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Literature summary 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

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

Crystallization (Commentary)

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

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.11.21 1-(2-fluorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
 Danio rerio
2.7.11.21 1-(2-methoxyphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
 Danio rerio
2.7.11.21 1-(3,5-dichlorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
 Danio rerio
2.7.11.21 1-(3,5-dimethylphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
 Danio rerio
2.7.11.21 1-(3-bromo-5-chlorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
 Danio rerio
2.7.11.21 1-(3-chlorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
 Danio rerio
2.7.11.21 1-(3-fluorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
 Danio rerio
2.7.11.21 1-(3-methoxyphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
 Danio rerio
2.7.11.21 1-(4-fluorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
 Danio rerio
2.7.11.21 1-(4-methoxyphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
 Danio rerio
2.7.11.21 1-[3-(3-aminopropyl)phenyl]-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
 Danio rerio
2.7.11.21 1-[3-(dimethylamino)phenyl]-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
 Danio rerio
2.7.11.21 3-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)benzonitrile
-
 Danio rerio
2.7.11.21 3-methyl-1-(2-methylphenyl)-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
 Danio rerio
2.7.11.21 3-methyl-1-(3-methylphenyl)-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
 Danio rerio
2.7.11.21 3-methyl-1-(4-methylphenyl)-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
 Danio rerio
2.7.11.21 3-methyl-1-phenyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
 Danio rerio
2.7.11.21 3-methyl-1-[3-(1-methylethyl)phenyl]-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
 Danio rerio
2.7.11.21 3-methyl-1-[3-(methylsulfonyl)phenyl]-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
-
 Danio rerio
2.7.11.21 3-[3-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)phenyl]propanamide
-
 Danio rerio
2.7.11.21 3-[3-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)phenyl]propanoic acid
-
 Danio rerio
2.7.11.21 N-(2-hydroxyethyl)-3-[3-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)phenyl]propanamide
-
 Danio rerio
2.7.11.21 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)

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

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.21 Danio rerio
-
-
-

Substrates and Products (Substrate)

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

Synonyms

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

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.11.21 0.000021
-
-
 Danio rerio 3-[3-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)phenyl]propanoic acid
2.7.11.21 0.000032
-
-
 Danio rerio 3-[3-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)phenyl]propanamide
2.7.11.21 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
2.7.11.21 0.000059
-
-
 Danio rerio 1-[3-(3-aminopropyl)phenyl]-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
2.7.11.21 0.000121
-
-
 Danio rerio 1-(3-chlorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
2.7.11.21 0.000149
-
-
 Danio rerio 1-(3,5-dimethylphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
2.7.11.21 0.000207
-
-
 Danio rerio N-[2-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)phenyl]-2-phenylacetamide
2.7.11.21 0.000225
-
-
 Danio rerio 3-methyl-1-[3-(methylsulfonyl)phenyl]-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
2.7.11.21 0.000274
-
-
 Danio rerio 1-(3-bromo-5-chlorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
2.7.11.21 0.000412
-
-
 Danio rerio 3-(3-methyl-6-[[(1S)-1-phenylethyl]amino]-1H-pyrazolo[4,3-c]pyridin-1-yl)benzonitrile
2.7.11.21 0.000464
-
-
 Danio rerio 1-(3-fluorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
2.7.11.21 0.000474
-
-
 Danio rerio 3-methyl-1-(3-methylphenyl)-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
2.7.11.21 0.000641
-
-
 Danio rerio 1-(3,5-dichlorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
2.7.11.21 0.000703
-
-
 Danio rerio 1-(4-methoxyphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
2.7.11.21 0.000977
-
-
 Danio rerio 1-[3-(dimethylamino)phenyl]-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
2.7.11.21 0.001301
-
-
 Danio rerio 3-methyl-1-phenyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
2.7.11.21 0.001476
-
-
 Danio rerio 3-methyl-1-[3-(1-methylethyl)phenyl]-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
2.7.11.21 0.003241
-
-
 Danio rerio 1-(4-fluorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
2.7.11.21 0.004516
-
-
 Danio rerio 1-(2-fluorophenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
2.7.11.21 0.004528
-
-
 Danio rerio 3-methyl-1-(4-methylphenyl)-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
2.7.11.21 0.005928
-
-
 Danio rerio 1-(3-methoxyphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
2.7.11.21 0.007685
-
-
 Danio rerio 3-methyl-1-(2-methylphenyl)-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine
2.7.11.21 0.01445
-
-
 Danio rerio 1-(2-methoxyphenyl)-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine