Information on EC 2.7.11.22 - cyclin-dependent kinase and Organism(s) Homo sapiens and UniProt Accession Q00536

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Homo sapiens
UNIPROT: Q00536


The taxonomic range for the selected organisms is: Homo sapiens

The enzyme appears in selected viruses and cellular organisms

EC NUMBER
COMMENTARY hide
2.7.11.22
-
RECOMMENDED NAME
GeneOntology No.
cyclin-dependent kinase
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
ATP + a protein = ADP + a phosphoprotein
show the reaction diagram
catalytic aspartate residue
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phospho group transfer
-
-
-
-
SYSTEMATIC NAME
IUBMB Comments
ATP:cyclin phosphotransferase
Activation of cyclin-dependent kinases requires association of the enzyme with a regulatory subunit referred to as a cyclin. It is the sequential activation and inactivation of cyclin-dependent kinases, through the periodic synthesis and destruction of cyclins, that provides the primary means of cell-cycle regulation.
CAS REGISTRY NUMBER
COMMENTARY hide
150428-23-2
-
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
-
SwissProt
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
evolution
malfunction
metabolism
physiological function
additional information
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
-
-
-
-
?
ATP + a protein
ADP + phosphorylated protein
show the reaction diagram
-
-
-
-
?
ATP + axonal cytoskeleton protein
ADP + phosphorylated axonal cytoskeleton protein
show the reaction diagram
ATP + biotin-TVSEESNVLCLSKSPNKHNRLYMKARPFF
ADP + biotin-TVSEESNVLCLSKpSPNKHNRLYMKARPFF
show the reaction diagram
-
-
phosphorylated on Ser595
-
?
ATP + bloom syndrome helicase
ADP + phosphorylated bloom syndrome helicase
show the reaction diagram
ATP + BRCA2
ADP + phosphorylated BRCA2
show the reaction diagram
ATP + c-Jun N-terminal kinase 3
ADP + phosphorylated c-Jun N-terminal kinase 3
show the reaction diagram
ATP + C-terminal domain of RNA polymerase II
ADP + phosphorylated C-terminal domain of RNA polymerase II
show the reaction diagram
ATP + CALD1 protein
ADP + CALD1 phosphoprotein
show the reaction diagram
-
reccombinant human GST-tagged substrate, with CDK6
-
-
?
ATP + Cdc20
ADP + phosphorylated Cdc20
show the reaction diagram
ATP + Cdc6
ADP + phosphorylated Cdc6
show the reaction diagram
-
-
-
-
?
ATP + CDK1
ADP + phosphorylated CDK1
show the reaction diagram
-
CDK7 phosphorylates the activation segment or T-loop of CDK1
-
-
?
ATP + Cdk1
ADP + phosphorylated Cdk2
show the reaction diagram
-
Cdk7
-
-
?
ATP + cdk2
ADP + phosphorylated cdk2
show the reaction diagram
-
CDK7 phosphorylates the activation segment or T-loop of CDK2
-
-
?
ATP + Cprk
ADP + phosphorylated Cprk
show the reaction diagram
-
i.e. Cdk5/p35-regulated kinase
-
-
?
ATP + CREB-binding protein
ADP + phosphorylated CREB-binding protein
show the reaction diagram
-
-
-
-
?
ATP + cyclin H protein
ADP + cyclin H phosphoprotein
show the reaction diagram
-
CDK8
-
-
?
ATP + Dab1 protein
ADP + Dab1 phosphoprotein
show the reaction diagram
ATP + dephosphin
ADP + phosphorylated dephosphin
show the reaction diagram
ATP + DNA polymerase alpha
ADP + phosphorylated DNA polymerase alpha
show the reaction diagram
-
-
-
-
?
ATP + DNA polymerase sigma
ADP + phosphorylated DNA polymerase sigma
show the reaction diagram
-
-
-
-
?
ATP + E2F1 protein
ADP + E2F1 phosphoprotein
show the reaction diagram
-
CDK8
-
-
?
ATP + early mitotic inhibitor 1 protein
ADP + early mitotic inhibitor 1 phosphoprotein
show the reaction diagram
ATP + ErbB2
ADP + phosphorylated ErbB2
show the reaction diagram
ATP + ErbB3
ADP + phosphorylated ErbB3
show the reaction diagram
ATP + estrogen receptor
ADP + phosphorylated estrogen receptor
show the reaction diagram
-
Cdk2 phosphorylation at Ser104 and Ser106
-
-
?
ATP + eukaryotic elongation factor 2
ADP + phosphorylated eukaryotic elongation factor 2
show the reaction diagram
ATP + ezrin
ADP + phosphorylated ezrin
show the reaction diagram
-
phosphorylation by cdk5 at Thr235 in the NH2-terminal region and consequent dissociation of Rho GDP dissociation inhibitor from an ezrin/Rho-GDI complex
-
-
?
ATP + glucocorticoid receptor
ADP + phosphorylated glucocorticoid receptor
show the reaction diagram
-
-
-
-
?
ATP + HHASPRK
ADP + HHAS(P)PRK
show the reaction diagram
-
-
-
-
?
ATP + HHASPRK
ADP + phosphorylated HHASPRK
show the reaction diagram
-
-
-
-
?
ATP + histone 1
ADP + phosphorylated histone 1
show the reaction diagram
-
-
-
-
?
ATP + histone H1
ADP + phosphorylated histone H1
show the reaction diagram
ATP + histone H1
ADP + phosphorylated steroid histone H1
show the reaction diagram
-
-
-
-
?
ATP + histone H1-derived peptide
ADP + histone H1-derived peptide phosphate
show the reaction diagram
-
-
-
-
?
ATP + histone H3 protein
ADP + histone H3 phosphoprotein
show the reaction diagram
-
CDK8
-
-
?
ATP + human cytomegalovirus tegument protein pp65
ADP + phosphorylated human cytomegalovirus tegument protein pp65
show the reaction diagram
-
-
-
-
?
ATP + huntingtin
ADP + phosphorylated huntingtin
show the reaction diagram
-
-
-
-
?
ATP + Mcm3
ADP + phosphorylated Mcm3
show the reaction diagram
-
-
-
-
?
ATP + Mcm4
ADP + phosphorylated Mcm4
show the reaction diagram
-
-
-
-
?
ATP + Med13 protein
ADP + Med13 phosphoprotein
show the reaction diagram
-
CDK8
-
-
?
ATP + MEK1
ADP + phosphorylated MEK1
show the reaction diagram
ATP + MEP50 protein
ADP + MEP50 phosphoprotein
show the reaction diagram
ATP + Munc-18
ADP + phosphorylated Munc-18
show the reaction diagram
ATP + NF-H
ADP + phosphorylated NF-H
show the reaction diagram
ATP + NF-M
ADP + phosphorylated NF-M
show the reaction diagram
ATP + NR1 receptor
ADP + phosphorylated NR1 receptor
show the reaction diagram
ATP + NR2 receptor
ADP + phosphorylated NR2 receptor
show the reaction diagram
ATP + Orc2
ADP + phosphorylated Orc2
show the reaction diagram
-
-
-
-
?
ATP + Orc6
ADP + phosphorylated Orc6
show the reaction diagram
-
-
-
-
?
ATP + p35 protein
ADP + p35 phosphoprotein
show the reaction diagram
-
a nuclear transcription factor, Cdk5-p25 phosphorylates p53 on Ser15, Ser33, and Ser44
-
-
?
ATP + parkin
ADP + phosphorylated parkin
show the reaction diagram
ATP + PKTPKKAKKL
ADP + PKpTPKKAKKL
show the reaction diagram
ATP + pocket protein p107
ADP + phosphorylated pocket protein 107
show the reaction diagram
ATP + pocket protein p130
ADP + phosphorylated pocket protein 130
show the reaction diagram
ATP + polymerase II C-terminal domain
ADP + phosphorylated polymerase II C-terminal domain
show the reaction diagram
Q140014
-
-
-
?
ATP + progesterone receptor
ADP + phosphorylated progesterone receptor
show the reaction diagram
ATP + promyelocytic leukemia zinc finger
ADP + phosphorylated promyelocytic leukemia zinc finger
show the reaction diagram
-
can also be phosphorylated by CDK1 albeit in a less efficient fashion than by CDK2
-
-
?
ATP + protein
ADP + phosphoprotein
show the reaction diagram
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
-
?
ATP + Rb peptide
ADP + Rb phosphopeptide
show the reaction diagram
-
from retinoblastoma-associated protein
-
-
?
ATP + replication factor C
ADP + phosphorylated replication factor C
show the reaction diagram
-
-
-
-
?
ATP + retinoblastoma protein
ADP + phosphorylated retinoblastoma protein
show the reaction diagram
ATP + retinoblastoma protein
ADP + retinoblastoma phosphoprotein
show the reaction diagram
ATP + RNA polymerase II
ADP + phosphorylated RNA polymerase II
show the reaction diagram
ATP + RNA polymerase II C-terminal domain
ADP + phosphorylated RNA polymerase II C-terminal domain
show the reaction diagram
ATP + RNA polymerase II C-terminal domain protein
ADP + RNA polymerase II C-terminal domain phosphoprotein
show the reaction diagram
-
-
-
-
?
ATP + RNA polymerase II carboxy-terminal domain
ADP + phosphorylated RNA polymerase II carboxy-terminal domain
show the reaction diagram
-
CDK8
-
-
?
ATP + RXL motif-containing peptide
ADP + RXL motif-containing phosphopeptide
show the reaction diagram
-
peptide sequence corresponding to amino acids 866-880 of RNA polymerase II C-terminal domain. Substrate phosphorylation by CDK6 with K-cyclin from Kaposi sarcoma herpesvirus, but addition of this peptide significantly reduces substrate phosphorylation by cyclin E-CDK2 and cyclin D2-CDK6
-
-
?
ATP + SCR-1
ADP + phosphorylated SCR-1
show the reaction diagram
ATP + SIRT2
ADP + phosphorylated SIRT2
show the reaction diagram
-
-
-
-
?
ATP + SMAD protein
ADP + SMAD phosphoprotein
show the reaction diagram
-
CDK8
-
-
?
ATP + STAT3
ADP + phosphorylated STAT3
show the reaction diagram
-
substrate of CDK5
-
-
?
ATP + STAT3 protein
ADP + STAT3 phosphoprotein
show the reaction diagram
-
Cdk5 phosphorylates at Ser727
-
-
?
ATP + steroid receptor coactivator-1
ADP + phosphorylated steroid receptor coactivator-1
show the reaction diagram
-
-
-
-
?
ATP + steroidogenic factor 1
ADP + phosphorylated steroidogenic factor 1
show the reaction diagram
-
also known as Ad4BP, systematic name NR5A1, the phosphorylation site is at Ser203
-
-
?
ATP + T-cell protein tyrosine phosphatase
ADP + phosphorylated T-cell protein tyrosine phosphatase
show the reaction diagram
ATP + tau protein
ADP + phosphorylated tau protein
show the reaction diagram
ATP + Tau protein
ADP + Tau phosphoprotein
show the reaction diagram
ATP + tumor suppressor Rb
ADP + phosphorylated tumor suppressor Rb
show the reaction diagram
-
-
-
-
?
ATP + VGCC
ADP + phosphorylated NR1 receptor
show the reaction diagram
ATP + Wee1A
ADP + phosphorylated Wee1A
show the reaction diagram
ATP + [elongation factor 2]
ADP + [elongation factor 2]phosphate
show the reaction diagram
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
additional information
?
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
-
-
-
-
?
ATP + a protein
ADP + phosphorylated protein
show the reaction diagram
-
-
-
-
?
ATP + axonal cytoskeleton protein
ADP + phosphorylated axonal cytoskeleton protein
show the reaction diagram
-
regulated by integrin alpha1beta1
-
-
?
ATP + bloom syndrome helicase
ADP + phosphorylated bloom syndrome helicase
show the reaction diagram
-
-
-
-
?
ATP + BRCA2
ADP + phosphorylated BRCA2
show the reaction diagram
-
phosphorylates at Ser3291, phosphorylation reaches maximal levels in G2/M
-
-
?
ATP + c-Jun N-terminal kinase 3
ADP + phosphorylated c-Jun N-terminal kinase 3
show the reaction diagram
-
i.e. JNK3, phosphorylation inhibits JNK3 and leads to reduced phosphorylation of c-jun and to reduced apoptosis
-
-
?
ATP + Cdc20
ADP + phosphorylated Cdc20
show the reaction diagram
-
Cdk phosphorylation affects interaction of Cdc20 with Mad2 and the anaphase-promoting complex-cyclosome in HeLa cells
-
-
?
ATP + CDK1
ADP + phosphorylated CDK1
show the reaction diagram
-
CDK7 phosphorylates the activation segment or T-loop of CDK1
-
-
?
ATP + Cdk1
ADP + phosphorylated Cdk2
show the reaction diagram
-
Cdk7
-
-
?
ATP + cdk2
ADP + phosphorylated cdk2
show the reaction diagram
-
CDK7 phosphorylates the activation segment or T-loop of CDK2
-
-
?
ATP + Cprk
ADP + phosphorylated Cprk
show the reaction diagram
-
i.e. Cdk5/p35-regulated kinase
-
-
?
ATP + Dab1 protein
ADP + Dab1 phosphoprotein
show the reaction diagram
-
-
-
-
?
ATP + dephosphin
ADP + phosphorylated dephosphin
show the reaction diagram
-
Cdk5 regulates endocytosis involving dephosphin activity, overview
-
-
?
ATP + early mitotic inhibitor 1 protein
ADP + early mitotic inhibitor 1 phosphoprotein
show the reaction diagram
-
i.e. Emi1, is phosphorylated by CDKs in mitotic but not S-phase cell extracts
-
-
?
ATP + ErbB2
ADP + phosphorylated ErbB2
show the reaction diagram
-
phosphorylation of the neuregulin receptor by Cdk5 is involved in regulation of neuregulin
-
-
?
ATP + ErbB3
ADP + phosphorylated ErbB3
show the reaction diagram
-
phosphorylation of the neuregulin receptor by Cdk5 is involved in regulation of neuregulin
-
-
?
ATP + eukaryotic elongation factor 2
ADP + phosphorylated eukaryotic elongation factor 2
show the reaction diagram
-
phosphorylation on Ser595 by Cdk2
-
-
?
ATP + histone H1
ADP + phosphorylated steroid histone H1
show the reaction diagram
-
-
-
-
?
ATP + MEK1
ADP + phosphorylated MEK1
show the reaction diagram
-
Cdk5 regulates the ERK1/2 pathway through phosphorylation of MEK1, overview
-
-
?
ATP + MEP50 protein
ADP + MEP50 phosphoprotein
show the reaction diagram
-
a PRMT5 co-regulatory factor
-
-
?
ATP + Munc-18
ADP + phosphorylated Munc-18
show the reaction diagram
-
involved in regulation of exocytosis involving SNARE proteins, Munc-18 is required for mediating secretory responsesoverview
-
-
?
ATP + NF-H
ADP + phosphorylated NF-H
show the reaction diagram
-
neurofilament protein that correlates neurit outgrowth, phosphorylation at the KSP repeats, regulated by the myelin-associate glycoprotein
-
-
?
ATP + NF-M
ADP + phosphorylated NF-M
show the reaction diagram
-
neurofilament protein, phosphorylation at the KSP repeats, regulated by the myelin-associate glycoprotein
-
-
?
ATP + NR1 receptor
ADP + phosphorylated NR1 receptor
show the reaction diagram
-
involved in synaptic transmission, overview
-
-
?
ATP + NR2 receptor
ADP + phosphorylated NR2 receptor
show the reaction diagram
-
involved in synaptic transmission, phosphorylation of Ser1232 on the A subunit upregulates NMCAR activity, overview
-
-
?
ATP + p35 protein
ADP + p35 phosphoprotein
show the reaction diagram
-
a nuclear transcription factor, Cdk5-p25 phosphorylates p53 on Ser15, Ser33, and Ser44
-
-
?
ATP + parkin
ADP + phosphorylated parkin
show the reaction diagram
-
Ser-131 located at the linker region of parkin is the major Cdk5 phosphorylation site, phosphorylation by Cdk5 decreases the auto-ubiquitylation of parkin, parkin S131A mutant has 40% lower phosphorylation levels in vivo than wild-type parkin
-
-
?
