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Literature summary for 2.7.11.22 extracted from

  • Ngompaza-Diarra, J.; Bettayeb, K.; Gresh, N.; Meijer, L.; Oumata, N.
    Synthesis and biological evaluation of selective and potent cyclin-dependent kinase inhibitors (2012), Eur. J. Med. Chem., 56, 210-216.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expression of CDK2/cyclin A, CDK7/cyclin H, and CDK9/cyclin T in baculovirus-infected insect cells, and expression of CDK5/p25 in Escherichia coli Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(1S,2R,3R)-3-[[9-iso-propyl-6-[[4-(2-pyridyl)phenyl]methylamino]purin-2-yl]amino]cyclohexane-1,2-diol
-
Asteroidea
(1S,2R,3R)-3-[[9-iso-propyl-6-[[4-(2-pyridyl)phenyl]methylamino]purin-2-yl]amino]cyclohexane-1,2-diol
-
Homo sapiens
(2R)-2-hydroxy-3-[[9-(propan-2-yl)-6-[[4-(pyridin-2-yl)benzyl]amino]-9H-purin-2-yl]amino]propyl L-valinate
-
Asteroidea
(2R)-2-hydroxy-3-[[9-(propan-2-yl)-6-[[4-(pyridin-2-yl)benzyl]amino]-9H-purin-2-yl]amino]propyl L-valinate
-
Homo sapiens
(2R)-3-[[9-iso-propyl-6-[[4-(2-pyridyl)phenyl]methylamino]purin-2-yl]amino]propane-1,2-diol
-
Asteroidea
(2R)-3-[[9-iso-propyl-6-[[4-(2-pyridyl)phenyl]methylamino]purin-2-yl]amino]propane-1,2-diol
-
Homo sapiens
(2S)-4-[[9-iso-propyl-6-[[4-(2-pyridyl)phenyl]methylamino]purin-2-yl]amino]butane-1,2-diol
-
Asteroidea
(2S)-4-[[9-iso-propyl-6-[[4-(2-pyridyl)phenyl]methylamino]purin-2-yl]amino]butane-1,2-diol
-
Homo sapiens
(3R,5S)-5-(hydroxymethyl)-1-[9-iso-propyl-6-[[4-(2-pyridyl)phenyl]methylamino]- purin-2-yl]pyrrolidin-3-ol
-
Homo sapiens
(3R,5S)-5-(hydroxymethyl)-1-[9-iso-propyl-6-[[4-(2-pyridyl)phenyl]methylamino]-purin-2-yl]pyrrolidin-3-ol
-
Asteroidea
(R)-roscovitine
-
Asteroidea
(R)-roscovitine
-
Homo sapiens
flavopiridol
-
Asteroidea
flavopiridol
-
Homo sapiens
additional information inhibitor synthesis and screening, docking study, overview Asteroidea
additional information inhibitor synthesis and screening, docking study, overview Homo sapiens

Organism

Organism UniProt Comment Textmining
Asteroidea
-
-
-
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
native CDK1/cyclin B from oocyte by affinity chromatography Asteroidea

Source Tissue

Source Tissue Comment Organism Textmining
neuroblastoma cell
-
Homo sapiens
-
oocyte
-
Asteroidea
-
SH-SY5Y cell
-
Homo sapiens
-

Synonyms

Synonyms Comment Organism
CDK
-
Homo sapiens
CDK
-
Asteroidea
Cdk1
-
Asteroidea
CDK2
-
Homo sapiens
Cdk5
-
Homo sapiens
cdk7
-
Homo sapiens
CDK9
-
Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
Homo sapiens
ATP
-
Asteroidea

