Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary extracted from

  • Cheung, M.; Kuntz, K.W.; Pobanz, M.; Salovich, J.M.; Wilson, B.J.; Andrews, C.W.; Shewchuk, L.M.; Epperly, A.H.; Hassler, D.F.; Leesnitzer, M.A.; Smith, J.L.; Smith, G.K.; Lansing, T.J.; Mook, R.A.
    Imidazo[5,1-f][1,2,4]triazin-2-amines as novel inhibitors of polo-like kinase 1 (2008), Bioorg. Med. Chem. Lett., 18, 6214-6217.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.7.11.21 medicine Plk1 is a target for the development of anticancer therapeutics Mammalia

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.11.21 (3-[5-methyl-2-[(3,4,5-trimethoxyphenyl)amino]imidazo[5,1-f][1,2,4]triazin-7-yl]phenyl)(phenyl)methanone
-
 Mammalia
2.7.11.21 4-[(5-methyl-7-phenylimidazo[5,1-f][1,2,4]triazin-2-yl)amino]benzenesulfonamide
-
 Mammalia
2.7.11.21 5-methyl-7-(2-nitrophenyl)-N-(3,4,5-trimethoxyphenyl)imidazo[5,1-f][1,2,4]triazin-2-amine
-
 Mammalia
2.7.11.21 5-methyl-7-(3-phenoxyphenyl)-N-(3,4,5-trimethoxyphenyl)imidazo[5,1-f][1,2,4]triazin-2-amine
-
 Mammalia
2.7.11.21 5-methyl-7-phenyl-N-(2-pyridin-4-ylethyl)imidazo[5,1-f][1,2,4]triazin-2-amine >0.010 Mammalia
2.7.11.21 5-methyl-7-phenyl-N-(3,4,5-trimethoxyphenyl)imidazo[5,1-f][1,2,4]triazin-2-amine
-
 Mammalia
2.7.11.21 5-methyl-7-phenyl-N-[3-(trifluoromethyl)phenyl]imidazo[5,1-f][1,2,4]triazin-2-amine >0.010 Mammalia
2.7.11.21 5-methyl-7-phenylimidazo[5,1-f][1,2,4]triazin-2-amine >0.010 Mammalia
2.7.11.21 5-methyl-7-[3-(trifluoromethyl)phenyl]-N-(3,4,5-trimethoxyphenyl)imidazo[5,1-f][1,2,4]triazin-2-amine
-
 Mammalia
2.7.11.21 5-methyl-7-[4-(trifluoromethyl)phenyl]-N-(3,4,5-trimethoxyphenyl)imidazo[5,1-f][1,2,4]triazin-2-amine
-
 Mammalia
2.7.11.21 5-methyl-N,7-diphenylimidazo[5,1-f][1,2,4]triazin-2-amine
-
 Mammalia
2.7.11.21 5-methyl-N-(3-morpholin-4-ylpropyl)-7-phenylimidazo[5,1-f][1,2,4]triazin-2-amine >0.010 Mammalia
2.7.11.21 5-methyl-N-(4-nitrophenyl)-7-phenylimidazo[5,1-f][1,2,4]triazin-2-amine
-
 Mammalia
2.7.11.21 7-(2-bromophenyl)-5-methyl-N-(3,4,5-trimethoxyphenyl)imidazo[5,1-f][1,2,4]triazin-2-amine
-
 Mammalia
2.7.11.21 7-(2-methoxyphenyl)-5-methyl-N-(3,4,5-trimethoxyphenyl)imidazo[5,1-f][1,2,4]triazin-2-amine
-
 Mammalia
2.7.11.21 7-(3-bromophenyl)-5-methyl-N-(3,4,5-trimethoxyphenyl)imidazo[5,1-f][1,2,4]triazin-2-amine
-
 Mammalia
2.7.11.21 7-(4-fluorophenyl)-5-methyl-N-(3,4,5-trimethoxyphenyl)imidazo[5,1-f][1,2,4]triazin-2-amine
-
 Mammalia
2.7.11.21 BI 2536
-
 Mammalia
2.7.11.21 GSK461364
-
 Mammalia
2.7.11.21 N-(3,4-dimethoxyphenyl)-5-methyl-7-phenylimidazo[5,1-f][1,2,4]triazin-2-amine
-
 Mammalia
2.7.11.21 N-(3-methoxyphenyl)-5-methyl-7-phenylimidazo[5,1-f][1,2,4]triazin-2-amine
-
 Mammalia
2.7.11.21 N-(4-methoxyphenyl)-5-methyl-7-phenylimidazo[5,1-f][1,2,4]triazin-2-amine
-
 Mammalia
2.7.11.21 N-benzyl-5-methyl-7-phenylimidazo[5,1-f][1,2,4]triazin-2-amine
-
 Mammalia
2.7.11.21 N-cyclohexyl-5-methyl-7-phenylimidazo[5,1-f][1,2,4]triazin-2-amine >0.010 Mammalia
2.7.11.21 N-[4-[2-(dimethylamino)ethoxy]phenyl]-5-methyl-7-phenylimidazo[5,1-f][1,2,4]triazin-2-amine
-
 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 + protein Mammalia
-
 ADP + 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 + protein
-
 Mammalia ADP + phosphoprotein
-
 ?

