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 | 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 (Comment) | Organism |
---|---|
cdk5 in complex with inhibitor 4a, X-ray diffraction structure determination and analysis at 1.90 A resolution | Homo sapiens |
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 | Comment | Organism | Structure |
---|---|---|---|
Mn2+ | required | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | Q00535 | - |
- |
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 | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + PKTPKKAKKL | GST-tagged recombinant peptide substrate | Homo sapiens | ADP + PKpTPKKAKKL | - |
? |
Synonyms | Comment | Organism |
---|---|---|
CDK2 | - |
Homo sapiens |
Cdk5 | - |
Homo sapiens |
cyclin-dependent kinase 2 | - |
Homo sapiens |
cyclin-dependent kinase 5 | - |
Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.35 | - |
assay at | Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ATP | - |
Homo sapiens |
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 | Comment | Organism |
---|---|---|
evolution | cyclin-dependent kinase 5 belongs to a family of proline-directed serine/threonine kinases | Homo sapiens |