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Literature summary for 2.7.11.21 extracted from

  • Fucini, R.V.; Hanan, E.J.; Romanowski, M.J.; Elling, R.A.; Lew, W.; Barr, K.J.; Zhu, J.; Yoburn, J.C.; Liu, Y.; Fahr, B.T.; Fan, J.; Lu, Y.; Pham, P.; Choong, I.C.; VanderPorten, E.C.; Bui, M.; Purkey, H.E.; Evanchik, M.J.; Yang, W.
    Design and synthesis of 2-amino-pyrazolopyridines as Polo-like kinase 1 inhibitors (2008), Bioorg. Med. Chem. Lett., 18, 5648-5652.
    View publication on PubMed

Application

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

Crystallization (Commentary)

Crystallization (Comment) Organism
zPlk1 is crystallized in complex with compound38 Danio rerio

Inhibitors

Inhibitors Comment Organism Structure
1-(2-fluorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
Danio rerio
1-(2-methoxyphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
Danio rerio
1-(3,5-dichlorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
Danio rerio
1-(3,5-dimethylphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
Danio rerio
1-(3-bromo-5-chlorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
Danio rerio
1-(3-chlorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
Danio rerio
1-(3-fluorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
Danio rerio
1-(3-methoxyphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
Danio rerio
1-(4-fluorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
Danio rerio
1-(4-methoxyphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
Danio rerio
1-[3-(3-aminopropyl)phenyl]-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
Danio rerio
1-[3-(dimethylamino)phenyl]-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
Danio rerio
3-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)benzonitrile
-
Danio rerio
3-methyl-1-(2-methylphenyl)-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
Danio rerio
3-methyl-1-(3-methylphenyl)-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
Danio rerio
3-methyl-1-(4-methylphenyl)-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
Danio rerio
3-methyl-1-phenyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
Danio rerio
3-methyl-1-[3-(1-methylethyl)phenyl]-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
Danio rerio
3-methyl-1-[3-(methylsulfonyl)phenyl]-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
Danio rerio
3-[3-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)phenyl]propanamide
-
Danio rerio
3-[3-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)phenyl]propanoic acid
-
Danio rerio
N-(2-hydroxyethyl)-3-[3-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)phenyl]propanamide
-
Danio rerio
N-[2-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)phenyl]-2-phenylacetamide
-
Danio rerio

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Danio rerio
-
-
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
Plk1
-
Danio rerio
Polo-like kinase 1
-
Danio rerio
zPlk1
-
Danio rerio

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000021
-
-
Danio rerio 3-[3-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)phenyl]propanoic acid
0.000032
-
-
Danio rerio 3-[3-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)phenyl]propanamide
0.000048
-
-
Danio rerio N-(2-hydroxyethyl)-3-[3-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)phenyl]propanamide
0.000059
-
-
Danio rerio 1-[3-(3-aminopropyl)phenyl]-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
0.000121
-
-
Danio rerio 1-(3-chlorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
0.000149
-
-
Danio rerio 1-(3,5-dimethylphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
0.000207
-
-
Danio rerio N-[2-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)phenyl]-2-phenylacetamide
0.000225
-
-
Danio rerio 3-methyl-1-[3-(methylsulfonyl)phenyl]-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
0.000274
-
-
Danio rerio 1-(3-bromo-5-chlorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
0.000412
-
-
Danio rerio 3-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)benzonitrile
0.000464
-
-
Danio rerio 1-(3-fluorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
0.000474
-
-
Danio rerio 3-methyl-1-(3-methylphenyl)-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
0.000641
-
-
Danio rerio 1-(3,5-dichlorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
0.000703
-
-
Danio rerio 1-(4-methoxyphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
0.000977
-
-
Danio rerio 1-[3-(dimethylamino)phenyl]-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
0.001301
-
-
Danio rerio 3-methyl-1-phenyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
0.001476
-
-
Danio rerio 3-methyl-1-[3-(1-methylethyl)phenyl]-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
0.003241
-
-
Danio rerio 1-(4-fluorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
0.004516
-
-
Danio rerio 1-(2-fluorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
0.004528
-
-
Danio rerio 3-methyl-1-(4-methylphenyl)-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
0.005928
-
-
Danio rerio 1-(3-methoxyphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
0.007685
-
-
Danio rerio 3-methyl-1-(2-methylphenyl)-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
0.01445
-
-
Danio rerio 1-(2-methoxyphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine