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Literature summary for 3.1.1.4 extracted from

  • Fritsche, A.; Elfringhoff, A.S.; Fabian, J.; Lehr, M.
    1-(2-Carboxyindol-5-yloxy)propan-2-ones as inhibitors of human cytosolic phospholipase A2alpha: synthesis, biological activity, metabolic stability, and solubility (2008), Bioorg. Med. Chem., 16, 3489-3500.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(6Z,9Z,12Z,15Z)-1,1,1-trifluorohenicosa-6,9,12,15-tetraen-2-one arachidonic acid with the COOH group replaced by COCF3, i.e. AACOCF3 Homo sapiens
1-(2-dimethylaminoethyl)-5-[3-(4-octylphenoxy)-2-oxopropoxy]indole-2-carboxylic acid
-
Homo sapiens
1-(4-carboxybenzyl)-5-[3-(4-octylphenoxy)-2-oxopropoxy]indole-2-carboxylic acid
-
Homo sapiens
1-(carboxymethyl)-5-[3-(4-octylphenoxy)-2-oxopropoxy]indole-2-carboxylic acid
-
Homo sapiens
1-(carboxypentyl)-5-[3-(4-octylphenoxy)-2-oxopropoxy]indole-2-carboxylic acid
-
Homo sapiens
1-(carboxypropyl)-5-[3-(4-octylphenoxy)-2-oxopropoxy]indole-2-carboxylic acid
-
Homo sapiens
1-benzyl-5-[3-(4-octylphenoxy)-2-oxopropoxy]-indole-2-carboxylic acid
-
Homo sapiens
1-hexyl-5-[3-(4-octylphenoxy)-2-oxopropoxy]indole-2-carboxylic acid
-
Homo sapiens
1-methyl 5-[3-(4-octylphenoxy)-2-oxopropoxy]-indole-2-carboxylic acid
-
Homo sapiens
1-[3-(4-octylphenoxy)-2-oxopropyl]-2,3-dihydro-1H-indole-5-carboxylic acid
-
Homo sapiens
5-[3-(4-octylphenoxy)-2-oxopropoxy]-1-propylindole-2-carboxylic acid
-
Homo sapiens
5-[3-(4-octylphenoxy)-2-oxopropoxy]indole-2-carboxylic acid
-
Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
blood platelet
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1,2-dioleoyl-sn-glycerol + H2O
-
Homo sapiens 1-oleoyl-sn-glycerol + oleic acid
-
?
1-stearoyl-2-arachidonoyl-sn-glycero-3-phosphocholine + H2O
-
Homo sapiens 1-stearoyl-sn-glycero-3-phosphocholine + arachidonic acid
-
?

Synonyms

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

pH Optimum

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
additional information
-
inhibition of cPLA2a activity in the isolated enzyme assay and in the cellular assay, overview Homo sapiens additional information
0.000035
-
pH 7.4 Homo sapiens 1-[3-(4-octylphenoxy)-2-oxopropyl]-2,3-dihydro-1H-indole-5-carboxylic acid
0.0012
-
pH 7.4 Homo sapiens 1-methyl 5-[3-(4-octylphenoxy)-2-oxopropoxy]-indole-2-carboxylic acid
0.0015
-
pH 7.4 Homo sapiens 1-(4-carboxybenzyl)-5-[3-(4-octylphenoxy)-2-oxopropoxy]indole-2-carboxylic acid
0.0021
-
pH 7.4 Homo sapiens 5-[3-(4-octylphenoxy)-2-oxopropoxy]-1-propylindole-2-carboxylic acid
0.0023
-
pH 7.4 Homo sapiens (6Z,9Z,12Z,15Z)-1,1,1-trifluorohenicosa-6,9,12,15-tetraen-2-one
0.0033
-
pH 7.4 Homo sapiens 5-[3-(4-octylphenoxy)-2-oxopropoxy]indole-2-carboxylic acid
0.01
-
pH 7.4 Homo sapiens 1-benzyl-5-[3-(4-octylphenoxy)-2-oxopropoxy]-indole-2-carboxylic acid
0.01
-
above, pH 7.4 Homo sapiens 1-hexyl-5-[3-(4-octylphenoxy)-2-oxopropoxy]indole-2-carboxylic acid
0.01
-
above, pH 7.4 Homo sapiens 1-(2-dimethylaminoethyl)-5-[3-(4-octylphenoxy)-2-oxopropoxy]indole-2-carboxylic acid
0.3
-
pH 7.4 Homo sapiens 1-(carboxymethyl)-5-[3-(4-octylphenoxy)-2-oxopropoxy]indole-2-carboxylic acid
0.4
-
pH 7.4 Homo sapiens 1-(carboxypropyl)-5-[3-(4-octylphenoxy)-2-oxopropoxy]indole-2-carboxylic acid
0.6
-
pH 7.4 Homo sapiens 1-(carboxypentyl)-5-[3-(4-octylphenoxy)-2-oxopropoxy]indole-2-carboxylic acid