinase beta-2Homo sapiens (human)
peptide bindingRibosomal protein S6 kinase beta-2Homo sapiens (human)
protein serine kinase activityRibosomal protein S6 kinase beta-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (62)

Processvia Protein(s)Taxonomy
nucleolusCyclin-T1Homo sapiens (human)
nucleusCyclin-T1Homo sapiens (human)
nucleusCyclin-T1Homo sapiens (human)
nucleoplasmCyclin-T1Homo sapiens (human)
cytosolCyclin-T1Homo sapiens (human)
cyclin/CDK positive transcription elongation factor complexCyclin-T1Homo sapiens (human)
P-TEFb complexCyclin-T1Homo sapiens (human)
centrosomeG2/mitotic-specific cyclin-B2Homo sapiens (human)
cytosolG2/mitotic-specific cyclin-B2Homo sapiens (human)
microtubule cytoskeletonG2/mitotic-specific cyclin-B2Homo sapiens (human)
membraneG2/mitotic-specific cyclin-B2Homo sapiens (human)
centrosomeG2/mitotic-specific cyclin-B2Homo sapiens (human)
cytoplasmG2/mitotic-specific cyclin-B2Homo sapiens (human)
cyclin-dependent protein kinase holoenzyme complexG2/mitotic-specific cyclin-B2Homo sapiens (human)
nucleusG2/mitotic-specific cyclin-B2Homo sapiens (human)
nucleoplasmG1/S-specific cyclin-E2Homo sapiens (human)
cytosolG1/S-specific cyclin-E2Homo sapiens (human)
cyclin E2-CDK2 complexG1/S-specific cyclin-E2Homo sapiens (human)
nucleusG1/S-specific cyclin-E2Homo sapiens (human)
cytoplasmG1/S-specific cyclin-E2Homo sapiens (human)
centrosomeG1/S-specific cyclin-E2Homo sapiens (human)
cyclin E1-CDK2 complexG1/S-specific cyclin-E2Homo sapiens (human)
mitochondrial matrixCyclin-dependent kinase 1Homo sapiens (human)
chromosome, telomeric regionCyclin-dependent kinase 1Homo sapiens (human)
nucleusCyclin-dependent kinase 1Homo sapiens (human)
nucleoplasmCyclin-dependent kinase 1Homo sapiens (human)
mitochondrionCyclin-dependent kinase 1Homo sapiens (human)
endoplasmic reticulum membraneCyclin-dependent kinase 1Homo sapiens (human)
centrosomeCyclin-dependent kinase 1Homo sapiens (human)
cytosolCyclin-dependent kinase 1Homo sapiens (human)
spindle microtubuleCyclin-dependent kinase 1Homo sapiens (human)
membraneCyclin-dependent kinase 1Homo sapiens (human)
midbodyCyclin-dependent kinase 1Homo sapiens (human)
extracellular exosomeCyclin-dependent kinase 1Homo sapiens (human)
mitotic spindleCyclin-dependent kinase 1Homo sapiens (human)
cyclin A1-CDK1 complexCyclin-dependent kinase 1Homo sapiens (human)
cyclin A2-CDK1 complexCyclin-dependent kinase 1Homo sapiens (human)
cyclin B1-CDK1 complexCyclin-dependent kinase 1Homo sapiens (human)
cyclin-dependent protein kinase holoenzyme complexCyclin-dependent kinase 1Homo sapiens (human)
cytoplasmCyclin-dependent kinase 1Homo sapiens (human)
nucleusCyclin-dependent kinase 1Homo sapiens (human)
nucleusCyclin-dependent kinase 4Homo sapiens (human)
nucleoplasmCyclin-dependent kinase 4Homo sapiens (human)
nucleolusCyclin-dependent kinase 4Homo sapiens (human)
cytosolCyclin-dependent kinase 4Homo sapiens (human)
bicellular tight junctionCyclin-dependent kinase 4Homo sapiens (human)
nuclear membraneCyclin-dependent kinase 4Homo sapiens (human)
cyclin D1-CDK4 complexCyclin-dependent kinase 4Homo sapiens (human)
cyclin D2-CDK4 complexCyclin-dependent kinase 4Homo sapiens (human)
cyclin D3-CDK4 complexCyclin-dependent kinase 4Homo sapiens (human)
cyclin-dependent protein kinase holoenzyme complexCyclin-dependent kinase 4Homo sapiens (human)
chromatinCyclin-dependent kinase 4Homo sapiens (human)
transcription regulator complexCyclin-dependent kinase 4Homo sapiens (human)
nucleusCyclin-dependent kinase 4Homo sapiens (human)
cytoplasmCyclin-dependent kinase 4Homo sapiens (human)
mitochondrial matrixG2/mitotic-specific cyclin-B1Homo sapiens (human)
spindle poleG2/mitotic-specific cyclin-B1Homo sapiens (human)
nucleusG2/mitotic-specific cyclin-B1Homo sapiens (human)
nucleoplasmG2/mitotic-specific cyclin-B1Homo sapiens (human)
cytoplasmG2/mitotic-specific cyclin-B1Homo sapiens (human)
centrosomeG2/mitotic-specific cyclin-B1Homo sapiens (human)
cytosolG2/mitotic-specific cyclin-B1Homo sapiens (human)
membraneG2/mitotic-specific cyclin-B1Homo sapiens (human)
cyclin B1-CDK1 complexG2/mitotic-specific cyclin-B1Homo sapiens (human)
