Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(5E)-5-(4-methoxybenzylidene)-3-[1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indol-5-yl]-1,3-thiazolidine-2,4-dione | - |
Rattus norvegicus | |
1-(2-oxo-3-[4-[4-(trifluoromethyl)phenoxy]phenoxy]propyl)-1H-indole-5-carboxylic acid | 21% inhibition at 0.01 mM | Rattus norvegicus | |
1-(2-oxo-3-[[4'-(propan-2-yl)biphenyl-4-yl]oxy]propyl)-1H-indole-5-carboxylic acid | - |
Rattus norvegicus | |
1-(4-octylphenoxy)-3-[5-(1H-tetrazol-5-yl)-1H-indol-1-yl]propan-2-one | - |
Rattus norvegicus | |
1-([1,3]oxazolo[4,5-b]pyridin-2-yl)-6-phenylhexan-1-one | - |
Rattus norvegicus | |
1-[1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indol-5-yl]-1H-benzimidazole-7-carboxylic acid | - |
Rattus norvegicus | |
1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indole-5-carboxylic acid | - |
Rattus norvegicus | |
1-[2-oxo-3-[4-(2-phenoxyethoxy)phenoxy]propyl]-1H-indole-5-carboxylic acid | - |
Rattus norvegicus | |
1-[2-oxo-3-[4-(2-phenylpropan-2-yl)phenoxy]propyl]-1H-indole-5-carboxylic acid | - |
Rattus norvegicus | |
1-[3-(4-benzylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid | - |
Rattus norvegicus | |
1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indazole-5-carboxylic acid | - |
Rattus norvegicus | |
1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxamide | - |
Rattus norvegicus | |
1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid | - |
Rattus norvegicus | |
1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-sulfonamide | - |
Rattus norvegicus | |
1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-carboxylic acid | - |
Homo sapiens | |
1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-carboxylic acid | structure-activity relationship, overview | Rattus norvegicus | |
1-[3-(biphenyl-2-yloxy)-2-oxopropyl]-1H-indole-5-carboxylic acid | - |
Rattus norvegicus | |
1-[3-(biphenyl-3-yloxy)-2-oxopropyl]-1H-indole-5-carboxylic acid | - |
Rattus norvegicus | |
1-[3-(biphenyl-4-yloxy)-2-oxopropyl]-1H-indole-5-carboxylic acid | - |
Rattus norvegicus | |
1-[3-[(3'-chlorobiphenyl-4-yl)oxy]-2-oxopropyl]-1H-indole-5-carboxylic acid | - |
Rattus norvegicus | |
1-[3-[(3'-fluorobiphenyl-4-yl)oxy]-2-oxopropyl]-1H-indole-5-carboxylic acid | - |
Rattus norvegicus | |
1-[3-[(3-chlorobiphenyl-4-yl)oxy]-2-oxopropyl]-1H-indole-5-carboxylic acid | - |
Rattus norvegicus | |
1-[3-[(3-fluorobiphenyl-4-yl)oxy]-2-oxopropyl]-1H-indole-5-carboxylic acid | - |
Rattus norvegicus | |
1-[3-[(3-methoxybiphenyl-4-yl)oxy]-2-oxopropyl]-1H-indole-5-carboxylic acid | - |
Rattus norvegicus | |
1-[3-[(3-methylbiphenyl-4-yl)oxy]-2-oxopropyl]-1H-indole-5-carboxylic acid | 39% inhibition at 0.01 mM | Rattus norvegicus | |
1-[3-[(4'-chlorobiphenyl-4-yl)oxy]-2-oxopropyl]-1H-indole-5-carboxylic acid | - |
Rattus norvegicus | |
1-[3-[(4'-fluorobiphenyl-4-yl)oxy]-2-oxopropyl]-1H-indole-5-carboxylic acid | - |
Rattus norvegicus | |
1-[3-[(4'-methoxybiphenyl-4-yl)oxy]-2-oxopropyl]-1H-indole-5-carboxylic acid | - |
Rattus norvegicus | |
1-[3-[(4'-methylbiphenyl-4-yl)oxy]-2-oxopropyl]-1H-indole-5-carboxylic acid | - |
Rattus norvegicus | |
1-[3-[4-(4-fluorophenyl)phenoxy]-2-oxopropyl]indazole-5-carboxylic acid | - |
Rattus norvegicus | |
1-[3-[4-(decyloxy)phenoxy]-2-oxopropyl]-1H-indole-5-carboxylic acid | - |
Rattus norvegicus | |
1-[3-[4-(heptyloxy)phenoxy]-2-oxopropyl]-1H-indole-5-carboxylic acid | - |
Rattus norvegicus | |
1-[3-[4-(hexyloxy)phenoxy]-2-oxopropyl]-1H-indole-5-carboxylic acid | - |
Rattus norvegicus | |
1-[3-[4-(nonyloxy)phenoxy]-2-oxopropyl]-1H-indole-5-carboxylic acid | - |
Rattus norvegicus | |
1-[3-[4-(octyloxy)phenoxy]-2-oxopropyl]-1H-indole-5-carboxylic acid | - |
Rattus norvegicus | |
1-[5-(3-benzyl-1,2,4-oxadiazol-5-yl)-1H-indol-1-yl]-3-(4-octylphenoxy)propan-2-one | - |
Rattus norvegicus | |
1-[5-(3-ethyl-1,2,4-oxadiazol-5-yl)-1H-indol-1-yl]-3-(4-octylphenoxy)propan-2-one | - |
Rattus norvegicus | |
1-[5-(morpholin-4-ylcarbonyl)-1H-indol-1-yl]-3-(4-octylphenoxy)propan-2-one | - |
