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Literature summary for 2.7.11.22 extracted from

  • Malmstroem, J.; Viklund, J.; Slivo, C.; Costa, A.; Maudet, M.; Sandelin, C.; Hiller, G.; Olsson, L.L.; Aagaard, A.; Geschwindner, S.; Xue, Y.; Vasaenge, M.
    Synthesis and structure-activity relationship of 4-(1,3-benzothiazol-2-yl)-thiophene-2-sulfonamides as cyclin-dependent kinase 5 (cdk5)/p25 inhibitors (2012), Bioorg. Med. Chem. Lett., 22, 5919-5923.
    View publication on PubMed
Search for more literature for 2.7.11.22

Activating Compound

Activating Compound Comment Organism Structure
cyclin E required by cdk2 Homo sapiens
additional information the anomalous cdk5/p25 complex is active Homo sapiens
p35 p35 or p39 are required by cdk5 Homo sapiens
p39 p35 or p39 are required by cdk5 Homo sapiens

Application

Application Comment Organism
pharmacology inhibition of the anomalous cdk5/p25 complex is a viable target for treating Alzheimer disease by preventing hyperphosphorylation of tau and neurofibrillary tangle formation Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
cdk5 in complex with inhibitor 4a, X-ray diffraction structure determination and analysis at 1.90 A resolution Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(R)-roscovitine
-
 Homo sapiens
2-[(3,4-dimethoxyphenyl)amino]-8-ethylpyrido[2,3-d]pyrimidin-7(8H)-one
-
 Homo sapiens
4-(1,3-benzothiazol-2-yl)-N-(1,3-thiazol-2-yl)thiophene-2-sulfonamide
-
 Homo sapiens
4-(1,3-benzothiazol-2-yl)-N-(2-fluoroethyl)thiophene-2-sulfonamide poor inhibition of cdk5/p25 Homo sapiens
4-(1,3-benzothiazol-2-yl)-N-(4,5-dimethyl-1,3-thiazol-2-yl)thiophene-2-sulfonamide
-
 Homo sapiens
4-(1,3-benzothiazol-2-yl)-N-(4-methylpyridin-2-yl)thiophene-2-sulfonamide
-
 Homo sapiens
4-(1,3-benzothiazol-2-yl)-N-(5-hydroxypyridin-2-yl)thiophene-2-sulfonamide
-
 Homo sapiens
4-(1,3-benzothiazol-2-yl)-N-(pyridin-2-ylmethyl)thiophene-2-sulfonamide
-
 Homo sapiens
4-(1,3-benzothiazol-2-yl)-N-hydroxythiophene-2-sulfonamide
-
 Homo sapiens
4-(1,3-benzothiazol-2-yl)-N-[5-(morpholin-4-yl)pyridin-2-yl]thiophene-2-sulfonamide
-
 Homo sapiens
4-(1,3-benzothiazol-2-yl)thiophene-2-sulfonamide binds to Ile10 and Asp86 in the active site of cdk2 Homo sapiens
4-(6-acetyl-1,3-benzothiazol-2-yl)thiophene-2-sulfonamide poor inhibition of cdk2/cyclin E Homo sapiens
4-(6-chloro-1,3-benzothiazol-2-yl)thiophene-2-sulfonamide
-
 Homo sapiens
4-(6-fluoro-1,3-benzothiazol-2-yl)thiophene-2-sulfonamide
-
 Homo sapiens
4-(6-methyl-1,3-benzothiazol-2-yl)thiophene-2-sulfonamide
-
 Homo sapiens
4-(6-nitro-1,3-benzothiazol-2-yl)thiophene-2-sulfonamide
-
 Homo sapiens
4-chloro-N-(cis-3-[4-[(naphthalen-1-ylacetyl)amino]-1H-imidazol-1-yl]cyclobutyl)benzamide
-
 Homo sapiens
4-[7-(4-chloro-3-fluorophenyl)-1,3-benzothiazol-2-yl]thiophene-2-sulfonamide
-
 Homo sapiens
4-[7-(4-fluorophenyl)-1,3-benzothiazol-2-yl]thiophene-2-sulfonamide poor inhibition of cdk2/cyclin E Homo sapiens
aloisine-A
-
 Homo sapiens
ethyl [2-([[4-(1,3-benzothiazol-2-yl)thiophen-2-yl]sulfonyl]amino)-1,3-thiazol-4-yl]acetate
-
 Homo sapiens
indirubin-3'-oxime
-
 Homo sapiens
additional information inhibitor synthesis and evaluation of inhibitory potencies with cdk2/cyclin E and cdk5/p25, overview Homo sapiens
[(2R)-1-[[4-(1,3-benzothiazol-2-yl)thiophen-2-yl]sulfonyl]pyrrolidin-2-yl]methanol poor inhibition of cdk2/cyclin E Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Mn2+ required Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q00535
-
-