outer kinetochoreG2/mitotic-specific cyclin-B1Homo sapiens (human)
cytoplasmG2/mitotic-specific cyclin-B1Homo sapiens (human)
nucleusG2/mitotic-specific cyclin-B1Homo sapiens (human)
centrosomeG2/mitotic-specific cyclin-B1Homo sapiens (human)
female pronucleusCyclin-A2Homo sapiens (human)
male pronucleusCyclin-A2Homo sapiens (human)
nucleusCyclin-A2Homo sapiens (human)
nucleoplasmCyclin-A2Homo sapiens (human)
cytoplasmCyclin-A2Homo sapiens (human)
cytosolCyclin-A2Homo sapiens (human)
cyclin A2-CDK1 complexCyclin-A2Homo sapiens (human)
cyclin A2-CDK2 complexCyclin-A2Homo sapiens (human)
cyclin-dependent protein kinase holoenzyme complexCyclin-A2Homo sapiens (human)
nucleusCyclin-A2Homo sapiens (human)
centrosomeCyclin-A2Homo sapiens (human)
cytoplasmCyclin-A2Homo sapiens (human)
nucleoplasmRibosomal protein S6 kinase beta-1Homo sapiens (human)
mitochondrionRibosomal protein S6 kinase beta-1Homo sapiens (human)
mitochondrial outer membraneRibosomal protein S6 kinase beta-1Homo sapiens (human)
cytosolRibosomal protein S6 kinase beta-1Homo sapiens (human)
cell surfaceRibosomal protein S6 kinase beta-1Homo sapiens (human)
neuron projectionRibosomal protein S6 kinase beta-1Homo sapiens (human)
perinuclear region of cytoplasmRibosomal protein S6 kinase beta-1Homo sapiens (human)
postsynapseRibosomal protein S6 kinase beta-1Homo sapiens (human)
glutamatergic synapseRibosomal protein S6 kinase beta-1Homo sapiens (human)
nucleoplasmRibosomal protein S6 kinase beta-1Homo sapiens (human)
cytoplasmRibosomal protein S6 kinase beta-1Homo sapiens (human)
nucleusG1/S-specific cyclin-D1Homo sapiens (human)
nucleoplasmG1/S-specific cyclin-D1Homo sapiens (human)
cytosolG1/S-specific cyclin-D1Homo sapiens (human)
bicellular tight junctionG1/S-specific cyclin-D1Homo sapiens (human)
nuclear membraneG1/S-specific cyclin-D1Homo sapiens (human)
cyclin D1-CDK4 complexG1/S-specific cyclin-D1Homo sapiens (human)
cyclin D1-CDK6 complexG1/S-specific cyclin-D1Homo sapiens (human)
cyclin-dependent protein kinase holoenzyme complexG1/S-specific cyclin-D1Homo sapiens (human)
transcription repressor complexG1/S-specific cyclin-D1Homo sapiens (human)
centrosomeG1/S-specific cyclin-D1Homo sapiens (human)
cytoplasmG1/S-specific cyclin-D1Homo sapiens (human)
nucleusG1/S-specific cyclin-D1Homo sapiens (human)
nucleusG1/S-specific cyclin-E1Homo sapiens (human)
nucleoplasmG1/S-specific cyclin-E1Homo sapiens (human)
cytosolG1/S-specific cyclin-E1Homo sapiens (human)
cyclin E1-CDK2 complexG1/S-specific cyclin-E1Homo sapiens (human)
centrosomeG1/S-specific cyclin-E1Homo sapiens (human)
nucleusG1/S-specific cyclin-E1Homo sapiens (human)
cytoplasmG1/S-specific cyclin-E1Homo sapiens (human)
chromosome, telomeric regionCyclin-dependent kinase 2Homo sapiens (human)
condensed chromosomeCyclin-dependent kinase 2Homo sapiens (human)
X chromosomeCyclin-dependent kinase 2Homo sapiens (human)
Y chromosomeCyclin-dependent kinase 2Homo sapiens (human)
male germ cell nucleusCyclin-dependent kinase 2Homo sapiens (human)
nucleusCyclin-dependent kinase 2Homo sapiens (human)
nuclear envelopeCyclin-dependent kinase 2Homo sapiens (human)
nucleoplasmCyclin-dependent kinase 2Homo sapiens (human)
cytoplasmCyclin-dependent kinase 2Homo sapiens (human)
endosomeCyclin-dependent kinase 2Homo sapiens (human)
centrosomeCyclin-dependent kinase 2Homo sapiens (human)
cytosolCyclin-dependent kinase 2Homo sapiens (human)
Cajal bodyCyclin-dependent kinase 2Homo sapiens (human)
cyclin A1-CDK2 complexCyclin-dependent kinase 2Homo sapiens (human)
cyclin A2-CDK2 complexCyclin-dependent kinase 2Homo sapiens (human)
cyclin E1-CDK2 complexCyclin-dependent kinase 2Homo sapiens (human)
cyclin E2-CDK2 complexCyclin-dependent kinase 2Homo sapiens (human)
cyclin-dependent protein kinase holoenzyme complexCyclin-dependent kinase 2Homo sapiens (human)
transcription regulator complexCyclin-dependent kinase 2Homo sapiens (human)
cytoplasmCyclin-dependent kinase 2Homo sapiens (human)
nucleusCyclin-dependent kinase 2Homo sapiens (human)
cyclin-dependent protein kinase holoenzyme complexCyclin-dependent kinase 7Homo sapiens (human)