Rattus norvegicus | |
3'-carbamoylbiphenyl-3-yl cyclohexylcarbamate | - |
Rattus norvegicus | |
4-[3-[4-(decyloxy)phenoxy]-2-oxopropoxy]benzoic acid | - |
Rattus norvegicus | |
methyl (5Z,8Z,11Z,14Z)-icosa-5,8,11,14-tetraen-1-ylphosphonofluoridate | - |
Rattus norvegicus | |
additional information | 1-(3-biaryloxy-2-oxopropyl)indole-5-carboxylic acids and related compounds can act as dual inhibitors of human cytosolic phospholipase A2alpha, EC 3.1.1.4, and fatty acid amide hydrolase, overview. Substituents at the indole 3- and 5-positions and replacement of the indole scaffold of this compound by other heterocycles strongly influences the inhibitory potency against FAAH | Homo sapiens | |
additional information | 1-(3-biaryloxy-2-oxopropyl)indole-5-carboxylic acids and related compounds can act as dual inhibitors of cytosolic phospholipase A2alpha, EC 3.1.1.4, and fatty acid amide hydrolase, overview. Substituents at the indole 3- and 5-positions and replacement of the indole scaffold of this compound by other heterocycles strongly influences the inhibitory potency against FAAH. No inhibition by 1-[3-(biphenyl-2-yloxy)-2-oxopropyl]-1H-indole-5-carboxylic acid, N-methyl-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxamide, N,N-dimethyl-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxamide, 1-[5-(morpholin-4-ylcarbonyl)-1H-indol-1-yl]-3-(4-octylphenoxy)propan-2-one, (5E)-5-(4-methoxybenzylidene)-3-[1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indol-5-yl]-1,3-thiazolidine-2,4-dione, 1-[5-(3-benzyl-1,2,4-oxadiazol-5-yl)-1H-indol-1-yl]-3-(4-octylphenoxy)propan-2-one, 1-[5-(3-ethyl-1,2,4-oxadiazol-5-yl)-1H-indol-1-yl]-3-(4-octylphenoxy)propan-2-one, 1-[1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indol-5-yl]-1H-benzimidazole-7-carboxylic acid, and 1-(4-octylphenoxy)-3-[5-(1H-tetrazol-5-yl)-1H-indol-1-yl]propan-2-one at 0.01 mM | Rattus norvegicus | |
N,N-dimethyl-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxamide | - |
Rattus norvegicus | |
N,N-dimethyl-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-sulfonamide | - |
Rattus norvegicus | |
N-methyl-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxamide | - |
Rattus norvegicus | |
N-methyl-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-sulfonamide | - |
Rattus norvegicus |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
microsome | - |
Homo sapiens | - |
- |
microsome | - |
Rattus norvegicus | - |
- |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Rattus norvegicus | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
brain | - |
Rattus norvegicus | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide + H2O | - |
Rattus norvegicus | 4-pyren-1-ylbutanoic acid + ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
FAAH | - |
Homo sapiens |
FAAH | - |
Rattus norvegicus |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.000006 | - |
pH and temperature not specified in the publication | Rattus norvegicus | 1-([1,3]oxazolo[4,5-b]pyridin-2-yl)-6-phenylhexan-1-one | |
0.000025 | - |
pH and temperature not specified in the publication | Rattus norvegicus | methyl (5Z,8Z,11Z,14Z)-icosa-5,8,11,14-tetraen-1-ylphosphonofluoridate | |
0.000053 | - |
pH and temperature not specified in the publication | Rattus norvegicus | 4-[3-[4-(decyloxy)phenoxy]-2-oxopropoxy]benzoic acid | |
0.00009 | - |
pH and temperature not specified in the publication | Rattus norvegicus | 1-[3-[4-(4-fluorophenyl)phenoxy]-2-oxopropyl]indazole-5-carboxylic acid | |
0.00016 | - |
pH and temperature not specified in the publication | Rattus norvegicus | 1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indazole-5-carboxylic acid | |
0.00022 | - |
pH and temperature not specified in the publication | Rattus norvegicus | 3'-carbamoylbiphenyl-3-yl cyclohexylcarbamate | |
0.00023 | - |
pH and temperature not specified in the publication | Rattus norvegicus | 1-[3-[(3'-chlorobiphenyl-4-yl)oxy]-2-oxopropyl]-1H-indole-5-carboxylic acid | |
0.00024 | - |
pH and temperature not specified in the publication | Rattus norvegicus | 1-[3-[(4'-fluorobiphenyl-4-yl)oxy]-2-oxopropyl]-1H-indole-5-carboxylic acid | |
0.00025 | - |
pH and temperature not specified in the publication | Rattus norvegicus | 1-[3-[(3'-fluorobiphenyl-4-yl)oxy]-2-oxopropyl]-1H-indole-5-carboxylic acid | |
0.00046 | - |
pH and temperature not specified in the publication | Rattus norvegicus | 1-[3-(biphenyl-4-yloxy)-2-oxopropyl]-1H-indole-5-carboxylic acid | |
0.00053 | - |
pH and temperature not specified in the publication | Rattus norvegicus | 1-[3-[(4'-chlorobiphenyl-4-yl)oxy]-2-oxopropyl]-1H-indole-5-carboxylic acid | |
0.00053 | - |
pH and temperature not specified in the publication | Rattus norvegicus | 1-[3-[(4'-methoxybiphenyl-4-yl)oxy]-2-oxopropyl]-1H-indole-5-carboxylic acid | |
0.00053 | - |
pH and temperature not specified in the publication | Rattus norvegicus | N,N-dimethyl-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-sulfonamide | |
0.00058 | - |
pH and temperature not specified in the publication | Rattus norvegicus | 1-[3-[(4'-methylbiphenyl-4-yl)oxy]-2-oxopropyl]-1H-indole-5-carboxylic acid | |
0.00059 | - |
pH and temperature not specified in the publication | Rattus norvegicus | 1-[3-[(3-fluorobiphenyl-4-yl)oxy]-2-oxopropyl]-1H-indole-5-carboxylic acid | |
0.00075 | - |
pH and temperature not specified in the publication | Rattus norvegicus | N-methyl-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-sulfonamide | |
0.0012 | - |
pH and temperature not specified in the publication | Rattus norvegicus | 1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indole-5-carboxylic acid | |
0.0016 | - |
pH and temperature not specified in the publication | Rattus norvegicus | 1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-sulfonamide | |
0.0017 | - |
pH and temperature not specified in the publication | Rattus norvegicus | 1-[2-oxo-3-[4-(2-phenoxyethoxy)phenoxy]propyl]-1H-indole-5-carboxylic acid | |
0.0018 | - |
pH and temperature not specified in the publication | Rattus norvegicus | 1-[3-[4-(nonyloxy)phenoxy]-2-oxopropyl]-1H-indole-5-carboxylic acid | |
0.0019 | - |
pH and temperature not specified in the publication | Rattus norvegicus | 1-[3-(4-benzylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid | |
0.0022 | - |
pH and temperature not specified in the publication | Rattus norvegicus | 1-[3-[4-(octyloxy)phenoxy]-2-oxopropyl]-1H-indole-5-carboxylic acid | |
0.0023 | - |
pH and temperature not specified in the publication | Rattus norvegicus | 1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid | |
0.0026 | - |
pH and temperature not specified in the publication | Rattus norvegicus | 1-[3-[4-(decyloxy)phenoxy]-2-oxopropyl]-1H-indole-5-carboxylic acid | |
0.0029 | - |
pH and temperature not specified in the publication | Rattus norvegicus | 1-[2-oxo-3-[4-(2-phenylpropan-2-yl)phenoxy]propyl]-1H-indole-5-carboxylic acid | |
0.0034 | - |
pH and temperature not specified in the publication | Rattus norvegicus | 1-[3-(biphenyl-3-yloxy)-2-oxopropyl]-1H-indole-5-carboxylic acid | |
0.0034 | - |
pH and temperature not specified in the publication | Rattus norvegicus | 1-[3-[4-(heptyloxy)phenoxy]-2-oxopropyl]-1H-indole-5-carboxylic acid | |
0.0035 | - |
pH and temperature not specified in the publication | Rattus norvegicus | 1-[3-[4-(hexyloxy)phenoxy]-2-oxopropyl]-1H-indole-5-carboxylic acid | |
0.005 | - |
pH and temperature not specified in the publication | Rattus norvegicus | 1-[3-[(3-chlorobiphenyl-4-yl)oxy]-2-oxopropyl]-1H-indole-5-carboxylic acid | |
0.0051 | - |
pH and temperature not specified in the publication | Rattus norvegicus | 1-(2-oxo-3-[[4'-(propan-2-yl)biphenyl-4-yl]oxy]propyl)-1H-indole-5-carboxylic acid | |
0.0064 | - |
pH and temperature not specified in the publication | Rattus norvegicus | 1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxamide | |
0.0074 | - |
pH and temperature not specified in the publication | Rattus norvegicus | 1-[3-[(3-methoxybiphenyl-4-yl)oxy]-2-oxopropyl]-1H-indole-5-carboxylic acid |