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Literature summary extracted from

  • Sorrenti, V.; Guccione, S.; Di Giacomo, C.; Modica, M.N.; Pittala, V.; Acquaviva, R.; Basile, L.; Pappalardo, M.; Salerno, L.
    Evaluation of imidazole-based compounds as heme oxygenase-1 inhibitors (2012), Chem. Biol. Drug Des., 80, 876-886.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.14.14.18 1-(2-phenoxyethyl)-1H-imidazole
-
 Rattus norvegicus
1.14.14.18 1-(4-bromophenyl)-2-(1H-imidazol-1-yl)ethanone
-
 Rattus norvegicus
1.14.14.18 1-(4-bromophenyl)-2-[2-(1-methylethyl)-1H-imidazol-1-yl]ethanone 27% inhibition at 0.1 mM Homo sapiens
1.14.14.18 1-(4-bromophenyl)-2-[2-(1-methylethyl)-1H-imidazol-1-yl]ethanone
-
 Rattus norvegicus
1.14.14.18 1-(adamantan-1-yl)-2-(1H-imidazol-1-yl)ethanone
-
 Homo sapiens
1.14.14.18 1-(adamantan-1-yl)-2-(1H-imidazol-1-yl)ethanone i.e. ADB_901 Rattus norvegicus
1.14.14.18 1-[4-(3-bromophenoxy)butyl]-1H-imidazole 54% inhibition at 0.1 mM Homo sapiens
1.14.14.18 1-[4-(3-bromophenoxy)butyl]-1H-imidazole
-
 Rattus norvegicus
1.14.14.18 1-[6-(4-bromophenoxy)exyl]-1H-imidazole
-
 Rattus norvegicus
1.14.14.18 2-(1H-imidazol-1-yl)-1-(4-nitrophenyl)ethanol
-
 Rattus norvegicus
1.14.14.18 4-phenyl-1-(1H-1,2,4-triazol-1-yl)butan-2-one
-
 Homo sapiens
1.14.14.18 4-phenyl-1-(1H-1,2,4-triazol-1-yl)butan-2-one
-
 Rattus norvegicus
1.14.14.18 azalanstat
-
 Homo sapiens
1.14.14.18 azalanstat
-
 Rattus norvegicus
1.14.14.18 additional information synthesis and inhibitory potency on isozyme HO-1 of imidazole-based compounds, molecular docking and modelling, overview. No inhibition by 1-[6-(4-bromophenoxy)exyl]-1H-imidazole, 1-(2-phenoxyethyl)-1H-imidazole, 2-(1H-imidazol-1-yl)-1-(4-nitrophenyl)ethanol, and 1-(4-bromophenyl)-2-(1H-imidazol-1-yl)ethanone Homo sapiens
1.14.14.18 additional information synthesis and inhibitory potency on isozyme HO-1 of imidazole-based compounds, molecular docking and modelling, overview Rattus norvegicus
1.14.14.18 tin protoporphyrin
-
 Homo sapiens
1.14.14.18 tin protoporphyrin
-
 Rattus norvegicus

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
1.14.14.18 membrane
-
 Homo sapiens 16020
-
1.14.14.18 microsome
-
 Rattus norvegicus
-
-

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.14.14.18 heme + 3 AH2 + 3 O2 Homo sapiens
-
 biliverdin + Fe2+ + CO + 3 A + 3 H2O
-
 ?
1.14.14.18 heme + 3 AH2 + 3 O2 Rattus norvegicus
-
 biliverdin + Fe2+ + CO + 3 A + 3 H2O
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
1.14.14.18 Homo sapiens P09601
-
-
1.14.14.18 Rattus norvegicus P06762
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.14.14.18 spleen
-
 Rattus norvegicus
-

Specific Activity [micromol/min/mg]

EC Number Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
1.14.14.18 0.00004
-
 spleen microsomes, pH 7.4, 37°C Rattus norvegicus

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.14.14.18 heme + 3 AH2 + 3 O2
-
 Homo sapiens biliverdin + Fe2+ + CO + 3 A + 3 H2O
-
 ?
1.14.14.18 heme + 3 AH2 + 3 O2
-
 Rattus norvegicus biliverdin + Fe2+ + CO + 3 A + 3 H2O
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.14.14.18 heme oxygenase-1
-
 Homo sapiens
1.14.14.18 heme oxygenase-1
-
 Rattus norvegicus
1.14.14.18 HO-1
-
 Homo sapiens
1.14.14.18 HO-1
-
 Rattus norvegicus

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
1.14.14.18 37
-
 assay at Homo sapiens
1.14.14.18 37
-
 assay at Rattus norvegicus

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
1.14.14.18 7.4
-
 assay at Homo sapiens
1.14.14.18 7.4
-
 assay at Rattus norvegicus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.14.14.18 0.0021
-
 pH 7.4, 37°C Rattus norvegicus 1-[4-(3-bromophenoxy)butyl]-1H-imidazole
1.14.14.18 0.0025
-
 pH 7.4, 37°C Rattus norvegicus 1-(4-bromophenyl)-2-(1H-imidazol-1-yl)ethanone
1.14.14.18 0.01
-
 pH 7.4, 37°C Rattus norvegicus 1-[6-(4-bromophenoxy)exyl]-1H-imidazole
1.14.14.18 0.01
-
 pH 7.4, 37°C Rattus norvegicus 2-(1H-imidazol-1-yl)-1-(4-nitrophenyl)ethanol
1.14.14.18 0.028
-
 pH 7.4, 37°C Rattus norvegicus 1-(2-phenoxyethyl)-1H-imidazole
1.14.14.18 0.1
-
 pH 7.4, 37°C Rattus norvegicus 1-(4-bromophenyl)-2-[2-(1-methylethyl)-1H-imidazol-1-yl]ethanone