fibrillar centerCyclin-dependent kinase 7Homo sapiens (human)
male germ cell nucleusCyclin-dependent kinase 7Homo sapiens (human)
nucleusCyclin-dependent kinase 7Homo sapiens (human)
nucleoplasmCyclin-dependent kinase 7Homo sapiens (human)
cytosolCyclin-dependent kinase 7Homo sapiens (human)
plasma membraneCyclin-dependent kinase 7Homo sapiens (human)
perinuclear region of cytoplasmCyclin-dependent kinase 7Homo sapiens (human)
transcription factor TFIIH core complexCyclin-dependent kinase 7Homo sapiens (human)
transcription factor TFIIH holo complexCyclin-dependent kinase 7Homo sapiens (human)
CAK-ERCC2 complexCyclin-dependent kinase 7Homo sapiens (human)
transcription factor TFIIK complexCyclin-dependent kinase 7Homo sapiens (human)
cytoplasmCyclin-dependent kinase 7Homo sapiens (human)
nucleusCyclin-dependent kinase 7Homo sapiens (human)
nucleusCyclin-dependent kinase 9Homo sapiens (human)
nucleusCyclin-dependent kinase 9Homo sapiens (human)
nucleoplasmCyclin-dependent kinase 9Homo sapiens (human)
cyclin/CDK positive transcription elongation factor complexCyclin-dependent kinase 9Homo sapiens (human)
membraneCyclin-dependent kinase 9Homo sapiens (human)
PML bodyCyclin-dependent kinase 9Homo sapiens (human)
cytoplasmic ribonucleoprotein granuleCyclin-dependent kinase 9Homo sapiens (human)
transcription elongation factor complexCyclin-dependent kinase 9Homo sapiens (human)
P-TEFb complexCyclin-dependent kinase 9Homo sapiens (human)
cyclin-dependent protein kinase holoenzyme complexCyclin-HHomo sapiens (human)
nucleoplasmCyclin-HHomo sapiens (human)
transcription factor TFIIH core complexCyclin-HHomo sapiens (human)
transcription factor TFIIH holo complexCyclin-HHomo sapiens (human)
CAK-ERCC2 complexCyclin-HHomo sapiens (human)
transcription factor TFIIK complexCyclin-HHomo sapiens (human)
nucleusCyclin-HHomo sapiens (human)
nucleoplasmCyclin-A1Homo sapiens (human)
cytosolCyclin-A1Homo sapiens (human)
microtubule cytoskeletonCyclin-A1Homo sapiens (human)
cyclin A1-CDK1 complexCyclin-A1Homo sapiens (human)
cyclin A1-CDK2 complexCyclin-A1Homo sapiens (human)
centrosomeCyclin-A1Homo sapiens (human)
cyclin A2-CDK2 complexCyclin-A1Homo sapiens (human)
cytoplasmCyclin-A1Homo sapiens (human)
nucleusCyclin-A1Homo sapiens (human)
nuclear speckG2/mitotic-specific cyclin-B3Homo sapiens (human)
cyclin-dependent protein kinase holoenzyme complexG2/mitotic-specific cyclin-B3Homo sapiens (human)
cytoplasmG2/mitotic-specific cyclin-B3Homo sapiens (human)
nucleusG2/mitotic-specific cyclin-B3Homo sapiens (human)
centrosomeG2/mitotic-specific cyclin-B3Homo sapiens (human)
nucleoplasmRibosomal protein S6 kinase beta-2Homo sapiens (human)
nucleoplasmRibosomal protein S6 kinase beta-2Homo sapiens (human)
cytoplasmRibosomal protein S6 kinase beta-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (258)

Assay IDTitleYearJournalArticle
AID617779Inhibition of PAK2 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617415Cytotoxicity against human SKOV3 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID1375009Inhibition of recombinant human CDK9/cyclin T1 using Ulight-CFFKNIVTPRTPPPSQGK-amide as substrate after 90 mins by fluorescence assay relative to control2018Bioorganic & medicinal chemistry letters, 05-01, Volume: 28, Issue:8
Discovery of novel CDK inhibitors via scaffold hopping from CAN508.
AID272433Activity of PKBalpha at 10 uM2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID272418Inhibition of CDK2/Cyclin E in presence of 100 uM ATP2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID617724Inhibition of MLK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617627Inhibition of HIPK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617390Cytotoxicity against human NCI-H23 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617295Cytotoxicity against human SF295 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617626Inhibition of HER4 assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617704Inhibition of IKK-epsilon assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617618Inhibition of EPH-B3 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID616322Antiangiogenic activity against HUVEC cells assessed as inhibition of VEGF-induced cell migration-associated wound closure at >10 uM after 16 hrs by microscopic analysis2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID272441Cell cycle arrest in HT29 cells by accumulation at G0/G1 phase at 50 uM after 12 hrs2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID1194736Cytotoxicity against human K562 cells after 72 hrs by calcein AM staining-based fluorescence assay2015Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
