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Literature summary for 2.7.11.19 extracted from

  • Begum, J.; Skamnaki, V.T.; Moffatt, C.; Bischler, N.; Sarrou, J.; Skaltsounis, A.L.; Leonidas, D.D.; Oikonomakos, N.G.; Hayes, J.M.
    An evaluation of indirubin analogues as phosphorylase kinase inhibitors (2015), J. Mol. Graph. Model., 61, 231-242.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
6'-bromoindirubin-3'-oxime
-
Oryctolagus cuniculus
6,5-dichloroindirubin
-
Oryctolagus cuniculus
6,5-dichloroindirubin-3'-acetoxime
-
Oryctolagus cuniculus
6,5-dichloroindirubin-3'-oxime
-
Oryctolagus cuniculus
6,6'-dibromoindirubin-3'-oxime
-
Oryctolagus cuniculus
6-bromo-5-methylindirubin
-
Oryctolagus cuniculus
6-bromo-5-methylindirubin-3'-acetoxime
-
Oryctolagus cuniculus
6-bromo-5-nitroindirubin
-
Oryctolagus cuniculus
6-bromo-5-nitroindirubin-3'-acetoxime
-
Oryctolagus cuniculus
6-bromo-5-nitroindirubin-3'-oxime
-
Oryctolagus cuniculus
6-bromo-N-methylindirubin
-
Oryctolagus cuniculus
6-bromo-N-methylindirubin-3'-acetoxime
-
Oryctolagus cuniculus
6-bromoindirubin
-
Oryctolagus cuniculus
6-bromoindirubin-3'-acetoxime
-
Oryctolagus cuniculus
6-bromoindirubin-3'-oxime
-
Oryctolagus cuniculus
6-chloroindirubin
-
Oryctolagus cuniculus
6-chloroindirubin-3'-oxime
-
Oryctolagus cuniculus
6-fluoroindirubin
-
Oryctolagus cuniculus
6-fluoroindirubin-3'-oxime
-
Oryctolagus cuniculus
6-iodoindirubin-3'-oxime
-
Oryctolagus cuniculus
6-methoxindirubin-3'-acetoxime
-
Oryctolagus cuniculus
6-methoxindirubin-3'-oxime
-
Oryctolagus cuniculus
6-vinylindirubin
-
Oryctolagus cuniculus
6-vinylindirubin-3'-acetoxime
-
Oryctolagus cuniculus
6-vinylindirubin-3'-oxime
-
Oryctolagus cuniculus
7-bromo-N-methylindirubin
-
Oryctolagus cuniculus
7-bromo-N-methylindirubin-3'-acetoxime
-
Oryctolagus cuniculus
7-bromo-N-methylindirubin-3'-methoxime
-
Oryctolagus cuniculus
7-bromo-N-methylindirubin-3'-oxime
-
Oryctolagus cuniculus
7-bromoindirubin
-
Oryctolagus cuniculus
7-bromoindirubin-3'-acetoxime
-
Oryctolagus cuniculus
7-bromoindirubin-3'-methoxime
-
Oryctolagus cuniculus
7-bromoindirubin-3'-oxime
-
Oryctolagus cuniculus
7-carboxylindirubin
-
Oryctolagus cuniculus
indirubin
-
Oryctolagus cuniculus
indirubin 3'-oxime
-
Oryctolagus cuniculus
indirubin-3'-acetoxime
-
Oryctolagus cuniculus
indirubin-3'-methoxime
-
Oryctolagus cuniculus
additional information evaluation of indirubin analogues as phosphorylase kinase inhibitors, structure-activity relationship analysis, docking, overview. The inhibitory effects arises from binding at the kinase domain, i.e. gamma-subunit Oryctolagus cuniculus

Metals/Ions

Metals/Ions Comment Organism Structure
Ca2+ required Oryctolagus cuniculus
Mg2+ required Oryctolagus cuniculus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2 ATP + glycogen phosphorylase b Oryctolagus cuniculus
-
2 ADP + glycogen phosphorylase a
-
?
2 ATP + glycogen phosphorylase b Oryctolagus cuniculus New Zealand White
-
2 ADP + glycogen phosphorylase a
-
?

Organism

Organism UniProt Comment Textmining
Oryctolagus cuniculus
-
-
-
Oryctolagus cuniculus New Zealand White
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
skeletal muscle
-
Oryctolagus cuniculus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2 ATP + glycogen phosphorylase b
-
Oryctolagus cuniculus 2 ADP + glycogen phosphorylase a
-
?
2 ATP + glycogen phosphorylase b
-
Oryctolagus cuniculus New Zealand White 2 ADP + glycogen phosphorylase a
-
?

