Inhibitors | Comment | Organism | Structure |
---|---|---|---|
1-(3,4-dichlorobenzyl)-3-(2-morpholin-4-yl-2-oxoethyl)-1H-indole | 82% inhibition at 0.005 mM | Rattus norvegicus | |
1-(3,4-dichlorobenzyl)-3-(3-morpholin-4-yl-3-oxopropyl)-1H-indole | 38.5% inhibition at 0.005 mM | Rattus norvegicus | |
1-(4-chlorophenoxy)-3-(2-morpholin-4-yl-2-oxoethyl)-1H-indole | 22% inhibition at 0.005 mM | Rattus norvegicus | |
1-(4-chlorophenoxy)-3-(3-morpholin-4-yl-3-oxopropyl)-1H-indole | 26% inhibition at 0.005 mM | Rattus norvegicus | |
1-(4-chlorophenoxy)-5-methoxy-2-methyl-3-(4-morpholin-4-yl-4-oxobutyl)-1H-indole | 70% inhibition at 0.005 mM | Rattus norvegicus | |
1-(4-methylbenzyl)-3-(2-morpholin-4-yl-2-oxoethyl)-1H-indole | 35% inhibition at 0.005 mM | Rattus norvegicus | |
1-(4-methylbenzyl)-3-(3-morpholin-4-yl-3-oxopropyl)-1H-indole | 55% inhibition at 0.005 mM | Rattus norvegicus | |
1-benzyl-3-(2-morpholin-4-yl-2-oxoethyl)-1H-indole | 41% inhibition at 0.005 mM | Rattus norvegicus | |
1-benzyl-3-(3-morpholin-4-yl-3-oxopropyl)-1H-indole | 64% inhibition at 0.005 mM | Rattus norvegicus | |
1-benzyl-3-(4-morpholin-4-ylbutyl)-1H-indole | 42% inhibition at 0.005 mM | Rattus norvegicus | |
1-benzyl-3-(4-oxo-4-piperazin-1-ylbutyl)-1H-indole | 95% inhibition at 0.005 mM | Rattus norvegicus | |
1-benzyl-3-[2-[3-fluoro-5-(4-methoxytetrahydro-2H-pyran-4-yl)phenoxy]ethyl]-1H-indole | 32% inhibition at 0.005 mM | Rattus norvegicus | |
1-benzyl-3-[3-[3-fluoro-5-(4-methoxytetrahydro-2H-pyran-4-yl)phenoxy]propyl]-5-methoxy-2-methyl-1H-indole | 46.5% inhibition at 0.005 mM | Rattus norvegicus | |
1-benzyl-5-chloro-2-methyl-3-(4-morpholin-4-yl-4-oxobutyl)-1H-indole | 80% inhibition at 0.005 mM | Rattus norvegicus | |
1-benzyl-5-methoxy-2-methyl-3-(4-morpholin-4-yl-4-oxobutyl)-1H-indole | 54% inhibition at 0.005 mM | Rattus norvegicus | |
1-benzyl-5-methoxy-2-methyl-3-(4-oxo-4-piperazin-1-ylbutyl)-1H-indole | 65% inhibition at 0.005 mM | Rattus norvegicus | |
3-(2-morpholin-4-yl-2-oxoethyl)-1-phenoxy-1H-indole | 21% inhibition at 0.005 mM | Rattus norvegicus | |
3-(2-morpholin-4-yl-2-oxoethyl)-1H-indole | 16% inhibition at 0.005 mM | Rattus norvegicus | |
3-(3-morpholin-4-yl-3-oxopropyl)-1-phenoxy-1H-indole | 23% inhibition at 0.005 mM | Rattus norvegicus | |
3-(3-morpholin-4-yl-3-oxopropyl)-1H-indole | 33% inhibition at 0.005 mM | Rattus norvegicus | |
3-(4-morpholin-4-yl-4-oxobutyl)-1H-indole | 62% inhibition at 0.005 mM | Rattus norvegicus | |
3-[2-[3-fluoro-5-(4-methoxytetrahydro-2H-pyran-4-yl)phenoxy]ethyl]-1H-indole | 64% inhibition at 0.005 mM | Rattus norvegicus | |
4-((3,4-dichlorobenzyl)-1H-indol-3-yl)-1-morpholinobutan-1-one | 27% inhibition at 0.005 mM | Rattus norvegicus | |
4-((4-chlorobenzoyl)-1H-indol-3-yl)-1-morpholinobutan-1-one | 32% inhibition at 0.005 mM | Rattus norvegicus | |
4-(1-(4-methylbenzyl)-1H-indol-3-yl)-1-morpholinobutan-1-one | 34% inhibition at 0.005 mM | Rattus norvegicus | |
4-(1-benzoyl-1H-indol-3-yl)-1-morpholinobutan-1-one | 58% inhibition at 0.005 mM | Rattus norvegicus | |
4-(1-benzyl-1H-indol-3-yl)-1-morpholinobutan-1-one | 26% inhibition at 0.005 mM | Rattus norvegicus | |
5-chloro-1-(4-chlorophenoxy)-2-methyl-3-(4-morpholin-4-yl-4-oxobutyl)-1H-indole | 38% inhibition at 0.005 mM | Rattus norvegicus | |
5-chloro-2-methyl-3-(4-morpholin-4-yl-4-oxobutyl)-1H-indole | 71% inhibition at 0.005 mM | Rattus norvegicus | |
5-methoxy-2-methyl-1-(4-methylbenzyl)-3-(4-morpholin-4-yl-4-oxobutyl)-1H-indole | 26% inhibition at 0.005 mM | Rattus norvegicus | |