Synonyms

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

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.11.21 0.00003
-
-
 Mammalia 5-methyl-7-[3-(trifluoromethyl)phenyl]-N-(3,4,5-trimethoxyphenyl)imidazo[5,1-f][1,2,4]triazin-2-amine
2.7.11.21 0.00004
-
-
 Mammalia 5-methyl-7-phenyl-N-(3,4,5-trimethoxyphenyl)imidazo[5,1-f][1,2,4]triazin-2-amine
2.7.11.21 0.00007
-
-
 Mammalia 7-(3-bromophenyl)-5-methyl-N-(3,4,5-trimethoxyphenyl)imidazo[5,1-f][1,2,4]triazin-2-amine
2.7.11.21 0.00008
-
-
 Mammalia 7-(4-fluorophenyl)-5-methyl-N-(3,4,5-trimethoxyphenyl)imidazo[5,1-f][1,2,4]triazin-2-amine
2.7.11.21 0.00009
-
-
 Mammalia N-(3,4-dimethoxyphenyl)-5-methyl-7-phenylimidazo[5,1-f][1,2,4]triazin-2-amine
2.7.11.21 0.0003
-
-
 Mammalia N-(3-methoxyphenyl)-5-methyl-7-phenylimidazo[5,1-f][1,2,4]triazin-2-amine
2.7.11.21 0.00038
-
-
 Mammalia N-[4-[2-(dimethylamino)ethoxy]phenyl]-5-methyl-7-phenylimidazo[5,1-f][1,2,4]triazin-2-amine
2.7.11.21 0.00041
-
-
 Mammalia (3-[5-methyl-2-[(3,4,5-trimethoxyphenyl)amino]imidazo[5,1-f][1,2,4]triazin-7-yl]phenyl)(phenyl)methanone
2.7.11.21 0.0005
-
-
 Mammalia 5-methyl-7-(3-phenoxyphenyl)-N-(3,4,5-trimethoxyphenyl)imidazo[5,1-f][1,2,4]triazin-2-amine
2.7.11.21 0.00068
-
-
 Mammalia N-(4-methoxyphenyl)-5-methyl-7-phenylimidazo[5,1-f][1,2,4]triazin-2-amine
2.7.11.21 0.00106
-
-
 Mammalia 5-methyl-7-[4-(trifluoromethyl)phenyl]-N-(3,4,5-trimethoxyphenyl)imidazo[5,1-f][1,2,4]triazin-2-amine
2.7.11.21 0.0012
-
-
 Mammalia 5-methyl-N,7-diphenylimidazo[5,1-f][1,2,4]triazin-2-amine
2.7.11.21 0.0015
-
-
 Mammalia N-benzyl-5-methyl-7-phenylimidazo[5,1-f][1,2,4]triazin-2-amine
2.7.11.21 0.00198
-
-
 Mammalia 5-methyl-7-(2-nitrophenyl)-N-(3,4,5-trimethoxyphenyl)imidazo[5,1-f][1,2,4]triazin-2-amine
2.7.11.21 0.00267
-
-
 Mammalia 7-(2-bromophenyl)-5-methyl-N-(3,4,5-trimethoxyphenyl)imidazo[5,1-f][1,2,4]triazin-2-amine
2.7.11.21 0.00274
-
-
 Mammalia 4-[(5-methyl-7-phenylimidazo[5,1-f][1,2,4]triazin-2-yl)amino]benzenesulfonamide
2.7.11.21 0.00281
-
-
 Mammalia 5-methyl-N-(4-nitrophenyl)-7-phenylimidazo[5,1-f][1,2,4]triazin-2-amine
2.7.11.21 0.00566
-
-
 Mammalia 7-(2-methoxyphenyl)-5-methyl-N-(3,4,5-trimethoxyphenyl)imidazo[5,1-f][1,2,4]triazin-2-amine
2.7.11.21 0.01
-
 >0.010 Mammalia 5-methyl-7-phenylimidazo[5,1-f][1,2,4]triazin-2-amine
2.7.11.21 0.01
-
 >0.010 Mammalia 5-methyl-7-phenyl-N-(2-pyridin-4-ylethyl)imidazo[5,1-f][1,2,4]triazin-2-amine
2.7.11.21 0.01
-
 >0.010 Mammalia 5-methyl-N-(3-morpholin-4-ylpropyl)-7-phenylimidazo[5,1-f][1,2,4]triazin-2-amine
2.7.11.21 0.01
-
 >0.010 Mammalia N-cyclohexyl-5-methyl-7-phenylimidazo[5,1-f][1,2,4]triazin-2-amine
2.7.11.21 0.01
-
 >0.010 Mammalia 5-methyl-7-phenyl-N-[3-(trifluoromethyl)phenyl]imidazo[5,1-f][1,2,4]triazin-2-amine