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00015
-
CDK9/cyclin T, pH 7.5, 30°C Homo sapiens (2R)-3-[[9-iso-propyl-6-[[4-(2-pyridyl)phenyl]methylamino]purin-2-yl]amino]propane-1,2-diol
0.00018
-
CDK5/p25, pH 7.5, 30°C Homo sapiens (2R)-2-hydroxy-3-[[9-(propan-2-yl)-6-[[4-(pyridin-2-yl)benzyl]amino]-9H-purin-2-yl]amino]propyl L-valinate
0.00018
-
CDK9/cyclin T, pH 7.5, 30°C Homo sapiens (2R)-2-hydroxy-3-[[9-(propan-2-yl)-6-[[4-(pyridin-2-yl)benzyl]amino]-9H-purin-2-yl]amino]propyl L-valinate
0.00019
-
CDK5/p25, pH 7.5, 30°C Homo sapiens (2R)-3-[[9-iso-propyl-6-[[4-(2-pyridyl)phenyl]methylamino]purin-2-yl]amino]propane-1,2-diol
0.00021
-
CDK2/cyclin A, pH 7.5, 30°C Homo sapiens (R)-roscovitine
0.00023
-
CDK9/cyclin T, pH 7.5, 30°C Homo sapiens (R)-roscovitine
0.00027
-
CDK5/p25, pH 7.5, 30°C Homo sapiens (1S,2R,3R)-3-[[9-iso-propyl-6-[[4-(2-pyridyl)phenyl]methylamino]purin-2-yl]amino]cyclohexane-1,2-diol
0.00028
-
CDK5/p25, pH 7.5, 30°C Homo sapiens (R)-roscovitine
0.00033
-
CDK1/cyclin B, pH 7.5, 30°C Asteroidea (R)-roscovitine
0.00037
-
CDK1/cyclin B, pH 7.5, 30°C Asteroidea (2S)-4-[[9-iso-propyl-6-[[4-(2-pyridyl)phenyl]methylamino]purin-2-yl]amino]butane-1,2-diol
0.00037
-
CDK9/cyclin T, pH 7.5, 30°C Homo sapiens (1S,2R,3R)-3-[[9-iso-propyl-6-[[4-(2-pyridyl)phenyl]methylamino]purin-2-yl]amino]cyclohexane-1,2-diol
0.00045
-
CDK1/cyclin B, pH 7.5, 30°C Asteroidea (3R,5S)-5-(hydroxymethyl)-1-[9-iso-propyl-6-[[4-(2-pyridyl)phenyl]methylamino]-purin-2-yl]pyrrolidin-3-ol
0.00045
-
CDK9/cyclin T, pH 7.5, 30°C Homo sapiens (3R,5S)-5-(hydroxymethyl)-1-[9-iso-propyl-6-[[4-(2-pyridyl)phenyl]methylamino]- purin-2-yl]pyrrolidin-3-ol
0.00048
-
CDK2/cyclin A, pH 7.5, 30°C Homo sapiens (2R)-3-[[9-iso-propyl-6-[[4-(2-pyridyl)phenyl]methylamino]purin-2-yl]amino]propane-1,2-diol
0.0006
-
CDK1/cyclin B, pH 7.5, 30°C Asteroidea (2R)-3-[[9-iso-propyl-6-[[4-(2-pyridyl)phenyl]methylamino]purin-2-yl]amino]propane-1,2-diol
0.00061
-
CDK2/cyclin A, pH 7.5, 30°C Homo sapiens (1S,2R,3R)-3-[[9-iso-propyl-6-[[4-(2-pyridyl)phenyl]methylamino]purin-2-yl]amino]cyclohexane-1,2-diol
0.00061
-
CDK5/p25, pH 7.5, 30°C Homo sapiens (3R,5S)-5-(hydroxymethyl)-1-[9-iso-propyl-6-[[4-(2-pyridyl)phenyl]methylamino]- purin-2-yl]pyrrolidin-3-ol
0.00065
-
CDK2/cyclin A, pH 7.5, 30°C Homo sapiens (3R,5S)-5-(hydroxymethyl)-1-[9-iso-propyl-6-[[4-(2-pyridyl)phenyl]methylamino]- purin-2-yl]pyrrolidin-3-ol
0.00082
-
CDK5/p25, pH 7.5, 30°C Homo sapiens (2S)-4-[[9-iso-propyl-6-[[4-(2-pyridyl)phenyl]methylamino]purin-2-yl]amino]butane-1,2-diol
0.00087
-
CDK1/cyclin B, pH 7.5, 30°C Asteroidea (1S,2R,3R)-3-[[9-iso-propyl-6-[[4-(2-pyridyl)phenyl]methylamino]purin-2-yl]amino]cyclohexane-1,2-diol
0.00087
-
CDK2/cyclin A, pH 7.5, 30°C Homo sapiens (2R)-2-hydroxy-3-[[9-(propan-2-yl)-6-[[4-(pyridin-2-yl)benzyl]amino]-9H-purin-2-yl]amino]propyl L-valinate
0.00098
-
CDK2/cyclin A, pH 7.5, 30°C Homo sapiens (2S)-4-[[9-iso-propyl-6-[[4-(2-pyridyl)phenyl]methylamino]purin-2-yl]amino]butane-1,2-diol
0.00101
-
CDK9/cyclin T, pH 7.5, 30°C Homo sapiens (2S)-4-[[9-iso-propyl-6-[[4-(2-pyridyl)phenyl]methylamino]purin-2-yl]amino]butane-1,2-diol
0.0014
-
CDK1/cyclin B, pH 7.5, 30°C Asteroidea (2R)-2-hydroxy-3-[[9-(propan-2-yl)-6-[[4-(pyridin-2-yl)benzyl]amino]-9H-purin-2-yl]amino]propyl L-valinate