Literature summary for 1.14.14.18 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.

Search for more literature for 1.14.14.18

Inhibitors

Inhibitors	Comment	Organism	Structure
1-(2-phenoxyethyl)-1H-imidazole	-	Rattus norvegicus
1-(4-bromophenyl)-2-(1H-imidazol-1-yl)ethanone	-	Rattus norvegicus
1-(4-bromophenyl)-2-[2-(1-methylethyl)-1H-imidazol-1-yl]ethanone	27% inhibition at 0.1 mM	Homo sapiens
1-(4-bromophenyl)-2-[2-(1-methylethyl)-1H-imidazol-1-yl]ethanone	-	Rattus norvegicus
1-(adamantan-1-yl)-2-(1H-imidazol-1-yl)ethanone	-	Homo sapiens
1-(adamantan-1-yl)-2-(1H-imidazol-1-yl)ethanone	i.e. ADB_901	Rattus norvegicus
1-[4-(3-bromophenoxy)butyl]-1H-imidazole	54% inhibition at 0.1 mM	Homo sapiens
1-[4-(3-bromophenoxy)butyl]-1H-imidazole	-	Rattus norvegicus
1-[6-(4-bromophenoxy)exyl]-1H-imidazole	-	Rattus norvegicus
2-(1H-imidazol-1-yl)-1-(4-nitrophenyl)ethanol	-	Rattus norvegicus
4-phenyl-1-(1H-1,2,4-triazol-1-yl)butan-2-one	-	Homo sapiens
4-phenyl-1-(1H-1,2,4-triazol-1-yl)butan-2-one	-	Rattus norvegicus
azalanstat	-	Homo sapiens
azalanstat	-	Rattus norvegicus
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
additional information	synthesis and inhibitory potency on isozyme HO-1 of imidazole-based compounds, molecular docking and modelling, overview	Rattus norvegicus
tin protoporphyrin	-	Homo sapiens
tin protoporphyrin	-	Rattus norvegicus

Localization

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

Natural Substrates/ Products (Substrates)

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

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	P09601	-	-
Rattus norvegicus	P06762	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
spleen	-	Rattus norvegicus	-

Specific Activity [micromol/min/mg]

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

Substrates and Products (Substrate)

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

Synonyms

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

Temperature Optimum [°C]

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

pH Optimum

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

IC50 Value

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

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Release 2023.1 (January 2023)