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Literature summary extracted from

  • Chan, K.F.; Wong, I.L.; Kan, J.W.; Yan, C.S.; Chow, L.M.; Chan, T.H.
    Amine linked flavonoid dimers as modulators for P-glycoprotein-based multidrug resistance: structure-activity relationship and mechanism of modulation (2012), J. Med. Chem., 55, 1999-2014.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
7.6.2.2 1,13-bis[4'-(4H-chromen-4-on-2-yl)phenyl]-N-(benzyl)-1,4,10,13-tetraoxa-7-azatridecane stimulates ATPase activity by 2.7-fold Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
7.6.2.2 1,13-bis[4'-(4H-chromen-4-on-2-yl)phenyl]-N-(benzyl)-1,4,10,13-tetraoxa-7-azatridecane competitive inhibitor to doxorubicin binding by P-glycoprotein Homo sapiens
7.6.2.2 apigenin
-
Homo sapiens
7.6.2.2 cyclosporine A
-
Homo sapiens
7.6.2.2 Ko143
-
Homo sapiens
7.6.2.2 valspodar
-
Homo sapiens
7.6.2.2 verapamil
-
Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
7.6.2.2 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
7.6.2.2 MDA435/LCC6MDR1 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
7.6.2.2 ATP + H2O + 1,13-bis[4'-(4H-chromen-4-on-2-yl)phenyl]-N-(benzyl)-1,4,10,13-tetraoxa-7-azatridecane/in
-
Homo sapiens ADP + phosphate + 1,13-bis[4'-(4H-chromen-4-on-2-yl)phenyl]-N-(benzyl)-1,4,10,13-tetraoxa-7-azatridecane/out
-
?
7.6.2.2 ATP + H2O + doxorubicin/in
-
Homo sapiens ADP + phosphate + doxorubicin/out
-
?

Synonyms

EC Number Synonyms Comment Organism
7.6.2.2 P-glycoprotein
-
Homo sapiens
7.6.2.2 P-gp
-
Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
7.6.2.2 0.00028 0.00034 1,13-bis[4'-(4H-chromen-4-on-2-yl)phenyl]-N-(benzyl)-1,4,10,13-tetraoxa-7-azatridecane at 37°C, pH not specified in the publication Homo sapiens