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Literature summary for 2.7.11.21 extracted from

  • Emmitte, K.A.; Adjabeng, G.M.; Adjebang, G.M.; Andrews, C.W.; Alberti, J.G.; Bambal, R.; Chamberlain, S.D.; Davis-Ward, R.G.; Dickson, H.D.; Hassler, D.F.; Hornberger, K.R.; Jackson, J.R.; Kuntz, K.W.; Lansing, T.J.; Mook, R.A.; Nailor, K.E.; Pobanz, M.A.; Smith, S.C.; Sung, C.M.; Cheung, M.
    Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding (2009), Bioorg. Med. Chem. Lett., 19, 1694-1697.
    View publication on PubMed
Search for more literature for 2.7.11.21

Application

Application Comment Organism
medicine polo-like kinases represent an attractive target for cancer treatment through interference with the cell cycle Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
-
 Homo sapiens
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-methoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
-
 Homo sapiens
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(2R)-2,3-dihydroxypropyl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
-
 Homo sapiens
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(2R)-2-hydroxy-3-pyrrolidin-1-ylpropyl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
-
 Homo sapiens
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(4R)-1-methylazepan-4-yl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
-
 Homo sapiens
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(4S)-1-methylazepan-4-yl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
-
 Homo sapiens
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[(1-methylpiperidin-4-yl)methoxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
-
 Homo sapiens
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
-
 Homo sapiens
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[3-(dimethylamino)propoxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
-
 Homo sapiens
3-[(1S)-1-(2-chlorophenyl)ethoxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
-
 Homo sapiens
3-[(2-chlorobenzyl)oxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
-
 Homo sapiens
5-(5,6-dimethoxy-1H-benzimidazol-1-yl)-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide
-
 Homo sapiens
5-(6-methoxy-1H-benzimidazol-1-yl)-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
-
 Homo sapiens
5-[6-(piperidin-4-yloxy)-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
-
 Homo sapiens
5-[6-[(1-methylpiperidin-4-yl)methoxy]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
-
 Homo sapiens
5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Homo sapiens P53350
-
-
Homo sapiens Q9H4B4
-
-

Source Tissue

Source Tissue Comment Organism Textmining
A-549 cell
-
 Homo sapiens
-
Colo-205 cell
-
 Homo sapiens
-
HCT-116 cell
-
 Homo sapiens
-
HT-29 cell
-
 Homo sapiens
-
MX-1 cell
-
 Homo sapiens
-
SKOV-3 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + a protein
-
 Homo sapiens ADP + a phosphoprotein
-
 ?