5-methoxy-2-methyl-3-(4-morpholin-4-yl-4-oxobutyl)-1H-indole | 73% inhibition at 0.005 mM | Rattus norvegicus | |
additional information | inhibitor design, synthesis, biological evaluation, and molecular modeling, overview | Rattus norvegicus | |
tert-butyl 4-[4-(1-benzyl-1H-indol-3-yl)butanoyl]piperazine-1-carboxylate | 38% inhibition at 0.005 mM | Rattus norvegicus | |
tert-butyl 4-[4-(1-benzyl-5-methoxy-2-methyl-1H-indol-3-yl)butanoyl]piperazine-1-carboxylate | 51.5% inhibition at 0.005 mM | Rattus norvegicus | |
tert-butyl 4-[4-(1H-indol-3-yl)butanoyl]piperazine-1-carboxylate | 84% inhibition at 0.005 mM | Rattus norvegicus | |
tert-butyl 4-[4-(5-methoxy-2-methyl-1H-indol-3-yl)butanoyl]piperazine-1-carboxylate | 71% inhibition at 0.005 mM | Rattus norvegicus | |
ZD-2138 | - |
Rattus norvegicus | |
zileuton | 87% inhibition at 0.005 mM | Rattus norvegicus |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
(6E,8Z,11Z,14Z)-(5S)-5-hydroperoxyeicosa-6,8,11,14-tetraenoate | Rattus norvegicus | - |
leukotriene A4 + H2O | is unstable and metabolized to leukotriene B4 | ? | |
arachidonic acid + O2 | Rattus norvegicus | - |
(6E,8Z,11Z,14Z)-(5S)-5-hydroperoxyeicosa-6,8,11,14-tetraenoate | - |
? | |
additional information | Rattus norvegicus | 5-LOX is the key enzyme in the biosynthesis of leukotrienes through catalyzing the initial two steps in conversion of arachidonic acid to leukotrienes | ? | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Rattus norvegicus | P12527 | - |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
leukocyte | peritoneal | Rattus norvegicus | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
(6E,8Z,11Z,14Z)-(5S)-5-hydroperoxyeicosa-6,8,11,14-tetraenoate | - |
Rattus norvegicus | leukotriene A4 + H2O | - |
? | |
(6E,8Z,11Z,14Z)-(5S)-5-hydroperoxyeicosa-6,8,11,14-tetraenoate | - |
Rattus norvegicus | leukotriene A4 + H2O | is unstable and metabolized to leukotriene B4 | ? | |
arachidonic acid + O2 | - |
Rattus norvegicus | (6E,8Z,11Z,14Z)-(5S)-5-hydroperoxyeicosa-6,8,11,14-tetraenoate | - |
? | |
additional information | 5-LOX is the key enzyme in the biosynthesis of leukotrienes through catalyzing the initial two steps in conversion of arachidonic acid to leukotrienes | Rattus norvegicus | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
5-lipoxygenase | - |
Rattus norvegicus |
5-LOX | - |
Rattus norvegicus |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00074 | - |
- |
Rattus norvegicus | tert-butyl 4-[4-(1H-indol-3-yl)butanoyl]piperazine-1-carboxylate | |
0.00083 | - |
- |
Rattus norvegicus | zileuton | |
0.00085 | - |
- |
Rattus norvegicus | 1-benzyl-3-(4-oxo-4-piperazin-1-ylbutyl)-1H-indole | |
0.00087 | - |
- |
Rattus norvegicus | 1-(3,4-dichlorobenzyl)-3-(2-morpholin-4-yl-2-oxoethyl)-1H-indole | |
0.00095 | - |
- |
Rattus norvegicus | 1-benzyl-5-chloro-2-methyl-3-(4-morpholin-4-yl-4-oxobutyl)-1H-indole | |
0.00133 | - |
- |
Rattus norvegicus | 5-chloro-2-methyl-3-(4-morpholin-4-yl-4-oxobutyl)-1H-indole | |
0.00206 | - |
- |
Rattus norvegicus | 3-(4-morpholin-4-yl-4-oxobutyl)-1H-indole | |
0.00225 | - |
- |
Rattus norvegicus | 1-(4-chlorophenoxy)-5-methoxy-2-methyl-3-(4-morpholin-4-yl-4-oxobutyl)-1H-indole | |
0.00238 | - |
- |
Rattus norvegicus | 3-[2-[3-fluoro-5-(4-methoxytetrahydro-2H-pyran-4-yl)phenoxy]ethyl]-1H-indole | |
0.00316 | - |
- |
Rattus norvegicus | 5-methoxy-2-methyl-3-(4-morpholin-4-yl-4-oxobutyl)-1H-indole | |
0.00317 | - |
- |
Rattus norvegicus | 1-benzyl-3-(3-morpholin-4-yl-3-oxopropyl)-1H-indole | |
0.074 | - |
- |
Rattus norvegicus | 4-(1-benzyl-1H-indol-3-yl)-1-morpholinobutan-1-one |