Source Tissue

Source Tissue Comment Organism Textmining
commercial preparation recombinant enzymes Homo sapiens
-
neuron Cdk5 is mainly active in postmitotic neurons due to the selective neuronal expression of its non-cyclin activators p35 and p39 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + PKTPKKAKKL GST-tagged recombinant peptide substrate Homo sapiens ADP + PKpTPKKAKKL
-
 ?

Synonyms

Synonyms Comment Organism
CDK2
-
 Homo sapiens
Cdk5
-
 Homo sapiens
cyclin-dependent kinase 2
-
 Homo sapiens
cyclin-dependent kinase 5
-
 Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.35
-
 assay at Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000006
-
 pH 7.35, temperature not specified in the publication, inhibition of cdk5/p25 Homo sapiens 4-chloro-N-(cis-3-[4-[(naphthalen-1-ylacetyl)amino]-1H-imidazol-1-yl]cyclobutyl)benzamide
0.00003
-
 pH 7.35, temperature not specified in the publication, inhibition of cdk5/p25 Homo sapiens 2-[(3,4-dimethoxyphenyl)amino]-8-ethylpyrido[2,3-d]pyrimidin-7(8H)-one
0.000204
-
 pH 7.35, temperature not specified in the publication, inhibition of cdk2/cyclin E Homo sapiens 4-chloro-N-(cis-3-[4-[(naphthalen-1-ylacetyl)amino]-1H-imidazol-1-yl]cyclobutyl)benzamide
0.000226
-
 pH 7.35, temperature not specified in the publication, inhibition of cdk2/cyclin E Homo sapiens 4-(6-methyl-1,3-benzothiazol-2-yl)thiophene-2-sulfonamide
0.000331
-
 pH 7.35, temperature not specified in the publication, inhibition of cdk5/p25 Homo sapiens 4-(6-fluoro-1,3-benzothiazol-2-yl)thiophene-2-sulfonamide
0.000355
-
 pH 7.35, temperature not specified in the publication, inhibition of cdk5/p25 Homo sapiens 4-(6-chloro-1,3-benzothiazol-2-yl)thiophene-2-sulfonamide
0.000452
-
 pH 7.35, temperature not specified in the publication, inhibition of cdk2/cyclin E Homo sapiens 4-(6-nitro-1,3-benzothiazol-2-yl)thiophene-2-sulfonamide
0.000492
-
 pH 7.35, temperature not specified in the publication, inhibition of cdk2/cyclin E Homo sapiens 4-[7-(4-chloro-3-fluorophenyl)-1,3-benzothiazol-2-yl]thiophene-2-sulfonamide
0.00054
-
 pH 7.35, temperature not specified in the publication, inhibition of cdk2/cyclin E Homo sapiens 2-[(3,4-dimethoxyphenyl)amino]-8-ethylpyrido[2,3-d]pyrimidin-7(8H)-one
0.000551
-
 pH 7.35, temperature not specified in the publication, inhibition of cdk5/p25 Homo sapiens 4-(1,3-benzothiazol-2-yl)thiophene-2-sulfonamide
0.000672
-
 pH 7.35, temperature not specified in the publication, inhibition of cdk5/p25 Homo sapiens 4-[7-(4-chloro-3-fluorophenyl)-1,3-benzothiazol-2-yl]thiophene-2-sulfonamide
0.00072
-
 pH 7.35, temperature not specified in the publication, inhibition of cdk2/cyclin E Homo sapiens 4-(6-fluoro-1,3-benzothiazol-2-yl)thiophene-2-sulfonamide
0.00086
-
 pH 7.35, temperature not specified in the publication, inhibition of cdk2/cyclin E Homo sapiens 4-(6-chloro-1,3-benzothiazol-2-yl)thiophene-2-sulfonamide
0.00126
-