ATP + pocket protein p107
ADP + phosphorylated pocket protein 107
show the reaction diagram
-
hyperphosphorylation by CDK/cyclin contributes to the transactivation of genes with functional E2F-binding sites, including growth and cell-cycle regulators, i.e. c-myc, Rb protein, cdc2, cyclin E, and cyclin A, and genes encoding proteins required for nucleotide and DNA biosynthesis
-
-
?
ATP + pocket protein p130
ADP + phosphorylated pocket protein 130
show the reaction diagram
-
hyperphosphorylation by CDK/cyclin contributes to the transactivation of genes with functional E2F-binding sites, including growth and cell-cycle regulators, i.e. c-myc, Rb protein, cdc2, cyclin E, and cyclin A, and genes encoding proteins required for nucleotide and DNA biosynthesis
-
-
?
ATP + polymerase II C-terminal domain
ADP + phosphorylated polymerase II C-terminal domain
show the reaction diagram
Q140014
-
-
-
?
ATP + progesterone receptor
ADP + phosphorylated progesterone receptor
show the reaction diagram
ATP + retinoblastoma protein
ADP + phosphorylated retinoblastoma protein
show the reaction diagram
ATP + retinoblastoma protein
ADP + retinoblastoma phosphoprotein
show the reaction diagram
-
a tumor suppressor protein
-
-
?
ATP + RNA polymerase II
ADP + phosphorylated RNA polymerase II
show the reaction diagram
-
CDK7 and CDK8 phosphorylate the C-terminal domain of RNA Pol II
-
-
?
ATP + RNA polymerase II C-terminal domain
ADP + phosphorylated RNA polymerase II C-terminal domain
show the reaction diagram
-
phosphorylation by Cdk7 and Cdk9, phosphorylation at serine residues 2 and 5
-
-
?
ATP + RNA polymerase II C-terminal domain protein
ADP + RNA polymerase II C-terminal domain phosphoprotein
show the reaction diagram
-
-
-
-
?
ATP + SCR-1
ADP + phosphorylated SCR-1
show the reaction diagram
-
Cdk2-cyclin A, phosphorylation at Lys5 regulates SCR-1 interaction with the progesterone receptor
-
-
?
ATP + STAT3
ADP + phosphorylated STAT3
show the reaction diagram
-
substrate of CDK5
-
-
?
ATP + STAT3 protein
ADP + STAT3 phosphoprotein
show the reaction diagram
-
Cdk5 phosphorylates at Ser727
-
-
?
ATP + T-cell protein tyrosine phosphatase
ADP + phosphorylated T-cell protein tyrosine phosphatase
show the reaction diagram
-
phosphorylation of the two splicing varaints TC45 and TC48 at Ser304 in a cell cycle-dependent manner, optimally in mitosis, overview
-
-
?
ATP + tau protein
ADP + phosphorylated tau protein
show the reaction diagram
ATP + Tau protein
ADP + Tau phosphoprotein
show the reaction diagram
-
Cdk5-p25 has a stronger Tau-phosphorylating activity than Cdk5-p35 in neurons
-
-
?
ATP + VGCC
ADP + phosphorylated NR1 receptor
show the reaction diagram
-
a voltage-dependent calcium channel, phosphorylation within the intracellular loop of the channel inhibiting interaction with SNARE proteins, SNAP-25, and synaptotagmin I required for neurotransmitter release, overview
-
-
?
ATP + Wee1A
ADP + phosphorylated Wee1A
show the reaction diagram
-
phosphorylation at S123, S53, and S121 promotes binding of Wee1A by beta-TrCP, the beta-transducin repeat-containing protein, which is the substrate recognition component of the ubiquitin ligase, leading to proteasomal degradation of Wee1A, overview
-
-
?
ATP + [elongation factor 2]
ADP + [elongation factor 2]phosphate
show the reaction diagram
-
the enzyme phosphorylates Ser595. Ser595 phosphorylation varies during the cell cycle and is required for efficient Thr56 phosphorylation (by elongation factor 2 kinase) in vivo
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
additional information
?
-
COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
cyclin
-
cyclin A
-
cyclin B
-
cyclin B1
-
required regulatory subunit of CDKs
-
cyclin C
-
cofactor of CDK3
-
cyclin D
-
cyclin D1
-
cyclin D2
-
cyclin D3
-
cyclin E
-
cyclin E2
-
cofactor of CDK3
-
cyclin H
-
cofactor of CDK7
-
cyclin K
-
-
-
cyclin L
-
cofactor of CDK11
-
cyclin T
-
cyclin V
-
regulatory subunit of CDK6
-
additional information
-
viral K-cyclin has a much longer half-life compared to cellular cyclins because it lacks the PEST degradation sequence, the viral K-cyclin can substitute the cellular cyclins in binding to the cellular CDKs, which is important for the virus development
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(-)-cis-5,7-dihydroxyphenyl-8-[4-(3-hydroxy-1-methyl)piperidinyl]-4H-1-benzopyran-4-one hydrochloride hemihydrate
-
-
-
(1S,2R,3R)-3-[[9-iso-propyl-6-[[4-(2-pyridyl)phenyl]methylamino]purin-2-yl]amino]cyclohexane-1,2-diol
-
-
(2R)-2-hydroxy-3-[[9-(propan-2-yl)-6-[[4-(pyridin-2-yl)benzyl]amino]-9H-purin-2-yl]amino]propyl L-valinate
-
-
(2R)-3-[[9-iso-propyl-6-[[4-(2-pyridyl)phenyl]methylamino]purin-2-yl]amino]propane-1,2-diol
-
-
(2S)-4-[[9-iso-propyl-6-[[4-(2-pyridyl)phenyl]methylamino]purin-2-yl]amino]butane-1,2-diol
-
-
(3-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]phenyl)acetonitrile
-
-
(3-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]phenyl)methanol
-
-
(3-[[4-amino-6-(cyclohexylmethoxy)pyrimidin-2-yl]amino]phenyl)acetonitrile
-
41% inhibition at 0.01 mM
(3R,5S)-5-(hydroxymethyl)-1-[9-iso-propyl-6-[[4-(2-pyridyl)phenyl]methylamino]- purin-2-yl]pyrrolidin-3-ol
-
-
(3Z)-3-(2-oxo-2-phenylethylidene)-1,3-dihydro-2H-indol-2-one
-
IC50 for CDK1 is above 0.016 mM
(3Z)-3-[2-(4-bromophenyl)-2-oxoethylidene]-1,3-dihydro-2H-indol-2-one
-
IC50 for CDK1 is 0.012 mM
(3Z)-5-bromo-3-(2-oxo-2-phenylethylidene)-1,3-dihydro-2H-indol-2-one
-
IC50 for CDK1 is 0.030 mM
(3Z)-5-bromo-3-[2-(4-fluorophenyl)-2-oxoethylidene]-1,3-dihydro-2H-indol-2-one
-
IC50 for CDK1 is 0.029 mM
(3Z)-5-bromo-3-[2-(4-methylphenyl)-2-oxoethylidene]-1,3-dihydro-2H-indol-2-one
-
IC50 for CDK1 is 0.029 mM
(4,5-diphenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl)hydrazine trihydrochloride
-
-
(4-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]phenyl)acetonitrile
-
-
(4-[[4-amino-6-(cyclohexylmethoxy)pyrimidin-2-yl]amino]phenyl)acetonitrile
-
-
(5Z)-2-(benzylamino)-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-(butylamino)-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-(cyclopropylamino)-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-(methoxyamino)-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-(methylamino)-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-(phenylamino)-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[(2,6-dichlorobenzyl)amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[(2-bromobenzyl)amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[(2-chlorobenzyl)amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[(2-methoxybenzyl)amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[(2-phenylethyl)amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[(2-pyridin-2-ylethyl)amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[(3-hydroxy-2-phenylpropyl)amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[(3-phenylpropyl)amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[(pyridin-2-ylmethyl)amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[methyl(thiophen-2-ylmethyl)amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[[(1R)-1-benzyl-2-hydroxyethyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[[(1R)-2-hydroxy-1-phenylethyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[[(1R)-2-methoxy-1-phenylethyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[[(1R,2S)-2-phenylcyclopropyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[[(1S)-1-benzyl-2-hydroxyethyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[[(1S)-2-hydroxy-1-phenylethyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[[2-(2-chlorophenyl)ethyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[[2-(2-ethoxyphenyl)ethyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[[2-(2-fluorophenyl)ethyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[[2-(2-methoxyphenyl)ethyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[[2-(3-chlorophenyl)ethyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[[2-(3-fluorophenyl)ethyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[[2-(4-bromophenyl)ethyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[[2-(4-chlorophenyl)ethyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[[2-(4-fluorophenyl)ethyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-2-[[2-(4-methoxyphenyl)ethyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
-
-
(5Z)-5-(quinolin-6-ylmethylidene)-2-(thiophen-2-ylmethyl)-1,3-thiazol-4(5H)-one
-
-
(5Z)-5-(quinolin-6-ylmethylidene)-2-[(2-thiophen-2-ylethyl)amino]-1,3-thiazol-4(5H)-one
-
-
(5Z)-5-(quinolin-6-ylmethylidene)-2-[(thiophen-2-ylmethyl)amino]-1,3-thiazol-4(5H)-one
-
-
(R)-roscovitine
1,2-di(2-pyridyl)-1H-pyrazolo[3,4-c]pyridazine
-
-
1,2-dimethyl-1H-pyrazolo[3,4-c]pyridazine
-
-
1,25-dihydroxyvitamin D3
-
inhibition of CDK2 activity by 1,25-dihydroxyvitamin D3 is associated with decreased T160 phosphorylation, a residue whose phosphorylation in the nucleus is essential for CDK2 activity. 1,25-dihydroxyvitamin D3 increases the stability of the cyclin-dependent kinase inhibitor p27KIP1. Ectopic expression of cyclin E is sufficient to overcome 1,25-dihydroxyvitamin D3-mediated cytoplasmic mislocalization of CDK2 and all antiproliferative effects of 1,25-dihydroxyvitamin D3, yet endogenous levels of cyclin E or binding to CDK2 are not affected by 1,25-dihydroxyvitamin D3. Targeting CDK2 to the nucleus of 1,25-dihydroxyvitamin D3-sensitive cancer cells blocked G1 accumulation and growth inhibition by 1,25-dihydroxyvitamin D3
1-(1-acetylpiperidin-4-yl)-8-(cyclopentylamino)-4,5-dihydro-1Hpyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-(4,5-diphenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl)-3-ethylurea
-
-
1-(4,5-diphenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl)-3-phenylurea
-
-
1-(5-cyclobutyl-thiazol-2-yl)-3-isoquinolin-5-yl-urea
-
competitive inhibitor
1-acetyl-3-amino-4,5-diphenyl-1H-pyrazolo[3,4-c]pyridazine
-
-
1-amino-3H-dibenzo[f,h]pyrazolo[3,4-c]cinnoline
-
-
1-benzyl-8-(cyclopentylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]-quinazoline-3-carboxamide
-
-
1-methyl-8-([1-[(4-methylpiperazin-1-yl)carbonyl]piperidin-4-yl]amino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-8-[(1-methylpiperidin-4-yl)amino]-4,5-dihydro-1Hpyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-8-[(pyridin-2-ylmethyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-8-[(pyridin-3-ylmethyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-8-[(pyridin-4-ylmethyl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-8-[[1-(methylsulfonyl)piperidin-4-yl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-8-[[1-(phenylcarbonyl)piperidin-4-yl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-8-[[1-(phenylsulfonyl)piperidin-4-yl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-8-[[2-(morpholin-4-yl)ethyl]amino]-4,5-dihydro-1Hpyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-8-[[2-(piperidin-1-yl)ethyl]amino]-4,5-dihydro-1Hpyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-8-[[3-(4-methylpiperazin-1-yl)benzyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-8-[[4-(4-methylpiperazin-1-yl)benzyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-methyl-8-[[4-(methylsulfonyl)benzyl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
1-NMPP1
-
inhibits Cdk7, selective inhibition of Cdk7 in G1 prevents activation but not formation of Cdk2/cyclin complexes and delays S phase. Inhibiting Cdk7 in G2 blocks entry to mitosis and disrupts Cdk1/cyclin B complex assembly
1-[4-[(5-fluoro-6,8-dimethyl-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-yl)amino]phenyl]-N,N-dimethyl-L-prolinamide
-
-
2-(2-chlorophenyl)-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
-
-
2-(3-bromophenyl)-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
-
-
2-(3-chloro-4-piperazin-1-yl-phenylamino)-8-cyclopentyl-5-methyl-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
2-(3-chlorophenyl)-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
-
-
2-(4-aminophenyl)-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
-
-
2-(4-bromophenyl)-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
-
-
2-(4-chlorophenyl)-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
-
-
2-biphenyl-4-yl-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
-
-
2-[(3,4-dimethoxyphenyl)amino]-8-ethylpyrido[2,3-d]pyrimidin-7(8H)-one
-
-
2-[(3-amino-4,5-diphenyl-1H-pyrazolo[3,4-c]pyridazin-1-yl)methoxy]ethanol
-
-
2-[(4-[4-[(5-fluoro-6,8-dimethyl-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-yl)amino]phenyl]piperazin-1-yl)sulfonyl]-2-oxoethanol
-
-
2-[(4-[4-[(6,8-dimethyl-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-yl)amino]phenyl]piperazin-1-yl)sulfonyl]-1-(methylsulfanyl)-2-oxoethanol
-
-
2-[(4-[4-[(6,8-dimethyl-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-yl)amino]phenyl]piperazin-1-yl)sulfonyl]-2-oxoethanol
-
-
2-[2-(3-amino-4,5-diphenyl-1H-pyrazolo[3,4-c]pyridazin-1-yl)ethoxy]ethanol
-
-
2-[4-(4-acetyl-piperazin-1-yl)-phenylamino]-8-cyclopentyl-5-methyl-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
2-[4-(diethylamino)phenyl]-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
-
-
2-[4-(dimethylamino)phenyl]-N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]acetamide
-
-
3-acetamide-1-acetyl-4,5-diphenyl-1H-pyrazolo[3,4-c]-pyridazine
-
-
3-acetamide-4,5-diphenyl-1H-pyrazolo[3,4-c]pyridazine
-
-
3-amino-1-benzyl-4,5-diphenyl-1H-pyrazolo[3,4-c]pyridazine
-
-
3-amino-4,5-bis(p-aminophenyl)-1H-pyrazolo[3,4-c]-pyridazine
-
-
3-amino-4,5-bis(p-methoxyphenyl)-1H-pyrazolo[3,4-c]-pyridazine
-
-
3-amino-4,5-bis(p-nitrophenyl)-1H-pyrazolo[3,4-c]pyridazine
-
-
3-amino-4,5-bis(p-tert-butylphenyl)-1H-pyrazolo[3,4-c]-pyridazine
-
-
3-amino-4,5-bis(p-trifluoromethylphenyl)-1H-pyrazolo-[3,4-c]pyridazine
-
-
3-amino-4,5-di(2-furyl)-1H-pyrazolo[3,4-c]pyridazine
-
-
3-amino-4-phenyl-1H-pyrazolo[3,4-c]pyridazine
-
-
3-amino-5-(2-furyl)-1H-pyrazolo[3,4-c]pyridazine
-
-
3-amino-5-methyl-4-phenyl-1H-pyrazolo[3,4-c]pyridazine
-
-
3-amino-5-phenyl-1H-pyrazolo[3,4-c]pyridazine
-
-
3-isopropyl-5(R)-(2-hydroxypropyl)amino-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
-
3-isopropyl-5(R)-[1-(hydroxymethyl)propyl]amino-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
-
3-isopropyl-5,7-di[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
-
3-isopropyl-5-(2,3-dihydroxypropyl)amino-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
-
3-isopropyl-5-(2-aminoethyl)amino-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
-
3-isopropyl-5-(2-hydroxy-2-methylpropyl)amino-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
-
3-isopropyl-5-(2-hydroxyethyl)amino-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
-
3-isopropyl-5-(3-amino-2-hydroxypropyl)amino-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
-
3-isopropyl-5-(4-methoxybenzyl)amino-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
-
3-isopropyl-5-(N-morpholinyl)-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
-
3-isopropyl-5-(piperazin-1-yl)-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
-
3-isopropyl-5-(thiomorpholinyl)-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
-
3-isopropyl-5-(trans-2-aminocyclohexyl)amino-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
