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Literature summary 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

EC Number Inhibitors Comment Organism Structure
2.7.11.19 6'-bromoindirubin-3'-oxime
-
 Oryctolagus cuniculus
2.7.11.19 6,5-dichloroindirubin
-
 Oryctolagus cuniculus
2.7.11.19 6,5-dichloroindirubin-3'-acetoxime
-
 Oryctolagus cuniculus
2.7.11.19 6,5-dichloroindirubin-3'-oxime
-
 Oryctolagus cuniculus
2.7.11.19 6,6'-dibromoindirubin-3'-oxime
-
 Oryctolagus cuniculus
2.7.11.19 6-bromo-5-methylindirubin
-
 Oryctolagus cuniculus
2.7.11.19 6-bromo-5-methylindirubin-3'-acetoxime
-
 Oryctolagus cuniculus
2.7.11.19 6-bromo-5-nitroindirubin
-
 Oryctolagus cuniculus
2.7.11.19 6-bromo-5-nitroindirubin-3'-acetoxime
-
 Oryctolagus cuniculus
2.7.11.19 6-bromo-5-nitroindirubin-3'-oxime
-
 Oryctolagus cuniculus
2.7.11.19 6-bromo-N-methylindirubin
-
 Oryctolagus cuniculus
2.7.11.19 6-bromo-N-methylindirubin-3'-acetoxime
-
 Oryctolagus cuniculus
2.7.11.19 6-bromoindirubin
-
 Oryctolagus cuniculus
2.7.11.19 6-bromoindirubin-3'-acetoxime
-
 Oryctolagus cuniculus
2.7.11.19 6-bromoindirubin-3'-oxime
-
 Oryctolagus cuniculus
2.7.11.19 6-chloroindirubin
-
 Oryctolagus cuniculus
2.7.11.19 6-chloroindirubin-3'-oxime
-
 Oryctolagus cuniculus
2.7.11.19 6-fluoroindirubin
-
 Oryctolagus cuniculus
2.7.11.19 6-fluoroindirubin-3'-oxime
-
 Oryctolagus cuniculus
2.7.11.19 6-iodoindirubin-3'-oxime
-
 Oryctolagus cuniculus
2.7.11.19 6-methoxindirubin-3'-acetoxime
-
 Oryctolagus cuniculus
2.7.11.19 6-methoxindirubin-3'-oxime
-
 Oryctolagus cuniculus
2.7.11.19 6-vinylindirubin
-
 Oryctolagus cuniculus
2.7.11.19 6-vinylindirubin-3'-acetoxime
-
 Oryctolagus cuniculus
2.7.11.19 6-vinylindirubin-3'-oxime
-
 Oryctolagus cuniculus
2.7.11.19 7-bromo-N-methylindirubin
-
 Oryctolagus cuniculus
2.7.11.19 7-bromo-N-methylindirubin-3'-acetoxime
-
 Oryctolagus cuniculus
2.7.11.19 7-bromo-N-methylindirubin-3'-methoxime
-
 Oryctolagus cuniculus
2.7.11.19 7-bromo-N-methylindirubin-3'-oxime
-
 Oryctolagus cuniculus
2.7.11.19 7-bromoindirubin
-
 Oryctolagus cuniculus
2.7.11.19 7-bromoindirubin-3'-acetoxime
-
 Oryctolagus cuniculus
2.7.11.19 7-bromoindirubin-3'-methoxime
-
 Oryctolagus cuniculus
2.7.11.19 7-bromoindirubin-3'-oxime
-
 Oryctolagus cuniculus
2.7.11.19 7-carboxylindirubin
-
 Oryctolagus cuniculus
2.7.11.19 indirubin
-
 Oryctolagus cuniculus
2.7.11.19 indirubin 3'-oxime
-
 Oryctolagus cuniculus
2.7.11.19 indirubin-3'-acetoxime
-
 Oryctolagus cuniculus
2.7.11.19 indirubin-3'-methoxime
-
 Oryctolagus cuniculus
2.7.11.19 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

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

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.11.19 2 ATP + glycogen phosphorylase b Oryctolagus cuniculus
-
 2 ADP + glycogen phosphorylase a
-
 ?
2.7.11.19 2 ATP + glycogen phosphorylase b Oryctolagus cuniculus New Zealand White
-
 2 ADP + glycogen phosphorylase a
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.19 Oryctolagus cuniculus
-
-
-
2.7.11.19 Oryctolagus cuniculus New Zealand White
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.11.19 skeletal muscle
-
 Oryctolagus cuniculus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.11.19 2 ATP + glycogen phosphorylase b
-
 Oryctolagus cuniculus 2 ADP + glycogen phosphorylase a
-
 ?
2.7.11.19 2 ATP + glycogen phosphorylase b
-
 Oryctolagus cuniculus New Zealand White 2 ADP + glycogen phosphorylase a
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.11.19 PhK
-
 Oryctolagus cuniculus

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.7.11.19 30
-
 assay at Oryctolagus cuniculus

