Application | Comment | Organism |
---|---|---|
drug development | Plk1 is considered an attractive anti-cancer drug target due to its ability to promote tumorigenesis | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(4E)-4-(hydroxyimino)-5-methyl-2-(propan-2-yl)cyclohexa-2,5-dien-1-one | i.e. poloxime, PXE | Homo sapiens | |
(4E)-5-methyl-4-{[(2-methylbenzoyl)oxy]imino}-2-(propan-2-yl)cyclohexa-2,5-dien-1-one | i.e. poloxin | Homo sapiens | |
2-methyl-5-(propan-2-yl)cyclohexa-2,5-diene-1,4-dione | i.e. thymoquinone | Homo sapiens | |
2-[(3-cyano-6-methoxyquinolin-2-yl)sulfanyl]-N-(2-methoxy-5-methylphenyl)acetamide | i.e. I2 | Homo sapiens | |
BI 2536 | a dihydropteridinone and a ATP-competitive Plk1 inhibitor | Homo sapiens | |
BI 6727 | a ATP-competitive Plk1 inhibitor | Homo sapiens | |
additional information | design and synthesis of series of small-molecule non-ATP-competitive Plk1 inhibitors targeting the substrate-binding pocket are designed through rational drug design, molecular docking. Some comound are selective against inhibitory selectivity against polo kinases Plk2 and Plk3. Growth inhibition activity with HeLa and MCF-7 cells | Homo sapiens | |
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-2-methylbenzamide | - |
Homo sapiens | |
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-2-nitrobenzamide | - |
Homo sapiens | |
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-chlorobenzylaniline | - |
Homo sapiens | |
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-methoxybenzamide | - |
Homo sapiens | |
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-methoxybenzylaniline | - |
Homo sapiens | |
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-methylbenzamide | - |
Homo sapiens | |
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-methylbenzylaniline | - |
Homo sapiens | |
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-nitrobenzamide | - |
Homo sapiens | |
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-nitrobenzylaniline | - |
Homo sapiens | |
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-acetamide | - |
Homo sapiens | |
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-benzamide | - |
Homo sapiens | |
N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-benzylaniline | - |
Homo sapiens | |
N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)-2-methylbenzamide | - |
Homo sapiens | |
N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)-2-nitrobenzamide | - |
Homo sapiens | |
N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)-4-methoxybenzamide | a highly selective inhibitor of Plk1, in vitro kinase inhibitory profile of 5i, overview | Homo sapiens | |
N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)-4-nitrobenzamide | - |
Homo sapiens | |
N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)acetamide | - |
Homo sapiens | |
N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)benzamide | - |
Homo sapiens | |
N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)benzylaniline | - |
Homo sapiens | |
N-[2-methoxy-5-({[(E)-2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonyl}methyl)phenyl]glycine | i.e. ON01910, exhibits little activity against Plk1 in vitro, effective in inhibiting the cell proliferation | Homo sapiens |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Mg2+ | required | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + a protein | Homo sapiens | - |
ADP + a phosphoprotein | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P53350 | - |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + a protein | - |
Homo sapiens | ADP + a phosphoprotein | - |
? | |
ATP + Cdc25C | - |
Homo sapiens | ADP + phosphorylated Cdc25C | - |
? |
Synonyms | Comment | Organism |
---|---|---|
Plk1 | - |
Homo sapiens |
Polo-like kinase 1 | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
30 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.5 | - |
assay at | Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ATP | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00000083 | - |
pH 7.5, 30°C | Homo sapiens | BI 2536 | |
0.00000087 | - |
pH 7.5, 30°C | Homo sapiens | BI 6727 | |
0.00068 | - |
pH 7.5, 30°C | Homo sapiens | N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)-4-methoxybenzamide | |
0.00093 | - |
pH 7.5, 30°C | Homo sapiens | N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-methoxybenzamide | |
0.00205 | - |
pH 7.5, 30°C | Homo sapiens | N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-methoxybenzylaniline | |
0.00218 | - |
pH 7.5, 30°C | Homo sapiens | 2-methyl-5-(propan-2-yl)cyclohexa-2,5-diene-1,4-dione | |
0.0026 | - |
pH 7.5, 30°C | Homo sapiens | N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-2-methylbenzamide | |
0.00322 | - |
pH 7.5, 30°C | Homo sapiens | N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-chlorobenzylaniline | |
0.00466 | - |
pH 7.5, 30°C | Homo sapiens | N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-methylbenzylaniline | |
0.0047 | - |
pH 7.5, 30°C | Homo sapiens | N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)acetamide | |
0.00559 | - |
pH 7.5, 30°C | Homo sapiens | N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)-2-methylbenzamide | |
0.00633 | - |
pH 7.5, 30°C | Homo sapiens | N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-benzamide | |
0.00683 | - |
pH 7.5, 30°C | Homo sapiens | N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-acetamide | |
0.00702 | - |
pH 7.5, 30°C | Homo sapiens | N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)benzylaniline | |
0.00709 | - |
pH 7.5, 30°C | Homo sapiens | N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-methylbenzamide | |
0.00948 | - |
pH 7.5, 30°C | Homo sapiens | N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-benzylaniline | |
0.01 | - |
pH 7.5, 30°C | Homo sapiens | N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-2-nitrobenzamide | |
0.01 | - |
pH 7.5, 30°C | Homo sapiens | N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-nitrobenzamide | |
0.01 | - |
pH 7.5, 30°C | Homo sapiens | N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-nitrobenzylaniline | |
0.01 | - |
pH 7.5, 30°C | Homo sapiens | N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)-2-nitrobenzamide | |
0.01 | - |
pH 7.5, 30°C | Homo sapiens | N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)-4-nitrobenzamide | |
0.01 | - |
pH 7.5, 30°C | Homo sapiens | N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)benzamide |
General Information | Comment | Organism |
---|---|---|
evolution | the serine/threonine kinase Polo-like kinase 1 (Plk1) is a member of the Polo-like kinases family | Homo sapiens |
physiological function | enzyme Plk1 acts as a regulator in multiple stages of mitotic progression | Homo sapiens |