-
3-isopropyl-5-(trans-4-aminocyclohexyl)amino-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
-
3-isopropyl-5-methylsulfanyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
-
3-isopropyl-5-methylsulfonyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
-
3-isopropyl-5-[2-(2-hydroxyethyl)piperidin-1-yl]-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
-
3-isopropyl-5-[2-(dimethylamino)ethyl]amino-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
-
3-isopropyl-5-[4-(2-hydroxyethyl)piperazin-1-yl]-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
-
3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidine
-
-
-
3-[[(2,2-dioxido-1,3-dihydro-2-benzothien-5-yl)amino]methylene]-5-(1,3-oxazol-5-yl)-1,3-dihydro-2H-indol-2-one
-
-
3-[[4-([[amino(imino)methyl]amino]sulfonyl)anilino]methylene]-2-oxo-2,3-dihydro-1H-indole
-
-
4-(1,3-benzothiazol-2-yl)-N-(1,3-thiazol-2-yl)thiophene-2-sulfonamide
-
-
4-(1,3-benzothiazol-2-yl)-N-(2-fluoroethyl)thiophene-2-sulfonamide
-
poor inhibition of cdk5/p25
4-(1,3-benzothiazol-2-yl)-N-(4,5-dimethyl-1,3-thiazol-2-yl)thiophene-2-sulfonamide
-
-
4-(1,3-benzothiazol-2-yl)-N-(4-methylpyridin-2-yl)thiophene-2-sulfonamide
-
-
4-(1,3-benzothiazol-2-yl)-N-(5-hydroxypyridin-2-yl)thiophene-2-sulfonamide
-
-
4-(1,3-benzothiazol-2-yl)-N-(pyridin-2-ylmethyl)thiophene-2-sulfonamide
-
-
4-(1,3-benzothiazol-2-yl)-N-hydroxythiophene-2-sulfonamide
-
-
4-(1,3-benzothiazol-2-yl)-N-[5-(morpholin-4-yl)pyridin-2-yl]thiophene-2-sulfonamide
-
-
4-(1,3-benzothiazol-2-yl)thiophene-2-sulfonamide
-
binds to Ile10 and Asp86 in the active site of cdk2
4-(1,4-dioxo-1,4-dihydro-naphthalen-2-ylamino)-N-(2-hydroxy-ethyl)-benzenesulfonamide
-
-
4-(1-ethyl-2-methyl-1H-imidazol-5-yl)-N-[4-(methylsulfonyl)phenyl]pyrimidin-2-amine
-
-
4-(6-acetyl-1,3-benzothiazol-2-yl)thiophene-2-sulfonamide
-
poor inhibition of cdk2/cyclin E
4-(6-amino-4-cyclohexylmethoxy-5-nitrosopyrimidin-2-ylamino)-benzenesulfonamide
-
-
4-(6-amino-4-cyclohexylmethoxy-5-nitrosopyrimidin-2-ylamino)-N-(2,3-dihydroxypropyl)-benzenesulfonamide
-
-
4-(6-amino-4-cyclohexylmethoxy-5-nitrosopyrimidin-2-ylamino)-N-(2-hydroxyethyl)benzenesulfonamide
-
-
4-(6-chloro-1,3-benzothiazol-2-yl)thiophene-2-sulfonamide
-
-
4-(6-fluoro-1,3-benzothiazol-2-yl)thiophene-2-sulfonamide
-
-
4-(6-methyl-1,3-benzothiazol-2-yl)thiophene-2-sulfonamide
-
-
4-(6-nitro-1,3-benzothiazol-2-yl)thiophene-2-sulfonamide
-
-
4-chloro-N-(cis-3-[4-[(naphthalen-1-ylacetyl)amino]-1H-imidazol-1-yl]cyclobutyl)benzamide
-
-
4-[(4-imidazo[1,2-a]pyridin-3-ylpyrimidin-2-yl)amino]-N-(2-methoxyethyl)benzenesulfonamide
-
-
4-[(4-imidazo[1,2-a]pyridin-3-ylpyrimidin-2-yl)amino]benzenesulfonamide
-
-
4-[(4-imidazo[1,2-b]pyridazin-3-ylpyrimidin-2-yl)amino]-N-methylbenzenesulfonamide
-
-
4-[2-(5-bromo-2-oxo-1,2-dihydro-3H-indol-3-ylidene)hydrazino]benzenesulfonamide
-
-
4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]-N-(4-[[3-(1,3-oxazetidin-3-yl)propyl]sulfonyl]phenyl)pyrimidin-2-amine
-
-
4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]-N-[4-(methylsulfonyl)phenyl]pyrimidin-2-amine
-
-
4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]-N-[4-(propylsulfonyl)phenyl]pyrimidin-2-amine
-
-
4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]-N-[4-[(tetrahydrofuran-2-ylmethyl)sulfonyl]phenyl]pyrimidin-2-amine
-
-
4-[4-(8-cyclopentyl-5-methyl-7-oxo-7,8-dihydro-pyrido-[2,3-d]pyrimidin-2-ylamino)-phenyl]-piperazine-1-carbaldehyde
-
-
4-[4-(8-cyclopentyl-5-methyl-7-oxo-7,8-dihydro-pyrido-[2,3-d]pyrimidin-2-ylamino)-phenyl]-piperazine-1-carboxylic acid tert-butyl ester
-
-
4-[4-(8-cyclopentyl-7-oxo-5-trifluoromethyl-7,8-dihydropyrido[2,3-d]pyrimidin-2-ylamino)-phenyl]-piperazine-1-carboxylic acid tert-butyl ester
-
-
4-[7-(4-chloro-3-fluorophenyl)-1,3-benzothiazol-2-yl]thiophene-2-sulfonamide
-
-
4-[7-(4-fluorophenyl)-1,3-benzothiazol-2-yl]thiophene-2-sulfonamide
-
poor inhibition of cdk2/cyclin E
4-[[(2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]amino]-N-(1,3-thiazol-2-yl)benzenesulfonamide
-
-
4-[[(7-oxo-6,7-dihydro-8H-[1,3]thiazolo[5,4-e]indol-8-ylidene)methyl]amino]-N-(2-pyridinyl)benzenesulfonamide
-
-
4-[[4-(1,2-dimethyl-1H-imidazol-5-yl)pyrimidin-2-yl]amino]-N-(2-methoxyethyl)-N-methylbenzenesulfonamide
-
-
4-[[4-(1,2-dimethyl-1H-imidazol-5-yl)pyrimidin-2-yl]amino]-N-(2-methoxyethyl)benzenesulfonamide
-
-
4-[[4-(1,2-dimethyl-1H-imidazol-5-yl)pyrimidin-2-yl]amino]-N-methylbenzenesulfonamide
-
-
4-[[4-(1,2-dimethyl-1H-imidazol-5-yl)pyrimidin-2-yl]amino]-N-[3-(1-methylethoxy)propyl]benzenesulfonamide
-
-
4-[[4-(1,2-dimethyl-1H-imidazol-5-yl)pyrimidin-2-yl]amino]benzenesulfonamide
-
-
4-[[4-(1-cyclopentyl-2-methyl-1H-imidazol-5-yl)pyrimidin-2-yl]amino]-N-(2-methoxyethyl)benzenesulfonamide
-
-
4-[[4-(1-cyclopropyl-2-methyl-1H-imidazol-5-yl)pyrimidin-2-yl]amino]-N-(2-methoxyethyl)benzenesulfonamide
-
-
4-[[4-(1-ethyl-2-methyl-1H-imidazol-5-yl)pyrimidin-2-yl]amino]-N-(2-methoxyethyl)benzenesulfonamide
-
-
4-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]-N,N-diethylbenzamide
-
-
4-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]-N,N-diethylbenzenesulfonamide
-
-
4-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]-N,N-dimethylbenzamide
-
-
4-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]-N-(2-hydroxypropyl)benzenesulfonamide
-
-
4-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]-N-(tetrahydrofuran-2-ylmethyl)benzenesulfonamide
-
-
4-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]-N-1,3-thiazol-2-ylbenzenesulfonamide
-
-
4-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]phenol
-
-
4-[[4-amino-6-(cyclohexylmethoxy)pyrimidin-2-yl]amino]-N,N-diethylbenzamide
-
29% inhibition at 0.001 mM
4-[[4-amino-6-(cyclohexylmethoxy)pyrimidin-2-yl]amino]-N,N-diethylbenzenesulfonamide
-
33% inhibition at 0.01 mM
4-[[4-amino-6-(cyclohexylmethoxy)pyrimidin-2-yl]amino]-N,N-dimethylbenzamide
-
49% inhibition at 0.1 mM
4-[[4-amino-6-(cyclohexylmethoxy)pyrimidin-2-yl]amino]benzamide
-
-
5,6-dichloro-1-beta-D-ribofuranosyl benzimidazole
-
cdk9 inhibitor
5,6-dichloro-1-beta-D-ribofuranosyl-benzimidazole
-
-
-
5,6-dichloro-1-beta-D-ribofuranosylbenzimidazole
-
specific CDK7 and 9 inhibition drives resolution of neutrophil-dominant inflammation
5-fluoro-6,8-dimethyl-N-(4-morpholin-4-ylphenyl)-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-amine
-
-
6,7-dimethoxy-N-(3hydroxyphenyl)quinazolin-4-amine
-
-
6,8-dimethyl-N-(4-morpholin-4-ylphenyl)-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-amine
-
-
6,8-dimethyl-N-[4-[4-(methylsulfonyl)piperazin-1-yl]phenyl]-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-amine
-
-
6-(cyclohexylmethoxy)-N2-(3-methoxyphenyl)-5-nitrosopyrimidine-2,4-diamine
-
-
6-(cyclohexylmethoxy)-N2-(4-methoxyphenyl)-5-nitrosopyrimidine-2,4-diamine
-
-
6-(cyclohexylmethoxy)-N2-[3-(methylsulfanyl)phenyl]-5-nitrosopyrimidine-2,4-diamine
-
-
6-(cyclohexylmethoxy)-N2-[3-(methylsulfanyl)phenyl]pyrimidine-2,4-diamine
-
-
6-(cyclohexylmethoxy)-N2-[4-(methylsulfanyl)phenyl]-5-nitrosopyrimidine-2,4-diamine
-
-
6-acetyl-8-cyclopentyl-5-methyl-2-(4-piperazin-1-ylphenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
6-bromo-8-cyclopentyl-5-methyl-2-(4-piperazin-1-ylphenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
6-chloro-8-cyclopentyl-5-methyl-2-(4-piperazin-1-ylphenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
6-dimethylamino purine
-
potent inhibitor of CDK1/cyclin B
8-(1-ethyl-propyl)-5-methyl-2-(4-piperazin-1-yl-phenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
8-(benzylamino)-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-(cyclohexylamino)-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]-quinazoline-3-carboxamide