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.11.19 ATP
-
 Oryctolagus cuniculus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.11.19 0.00017
-
 pH not specified in the publication, 30°C Oryctolagus cuniculus indirubin-3'-acetoxime
2.7.11.19 0.0002
-
 pH not specified in the publication, 30°C Oryctolagus cuniculus 6,5-dichloroindirubin-3'-oxime
2.7.11.19 0.00021
-
 pH not spefified in the publication, 30°C Oryctolagus cuniculus indirubin 3'-oxime
2.7.11.19 0.00022
-
 pH not specified in the publication, 30°C Oryctolagus cuniculus 6-fluoroindirubin-3'-oxime
2.7.11.19 0.00023
-
 pH not specified in the publication, 30°C Oryctolagus cuniculus 6-chloroindirubin-3'-oxime
2.7.11.19 0.00029
-
 pH not specified in the publication, 30°C Oryctolagus cuniculus 6'-bromoindirubin-3'-oxime
2.7.11.19 0.00033
-
 pH not specified in the publication, 30°C Oryctolagus cuniculus 6-bromoindirubin-3'-acetoxime
2.7.11.19 0.00033
-
 pH not specified in the publication, 30°C Oryctolagus cuniculus 6-iodoindirubin-3'-oxime
2.7.11.19 0.00034
-
 pH not specified in the publication, 30°C Oryctolagus cuniculus 6-bromoindirubin-3'-oxime
2.7.11.19 0.00034
-
 pH not specified in the publication, 30°C Oryctolagus cuniculus indirubin-3'-methoxime
2.7.11.19 0.00036
-
 pH not specified in the publication, 30°C Oryctolagus cuniculus 6-bromo-5-methylindirubin-3'-acetoxime
2.7.11.19 0.00054
-
 pH not specified in the publication, 30°C Oryctolagus cuniculus 6-vinylindirubin-3'-acetoxime
2.7.11.19 0.00055
-
 pH not specified in the publication, 30°C Oryctolagus cuniculus 6-vinylindirubin-3'-oxime
2.7.11.19 0.0007
-
 pH not specified in the publication, 30°C Oryctolagus cuniculus 6-methoxindirubin-3'-oxime
2.7.11.19 0.00082
-
 pH not specified in the publication, 30°C Oryctolagus cuniculus 6,5-dichloroindirubin-3'-acetoxime
2.7.11.19 0.001
-
 pH not specified in the publication, 30°C Oryctolagus cuniculus 6-bromo-5-nitroindirubin-3'-oxime
2.7.11.19 0.00113
-
 pH not specified in the publication, 30°C Oryctolagus cuniculus 6-methoxindirubin-3'-acetoxime
2.7.11.19 0.0012
-
 pH not specified in the publication, 30°C Oryctolagus cuniculus 6-bromo-5-nitroindirubin-3'-acetoxime
2.7.11.19 0.0018
-
 pH not specified in the publication, 30°C Oryctolagus cuniculus 7-bromoindirubin-3'-oxime
2.7.11.19 0.00233
-
 pH not specified in the publication, 30°C Oryctolagus cuniculus 6,6'-dibromoindirubin-3'-oxime
2.7.11.19 0.01
-
 pH not specified in the publication, 30°C Oryctolagus cuniculus 7-bromoindirubin-3'-acetoxime
2.7.11.19 0.05
-
 pH not specified in the publication, 30°C Oryctolagus cuniculus 6-bromo-5-methylindirubin
2.7.11.19 0.05
-
 pH not specified in the publication, 30°C Oryctolagus cuniculus 6-bromo-5-nitroindirubin
2.7.11.19 0.05
-
 pH not specified in the publication, 30°C Oryctolagus cuniculus 6-bromo-N-methylindirubin
2.7.11.19 0.05
-
 pH not specified in the publication, 30°C Oryctolagus cuniculus 6-bromo-N-methylindirubin-3'-acetoxime
2.7.11.19 0.05
-
 pH not specified in the publication, 30°C Oryctolagus cuniculus 6-bromoindirubin
2.7.11.19 0.05
-
 pH not specified in the publication, 30°C Oryctolagus cuniculus 6-chloroindirubin
2.7.11.19 0.05
-
 pH not specified in the publication, 30°C Oryctolagus cuniculus 6-fluoroindirubin
2.7.11.19 0.05
-
 pH not specified in the publication, 30°C Oryctolagus cuniculus 6-vinylindirubin
2.7.11.19 0.05
-
 pH not specified in the publication, 30°C Oryctolagus cuniculus 6,5-dichloroindirubin
2.7.11.19 0.05
-
 pH not specified in the publication, 30°C Oryctolagus cuniculus 7-bromo-N-methylindirubin
2.7.11.19 0.05
-
 pH not specified in the publication, 30°C Oryctolagus cuniculus 7-bromo-N-methylindirubin-3'-acetoxime
2.7.11.19 0.05
-
 pH not specified in the publication, 30°C Oryctolagus cuniculus 7-bromo-N-methylindirubin-3'-methoxime
2.7.11.19 0.05
-
 pH not specified in the publication, 30°C Oryctolagus cuniculus 7-bromo-N-methylindirubin-3'-oxime
2.7.11.19 0.05
-
 pH not specified in the publication, 30°C Oryctolagus cuniculus 7-bromoindirubin
2.7.11.19 0.05
-
 pH not specified in the publication, 30°C Oryctolagus cuniculus 7-bromoindirubin-3'-methoxime
2.7.11.19 0.05
-
 pH not specified in the publication, 30°C Oryctolagus cuniculus 7-carboxylindirubin
2.7.11.19 0.05
-
 pH not spefified in the publication, 30°C Oryctolagus cuniculus indirubin