 pH 7.35, temperature not specified in the publication, inhibition of cdk5/p25 Homo sapiens 4-(6-methyl-1,3-benzothiazol-2-yl)thiophene-2-sulfonamide
0.00127
-
 pH 7.35, temperature not specified in the publication, inhibition of cdk5/p25 Homo sapiens 4-(6-nitro-1,3-benzothiazol-2-yl)thiophene-2-sulfonamide
0.001764
-
 pH 7.35, temperature not specified in the publication, inhibition of cdk5/p25 Homo sapiens 4-(1,3-benzothiazol-2-yl)-N-(1,3-thiazol-2-yl)thiophene-2-sulfonamide
0.0045
-
 pH 7.35, temperature not specified in the publication, inhibition of cdk2/cyclin E Homo sapiens 4-(1,3-benzothiazol-2-yl)thiophene-2-sulfonamide
0.00509
-
 pH 7.35, temperature not specified in the publication, inhibition of cdk5/p25 Homo sapiens ethyl [2-([[4-(1,3-benzothiazol-2-yl)thiophen-2-yl]sulfonyl]amino)-1,3-thiazol-4-yl]acetate
0.00547
-
 pH 7.35, temperature not specified in the publication, inhibition of cdk5/p25 Homo sapiens 4-(1,3-benzothiazol-2-yl)-N-(pyridin-2-ylmethyl)thiophene-2-sulfonamide
0.00548
-
 pH 7.35, temperature not specified in the publication, inhibition of cdk2/cyclin E Homo sapiens 4-(1,3-benzothiazol-2-yl)-N-(1,3-thiazol-2-yl)thiophene-2-sulfonamide
0.00631
-
 pH 7.35, temperature not specified in the publication, inhibition of cdk5/p25 Homo sapiens 4-(6-acetyl-1,3-benzothiazol-2-yl)thiophene-2-sulfonamide
0.00672
-
 pH 7.35, temperature not specified in the publication, inhibition of cdk2/cyclin E Homo sapiens 4-(1,3-benzothiazol-2-yl)-N-(pyridin-2-ylmethyl)thiophene-2-sulfonamide
0.00678
-
 pH 7.35, temperature not specified in the publication, inhibition of cdk5/p25 Homo sapiens 4-[7-(4-fluorophenyl)-1,3-benzothiazol-2-yl]thiophene-2-sulfonamide
0.00742
-
 pH 7.35, temperature not specified in the publication, inhibition of cdk5/p25 Homo sapiens 4-(1,3-benzothiazol-2-yl)-N-hydroxythiophene-2-sulfonamide
0.007704
-
 pH 7.35, temperature not specified in the publication, inhibition of cdk5/p25 Homo sapiens 4-(1,3-benzothiazol-2-yl)-N-[5-(morpholin-4-yl)pyridin-2-yl]thiophene-2-sulfonamide
0.00822
-
 pH 7.35, temperature not specified in the publication, inhibition of cdk5/p25 Homo sapiens 4-(1,3-benzothiazol-2-yl)-N-(4,5-dimethyl-1,3-thiazol-2-yl)thiophene-2-sulfonamide
0.008274
-
 pH 7.35, temperature not specified in the publication, inhibition of cdk5/p25 Homo sapiens 4-(1,3-benzothiazol-2-yl)-N-(4-methylpyridin-2-yl)thiophene-2-sulfonamide
0.00888
-
 pH 7.35, temperature not specified in the publication, inhibition of cdk5/p25 Homo sapiens [(2R)-1-[[4-(1,3-benzothiazol-2-yl)thiophen-2-yl]sulfonyl]pyrrolidin-2-yl]methanol
0.00994
-
 pH 7.35, temperature not specified in the publication, inhibition of cdk5/p25 Homo sapiens 4-(1,3-benzothiazol-2-yl)-N-(5-hydroxypyridin-2-yl)thiophene-2-sulfonamide

General Information

General Information Comment Organism
evolution cyclin-dependent kinase 5 belongs to a family of proline-directed serine/threonine kinases Homo sapiens