-
-
8-(cyclohexylamino)-N-1-dimethyl-4,5-dihydro-1H-pyrazolo-[4,3-h]quinazoline-3-carboxamide
-
-
8-(cyclopentylamino)-1-(2,2,2-trifluoroethyl)-4,5-dihydro-1Hpyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-(cyclopentylamino)-1-(2-hydroxyethyl)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-(cyclopentylamino)-1-(4-methoxyphenyl)-4,5-dihydro-1Hpyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-(cyclopentylamino)-1-(4-sulfamoylphenyl)-4,5-dihydro-1Hpyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-(cyclopentylamino)-1-(pyridin-2-yl)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-(cyclopentylamino)-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-(cyclopentylamino)-1-phenyl-4,5-dihydro-1H-pyrazolo[4,3-h]-quinazoline-3-carboxamide
-
-
8-(cyclopentylamino)-N-1-dimethyl-4,5-dihydro-1H-pyrazolo-[4,3-h]quinazoline-3-carboxamide
-
-
8-(cyclopentylamino)-N-hydroxy-N,1-dimethyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-(cyclopentylamino)-N-methyl-1-(1-methylpiperidin-4-yl)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-(cyclopentylamino)-N-[1-(dimethylamino)propan-2-yl]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-(cyclopentylamino)-N-[2-(dimethylamino)ethyl]-N-1-dimethyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-amino-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-cyclopentyl-2-(4-morpholin-4-yl-phenylamino)-8Hpyrido[2,3-d]pyrimidin-7-one
-
-
8-cyclopentyl-2-(4-piperazin-1-yl-phenylamino)-5-trifluoromethyl-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
8-cyclopentyl-2-(4-piperazin-1-yl-phenylamino)-8Hpyrido[2,3-d]pyrimidin-7-one
-
-
8-cyclopentyl-2-(4-piperidin-1-yl-phenylamino)-8Hpyrido[2,3-d]pyrimidin-7-one
-
-
8-cyclopentyl-2-(4-[1,4]diazepan-1-yl-phenylamino)-5-methyl-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
8-cyclopentyl-2-[4-(3,3-dimethyl-piperazin-1-yl)-phenylamino]-5-methyl-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
8-cyclopentyl-2-[4-(3,5-dimethyl-piperazin-1-yl)-phenylamino]-5-methyl-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
8-cyclopentyl-2-[4-(3-hydroxy-pyrrolidin-1-yl)-phenylamino]-5-methyl-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
8-cyclopentyl-2-{4-[4-(3-hydroxy-propyl)-piperidin-1-yl]-phenylamino}-5-methyl-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
8-cyclopentyl-5,6-dimethyl-2-(4-piperazin-1-yl-phenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
8-cyclopentyl-5-ethyl-2-(4-piperazin-1-yl-phenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
8-cyclopentyl-5-methyl-2-(4-morpholin-4-yl-phenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
8-cyclopentyl-5-methyl-2-(4-piperazin-1-yl-phenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
8-cyclopentyl-5-methyl-2-(4-piperidin-1-yl-phenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
8-cyclopentyl-5-methyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
8-cyclopentyl-5-methyl-7-oxo-2-(4-piperazin-1-yl-phenylamino)-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carboxylic acid
-
-
8-cyclopentyl-5-methyl-7-oxo-2-(4-piperazin-1-yl-phenylamino)-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carboxylic acid ethyl ester
-
-
8-cyclopentyl-5-methyl-7-oxo-2-(4-piperazin-1-yl-phenylamino)-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carboxylic acid methyl ester
-
-
8-cyclopentyl-6-ethyl-5-methyl-2-(4-piperazin-1-yl-phenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
8-cyclopentyl-6-fluoro-5-methyl-2-(4-piperazin-1-ylphenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
8-cyclopentyl-6-iodo-5-methyl-2-(4-piperazin-1-yl-phenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
8-ethyl-2-[4-(4-methylpiperazin-1-yl)phenylamino]-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
8-isopropyl-5-methyl-2-(4-piperazin-1-yl-phenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
-
-
8-[(1-acetylpiperidin-4-yl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-[(1-acetylpiperidin-4-yl)amino]-N,1-dimethyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-[(1-acetylpiperidin-4-yl)amino]-N,1-dimethyl-4,5-dihydro-1Hpyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-[(1-ethylpiperidin-4-yl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-[(2-hydroxyethyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo-[4,3-h]quinazoline-3-carboxamide
-
-
8-[(3-methoxybenzyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-[(4-bromobenzyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo-[4,3-h]quinazoline-3-carboxamide
-
-
8-[(4-methoxybenzyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
8-[[4-(acetylamino)benzyl]amino]-1-methyl-4,5-dihydro-1Hpyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
actinomycin D
-
is less effective than 1-NMPP1 at inhibiting Cdk2 T loop phosphorylation
aloisine-A
-
-
alsterpaullone
aminopurvalanol
-
-
AMP
-
competitive inhibitor
anilinopyrimidine 32
-
-
apigenin
-
a flavonoid inhibitor of CDK6, CDK5, and CDK1
arylazopyrazole 31b
-
-
BMS-387032
-
-
BS-181
butyrolactone-1
-
-
CDK inhibitory proteins
-
members of the family of CDK inhibitory proteins, e.g. INK4 proteins, overview, CKIs may play a role as regulators in neointimal hyperplasia
-
Cdk2 inhibitor II
-
-
Cdk2DN
-
inhibition of Cdk2, induces phosphorylation of ataxia-telangiectasia mutated substrates
-
Cdk4/'6 Inhibitor IV
-
-
chrysin
-
a flavonoid inhibitor of CDK6, CDK5, and CDK1
CIP (154-279)
-
-
-
Cks1
-
Cks 1 protein inactivates Cdk2, activation of Chk1 leads to inactivation of Cdk2 by promoting phosphorylation-dependent turnover of the Cdk activating phosphatase Cdc25A
-
CR8
-
-
-
cyclin D1
-
inhibits the association and activation of androgen receptor by CDK6
-
cyclin-dependent kinase inhibitor p27KIP1
-
-
-
deoxyvariolin B
-
-
dinaciclib
-
-
-
DN-CDK2
-
suppresses CDK2 activity and partially increases erlotinib sensitivity
-
E2F1 peptide
-
81PALGRPPVKRRLDLE95
-
erlotinib
ethyl 4-[[1-methyl-3-(methylcarbamoyl)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazolin-8-yl]amino]piperidine-1-carboxylate
-
-
ethyl [2-([[4-(1,3-benzothiazol-2-yl)thiophen-2-yl]sulfonyl]amino)-1,3-thiazol-4-yl]acetate
-
-
FAALS
-
five amino-acid peptide inhibitor that is directed toward a noncatalytic binding pocket and which disrupts the cdk2/cyklin E complex
fascaplysin
-
CDK4- and CDK6-specific inhibitor
fisetin
-
a flavonol inhibitor of CDK6, CDK5, and CDK1, binding structure with CDK6 involving V101, E61, K43, D163, and E99 of CDK6, overview
flavopiridol
ginsenoside F1
-
noncompetitive inhibition
ginsenoside Rb1
-
noncompetitive inhibition
ginsenoside Re
-
noncompetitive inhibition
ginsenoside Rf
-
noncompetitive inhibition
ginsenoside Rg1
-
noncompetitive inhibition
ginsenoside Rg2
-
noncompetitive inhibition
ginsenoside Rh1
-
noncompetitive inhibition
H1PAla
-
noncompetitive inhibitor
-
H1PPO4
-
noncompetitive inhibitor
-
hymenialdisine
-
-
IkappaBalpha
-
human protein, competes with INK4 proteins for binding sites on CDK4, CDK4 is bound at the N-terminal ankyrin repeats, while the C-terminal ankyrin repeats bind NF-kappaB, structure analysis
-
indirubin 3'-monoxime
-
-
indirubin-3'-monoxime
indirubin-3'-oxime
-
-
indirubin-5-sulfonic acid
-
-
INK4 proteins
-
inhibit CDK4
-
insulin-like growth factor binding protein-3
-
decreases the phosphorylation activity of CDK2 and CDK4
-
isopentenyladenine
kaempferol
-
a less potent flavonoid inhibitor of CDK6, CDK5, and CDK1
kenpaullone
-
78% inhibition of CDK2 at 0.01 mM
KSLNRPFPDKIPELK
-
-
LAALS
-
; five amino-acid peptide inhibitor that is directed toward a noncatalytic binding pocket and which disrupts the cdk2/cyklin E complex
