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Literature summary for 2.7.11.21 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

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

Inhibitors

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

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Mammalia
-
-
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
Plk1
-
Mammalia
Polo-like kinase 1
-
Mammalia

IC50 Value

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