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Literature summary extracted from

  • Chen, D.X.; Huang, J.; Liu, M.; Xu, Y.G.; Jiang, C.
    Design, synthesis, and evaluation of non-ATP-competitive small-molecule polo-like kinase 1 (Plk1) inhibitors (2015), Arch. Pharm., 348, 2-9.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.7.11.21 drug development Plk1 is considered an attractive anti-cancer drug target due to its ability to promote tumorigenesis Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.11.21 (4E)-4-(hydroxyimino)-5-methyl-2-(propan-2-yl)cyclohexa-2,5-dien-1-one i.e. poloxime, PXE Homo sapiens
2.7.11.21 (4E)-5-methyl-4-{[(2-methylbenzoyl)oxy]imino}-2-(propan-2-yl)cyclohexa-2,5-dien-1-one i.e. poloxin Homo sapiens
2.7.11.21 2-methyl-5-(propan-2-yl)cyclohexa-2,5-diene-1,4-dione i.e. thymoquinone Homo sapiens
2.7.11.21 2-[(3-cyano-6-methoxyquinolin-2-yl)sulfanyl]-N-(2-methoxy-5-methylphenyl)acetamide i.e. I2 Homo sapiens
2.7.11.21 BI 2536 a dihydropteridinone and a ATP-competitive Plk1 inhibitor Homo sapiens
2.7.11.21 BI 6727 a ATP-competitive Plk1 inhibitor Homo sapiens
2.7.11.21 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
2.7.11.21 N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-2-methylbenzamide
-
 Homo sapiens
2.7.11.21 N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-2-nitrobenzamide
-
 Homo sapiens
2.7.11.21 N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-chlorobenzylaniline
-
 Homo sapiens
2.7.11.21 N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-methoxybenzamide
-
 Homo sapiens
2.7.11.21 N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-methoxybenzylaniline
-
 Homo sapiens
2.7.11.21 N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-methylbenzamide
-
 Homo sapiens
2.7.11.21 N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-methylbenzylaniline
-
 Homo sapiens
2.7.11.21 N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-nitrobenzamide
-
 Homo sapiens
2.7.11.21 N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-nitrobenzylaniline
-
 Homo sapiens
2.7.11.21 N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-acetamide
-
 Homo sapiens
2.7.11.21 N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-benzamide
-
 Homo sapiens
2.7.11.21 N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-benzylaniline
-
 Homo sapiens
2.7.11.21 N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)-2-methylbenzamide
-
 Homo sapiens
2.7.11.21 N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)-2-nitrobenzamide
-
 Homo sapiens
2.7.11.21 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
2.7.11.21 N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)-4-nitrobenzamide
-
 Homo sapiens
2.7.11.21 N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)acetamide
-
 Homo sapiens
2.7.11.21 N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)benzamide
-
 Homo sapiens
2.7.11.21 N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)benzylaniline
-
 Homo sapiens
2.7.11.21 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

EC Number Metals/Ions Comment Organism Structure
2.7.11.21 Mg2+ required Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.11.21 ATP + a protein Homo sapiens
-
 ADP + a phosphoprotein
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.21 Homo sapiens P53350
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.11.21 ATP + a protein
-
 Homo sapiens ADP + a phosphoprotein
-
 ?
2.7.11.21 ATP + Cdc25C
-
 Homo sapiens ADP + phosphorylated Cdc25C
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.11.21 Plk1
-
 Homo sapiens
2.7.11.21 Polo-like kinase 1
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.7.11.21 30
-
 assay at Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.7.11.21 7.5
-
 assay at Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.11.21 ATP
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.11.21 0.00000083
-
 pH 7.5, 30°C Homo sapiens BI 2536
2.7.11.21 0.00000087
-
 pH 7.5, 30°C Homo sapiens BI 6727
2.7.11.21 0.00068
-
 pH 7.5, 30°C Homo sapiens N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)-4-methoxybenzamide
2.7.11.21 0.00093
-
 pH 7.5, 30°C Homo sapiens N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-methoxybenzamide
2.7.11.21 0.00205
-
 pH 7.5, 30°C Homo sapiens N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-methoxybenzylaniline
2.7.11.21 0.00218
-
 pH 7.5, 30°C Homo sapiens 2-methyl-5-(propan-2-yl)cyclohexa-2,5-diene-1,4-dione
2.7.11.21 0.0026
-
 pH 7.5, 30°C Homo sapiens N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-2-methylbenzamide
2.7.11.21 0.00322
-
 pH 7.5, 30°C Homo sapiens N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-chlorobenzylaniline
2.7.11.21 0.00466
-
 pH 7.5, 30°C Homo sapiens N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-methylbenzylaniline
2.7.11.21 0.0047
-
 pH 7.5, 30°C Homo sapiens N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)acetamide
2.7.11.21 0.00559
-
 pH 7.5, 30°C Homo sapiens N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)-2-methylbenzamide
2.7.11.21 0.00633
-
 pH 7.5, 30°C Homo sapiens N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-benzamide
2.7.11.21 0.00683
-
 pH 7.5, 30°C Homo sapiens N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-acetamide
2.7.11.21 0.00702
-
 pH 7.5, 30°C Homo sapiens N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)benzylaniline
2.7.11.21 0.00709
-
 pH 7.5, 30°C Homo sapiens N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-methylbenzamide
2.7.11.21 0.00948
-
 pH 7.5, 30°C Homo sapiens N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-benzylaniline
2.7.11.21 0.01
-
 pH 7.5, 30°C Homo sapiens N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-2-nitrobenzamide
2.7.11.21 0.01
-
 pH 7.5, 30°C Homo sapiens N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-nitrobenzamide
2.7.11.21 0.01
-
 pH 7.5, 30°C Homo sapiens N-(2-(3-(1H-benzo[d]imidazol-1-yl)propoxy)phenyl)-4-nitrobenzylaniline
2.7.11.21 0.01
-
 pH 7.5, 30°C Homo sapiens N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)-2-nitrobenzamide
2.7.11.21 0.01
-
 pH 7.5, 30°C Homo sapiens N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)-4-nitrobenzamide
2.7.11.21 0.01
-
 pH 7.5, 30°C Homo sapiens N-(2-(3-(1H-indol-1-yl)propoxy)phenyl)benzamide

General Information

EC Number General Information Comment Organism
2.7.11.21 evolution the serine/threonine kinase Polo-like kinase 1 (Plk1) is a member of the Polo-like kinases family Homo sapiens
2.7.11.21 physiological function enzyme Plk1 acts as a regulator in multiple stages of mitotic progression Homo sapiens