LDC000067
-
LiCl
-
slight inhibition of T231 phosphorylation by p25-Cdk5 kinase complex
luteolin
-
a flavonoid inhibitor of CDK5 and CDK1
meridianin A
-
-
meridianin G
-
-
meriolin
-
-
meriolin 1
-
-
meriolin 2
-
-
meriolin 3
-
-
Myt1
-
Cdk1 inhibitor
-
N-(1-[4-[(5-fluoro-6,8-dimethyl-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-yl)amino]phenyl]azetidin-3-yl)acetamide
-
-
N-(2-methoxyethyl)-4-([4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]pyrimidin-2-yl]amino)benzenesulfonamide
-
-
N-(2-methoxyethyl)-4-([4-[2-methyl-1-(2-methylpropyl)-1H-imidazol-5-yl]pyrimidin-2-yl]amino)benzenesulfonamide
-
-
N-(2-methoxyethyl)-4-[[4-(1,2,4-trimethyl-1H-imidazol-5-yl)pyrimidin-2-yl]amino]benzenesulfonamide
-
-
N-(4-[4-[(2-methoxyethyl)sulfonyl]piperazin-1-yl]phenyl)-6,8-dimethyl-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-amine
-
-
N-(4-[[3-(dimethylamino)propyl]sulfonyl]phenyl)-4-(1,2-dimethyl-1H-imidazol-5-yl)pyrimidin-2-amine
-
-
N-(4-[[3-(dimethylamino)propyl]sulfonyl]phenyl)-4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]pyrimidin-2-amine
-
-
N-(5-nitro-1H-indazol-3-yl)-2-phenylacetamide
-
-
N-(6-amino-pyrimidin-4-yl)-sulfanilic acid amide
-
-
N-1-dimethyl-8-([1-[(4-methylpiperazin-1-yl)carbonyl]piperidin-4-yl]amino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
N-1-dimethyl-8-[(1-methylpiperidin-4-yl)amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
N-1-dimethyl-8-[[1-(methylsulfonyl)piperidin-4-yl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
N-1-dimethyl-8-[[1-(phenylcarbonyl)piperidin-4-yl]amino]-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
N-benzyl-8-(cyclopentylamino)-N-hydroxy-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
N-cyclohexyl-8-(cyclopentylamino)-N-hydroxy-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
-
-
N-methyl-4-[[(2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]amino]benzenesulfonamide
-
-
N-methyl-[4-[2-(7-oxo-6,7-dihydro-8H-[1,3]thiazolo[5,4-e]indol-8-ylidene)hydrazino]phenyl]methanesulfonamide
-
-
N-[(3R)-1-[4-[(5-fluoro-6,8-dimethyl-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-yl)amino]phenyl]pyrrolidin-3-yl]acetamide
-
-
N-[(9bR)-5-oxo-2,3,5,9b-tetrahydro-1H-pyrrolo[2,1-alpha]isoindol-9-yl]-N'-pyridin-2-yl urea
-
-
N-[(9bR)-5-oxo-2,3,5,9b-tetrahydro-1H-pyrrolo[2,1-alpha]isoindol-9-yl]-N'-{5-[(2S)-pyrrolidin-2-yl]-1H-pyrazol-3-yl urea
-
-
N-[2-(1-aminohydrazino)ethyl]-4-[[4-(1,2-dimethyl-1H-imidazol-5-yl)pyrimidin-2-yl]amino]benzenesulfonamide
-
-
N-[2-(dimethylamino)ethyl]-4-[(4-imidazo[1,2-b]pyridazin-3-ylpyrimidin-2-yl)amino]benzenesulfonamide
-
-
N-[4-(4-[[(diethylamino)acetyl]sulfonyl]piperazin-1-yl)phenyl]-6,8-dimethyl-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-amine
-
-
N-[4-(4-[[(dimethylamino)acetyl]sulfonyl]piperazin-1-yl)phenyl]-6,8-dimethyl-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-amine
-
-
N-[4-(4-[[2-(dimethylamino)ethyl]sulfonyl]piperazin-1-yl)phenyl]-6,8-dimethyl-5,6-dihydroimidazo[1',5':1,2]pyrido[3,4-d]pyrimidin-2-amine
-
-
N-[4-(benzylsulfonyl)phenyl]-4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]pyrimidin-2-amine
-
-
N-[4-[(2-methoxyethyl)sulfonyl]phenyl]-4-[2-methyl-1-(1-methylethyl)-1H-imidazol-5-yl]pyrimidin-2-amine
-
-
N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(3-fluorophenyl)acetamide
-
-
N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(3-methylphenyl)acetamide
-
-
N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(4-fluorophenyl)acetamide
-
-
N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(4-hydroxyphenyl)acetamide
-
-
N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(4-methylphenyl)acetamide
-
-
N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(4-piperidin-1-ylphenyl)acetamide
-
-
N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-(4-pyridin-4-ylphenyl)acetamide
-
-
N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-naphthalen-1-ylacetamide
-
-
N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-naphthalen-2-ylacetamide
-
-
N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-phenylacetamide
-
-
N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-[4-(methylsulfanyl)phenyl]acetamide
-
-
N-[5-(1,1-dioxidoisothiazolidin-2-yl)-1H-indazol-3-yl]-2-[4-(methylsulfonyl)phenyl]acetamide
-
-
N-[5-(2,5-dioxoimidazolidin-1-yl)-1H-indazol-3-yl]-2-phenylacetamide
-
-
N-[5-(2-oxopiperidin-1-yl)-1H-indazol-3-yl]-2-phenylacetamide
-
-
N-[5-(2-oxopyrrolidin-1-yl)-1H-indazol-3-yl]-2-phenylacetamide
-
-
N-[5-(dibutylamino)-1H-indazol-3-yl]-2-phenylacetamide
-
-
N-[5-(diethylamino)-1H-indazol-3-yl]-2-phenylacetamide
-
-
N-[5-(dipropylamino)-1H-indazol-3-yl]-2-phenylacetamide
-
-
N-[5-(ethylamino)-1H-indazol-3-yl]-2-phenylacetamide
-
-
N2-(3-bromophenyl)-6-(cyclohexylmethoxy)-5-nitrosopyrimidine-2,4-diamine
-
-
N2-(3-bromophenyl)-6-(cyclohexylmethoxy)pyrimidine-2,4-diamine
-
-
N4-(6-aminopyrimidin-4-yl)-sulfanilamide
-
competitive inhibitor
NU-2058
-
-
NU-6027
-
-
NU6102
-
highly potent and selective ATP-competitive inhibitor of CDK2
Olomoucine
olomoucine II
-
-
p15Ink4b
-
INK4 protein
-
p16Ink4a
-
p18
-
wild-type and D76A mutant human INK4 protein, the mutant is only slightly inhibitory, p18 competes with IkappaBalpha for binding sites on CDK4, structure analysis
-
p18Ink4c
-
INK4 protein
-
p19Ink4d
-
INK4 protein
-
p21 protein
-
i.e. Cip1 or Waf1, a Cdk-inhibitor
-
p21CIP
-
as recombinant GST-tagged protein
-
p21Cip1
-
inhibits phosphorylation of tumor suppressor Rb
-
p21Clp1
-
forms a ternary complex with and is negatively regulated by p21Cip1, but not by its truncated fragment p21Cip1-D3
-
p21v1
-
endogenous CDK inhibitor
-
p21v2
-
endogenous CDK inhibitor
-
p21WAF1/CIP1
-
specific Cdk inhibitor, efficiently prevents etoposide-induced apoptotic cell death
-
P276-00
-
-
p27Kip1
-
p27Kip1 cyclin-dependent-kinase inhibitor
-
-
-
palbociclib
-
-
-
PD-0332991
-
-
-
PD183812
-
-
PHA-848125
-
-
PKF049-365
-
-
pRb peptide
-
866SNPPKPLKKLRFDIE880
-
progesterone
-
-
protopanaxatriol
-
noncompetitive inhibition
purvalanol
purvalanol A
-
-
purvalanol B
-
specific inhibitor of CDK1, 2, 5, and 7
pyrazolopyridazine
-
-
quercetin
-
a less potent flavonoid inhibitor of CDK6, CDK5, and CDK1
R547
-
-
RBG-286147
-
-
RO-3306
-
-
-
roscovitine
RXL motif-containing peptide
-
addition of this peptide significantly reduces substrate phosphorylation by cyclin E-CDK2 and cyclin D2-CDK6
-
SCH-727965
-
-
-
shRNA
-
cdk5 shRNA is able to efficiently inhibit the expression of endogenous cdk5
-
simvastatin
-
inhibition of CDK2
siRNA
-
SNS-032
staurosporine
SU-9516
-
-
SU9516
TAACS
-
; five amino-acid peptide inhibitor that is directed toward a noncatalytic binding pocket and which disrupts the cdk2/cyklin E complex
TAALD
-
five amino-acid peptide inhibitor that is directed toward a noncatalytic binding pocket and which disrupts the cdk2/cyklin E complex
TAALE
-
five amino-acid peptide inhibitor that is directed toward a noncatalytic binding pocket and which disrupts the cdk2/cyklin E complex
TAALS
-
disrupts the cdk2/cyclin E complex
THZ-1
-
-
-
tranilast
-
inhibition of CDK2 and CDK4
tumour suppressor p16INK4a
-
-
-
UCN-01
-
-
variolin B
-
-
Wee1
-
Cdk1 inhibitor
-
[(2R)-1-[[4-(1,3-benzothiazol-2-yl)thiophen-2-yl]sulfonyl]pyrrolidin-2-yl]methanol
-
poor inhibition of cdk2/cyclin E
[8-(cyclopentylamino)-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazolin-3-yl](4-methylpiperazin-1-yl)methanone
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additional information
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ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
Cdc25A
