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Literature summary for 7.6.2.2 extracted from

  • Meyer, M.R.; Orschiedt, T.; Maurer, H.H.
    Michaelis-Menten kinetic analysis of drugs of abuse to estimate their affinity to human P-glycoprotein (2013), Toxicol. Lett., 217, 137-142.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
2,5-dimethoxy-4-iodoamphetamine
-
Homo sapiens
3,4-methylenedioxy-alpha-ethylphenethylamine
-
Homo sapiens
glaucine
-
Homo sapiens
N-(1-phenylcyclohexyl)-3-ethoxypropanamine
-
Homo sapiens
N-isopropyl-1,2-diphenylethylamine
-
Homo sapiens
sertraline
-
Homo sapiens
verapamil
-
Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
ortho-vanadate specific inhibitor Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0023
-
verapamil/in at pH 6.8 and 37°C Homo sapiens
0.0027
-
2,5-dimethoxy-4-iodoamphetamine/in at pH 6.8 and 37°C Homo sapiens
0.0037
-
N-(1-phenylcyclohexyl)-3-ethoxypropanamine/in at pH 6.8 and 37°C Homo sapiens
0.0046
-
3,4-methylenedioxy-alpha-ethylphenethylamine/in at pH 6.8 and 37°C Homo sapiens
0.0046
-
N-isopropyl-1,2-diphenylethylamine/in at pH 6.8 and 37°C Homo sapiens
0.006
-
sertraline/in at pH 6.8 and 37°C Homo sapiens
0.0071
-
glaucine/in at pH 6.8 and 37°C Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
membrane
-
Homo sapiens 16020
-

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + H2O + 2,5-dimethoxy-4-iodoamphetamine/in
-
Homo sapiens ADP + phosphate + 2,5-dimethoxy-4-iodoamphetamine/out
-
?
ATP + H2O + 3,4-methylenedioxy-alpha-ethylphenethylamine/in
-
Homo sapiens ADP + phosphate + 3,4-methylenedioxy-alpha-ethylphenethylamine/out
-
?
ATP + H2O + glaucine/in
-
Homo sapiens ADP + phosphate + glaucine/out
-
?
ATP + H2O + N-(1-phenylcyclohexyl)-3-ethoxypropanamine/in
-
Homo sapiens ADP + phosphate + N-(1-phenylcyclohexyl)-3-ethoxypropanamine/out
-
?
ATP + H2O + N-isopropyl-1,2-diphenylethylamine/in
-
Homo sapiens ADP + phosphate + N-isopropyl-1,2-diphenylethylamine/out
-
?
ATP + H2O + sertraline/in
-
Homo sapiens ADP + phosphate + sertraline/out
-
?
ATP + H2O + verapamil/in
-
Homo sapiens ADP + phosphate + verapamil/out
-
?

Synonyms

Synonyms Comment Organism
P-glycoprotein
-
Homo sapiens
P-gp
-
Homo sapiens