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Literature summary for 3.1.1.4 extracted from

  • Touaibia, M.; Djimde, A.; Cao, F.; Boilard, E.; Bezzine, S.; Lambeau, G.; Redeuilh, C.; Lamouri, A.; Massicot, F.; Chau, F.; Dong, C.Z.; Heymans, F.
    Inhibition of secreted phospholipase A2. 4-glycerol derivatives of 4,5-dihydro-3-(4-tetradecyloxybenzyl)-1,2,4-4H-oxadiazol-5-one with broad activities (2007), J. Med. Chem., 50, 1618-1626.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(+-)-3-O-[4-(4,5-dihydro-5-oxo-1,2,4-4H-oxadiazol-3-yl)phenyl]-2-O-tetradecyl-1-O-triphenylmethylglycerol
-
Homo sapiens
(+-)-3-O-[4-(4,5-dihydro-5-oxo-1,2,4-4H-oxadiazol-3-yl)phenyl]-2-O-tetradecyl-1-O-triphenylmethylglycerol
-
Sus scrofa
3,3'-[[2-(pentyloxy)propane-1,3-diyl]bis(oxybenzene-4,1-diylethane-2,1-diyl)]bis(1,2,4-oxadiazol-5(4H)-one)
-
Homo sapiens
3,3'-[[2-(pentyloxy)propane-1,3-diyl]bis(oxybenzene-4,1-diylethane-2,1-diyl)]bis(1,2,4-oxadiazol-5(4H)-one)
-
Sus scrofa
3,3'-[[2-(tetradecyloxy)propane-1,3-diyl]bis(oxybenzene-4,1-diylethane-2,1-diyl)]bis(1,2,4-oxadiazol-5(4H)-one)
-
Homo sapiens
3,3'-[[2-(tetradecyloxy)propane-1,3-diyl]bis(oxybenzene-4,1-diylethane-2,1-diyl)]bis(1,2,4-oxadiazol-5(4H)-one)
-
Sus scrofa
3,3'-[[2-(tetradecyloxy)propane-1,3-diyl]bis(oxybenzene-4,1-diylmethanediyl)]bis(1,2,4-oxadiazol-5(4H)-one)
-
Homo sapiens
3,3'-[[2-(tetradecyloxy)propane-1,3-diyl]bis(oxybenzene-4,1-diylmethanediyl)]bis(1,2,4-oxadiazol-5(4H)-one)
-
Sus scrofa
3,3'-[[3-(tetradecyloxy)propane-1,2-diyl]bis(oxybenzene-4,1-diylethane-2,1-diyl)]bis(1,2,4-oxadiazol-5(4H)-one)
-
Homo sapiens
3,3'-[[3-(tetradecyloxy)propane-1,2-diyl]bis(oxybenzene-4,1-diylethane-2,1-diyl)]bis(1,2,4-oxadiazol-5(4H)-one)
-
Sus scrofa
3,3'-[[3-(tetradecyloxy)propane-1,2-diyl]bis(oxybenzene-4,1-diylmethanediyl)]bis(1,2,4-oxadiazol-5(4H)-one)
-
Homo sapiens
3,3'-[[3-(tetradecyloxy)propane-1,2-diyl]bis(oxybenzene-4,1-diylmethanediyl)]bis(1,2,4-oxadiazol-5(4H)-one)
-
Sus scrofa
3-[4-[3-(4-butylphenoxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
Homo sapiens
3-[4-[3-(4-butylphenoxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
Sus scrofa
3-[4-[3-(4-methylphenoxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
Homo sapiens
3-[4-[3-(4-methylphenoxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
Sus scrofa
3-[4-[3-(decyloxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
Homo sapiens
3-[4-[3-(decyloxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
Sus scrofa
3-[4-[3-(diphenylmethoxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
Homo sapiens
3-[4-[3-(diphenylmethoxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
Sus scrofa
3-[4-[3-(pentyloxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
Homo sapiens
3-[4-[3-(pentyloxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
Sus scrofa
3-[4-[3-ethoxy-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
Homo sapiens
3-[4-[3-ethoxy-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
Sus scrofa
Me-Indoxam
-
Homo sapiens
Me-Indoxam
-
Sus scrofa
additional information inhibitor synthesis and screening, overview, inhibitory potency of 3-[4-[3-ethoxy-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one derivatives with the different isozymes, overview Homo sapiens
additional information inhibitor screening, overview, inhibitory potency of 3-[4-[3-ethoxy-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one derivatives, overview Sus scrofa

Localization

Localization Comment Organism GeneOntology No. Textmining
extracellular
-
Homo sapiens
-
-
extracellular
-
Sus scrofa
-
-

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
isozymes hGIIA sPLA2, hGIB sPLA2, hGX sPLA2, and hGV sPLA2
-
Sus scrofa
-
isozyme hGIB sPLA2
-

Source Tissue

Source Tissue Comment Organism Textmining
commercial preparation from pancreas Sus scrofa
-
pancreas
-
Sus scrofa
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
(+/-)-3-O-(4-cyanomethylphenyl)-1,2-O-di-n-heptylglycerol + H2O
-
Homo sapiens ?
-
?
(+/-)-3-O-(4-cyanomethylphenyl)-1,2-O-di-n-heptylglycerol + H2O
-
Sus scrofa ?
-
?
(+/-)-3-O-(4-hydroxymethylphenyl)-1,2-O-di-n-heptylglycerol + H2O
-
Homo sapiens ?
-
?
(+/-)-3-O-(4-hydroxymethylphenyl)-1,2-O-di-n-heptylglycerol + H2O
-
Sus scrofa ?
-
?