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CDK-activating kinase
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the CDK-activating kinase (having three subunits, CDK7, cyclin H, and MAT1) plays a critical role in regulating cell cycle by mediating the activating phosphorylation of CDK1, CDK2, CDK4, and CDK6
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Cks2
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Cks 2 proteins activates Cdk2
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cyclin
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dependent on, forms complexes with cyclin A
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cyclin A
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cyclin B
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cyclin D1
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cyclin D2
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cyclin D3
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cyclin E
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cyclin H
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activates Cdk7
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cyclin I
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cyclin T
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CDK9 activating partner cyclin T1
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cyclin T1
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activates Cdk9
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dynein light chain 1
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interacts with cdk2 and enhances Cdk2 kinase activity in vivo, dynein light chain 1 accelerates the G1-S transition by enhancing the activity of Cdk2
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E2F1
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etoposide
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activity of Cdk2 selectively increases after 6-9 h and then continues to increase over the 24 h time course of etopside treatment
p34SEI-1
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i.e. TRIP-Br1, the protein binds directly to CDK4 and activates it at lower concentrations, but inhibits the enzyme at higher concentrations, p34SEI-1 has regulatory function, the binding is not affected by INK4 proteins p16 and p18, complex formation of CDK4, cyclin D2, p16, and p34SEI-1, p34SEI-1 has a LexA-mediated transactivation activity, determination of functional sequence units/fragments in the protein, overview
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p58
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regulatory subunit of CDK11
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progestin
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Protein phosphatase 2A
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PP2A, enhances CDK8 kinase activity in vitro for the RNA polymerase II carboxy-terminal domain but not for histone H3. PP2A enhancement of CDK8 is independent of RV-cyclin expression and likely plays a role in the normal regulation of CDK8
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RV-cyclin
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retroviral cyclin from Walleye dermal sarcoma virus, enhances CDK8 kinase activity in vitro for RNA polymerase II carboxy-terminal domain and histone H3. It is specific for cdk8, no activation of Cdk7 or Cdk9. The majority of the RV-cyclin structure is comprised of a cyclin box fold, which is responsible for binding to cyclin-dependent kinase-8. Two-hybrid interaction analysis in Saccharomyces cerevisiae strain Y190
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additional information
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KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00522 - 0.017
ATP
0.00285
PKTPKKAKKL
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pH 7.5, 37C
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.28
ATP
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in 20 mM MOPS (pH 7.5), at 30C
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00015
(5Z)-2-(benzylamino)-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
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0.00031
(5Z)-2-(butylamino)-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
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0.00027
(5Z)-2-(cyclopropylamino)-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
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-
0.002
(5Z)-2-(methoxyamino)-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
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Ki above 0.002 mM
0.00027
(5Z)-2-(methylamino)-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
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0.002
(5Z)-2-(phenylamino)-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
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Ki above 0.002 mM
0.00104
(5Z)-2-[(2,6-dichlorobenzyl)amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
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0.000038
(5Z)-2-[(2-bromobenzyl)amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
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0.000052
(5Z)-2-[(2-chlorobenzyl)amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
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0.000086
(5Z)-2-[(2-methoxybenzyl)amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
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0.00006
(5Z)-2-[(2-phenylethyl)amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
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0.00028
(5Z)-2-[(2-pyridin-2-ylethyl)amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
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0.00039
(5Z)-2-[(3-hydroxy-2-phenylpropyl)amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
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0.00024
(5Z)-2-[(3-phenylpropyl)amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
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0.00031
(5Z)-2-[(pyridin-2-ylmethyl)amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
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0.002
(5Z)-2-[methyl(thiophen-2-ylmethyl)amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
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Ki above 0.002 mM
0.00023
(5Z)-2-[[(1R)-1-benzyl-2-hydroxyethyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
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0.00035
(5Z)-2-[[(1R)-2-hydroxy-1-phenylethyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
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0.002
(5Z)-2-[[(1R)-2-methoxy-1-phenylethyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
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Ki above 0.002 mM
0.000023
(5Z)-2-[[(1R,2S)-2-phenylcyclopropyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
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0.002
(5Z)-2-[[(1S)-1-benzyl-2-hydroxyethyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
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0.00058
(5Z)-2-[[(1S)-2-hydroxy-1-phenylethyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
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0.000046
(5Z)-2-[[2-(2-chlorophenyl)ethyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
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0.000087
(5Z)-2-[[2-(2-ethoxyphenyl)ethyl]amino]-5-(quinolin-6-ylmethylidene)-1,3-thiazol-4(5H)-one
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