Novel arylazopyrazole inhibitors of cyclin-dependent kinases.
AID617776Inhibition of p38beta MAPK assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617398Cytotoxicity against human RPMI8226 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617705Inhibition of IR assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617777Inhibition of p38delta MAPK assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID1194738Cytotoxicity against human RPMI8226 cells after 72 hrs by calcein AM staining-based fluorescence assay2015Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
Novel arylazopyrazole inhibitors of cyclin-dependent kinases.
AID616301Inhibition of PKCzeta assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID616303Inhibition of PLK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617611Inhibition of CDK9/cyclin T assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID272417Inhibition of CDK2/Cyclin E2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID272443Cell cycle arrest in HT29 cells by accumulation at G2/M phase at 50 uM after 12 hrs2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID617785Inhibition of PIM1 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID272467Inhibition of EpCAM mRNA synthesis in HT29 cells measured as number of copies per 10^6 cells by RT PCR at 50 uM after 3 hrs2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID617773Inhibition of NEK6 assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617400Cytotoxicity against human LOXIMVI cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617707Inhibition of IRR assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617782Inhibition of PAK6 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617725Inhibition of MLK3 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617516Inhibition of CDK9-catalyzed RNA polymerase 2 phosphorylation at Ser2 in human HMEC1 cells after 2 hrs by immunoblotting2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617714Inhibition of MAPKAP-K2 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617720Inhibition of MEKK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID272423Inhibition of CDK9/Cyclin T1 in presence of 100 uM ATP2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID616302Inhibition of PKD1 assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617519Inhibition of CDK9 by [33P]gamma-ATP incorporation assay2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617391Cytotoxicity against human NCI-H322M cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID272422Inhibition of CDK7/Cyclin H in presence of 100 uM ATP2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID272434Activity of SAPK2-alpha at 10 uM2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID272416Viability of K562 cells at 100 uM2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID617771Inhibition of MST4 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID616311Inhibition of SGK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID272419Inhibition of CDK1/Cyclin B in presence of 100 uM ATP2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID617790Inhibition of PKBbeta assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID723732Stabilization of CDK2/Cyclin A (174 to 432 amino acid residues) (unknown origin) assessed as change in melting temperature at 20 uM by differential scanning fluorimetry assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Comparative structural and functional studies of 4-(thiazol-5-yl)-2-(phenylamino)pyrimidine-5-carbonitrile CDK9 inhibitors suggest the basis for isotype selectivity.
