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Literature summary for 3.1.1.4 extracted from

  • Arnsmann, M.; Hanekamp, W.; Elfringhoff, A.S.; Lehr, M.
    Structure-activity relationship studies on 1-(2-oxopropyl)indole-5-carboxylic acids acting as inhibitors of cytosolic phospholipase A2. Effect of substituents at the indole 3-position on activity, solubility, and metabolic stability (2017), Eur. J. Med. Chem., 125, 1107-1114 .
    View publication on PubMed

Application

Application Comment Organism
pharmacology the enzyme is an attractive target for the development of anti-inflammatory drugs Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
-
Homo sapiens
3-(2-methylpropanoyl)-1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indole-5-carboxylic acid
-
Homo sapiens
3-(2-methylpropanoyl)-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
-
Homo sapiens
3-(3-carboxypropanoyl)-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
-
Homo sapiens
3-(4-hydroxybutanoyl)-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
-
Homo sapiens
3-(4-methoxybutanoyl)-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
-
Homo sapiens
3-(5-carboxypentanoyl)-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
-
Homo sapiens
3-(6-hydroxyhexanoyl)-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
-
Homo sapiens
3-(6-methoxyhexanoyl)-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
-
Homo sapiens
3-butanoyl-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
-
Homo sapiens
3-hexanoyl-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
-
Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
cytosol
-
Homo sapiens 5829
-

Organism

Organism UniProt Comment Textmining
Homo sapiens P47712
-
-

Source Tissue

Source Tissue Comment Organism Textmining
blood platelet
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1-stearoyl-2-arachidonoyl-sn-glycero-3-phosphocholine + H2O
-
Homo sapiens 1-stearoyl-sn-glycero-3-phosphocholine + arachidonic acid
-
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Synonyms

Synonyms Comment Organism
cPLA2alpha
-
Homo sapiens
phospholipase A2alpha
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00001
-
pH and temperature not specified in the publication Homo sapiens 3-butanoyl-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
0.00001
-
pH and temperature not specified in the publication Homo sapiens 3-(2-methylpropanoyl)-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
0.000012
-
pH and temperature not specified in the publication Homo sapiens 3-(2-methylpropanoyl)-1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indole-5-carboxylic acid
0.000015
-
pH and temperature not specified in the publication Homo sapiens 3-(4-methoxybutanoyl)-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
0.000022
-
pH and temperature not specified in the publication Homo sapiens 3-(5-carboxypentanoyl)-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
0.000023
-
pH and temperature not specified in the publication Homo sapiens 3-(4-hydroxybutanoyl)-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
0.000031
-
pH and temperature not specified in the publication Homo sapiens 3-(6-hydroxyhexanoyl)-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
0.000049
-
pH and temperature not specified in the publication Homo sapiens 3-(6-methoxyhexanoyl)-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
0.000071
-
pH and temperature not specified in the publication Homo sapiens 3-hexanoyl-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
0.00021
-
pH and temperature not specified in the publication Homo sapiens 3-(3-carboxypropanoyl)-1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid
0.00035
-
pH and temperature not specified in the publication Homo sapiens 1-[3-(4-octylphenoxy)-2-oxopropyl]-1H-indole-5-carboxylic acid

General Information

General Information Comment Organism
metabolism key enzyme in the biosynthesis of pro-inflammatory lipid mediators Homo sapiens