Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 2.7.11.22 extracted from

  • Marchetti, F.; Sayle, K.L.; Bentley, J.; Clegg, W.; Curtin, N.J.; Endicott, J.A.; Golding, B.T.; Griffin, R.J.; Haggerty, K.; Harrington, R.W.; Mesguiche, V.; Newell, D.R.; Noble, M.E.; Parsons, R.J.; Pratt, D.J.; Wang, L.Z.; Hardcastle, I.R.
    Structure-based design of 2-arylamino-4-cyclohexylmethoxy-5-nitroso-6-aminopyrimidine inhibitors of cyclin-dependent kinase 2 (2007), Org. Biomol. Chem., 5, 1577-1585.
    View publication on PubMed
Search for more literature for 2.7.11.22

Inhibitors

Inhibitors Comment Organism Structure
(3-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]phenyl)acetonitrile
-
 Homo sapiens
(3-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]phenyl)methanol
-
 Homo sapiens
(3-[[4-amino-6-(cyclohexylmethoxy)pyrimidin-2-yl]amino]phenyl)acetonitrile 41% inhibition at 0.01 mM Homo sapiens
(4-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]phenyl)acetonitrile
-
 Homo sapiens
(4-[[4-amino-6-(cyclohexylmethoxy)pyrimidin-2-yl]amino]phenyl)acetonitrile
-
 Homo sapiens
4-(6-amino-4-cyclohexylmethoxy-5-nitrosopyrimidin-2-ylamino)-benzenesulfonamide
-
 Homo sapiens
4-(6-amino-4-cyclohexylmethoxy-5-nitrosopyrimidin-2-ylamino)-N-(2,3-dihydroxypropyl)-benzenesulfonamide
-
 Homo sapiens
4-(6-amino-4-cyclohexylmethoxy-5-nitrosopyrimidin-2-ylamino)-N-(2-hydroxyethyl)benzenesulfonamide
-
 Homo sapiens
4-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]-N,N-diethylbenzamide
-
 Homo sapiens
4-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]-N,N-diethylbenzenesulfonamide
-
 Homo sapiens
4-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]-N,N-dimethylbenzamide
-
 Homo sapiens
4-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]-N-(2-hydroxypropyl)benzenesulfonamide
-
 Homo sapiens
4-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]-N-(tetrahydrofuran-2-ylmethyl)benzenesulfonamide
-
 Homo sapiens
4-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]-N-1,3-thiazol-2-ylbenzenesulfonamide
-
 Homo sapiens
4-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]phenol
-
 Homo sapiens
4-[[4-amino-6-(cyclohexylmethoxy)pyrimidin-2-yl]amino]-N,N-diethylbenzamide 29% inhibition at 0.001 mM Homo sapiens
4-[[4-amino-6-(cyclohexylmethoxy)pyrimidin-2-yl]amino]-N,N-diethylbenzenesulfonamide 33% inhibition at 0.01 mM Homo sapiens
4-[[4-amino-6-(cyclohexylmethoxy)pyrimidin-2-yl]amino]-N,N-dimethylbenzamide 49% inhibition at 0.1 mM Homo sapiens
4-[[4-amino-6-(cyclohexylmethoxy)pyrimidin-2-yl]amino]benzamide
-
 Homo sapiens
6-(cyclohexylmethoxy)-N2-(3-methoxyphenyl)-5-nitrosopyrimidine-2,4-diamine
-
 Homo sapiens
6-(cyclohexylmethoxy)-N2-(4-methoxyphenyl)-5-nitrosopyrimidine-2,4-diamine
-
 Homo sapiens
6-(cyclohexylmethoxy)-N2-[3-(methylsulfanyl)phenyl]-5-nitrosopyrimidine-2,4-diamine
-
 Homo sapiens
6-(cyclohexylmethoxy)-N2-[3-(methylsulfanyl)phenyl]pyrimidine-2,4-diamine
-
 Homo sapiens
6-(cyclohexylmethoxy)-N2-[4-(methylsulfanyl)phenyl]-5-nitrosopyrimidine-2,4-diamine
-
 Homo sapiens
N2-(3-bromophenyl)-6-(cyclohexylmethoxy)-5-nitrosopyrimidine-2,4-diamine
-
 Homo sapiens
N2-(3-bromophenyl)-6-(cyclohexylmethoxy)pyrimidine-2,4-diamine
-
 Homo sapiens
NU2058
-
 Homo sapiens
NU6027
-
 Homo sapiens
NU6102 highly potent and selective ATP-competitive inhibitor of CDK2 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + histone H1
-
 Homo sapiens ADP + phosphorylated histone H1
-
 ?

Synonyms

Synonyms Comment Organism
CDK2
-
 Homo sapiens
cyclin-dependent kinase 2
-
 Homo sapiens

Cofactor

Cofactor Comment Organism Structure
cyclin A cofactor of CDK2 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000006
-
 NU6102
-
 Homo sapiens
0.0013
-
 NU6027
-
 Homo sapiens
0.012
-
 NU2058
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000007
-
-
 Homo sapiens 4-(6-amino-4-cyclohexylmethoxy-5-nitrosopyrimidin-2-ylamino)-N-(2-hydroxyethyl)benzenesulfonamide
0.0000008
-
-
 Homo sapiens 4-(6-amino-4-cyclohexylmethoxy-5-nitrosopyrimidin-2-ylamino)-N-(2,3-dihydroxypropyl)-benzenesulfonamide
0.000001
-
-
 Homo sapiens 4-(6-amino-4-cyclohexylmethoxy-5-nitrosopyrimidin-2-ylamino)-benzenesulfonamide
0.0000013
-
 with isozyme CDK2 Homo sapiens 4-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]-N-(2-hydroxypropyl)benzenesulfonamide
0.0000022
-
-
 Homo sapiens NU6027
0.0000081
-
 with isozyme CDK2 Homo sapiens 4-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]-N-(tetrahydrofuran-2-ylmethyl)benzenesulfonamide
0.000016
-
 with isozyme CDK2 Homo sapiens 4-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]phenol
0.000019
-
 with isozyme CDK2 Homo sapiens 4-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]-N-1,3-thiazol-2-ylbenzenesulfonamide
0.000034
-
-
 Homo sapiens 4-(6-amino-4-cyclohexylmethoxy-5-nitrosopyrimidin-2-ylamino)-N-(2,3-dihydroxypropyl)-benzenesulfonamide
0.000045
-
 with isozyme CDK2 Homo sapiens (3-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]phenyl)methanol
0.000064
-
 with isozyme CDK2 Homo sapiens (4-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]phenyl)acetonitrile
0.00008
-
 with isozyme CDK2 Homo sapiens 4-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]-N,N-dimethylbenzamide
0.000086
-
 with isozyme CDK2 Homo sapiens 4-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]-N,N-diethylbenzenesulfonamide
0.00012
-
 with isozyme CDK2 Homo sapiens 6-(cyclohexylmethoxy)-N2-[4-(methylsulfanyl)phenyl]-5-nitrosopyrimidine-2,4-diamine
0.0002
-
 with isozyme CDK2 Homo sapiens 4-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]-N,N-diethylbenzamide
0.000215
-
-
 Homo sapiens 6-(cyclohexylmethoxy)-N2-(4-methoxyphenyl)-5-nitrosopyrimidine-2,4-diamine
0.00034
-
 with isozyme CDK2 Homo sapiens 6-(cyclohexylmethoxy)-N2-(3-methoxyphenyl)-5-nitrosopyrimidine-2,4-diamine
0.0004
-
 with isozyme CDK2 Homo sapiens 6-(cyclohexylmethoxy)-N2-[3-(methylsulfanyl)phenyl]-5-nitrosopyrimidine-2,4-diamine
0.0005
-
 with isozyme CDK2 Homo sapiens N2-(3-bromophenyl)-6-(cyclohexylmethoxy)-5-nitrosopyrimidine-2,4-diamine
0.024
-
 with isozyme CDK2 Homo sapiens (4-[[4-amino-6-(cyclohexylmethoxy)pyrimidin-2-yl]amino]phenyl)acetonitrile
0.026
-
 with isozyme CDK2 Homo sapiens N2-(3-bromophenyl)-6-(cyclohexylmethoxy)pyrimidine-2,4-diamine
0.033
-
 with isozyme CDK2 Homo sapiens (3-[[4-amino-6-(cyclohexylmethoxy)-5-nitrosopyrimidin-2-yl]amino]phenyl)acetonitrile
0.059
-
 with isozyme CDK2 Homo sapiens 4-[[4-amino-6-(cyclohexylmethoxy)pyrimidin-2-yl]amino]benzamide
0.06
-
 with isozyme CDK2 Homo sapiens 6-(cyclohexylmethoxy)-N2-[3-(methylsulfanyl)phenyl]pyrimidine-2,4-diamine