AID723735Inhibition of CDK9/Cyclin T (1 to 330 amino acid residues) (unknown origin) by differential scanning fluorimetry assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Comparative structural and functional studies of 4-(thiazol-5-yl)-2-(phenylamino)pyrimidine-5-carbonitrile CDK9 inhibitors suggest the basis for isotype selectivity.
AID617423Cytotoxicity against human SN12C cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID272410Antiproliferative activity against HOS cell line2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID617394Cytotoxicity against human CCRF-CEM cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID272424Activity of CDK9/Cyclin T1 at 10 uM2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID1689408Inhibition of human full-length N-terminal GST/His6-tagged CDK9 (1 to 372 residues)/His6-tagged Cyclin-T1 (1 to 726 residues) expressed in sf9 cells using (YSPTSPS)2KK peptide as substrate in presence of [gamma33P]ATP2020European journal of medicinal chemistry, Mar-01, Volume: 189Sulfonamide-based ring-fused analogues for CAN508 as novel carbonic anhydrase inhibitors endowed with antitumor activity: Design, synthesis, and in vitro biological evaluation.
AID617706Inhibition of IRAK4 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617769Inhibition of MSK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID272469Inhibition of EpCAM mRNA synthesis in HT29 cells measured as number of copies per 10^6 cells by RT PCR at 50 uM after 12 hrs2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID617422Cytotoxicity against human RXF393 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617620Inhibition of ERK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID616319Inhibition of TTK assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617612Inhibition of CK1delta assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617506Antiangiogenic activity in VEGF-stimulated HMEC1 assessed as reduction in median length of tube at 20 uM after 16 hrs by photographic analysis2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617719Inhibition of MARK4 assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID272466Inhibition of EpCAM mRNA synthesis in HT29 cells measured as number of copies per 10^6 cells by RT PCR at 50 uM2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID617723Inhibition of MKK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617625Inhibition of GSK3b assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617709Inhibition of JNK1A1 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617393Cytotoxicity against human NCI-H522 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617526Inhibition of CAMK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617503Antiangiogenic activity against HUVEC cells assessed as inhibition of VEGF-induced cell migration-associated wound closure after 16 hrs by microscopic analysis2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617502Antiproliferative activity against HMEC1 cells assessed as decrease in cell viability at >50 uM within 72 hrs by calcein AM staining-based fluorescence assay2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID616310Inhibition of S6K1 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617300Cytotoxicity against human COLO205 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617408Cytotoxicity against human UACC62 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617419Cytotoxicity against human A498 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617781Inhibition of PAK5 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID616321Inhibition of YES1 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617291Cytotoxicity against human MCF7 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617722Inhibition of MINK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID272454Decrease in pRb phosphorylation in MCF7 cells after 24 hrs at 50 uM2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID617716Inhibition of MARK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617768Inhibition of MNK2alpha assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617619Inhibition of EPH-B4 assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617298Cytotoxicity against human SNB75 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617616Inhibition of EPHA2 assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617524Inhibition of BRSK2 assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617518Inhibition of CDK7-catalyzed RNA polymerase 2 phosphorylation at Ser5 in human HMEC1 cells at 5 to 40 uM after 2 hrs by immunoblotting2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617416Cytotoxicity against human DU145 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617418Cytotoxicity against human 786-0 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID616315Inhibition of SYK assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID272482Increase in p53 expression level in MCF7 cells at 100 uM after 24 hrs2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID272421Inhibition of CDK4/Cyclin D1 in presence of 100 uM ATP2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID617629Inhibition of HIPK3 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617622Inhibition of ERK8 assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID272455Increase in p53 expression level in MCF7 cells at 50 uM after 24 hrs2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID616304Inhibition of PRAK assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617783Inhibition of PDK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617523Inhibition of BRSK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617420Cytotoxicity against human ACHN cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617302Cytotoxicity against human HCT116 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617407Cytotoxicity against human UACC257 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617304Cytotoxicity against human HT-29 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID272457Reduction of RNA polymerase 2 CTD phosphorylation in MCF7 cells after 24 hrs2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID617632Inhibition of IGF-1R assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617509Decrease in VEGF expression in human MCF7 cells at >10 uM after 24 hrs by sandwich ELISA2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617289Cytotoxicity against human BT549 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617402Cytotoxicity against human MALME-3M cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID272460Inhibition of GAPDH mRNA synthesis in HT29 cells measured as number of copies per 10^6 cells by RT PCR at 50 uM after 6 hrs2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID617787Inhibition of PIM3 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID272425Activity of CDK2/Cyclin E at 10 uM2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID617613Inhibition of CK2alpha assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID272432Activity of PKA at 10 uM2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID617521Inhibition of Aurora A assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617708Inhibition of JAK2 assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617789Inhibition of PKBalpha assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617305Cytotoxicity against human KM12 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID616307Inhibition of ROCK2 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617772Inhibition of NEK2a assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617296Cytotoxicity against human SF539 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID1194741Inhibition of CDK7/cyclin H (unknown origin) expressed in baculovirus infected Sf9 cells2015Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
Novel arylazopyrazole inhibitors of cyclin-dependent kinases.
