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Literature summary extracted from

  • Lee, E.; Kim, J.H.; Shon, J.C.; Wu, Z.; Kim, H.J.; Gim, M.; Lee, T.; Liu, K.H.
    Terfenadone is a strong inhibitor of CYP2J2 present in the human liver and intestinal microsomes (2018), Drug Metab. Pharmacokinet., 33, 159-163 .
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.14.14.74 coexpression with NADPH-cytochrome P450 reductase in Sf9 cells Homo sapiens

Protein Variants

EC Number Protein Variants Comment Organism
1.14.14.74 G312R natural genetic variant, almost complete loss of enzymatic activity. Loss of CO binding to the heme, molecular modelling predicts a spatial hindrance between heme and the bulky side chain of the R312 residue in G312R Homo sapiens
1.14.14.74 additional information identification of 12 genetic variations from 93 Korean subjects Homo sapiens
1.14.14.74 P351L natural genetic variant, activity similar to wild-type Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.14.14.74 danazol
-
 Homo sapiens
1.14.14.74 hydroxyebastine
-
 Homo sapiens
1.14.14.74 telmisartan
-
 Homo sapiens
1.14.14.74 terfenadone
-
 Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
1.14.14.74 Homo sapiens P51589
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.14.14.74 liver
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.14.14.74 albendazole + [reduced NADPH-hemoprotein reductase] + O2
-
 Homo sapiens 4'-hydroxyalbendazole + [oxidized NADPH-hemoprotein reductase] + H2O
-
 ?
1.14.14.74 astemizole + [reduced NADPH-hemoprotein reductase] + O2
-
 Homo sapiens hydroxyastemizole + [oxidized NADPH-hemoprotein reductase] + H2O
-
 ?
1.14.14.74 ebastine + [reduced NADPH-hemoprotein reductase] + O2
-
 Homo sapiens hydroxyebastine + [oxidized NADPH-hemoprotein reductase] + H2O
-
 ?
1.14.14.74 terfenadine + [reduced NADPH-hemoprotein reductase] + O2
-
 Homo sapiens terfenadine alcohol + [oxidized NADPH-hemoprotein reductase] + H2O
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.14.14.74 CYP2J2
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.14.14.74 0.00015
-
 substrate astemizole, liver microsome, pH 7.4, 37°C Homo sapiens terfenadone
1.14.14.74 0.00031
-
 substrate albendazole, liver microsome, pH 7.4, 37°C Homo sapiens terfenadone
1.14.14.74 0.00195
-
 substrate ebastine, liver microsome, pH 7.4, 37°C Homo sapiens danazol
1.14.14.74 0.0021
-
 substrate terfenadine, liver microsome, pH 7.4, 37°C Homo sapiens terfenadone
1.14.14.74 0.00214
-
 substrate terfenadine, liver microsome, pH 7.4, 37°C Homo sapiens danazol
1.14.14.74 0.004
-
 substrate terfenadine, liver microsome, pH 7.4, 37°C Homo sapiens hydroxyebastine
1.14.14.74 0.00427
-
 substrate ebastine, liver microsome, pH 7.4, 37°C Homo sapiens terfenadone
1.14.14.74 0.00928
-
 substrate astemizole, liver microsome, pH 7.4, 37°C Homo sapiens hydroxyebastine
1.14.14.74 0.0111
-
 substrate albendazole, liver microsome, pH 7.4, 37°C Homo sapiens hydroxyebastine
1.14.14.74 0.0138
-
 substrate albendazole, liver microsome, pH 7.4, 37°C Homo sapiens danazol
1.14.14.74 0.0183
-
 substrate astemizole, liver microsome, pH 7.4, 37°C Homo sapiens danazol
1.14.14.74 0.0238
-
 substrate terfenadine, liver microsome, pH 7.4, 37°C Homo sapiens telmisartan
1.14.14.74 0.0472
-
 substrate albendazole, liver microsome, pH 7.4, 37°C Homo sapiens telmisartan