Application | Comment | Organism |
---|---|---|
medicine | inhibition of PLK1 activity in cancer cells causes mitotic arrest and finally induces strong cell-killing effect | Mammalia |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
3-(1-[2-chloro-4-[(3-hydroxypyrrolidin-1-yl)methyl]phenyl]ethoxy)-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | - |
Mammalia | |
3-[(1R)-1-(2-chloro-4-[[(1-methylethyl)amino]methyl]phenyl)ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | - |
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 | - |
Mammalia | |
3-[(1R)-1-(2-chloro-4-[[(2-hydroxyethyl)amino]methyl]phenyl)ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | - |
Mammalia | |
3-[(1R)-1-(2-chloro-4-[[(3-hydroxypropyl)amino]methyl]phenyl)ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | - |
Mammalia | |
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | - |
Mammalia | |
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-(hydroxymethyl)imidazo[1,2-a]pyridin-3-yl]thiophene-2-carboxamide | - |
Mammalia | |
3-[(1R)-1-[2-(hydroxymethyl)phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | - |
Mammalia | |
3-[(1R)-1-[2-chloro-4-(hydroxymethyl)phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | - |
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 | - |
Mammalia | |
3-[(1R)-1-[2-chloro-4-[(3-oxopiperazin-1-yl)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | - |
Mammalia | |
3-[(1R)-1-[2-chloro-4-[(4-fluoropiperidin-1-yl)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | - |
Mammalia | |
3-[(1R)-1-[2-chloro-4-[(4-hydroxypiperidin-1-yl)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | - |
Mammalia | |
3-[(1R)-1-[2-chloro-4-[(4-methylpiperazin-1-yl)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | - |
Mammalia | |
3-[(1R)-1-[2-chloro-4-[(cyclopentylamino)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | - |
Mammalia | |
3-[(1R)-1-[2-chloro-4-[(cyclopropylamino)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | - |
Mammalia | |
3-[(1R)-1-[2-chloro-4-[(dimethylamino)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | - |
Mammalia | |
3-[(1R)-1-[2-chloro-4-[(ethylamino)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | - |
Mammalia | |
3-[(1R)-1-[2-chloro-4-[(methylamino)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | - |
Mammalia | |
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 | |
3-[(1R)-1-[4-[(tert-butylamino)methyl]-2-(difluoromethyl)phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | - |
Mammalia | |
3-[(1R)-1-[4-[(tert-butylamino)methyl]-2-chlorophenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | - |
Mammalia | |
3-[(1R)-1-[4-[(tert-butylamino)methyl]-2-cyclopropylphenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | - |
Mammalia | |
3-[(1R)-1-[4-[(tert-butylamino)methyl]-2-fluorophenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | - |
Mammalia | |
3-[(1R)-1-[4-[(tert-butylamino)methyl]-2-methylphenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | - |
Mammalia | |
3-[(1S)-1-(2-chlorophenyl)ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | - |
Mammalia | |
3-[(2-chlorobenzyl)oxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | - |
Mammalia | |
3-[1-(2-chlorophenyl)ethoxy]-5-[7-(hydroxymethyl)imidazo[1,2-a]pyridin-3-yl]thiophene-2-carboxamide | - |
Mammalia | |
3-[1-[2-chloro-5-(hydroxymethyl)phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | - |
Mammalia | |
5-(1-methyl-1H-imidazol-5-yl)-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide | - |
Mammalia | |
5-(1H-benzimidazol-1-yl)-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide | - |
Mammalia | |
5-(2-amino-1,3-thiazol-5-yl)-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide | - |
Mammalia | |
5-imidazo[1,2-a]pyridin-3-yl-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide | - |
Mammalia | |
5-pyrazolo[1,5-a]pyridin-3-yl-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide | - |
Mammalia | |
5-[2-(phenylamino)-1,3-thiazol-5-yl]-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide | - |
Mammalia | |
5-[2-[(phenylcarbonyl)amino]-1,3-thiazol-5-yl]-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide | - |
Mammalia | |
BI 2536 | - |
Mammalia | |
GSK 461364 | - |
Mammalia |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + a protein | Mammalia | - |
ADP + a phosphoprotein | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Mammalia | - |
- |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + a protein | - |