Synonyms

Synonyms Comment Organism
PhK
-
Oryctolagus cuniculus

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
30
-
assay at Oryctolagus cuniculus

Cofactor

Cofactor Comment Organism Structure
ATP
-
Oryctolagus cuniculus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00017
-
pH not specified in the publication, 30°C Oryctolagus cuniculus indirubin-3'-acetoxime
0.0002
-
pH not specified in the publication, 30°C Oryctolagus cuniculus 6,5-dichloroindirubin-3'-oxime
0.00021
-
pH not spefified in the publication, 30°C Oryctolagus cuniculus indirubin 3'-oxime
0.00022
-
pH not specified in the publication, 30°C Oryctolagus cuniculus 6-fluoroindirubin-3'-oxime
0.00023
-
pH not specified in the publication, 30°C Oryctolagus cuniculus 6-chloroindirubin-3'-oxime
0.00029
-
pH not specified in the publication, 30°C Oryctolagus cuniculus 6'-bromoindirubin-3'-oxime
0.00033
-
pH not specified in the publication, 30°C Oryctolagus cuniculus 6-bromoindirubin-3'-acetoxime
0.00033
-
pH not specified in the publication, 30°C Oryctolagus cuniculus 6-iodoindirubin-3'-oxime
0.00034
-
pH not specified in the publication, 30°C Oryctolagus cuniculus 6-bromoindirubin-3'-oxime
0.00034
-
pH not specified in the publication, 30°C Oryctolagus cuniculus indirubin-3'-methoxime
0.00036
-
pH not specified in the publication, 30°C Oryctolagus cuniculus 6-bromo-5-methylindirubin-3'-acetoxime
0.00054
-
pH not specified in the publication, 30°C Oryctolagus cuniculus 6-vinylindirubin-3'-acetoxime
0.00055
-
pH not specified in the publication, 30°C Oryctolagus cuniculus 6-vinylindirubin-3'-oxime
0.0007
-
pH not specified in the publication, 30°C Oryctolagus cuniculus 6-methoxindirubin-3'-oxime
0.00082
-
pH not specified in the publication, 30°C Oryctolagus cuniculus 6,5-dichloroindirubin-3'-acetoxime
0.001
-
pH not specified in the publication, 30°C Oryctolagus cuniculus 6-bromo-5-nitroindirubin-3'-oxime
0.00113
-
pH not specified in the publication, 30°C Oryctolagus cuniculus 6-methoxindirubin-3'-acetoxime
0.0012
-
pH not specified in the publication, 30°C Oryctolagus cuniculus 6-bromo-5-nitroindirubin-3'-acetoxime
0.0018
-
pH not specified in the publication, 30°C Oryctolagus cuniculus 7-bromoindirubin-3'-oxime
0.00233
-
pH not specified in the publication, 30°C Oryctolagus cuniculus 6,6'-dibromoindirubin-3'-oxime
0.01
-
pH not specified in the publication, 30°C Oryctolagus cuniculus 7-bromoindirubin-3'-acetoxime
0.05
-
pH not specified in the publication, 30°C Oryctolagus cuniculus 6-bromo-5-methylindirubin
0.05
-
pH not specified in the publication, 30°C Oryctolagus cuniculus 6-bromo-5-nitroindirubin
0.05
-
pH not specified in the publication, 30°C Oryctolagus cuniculus 6-bromo-N-methylindirubin
0.05
-
pH not specified in the publication, 30°C Oryctolagus cuniculus 6-bromo-N-methylindirubin-3'-acetoxime
0.05
-
pH not specified in the publication, 30°C Oryctolagus cuniculus 6-bromoindirubin
0.05
-
pH not specified in the publication, 30°C Oryctolagus cuniculus 6-chloroindirubin
0.05
-
pH not specified in the publication, 30°C Oryctolagus cuniculus 6-fluoroindirubin
0.05
-
pH not specified in the publication, 30°C Oryctolagus cuniculus 6-vinylindirubin
0.05
-
pH not specified in the publication, 30°C Oryctolagus cuniculus 6,5-dichloroindirubin
0.05
-
pH not specified in the publication, 30°C Oryctolagus cuniculus 7-bromo-N-methylindirubin
0.05
-
pH not specified in the publication, 30°C Oryctolagus cuniculus 7-bromo-N-methylindirubin-3'-acetoxime
0.05
-
pH not specified in the publication, 30°C Oryctolagus cuniculus 7-bromo-N-methylindirubin-3'-methoxime
0.05
-
pH not specified in the publication, 30°C Oryctolagus cuniculus 7-bromo-N-methylindirubin-3'-oxime
0.05
-
pH not specified in the publication, 30°C Oryctolagus cuniculus 7-bromoindirubin
0.05
-
pH not specified in the publication, 30°C Oryctolagus cuniculus 7-bromoindirubin-3'-methoxime
0.05
-
pH not specified in the publication, 30°C Oryctolagus cuniculus 7-carboxylindirubin
0.05
-
pH not spefified in the publication, 30°C Oryctolagus cuniculus indirubin