AID617401Cytotoxicity against human M14 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617711Inhibition of JNK2alpha2 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617412Cytotoxicity against human OVCAR4 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617780Inhibition of PAK4 assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID272465Inhibition of CEA mRNA synthesis in HT29 cells measured as number of copies per 10^6 cells by RT PCR at 50 uM after 12 hrs2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID617778Inhibition of p38-gamma MAPK assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617395Cytotoxicity against human HL-60(TB) cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617299Cytotoxicity against human U251 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617309Cytotoxicity against human HOP62 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID272420Inhibition of CDK2/Cyclin A in presence of 100 uM ATP2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID616308Inhibition of RSK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617411Cytotoxicity against human OVCAR3 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617770Inhibition of MST2 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID723734Inhibition of CDK2/Cyclin A (174 to 432 amino acid residues) (unknown origin) by differential scanning fluorimetry assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Comparative structural and functional studies of 4-(thiazol-5-yl)-2-(phenylamino)pyrimidine-5-carbonitrile CDK9 inhibitors suggest the basis for isotype selectivity.
AID272431Activity of P70S6K at 10 uM2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID1194737Cytotoxicity against human MCF7 cells after 72 hrs by calcein AM staining-based fluorescence assay2015Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
Novel arylazopyrazole inhibitors of cyclin-dependent kinases.
AID617775Inhibition of p38alpha MAPK assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID272408Inhibition of CDK2/Cyclin E in presence of 15 uM ATP2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID617426Antiproliferative activity against HUVEC cells assessed as decrease in cell viability at >50 uM within 72 hrs by calcein AM staining-based fluorescence assay2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617712Inhibition of JNK3alpha1 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617425Cytotoxicity against human UO31 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617292Cytotoxicity against human MDA-MB-231 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617786Inhibition of PIM2 assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617520Inhibition of AMPK assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID272430Activity of MAPK1 at 10 uM2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID616410Antiproliferative activity against HUVEC cells assessed as decrease in cell viability at 10 to 40 uM within 72 hrs by calcein AM staining-based fluorescence assay2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID272412Antiproliferative activity against K562 cell line2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID617710Inhibition of Lck assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID272440Cell cycle arrest in HT29 cells by accumulation at G2/M phase at 50 uM after 6 hrs2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID1375008Inhibition of recombinant human CDK2/cyclin A using Ulight-CFFKNIVTPRTPPPSQGK-amide as substrate after 15 mins by fluorescence assay relative to control2018Bioorganic & medicinal chemistry letters, 05-01, Volume: 28, Issue:8
Discovery of novel CDK inhibitors via scaffold hopping from CAN508.
AID617294Cytotoxicity against human SF268 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617307Cytotoxicity against human A549 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID616312Inhibition of SmMLCK assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID272439Cell cycle arrest in HT29 cells by accumulation at S phase at 50 uM after 6 hrs2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID617389Cytotoxicity against human NCI-H226 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617788Inhibition of PKA assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID616306Inhibition of RIPK2 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID272461Inhibition of GAPDH mRNA synthesis in HT29 cells measured as number of copies per 10^6 cells by RT PCR at 50 uM after 12 hrs2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID617512Inhibition of TNF-alpha-induced Nuclear factor-kappa-B-mediated ICAM-1 expression in human HMEC1 cells after 24 hrs by FACS analysis2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617392Cytotoxicity against human NCI-H460 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617409Cytotoxicity against human IGROV1 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617414Cytotoxicity against human OVCAR8 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617623Inhibition of FGF-R1 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617522Inhibition of Aurora B assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617721Inhibition of MELK assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617791Inhibition of PKCalpha assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617507Antiangiogenic activity in VEGF-stimulated HMEC1 assessed as reduction in median length of tube at 40 uM after 16 hrs by photographic analysis2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617410Cytotoxicity against human NCI/ADR-RES cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID272483Inhibition of P70S6K2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID617397Cytotoxicity against human MOLT4 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617624Inhibition of GCK assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID272409Antiproliferative activity against MCF7 cell line2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID617306Cytotoxicity against human SW620 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID272438Cell cycle arrest in HT29 cells by accumulation at G0/G1 phase at 50 uM after 6 hrs2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID617784Inhibition of PHKG1 assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID616411Antiproliferative activity against HMEC1 cells assessed as decrease in cell viability at 10 to 40 uM within 72 hrs by calcein AM staining-based fluorescence assay2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID616313Inhibition of Src assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617774Inhibition of NUAK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617718Inhibition of MARK3 assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617767Inhibition of MNK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617405Cytotoxicity against human SK-MEL-28 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617628Inhibition of HIPK2 assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617717Inhibition of MARK2 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID272436Cell cycle arrest in HT29 cells by accumulation at S phase at 50 uM after 3 hrs2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID1689407Inhibition of CDK2/cyclin E (unknown origin) expressed in baculovirus infected Sf21 insect cells using histone H1 as substrate in presence of [gamma33P]ATP2020European journal of medicinal chemistry, Mar-01, Volume: 189Sulfonamide-based ring-fused analogues for CAN508 as novel carbonic anhydrase inhibitors endowed with antitumor activity: Design, synthesis, and in vitro biological evaluation.
AID616314Inhibition of SRPK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID616318Inhibition of TrkA assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617630Inhibition of CHK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617609Inhibition of CAMKKbeta assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617417Cytotoxicity against human PC3 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617310Cytotoxicity against human HOP92 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617293Cytotoxicity against human T47D cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID272468Inhibition of EpCAM mRNA synthesis in HT29 cells measured as number of copies per 10^6 cells by RT PCR at 50 uM after 6 hrs2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID272463Inhibition of CEA mRNA synthesis in HT29 cells measured as number of copies per 10^6 cells by RT PCR at 50 uM after 3 hrs2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID272411Antiproliferative activity against G361 cell line2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID617413Cytotoxicity against human OVCAR5 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617515Inhibition of CDK9-catalyzed RNA polymerase 2 phosphorylation at Ser2 in human MCF7 cells after 2 hrs by immunoblotting2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID272427Activity of CHK1 at 10 uM2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID272456Increase in p21 WAF1 expression level in MCF7 cells at 50 uM after 24 hrs2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID272453Decrease in pRb phosphorylation in MCF7 cells after 24 hrs at 25 uM2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID1194742Inhibition of CDK9/cyclin T1 (unknown origin) expressed in baculovirus infected Sf9 cells2015Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
Novel arylazopyrazole inhibitors of cyclin-dependent kinases.
AID272413Viability of MCF7 cells at 100 uM2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID617505Antiangiogenic activity in VEGF-stimulated HMEC1 assessed as reduction in total length of tube at 40 uM after 16 hrs by photographic analysis2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617631Inhibition of CHK2 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617610Inhibition of CDK2/cyclin A assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617396Cytotoxicity against human K562 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617514Inhibition of RNA synthesis in human HMEC1 cells assessed as decrease in [3H] Uridine incorporation after 2 hrs by scintillation counting2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617614Inhibition of CSK assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617715Inhibition of MAPKAP-K3 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID616320Inhibition of VEGFR assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID272459Inhibition of GAPDH mRNA synthesis in HT29 cells measured as number of copies per 10^6 cells by RT PCR at 50 uM after 3 hrs2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID617399Cytotoxicity against human SR cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617308Cytotoxicity against human EKVX cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617617Inhibition of EPHA4 assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617517Inhibition of CDK7-catalyzed RNA polymerase 2 phosphorylation at Ser5 in human MCF7 cells at 5 to 40 uM after 2 hrs by immunoblotting2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617421Cytotoxicity against human Caki1 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID272415Viability of G361 cells at 100 uM2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID617504Antiangiogenic activity in VEGF-stimulated HMEC1 assessed as reduction in total length of tube at 20 uM after 16 hrs by photographic analysis2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID616316Inhibition of TAK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617621Inhibition of ERK2 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID616309Inhibition of RSK2 assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617297Cytotoxicity against human SNB19 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617303Cytotoxicity against human HCT15 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617424Cytotoxicity against human TK10 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID1194739Inhibition of CDK1/cyclin B (unknown origin) expressed in baculovirus infected Sf9 cells2015Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
Novel arylazopyrazole inhibitors of cyclin-dependent kinases.
AID617703Inhibition of IKK-beta assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617301Cytotoxicity against human HCC2998 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID1194740Inhibition of CDK4/cyclin D1 (unknown origin) expressed in baculovirus infected Sf9 cells2015Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
Novel arylazopyrazole inhibitors of cyclin-dependent kinases.
AID617403Cytotoxicity against human MDA-MB-435 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID272428Activity of CK2 at 10 uM2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID617511Decrease in VEGF expression in human DU145 cells at >10 uM after 24 hrs by sandwich ELISA2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617404Cytotoxicity against human SK-MEL-2 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID616317Inhibition of TBK1 assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617525Inhibition of BTK assessed as residual activity at 10 uM by radioactivity assay in presence of 50 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617615Inhibition of EF2K assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID272464Inhibition of CEA mRNA synthesis in HT29 cells measured as number of copies per 10^6 cells by RT PCR at 50 uM after 6 hrs2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID617513Inhibition of RNA synthesis in human MCF7 cells assessed as decrease in [3H] Uridine incorporation after 2 hrs by scintillation counting2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID1194735Inhibition of CDK2/cyclin E (unknown origin) expressed in baculovirus infected Sf9 cells2015Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
Novel arylazopyrazole inhibitors of cyclin-dependent kinases.
AID617406Cytotoxicity against human SK-MEL-5 cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID617508Antiangiogenic activity in VEGF-stimulated HMEC1 assessed as reduction in tube nodes after 16 hrs by photographic analysis2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID272462Inhibition of CEA mRNA synthesis in HT29 cells measured as number of copies per 10^6 cells by RT PCR at 50 uM2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID617290Cytotoxicity against human Hs 578T cells2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID616305Inhibition of PRK2 assessed as residual activity at 10 uM by radioactivity assay in presence of 5 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID723733Stabilization of CDK9/Cyclin T (1 to 330 amino acid residues) (unknown origin) assessed as change in melting temperature at 20 uM by differential scanning fluorimetry assay2013Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
Comparative structural and functional studies of 4-(thiazol-5-yl)-2-(phenylamino)pyrimidine-5-carbonitrile CDK9 inhibitors suggest the basis for isotype selectivity.
AID617510Decrease in VEGF expression in human MDA-MB-231 cells at >10 uM after 24 hrs by sandwich ELISA2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID272458Inhibition of GAPDH mRNA synthesis in HT29 cells measured as number of copies per 10^6 cells by RT PCR at 50 uM2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID272426Activity of c-ABL at 10 uM2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID272414Viability of HOS cells at 100 uM2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID272442Cell cycle arrest in HT29 cells by accumulation at S phase at 50 uM after 12 hrs2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID617713Inhibition of LKB1 assessed as residual activity at 10 uM by radioactivity assay in presence of 20 uM ATP2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
AID272429Activity of GSK3-beta at 10 uM2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID272435Cell cycle arrest in HT29 cells by accumulation at G0/G1 phase at 50 uM after 3 hrs2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID272437Cell cycle arrest in HT29 cells by accumulation at G2/M phase at 50 uM after 3 hrs2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID1800495Kinase Selectivity from Article 10.1111/cbdd.12330: \\Arylazopyrazole AAP1742 inhibits CDKs and induces apoptosis in multiple myeloma cells via Mcl-1 downregulation.\\2014Chemical biology & drug design, Oct, Volume: 84, Issue:4
Arylazopyrazole AAP1742 inhibits CDKs and induces apoptosis in multiple myeloma cells via Mcl-1 downregulation.
AID1796840CDK Inhibition Assay from Article 10.1021/jm0605740: \\4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.\\2006Journal of medicinal chemistry, Nov-02, Volume: 49, Issue:22
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
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.
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.
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB2012ACS chemical biology, May-18, Volume: 7, Issue:5
The CDK9 C-helix exhibits conformational plasticity that may explain the selectivity of CAN508.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (10)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (10.00)29.6817
2010's8 (80.00)24.3611
2020's1 (10.00)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%
Other10 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]