Mammalia | ADP + a phosphoprotein | - |
? |
Synonyms | Comment | Organism |
---|---|---|
PLK | - |
Mammalia |
polo-like kinase | - |
Mammalia |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ATP | - |
Mammalia |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0000049 | - |
- |
Mammalia | 3-[(1R)-1-[2-chloro-4-(hydroxymethyl)phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | |
0.000007 | - |
- |
Mammalia | 3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | |
0.0000073 | - |
- |
Mammalia | 3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-[6-(hydroxymethyl)imidazo[1,2-a]pyridin-3-yl]thiophene-2-carboxamide | |
0.0000098 | - |
- |
Mammalia | 3-[(1R)-1-[4-[(tert-butylamino)methyl]-2-(difluoromethoxy)phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | |
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 | |
0.000012 | - |
- |
Mammalia | 3-[(1R)-1-[2-chloro-4-[(cyclopropylamino)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | |
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 | |
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 | |
0.000016 | - |
- |
Mammalia | 3-[(1R)-1-[2-chloro-4-[(methylamino)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | |
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 | |
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 | |
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 | |
0.00002 | - |
- |
Mammalia | 3-[(1R)-1-[4-[(tert-butylamino)methyl]-2-(difluoromethyl)phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | |
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 | |
0.000021 | - |
- |
Mammalia | 3-[(1R)-1-[2-chloro-4-[(ethylamino)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | |
0.000021 | - |
- |
Mammalia | 3-[(1R)-1-[4-[(tert-butylamino)methyl]-2-chlorophenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | |
0.000022 | - |
- |
Mammalia | 3-[(1R)-1-[2-chloro-4-[(dimethylamino)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | |
0.000022 | - |
- |
Mammalia | 5-imidazo[1,2-a]pyridin-3-yl-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide | |
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 | |
0.000025 | - |
- |
Mammalia | 3-[(1R)-1-[2-chloro-4-[(cyclopentylamino)methyl]phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | |
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 | |
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 | |
0.000035 | - |
- |
Mammalia | 3-[(2-chlorobenzyl)oxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | |
0.000035 | - |
- |
Mammalia | 5-(1H-benzimidazol-1-yl)-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide | |
0.000039 | - |
- |
Mammalia | 3-[1-[2-chloro-5-(hydroxymethyl)phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | |
0.000046 | - |
- |
Mammalia | 3-[(1R)-1-[4-[(tert-butylamino)methyl]-2-fluorophenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | |
0.000088 | - |
- |
Mammalia | 3-[(1R)-1-[2-(hydroxymethyl)phenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | |
0.000092 | - |
- |
Mammalia | 3-[1-(2-chlorophenyl)ethoxy]-5-[7-(hydroxymethyl)imidazo[1,2-a]pyridin-3-yl]thiophene-2-carboxamide | |
0.00013 | - |
- |
Mammalia | 5-pyrazolo[1,5-a]pyridin-3-yl-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide | |
0.00015 | - |
- |
Mammalia | 3-[(1R)-1-[4-[(tert-butylamino)methyl]-2-methylphenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | |
0.00021 | - |
- |
Mammalia | 3-[(1R)-1-[4-[(tert-butylamino)methyl]-2-cyclopropylphenyl]ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | |
0.0003 | - |
- |
Mammalia | 3-[(1S)-1-(2-chlorophenyl)ethoxy]-5-imidazo[1,2-a]pyridin-3-ylthiophene-2-carboxamide | |
0.00043 | - |
- |
Mammalia | 5-(1-methyl-1H-imidazol-5-yl)-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide | |
0.0021 | - |
- |
Mammalia | 5-[2-[(phenylcarbonyl)amino]-1,3-thiazol-5-yl]-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide | |
0.003 | - |
larger than 0.003 | Mammalia | 5-(2-amino-1,3-thiazol-5-yl)-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide | |
0.003 | - |
larger than 0.003 | Mammalia | 5-[2-(phenylamino)-1,3-thiazol-5-yl]-3-[[2-(trifluoromethyl)benzyl]oxy]thiophene-2-carboxamide |
Organism | Comment | Expression |
---|---|---|
Mammalia | PLK1 is overexpressed in many clinical cancer samples | up |
General Information | Comment | Organism |
---|---|---|
physiological function | PLK1 participates in multiple steps in mitosis | Mammalia |