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Literature summary extracted from

  • Sato, Y.; Onozaki, Y.; Sugimoto, T.; Kurihara, H.; Kamijo, K.; Kadowaki, C.; Tsujino, T.; Watanabe, A.; Otsuki, S.; Mitsuya, M.; Iida, M.; Haze, K.; Machida, T.; Nakatsuru, Y.; Komatani, H.; Kotani, H.; Iwasawa, Y.
    Imidazopyridine derivatives as potent and selective polo-like kinase (PLK) inhibitors (2009), Bioorg. Med. Chem. Lett., 19, 4673-4678.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.7.11.21 medicine inhibition of PLK1 activity in cancer cells causes mitotic arrest and finally induces strong cell-killing effect Mammalia

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.11.21 3-(1-[2-chloro-4-[(3-hydroxypyrrolidin-1-yl)methyl]phenyl]ethoxy)-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
 Mammalia
2.7.11.21 3-[(1R)-1-(2-chloro-4-[[(1-methylethyl)amino]methyl]phenyl)ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
 Mammalia
2.7.11.21 3-[(1R)-1-(2-chloro-4-[[(2-hydroxy-1,1-dimethylethyl)amino]methyl]phenyl)ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
 Mammalia
2.7.11.21 3-[(1R)-1-(2-chloro-4-[[(2-hydroxyethyl)amino]methyl]phenyl)ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
 Mammalia
2.7.11.21 3-[(1R)-1-(2-chloro-4-[[(3-hydroxypropyl)amino]methyl]phenyl)ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
 Mammalia
2.7.11.21 3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
 Mammalia
2.7.11.21 3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-(hydroxymethyl)imidazo[1,2-a]pyridin-3-yl]thiophene-2-carboxamide
-
 Mammalia
2.7.11.21 3-[(1R)-1-[2-(hydroxymethyl)phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
 Mammalia
2.7.11.21 3-[(1R)-1-[2-chloro-4-(hydroxymethyl)phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
 Mammalia
2.7.11.21 3-[(1R)-1-[2-chloro-4-[(1,1-dioxidothiomorpholin-4-yl)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
 Mammalia
2.7.11.21 3-[(1R)-1-[2-chloro-4-[(3-oxopiperazin-1-yl)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
 Mammalia
2.7.11.21 3-[(1R)-1-[2-chloro-4-[(4-fluoropiperidin-1-yl)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
 Mammalia
2.7.11.21 3-[(1R)-1-[2-chloro-4-[(4-hydroxypiperidin-1-yl)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
 Mammalia
2.7.11.21 3-[(1R)-1-[2-chloro-4-[(4-methylpiperazin-1-yl)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
 Mammalia
2.7.11.21 3-[(1R)-1-[2-chloro-4-[(cyclopentylamino)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
 Mammalia
2.7.11.21 3-[(1R)-1-[2-chloro-4-[(cyclopropylamino)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
 Mammalia
2.7.11.21 3-[(1R)-1-[2-chloro-4-[(dimethylamino)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
 Mammalia
2.7.11.21 3-[(1R)-1-[2-chloro-4-[(ethylamino)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
 Mammalia
2.7.11.21 3-[(1R)-1-[2-chloro-4-[(methylamino)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
 Mammalia
2.7.11.21 3-[(1R)-1-[4-[(tert-butylamino)methyl]-2-(difluoromethoxy)phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide tested in rat xenograft model Mammalia
2.7.11.21 3-[(1R)-1-[4-[(tert-butylamino)methyl]-2-(difluoromethyl)phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
 Mammalia
2.7.11.21 3-[(1R)-1-[4-[(tert-butylamino)methyl]-2-chlorophenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
 Mammalia
2.7.11.21 3-[(1R)-1-[4-[(tert-butylamino)methyl]-2-cyclopropylphenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
 Mammalia
2.7.11.21 3-[(1R)-1-[4-[(tert-butylamino)methyl]-2-fluorophenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
 Mammalia
2.7.11.21 3-[(1R)-1-[4-[(tert-butylamino)methyl]-2-methylphenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
 Mammalia
2.7.11.21 3-[(1S)-1-(2-chlorophenyl)ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
 Mammalia
2.7.11.21 3-[(2-chlorobenzyl)oxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
 Mammalia
2.7.11.21 3-[1-(2-chlorophenyl)ethoxy]-5-[7-(hydroxymethyl)imidazo[1,2-a]pyridin-3-yl]thiophene-2-carboxamide
-
 Mammalia
2.7.11.21 3-[1-[2-chloro-5-(hydroxymethyl)phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
-
 Mammalia
2.7.11.21 5-(1-methyl-1H-imidazol-5-yl)-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide
-
 Mammalia
2.7.11.21 5-(1H-benzimidazol-1-yl)-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide
-
 Mammalia
2.7.11.21 5-(2-amino-1,3-thiazol-5-yl)-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide
-
 Mammalia
2.7.11.21 5-imidazo[1,2-a]pyridin-3-yl-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide
-
 Mammalia
2.7.11.21 5-pyrazolo[1,5-a]pyridin-3-yl-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide
-
 Mammalia
2.7.11.21 5-[2-(phenylamino)-1,3-thiazol-5-yl]-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide
-
 Mammalia
2.7.11.21 5-[2-[(phenylcarbonyl)amino]-1,3-thiazol-5-yl]-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide
-
 Mammalia
2.7.11.21 BI 2536
-
 Mammalia
2.7.11.21 GSK 461364
-
 Mammalia

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 Mammalia
-
 ADP + a phosphoprotein
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.21 Mammalia
-
-
-

Substrates and Products (Substrate)

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

Synonyms

EC Number Synonyms Comment Organism
2.7.11.21 PLK
-
 Mammalia
2.7.11.21 polo-like kinase
-
 Mammalia