Synonyms

Synonyms Comment Organism
PLK
-
 Homo sapiens
Plk1
-
 Homo sapiens
Plk3
-
 Homo sapiens
polo-like kinase
-
 Homo sapiens
Polo-like kinase 1
-
 Homo sapiens
polo-like kinase 3
-
 Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000008
-
-
 Homo sapiens 3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.000001
-
-
 Homo sapiens 3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-methoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.000001
-
-
 Homo sapiens 3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(2R)-2,3-dihydroxypropyl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.000002
-
-
 Homo sapiens 3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
0.000002
-
-
 Homo sapiens 5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
0.000002
-
-
 Homo sapiens 3-[(2-chlorobenzyl)oxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.000002
-
-
 Homo sapiens 5-(5,6-dimethoxy-1H-benzimidazol-1-yl)-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide
0.000003
-
-
 Homo sapiens 3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(2R)-2-hydroxy-3-pyrrolidin-1-ylpropyl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.000003
-
-
 Homo sapiens 3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(4S)-1-methylazepan-4-yl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.000003
-
-
 Homo sapiens 5-(6-methoxy-1H-benzimidazol-1-yl)-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
0.000003
-
-
 Homo sapiens 5-[6-(piperidin-4-yloxy)-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
0.000003
-
 HT-29 cell Homo sapiens 3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
0.000003
-
 HT-29 cell Homo sapiens 5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
0.000004
-
-
 Homo sapiens 3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(4R)-1-methylazepan-4-yl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.000004
-
-
 Homo sapiens 3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[3-(dimethylamino)propoxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
0.000005
-
 Colo-205 cell Homo sapiens 3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
0.000005
-
 Colo-205 cell Homo sapiens 5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
0.000006
-
-
 Homo sapiens 3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.000006
-
-
 Homo sapiens 3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[(1-methylpiperidin-4-yl)methoxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
0.000007
-
-
 Homo sapiens 5-[6-[(1-methylpiperidin-4-yl)methoxy]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
0.000009
-
-
 Homo sapiens 3-[(2-chlorobenzyl)oxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.000009
-
-
 Homo sapiens 5-(5,6-dimethoxy-1H-benzimidazol-1-yl)-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide
0.000009
-
 MX-1 cell Homo sapiens 3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
0.00001
-
 MX-1 cell Homo sapiens 5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
0.000011
-
 A-549 cell Homo sapiens 3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
0.000011
-
 HCT-116 cell Homo sapiens 3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
0.000011
-
 SKOV-3 cell Homo sapiens 3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
0.000012
-
 HCT-116 cell Homo sapiens 5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
0.000013
-
 HCT-116 cell Homo sapiens 3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(4R)-1-methylazepan-4-yl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.000014
-
 A-549 cell Homo sapiens 5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
0.000015
-
 HCT-116 cell Homo sapiens 5-[6-(piperidin-4-yloxy)-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
0.000017
-
 HCT-116 cell Homo sapiens 3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(4S)-1-methylazepan-4-yl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.000025
-
 HCT-116 cell Homo sapiens 3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.00003
-
-
 Homo sapiens 3-[(1S)-1-(2-chlorophenyl)ethoxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.00003
-
 HCT-116 cell Homo sapiens 5-[6-[(1-methylpiperidin-4-yl)methoxy]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
0.000032
-
 HCT-116 cell Homo sapiens 3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[3-(dimethylamino)propoxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
0.000032
-
 SKOV-3 cell Homo sapiens 5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
0.000034
-
 HCT-116 cell Homo sapiens 3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[(1-methylpiperidin-4-yl)methoxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
0.000035
-
-
 Homo sapiens 3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-methoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.000041
-
-
 Homo sapiens 5-(6-methoxy-1H-benzimidazol-1-yl)-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
0.000044
-
-
 Homo sapiens 3-[(1S)-1-(2-chlorophenyl)ethoxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.000045
-
 HCT-116 cell Homo sapiens 3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(2R)-2-hydroxy-3-pyrrolidin-1-ylpropyl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.000061
-
-
 Homo sapiens 3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(2R)-2,3-dihydroxypropyl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.000073
-
 HCT-116 cell Homo sapiens 3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(2R)-2,3-dihydroxypropyl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.00024
-
-
 Homo sapiens 3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(4S)-1-methylazepan-4-yl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.00025
-
-
 Homo sapiens 3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(4R)-1-methylazepan-4-yl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.00027
-
-
 Homo sapiens 5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
0.000321
-
 HCT-116 cell Homo sapiens 3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-methoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.00035
-
-
 Homo sapiens 5-[6-(piperidin-4-yloxy)-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
0.00046
-
-
 Homo sapiens 3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[3-(dimethylamino)propoxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
0.000476
-
 HCT-116 cell Homo sapiens 5-(6-methoxy-1H-benzimidazol-1-yl)-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
0.00055
-
-
 Homo sapiens 5-[6-[(1-methylpiperidin-4-yl)methoxy]-1H-benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide
0.00061
-
-
 Homo sapiens 3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-[[(2R)-2-hydroxy-3-pyrrolidin-1-ylpropyl]oxy]-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.00063
-
-
 Homo sapiens 3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[(1-methylpiperidin-4-yl)oxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
0.000994
-
 HCT-116 cell Homo sapiens 3-[(1S)-1-(2-chlorophenyl)ethoxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide
0.0011
-
-
 Homo sapiens 3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-[(1-methylpiperidin-4-yl)methoxy]-1H-benzimidazol-1-yl]thiophene-2-carboxamide
0.00114
-
 HCT-116 cell Homo sapiens 3-[(2-chlorobenzyl)oxy]-5-(5,6-dimethoxy-1H-benzimidazol-1-yl)thiophene-2-carboxamide

General Information

General Information Comment Organism
physiological function PLK1 represents the most studied member of this familiy and has known roles throughout mitosis, including mitotic entry, spindle formation, chromosome segregation, and cytokinesis Homo sapiens