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Literature summary for 3.1.1.4 extracted from

  • Hess, M.; Schulze Elfringhoff, A.; Lehr, M.
    1-(5-Carboxy- and 5-carbamoylindol-1-yl)propan-2-ones as inhibitors of human cytosolic phospholipase A2alpha: bioisosteric replacement of the carboxylic acid and carboxamide moiety (2007), Bioorg. Med. Chem., 15, 2883-2891.
    View publication on PubMed
Search for more literature for 3.1.1.4

Inhibitors

Inhibitors Comment Organism Structure
1-(4-octylphenoxy)-3-[5-(1H-tetrazol-5-yl)indol-1-yl]propan-2-one inhibits isozyme cPLA2alpha Homo sapiens
1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-sulfonamide inhibits isozyme cPLA2alpha Homo sapiens
1-[5-(morpholine-4-carbonyl)indol-1-yl]-3-(4-octylphenoxy)propan-2-one inhibits isozyme cPLA2alpha Homo sapiens
3-(1-[3-(4-octylphenoxy)-2-oxopropyl]indol-5-yl)-4,5-dihydro-1,2,4-oxadiazol-5-one inhibits isozyme cPLA2alpha Homo sapiens
5-(1-[3-(4-octylphenoxy)-2-oxopropyl]indol-5-ylmethylidene)thiazolidine-2,4-dione inhibits isozyme cPLA2alpha Homo sapiens
indole-5-carboxamide inhibits isozyme cPLA2alpha Homo sapiens
indole-5-carboxylic acid inhibits isozyme cPLA2alpha Homo sapiens
additional information no inhibition of isozyme cPLA2alpha by 1-[5-(3-benzyl-1,2,4-oxadiazol-5-yl)indol-1-yl]-3-(4-octylphenoxy)propan-2-one and 1-[5-(3-ethyl-1,2,4-oxadiazol-5-yl)indol-1-yl]-3-(4-octylphenoxy)propan-2-one Homo sapiens
N,N-dimethyl-1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-carboxamide inhibits isozyme cPLA2alpha Homo sapiens
N,N-dimethyl-1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-sulfonamide inhibits isozyme cPLA2alpha Homo sapiens
N-methyl-1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-carboxamide inhibits isozyme cPLA2alpha Homo sapiens
N-methyl-1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-sulfonamide inhibits isozyme cPLA2alpha Homo sapiens

Localization

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

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-stearoyl-2-arachidonoyl-sn-glycero-3-phosphocholine + H2O
-
 Homo sapiens 1-stearoyl-sn-glycero-3-phosphocholine + arachidonate
-
 ?

Synonyms

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000035
-
-
 Homo sapiens indole-5-carboxylic acid
0.00012
-
-
 Homo sapiens indole-5-carboxamide
0.00031
-
-
 Homo sapiens N-methyl-1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-sulfonamide
0.00037
-
-
 Homo sapiens N-methyl-1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-carboxamide
0.00039
-
-
 Homo sapiens 1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-sulfonamide
0.0005
-
-
 Homo sapiens 1-[5-(morpholine-4-carbonyl)indol-1-yl]-3-(4-octylphenoxy)propan-2-one
0.0005
-
-
 Homo sapiens N,N-dimethyl-1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-sulfonamide
0.00084
-
-
 Homo sapiens N,N-dimethyl-1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-carboxamide
0.0011
-
-
 Homo sapiens 1-(4-octylphenoxy)-3-[5-(1H-tetrazol-5-yl)indol-1-yl]propan-2-one
0.0035
-
-
 Homo sapiens 3-(1-[3-(4-octylphenoxy)-2-oxopropyl]indol-5-yl)-4,5-dihydro-1,2,4-oxadiazol-5-one
0.01
-
 above Homo sapiens 5-(1-[3-(4-octylphenoxy)-2-oxopropyl]indol-5-ylmethylidene)thiazolidine-2,4-dione