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.11.21 ATP
-
 Mammalia

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.11.21 0.0000049
-
-
 Mammalia 3-[(1R)-1-[2-chloro-4-(hydroxymethyl)phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
2.7.11.21 0.000007
-
-
 Mammalia 3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
2.7.11.21 0.0000073
-
-
 Mammalia 3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-(hydroxymethyl)imidazo[1,2-a]pyridin-3-yl]thiophene-2-carboxamide
2.7.11.21 0.0000098
-
-
 Mammalia 3-[(1R)-1-[4-[(tert-butylamino)methyl]-2-(difluoromethoxy)phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
2.7.11.21 0.000012
-
-
 Mammalia 3-[(1R)-1-[2-chloro-4-[(cyclopropylamino)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
2.7.11.21 0.000012
-
-
 Mammalia 3-[(1R)-1-[2-chloro-4-[(3-oxopiperazin-1-yl)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
2.7.11.21 0.000013
-
-
 Mammalia 3-[(1R)-1-[2-chloro-4-[(4-fluoropiperidin-1-yl)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
2.7.11.21 0.000016
-
-
 Mammalia 3-[(1R)-1-[2-chloro-4-[(methylamino)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
2.7.11.21 0.000016
-
-
 Mammalia 3-[(1R)-1-[2-chloro-4-[(1,1-dioxidothiomorpholin-4-yl)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
2.7.11.21 0.000017
-
-
 Mammalia 3-[(1R)-1-[2-chloro-4-[(4-methylpiperazin-1-yl)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
2.7.11.21 0.000019
-
-
 Mammalia 3-[(1R)-1-(2-chloro-4-[[(3-hydroxypropyl)amino]methyl]phenyl)ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
2.7.11.21 0.00002
-
-
 Mammalia 3-(1-[2-chloro-4-[(3-hydroxypyrrolidin-1-yl)methyl]phenyl]ethoxy)-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
2.7.11.21 0.00002
-
-
 Mammalia 3-[(1R)-1-[4-[(tert-butylamino)methyl]-2-(difluoromethyl)phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
2.7.11.21 0.000021
-
-
 Mammalia 3-[(1R)-1-[2-chloro-4-[(ethylamino)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
2.7.11.21 0.000021
-
-
 Mammalia 3-[(1R)-1-[4-[(tert-butylamino)methyl]-2-chlorophenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
2.7.11.21 0.000021
-
-
 Mammalia 3-[(1R)-1-(2-chloro-4-[[(2-hydroxyethyl)amino]methyl]phenyl)ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
2.7.11.21 0.000022
-
-
 Mammalia 5-imidazo[1,2-a]pyridin-3-yl-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide
2.7.11.21 0.000022
-
-
 Mammalia 3-[(1R)-1-[2-chloro-4-[(dimethylamino)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
2.7.11.21 0.000023
-
-
 Mammalia 3-[(1R)-1-(2-chloro-4-[[(2-hydroxy-1,1-dimethylethyl)amino]methyl]phenyl)ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
2.7.11.21 0.000025
-
-
 Mammalia 3-[(1R)-1-[2-chloro-4-[(cyclopentylamino)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
2.7.11.21 0.000027
-
-
 Mammalia 3-[(1R)-1-[2-chloro-4-[(4-hydroxypiperidin-1-yl)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
2.7.11.21 0.000028
-
-
 Mammalia 3-[(1R)-1-(2-chloro-4-[[(1-methylethyl)amino]methyl]phenyl)ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
2.7.11.21 0.000035
-
-
 Mammalia 5-(1H-benzimidazol-1-yl)-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide
2.7.11.21 0.000035
-
-
 Mammalia 3-[(2-chlorobenzyl)oxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
2.7.11.21 0.000039
-
-
 Mammalia 3-[1-[2-chloro-5-(hydroxymethyl)phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
2.7.11.21 0.000046
-
-
 Mammalia 3-[(1R)-1-[4-[(tert-butylamino)methyl]-2-fluorophenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
2.7.11.21 0.000088
-
-
 Mammalia 3-[(1R)-1-[2-(hydroxymethyl)phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
2.7.11.21 0.000092
-
-
 Mammalia 3-[1-(2-chlorophenyl)ethoxy]-5-[7-(hydroxymethyl)imidazo[1,2-a]pyridin-3-yl]thiophene-2-carboxamide
2.7.11.21 0.00013
-
-
 Mammalia 5-pyrazolo[1,5-a]pyridin-3-yl-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide
2.7.11.21 0.00015
-
-
 Mammalia 3-[(1R)-1-[4-[(tert-butylamino)methyl]-2-methylphenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
2.7.11.21 0.00021
-
-
 Mammalia 3-[(1R)-1-[4-[(tert-butylamino)methyl]-2-cyclopropylphenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
2.7.11.21 0.0003
-
-
 Mammalia 3-[(1S)-1-(2-chlorophenyl)ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide
2.7.11.21 0.00043
-
-
 Mammalia 5-(1-methyl-1H-imidazol-5-yl)-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide
2.7.11.21 0.0021
-
-
 Mammalia 5-[2-[(phenylcarbonyl)amino]-1,3-thiazol-5-yl]-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide
2.7.11.21 0.003
-
 larger than 0.003 Mammalia 5-(2-amino-1,3-thiazol-5-yl)-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide
2.7.11.21 0.003
-
 larger than 0.003 Mammalia 5-[2-(phenylamino)-1,3-thiazol-5-yl]-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide

Expression

EC Number Organism Comment Expression
2.7.11.21 Mammalia PLK1 is overexpressed in many clinical cancer samples up

General Information

EC Number General Information Comment Organism
2.7.11.21 physiological function PLK1 participates in multiple steps in mitosis Mammalia