Synonyms

Synonyms Comment Organism
PLA2
-
Homo sapiens
PLA2
-
Sus scrofa
secreted phospholipase A2
-
Homo sapiens
secreted phospholipase A2
-
Sus scrofa
sPLA2
-
Homo sapiens
sPLA2
-
Sus scrofa

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
assay at Homo sapiens
7.5
-
assay at Sus scrofa

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
additional information
-
-
Homo sapiens additional information
0.00028
-
pH 7.5, isozyme hGIIA sPLA2 Homo sapiens 3-[4-[3-(decyloxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.00028
-
pH 7.5, isozyme hGIIA sPLA2 Homo sapiens 3-[4-[3-(diphenylmethoxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.00029
-
pH 7.5, isozyme hGIIA sPLA2 Homo sapiens 3-[4-[3-(4-butylphenoxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.00055
-
pH 7.5, isozyme hGV sPLA2 Homo sapiens 3-[4-[3-(decyloxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.0007
-
pH 7.5, isozyme hGV sPLA2 Homo sapiens (+-)-3-O-[4-(4,5-dihydro-5-oxo-1,2,4-4H-oxadiazol-3-yl)phenyl]-2-O-tetradecyl-1-O-triphenylmethylglycerol
0.0009
-
pH 7.5, isozyme hGIIA sPLA2 Homo sapiens (+-)-3-O-[4-(4,5-dihydro-5-oxo-1,2,4-4H-oxadiazol-3-yl)phenyl]-2-O-tetradecyl-1-O-triphenylmethylglycerol
0.001
-
pH 7.5, isozyme hGX sPLA2 Homo sapiens 3-[4-[3-(decyloxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.0013
-
pH 7.5, isozyme hGX sPLA2 Homo sapiens (+-)-3-O-[4-(4,5-dihydro-5-oxo-1,2,4-4H-oxadiazol-3-yl)phenyl]-2-O-tetradecyl-1-O-triphenylmethylglycerol
0.002
-
pH 7.5, isozyme hGV sPLA2 Homo sapiens 3-[4-[3-(diphenylmethoxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.0021
-
pH 7.5, isozyme hGIIA sPLA2 Homo sapiens 3,3'-[[2-(tetradecyloxy)propane-1,3-diyl]bis(oxybenzene-4,1-diylethane-2,1-diyl)]bis(1,2,4-oxadiazol-5(4H)-one)
0.0022
-
pH 7.5, isozyme hGIB sPLA2 Sus scrofa 3-[4-[3-(4-butylphenoxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.0031
-
pH 7.5, isozyme hGIIA sPLA2 Homo sapiens 3,3'-[[3-(tetradecyloxy)propane-1,2-diyl]bis(oxybenzene-4,1-diylethane-2,1-diyl)]bis(1,2,4-oxadiazol-5(4H)-one)
0.0053
-
pH 7.5, isozyme hGX sPLA2 Homo sapiens 3-[4-[3-(diphenylmethoxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.0056
-
pH 7.5, isozyme hGIB sPLA2 Sus scrofa 3-[4-[3-(diphenylmethoxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.0058
-
pH 7.5, isozyme hGIB sPLA2 Homo sapiens (+-)-3-O-[4-(4,5-dihydro-5-oxo-1,2,4-4H-oxadiazol-3-yl)phenyl]-2-O-tetradecyl-1-O-triphenylmethylglycerol
0.0083
-
pH 7.5, isozyme hGIIA sPLA2 Homo sapiens 3-[4-[3-(pentyloxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.01
-
pH 7.5, isozyme hGIB sPLA2 Homo sapiens 3-[4-[3-(decyloxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.012
-
pH 7.5, isozyme hGX sPLA2 Homo sapiens 3-[4-[3-(4-butylphenoxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.014
-
pH 7.5, isozyme hGX sPLA2 Homo sapiens 3-[4-[3-(4-methylphenoxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.0148
-
pH 7.5, isozyme hGIIA sPLA2 Homo sapiens 3-[4-[3-(4-methylphenoxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.015
-
pH 7.5, isozyme hGIB sPLA2 Homo sapiens 3-[4-[3-(4-butylphenoxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.018
-
pH 7.5, isozyme hGIB sPLA2 Homo sapiens 3-[4-[3-(diphenylmethoxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.021
-
pH 7.5, isozyme hGIIA sPLA2 Homo sapiens 3,3'-[[3-(tetradecyloxy)propane-1,2-diyl]bis(oxybenzene-4,1-diylmethanediyl)]bis(1,2,4-oxadiazol-5(4H)-one)
0.022
-
pH 7.5, isozyme hGV sPLA2 Homo sapiens 3-[4-[3-(4-butylphenoxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.025
-
pH 7.5, isozyme hGIB sPLA2 Sus scrofa 3-[4-[3-(4-methylphenoxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.0298
-
pH 7.5, isozyme hGIIA sPLA2 Homo sapiens 3-[4-[3-ethoxy-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.0305
-
above, pH 7.5, isozyme hGIIA sPLA2 Homo sapiens 3,3'-[[2-(pentyloxy)propane-1,3-diyl]bis(oxybenzene-4,1-diylethane-2,1-diyl)]bis(1,2,4-oxadiazol-5(4H)-one)
0.0399
-
pH 7.5, isozyme hGIB sPLA2 Sus scrofa 3,3'-[[2-(tetradecyloxy)propane-1,3-diyl]bis(oxybenzene-4,1-diylethane-2,1-diyl)]bis(1,2,4-oxadiazol-5(4H)-one)
0.04
-
pH 7.5, isozyme hGIB sPLA2 Sus scrofa 3-[4-[3-ethoxy-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.0477
-
above, pH 7.5, isozyme hGIIA sPLA2 Homo sapiens 3,3'-[[2-(tetradecyloxy)propane-1,3-diyl]bis(oxybenzene-4,1-diylmethanediyl)]bis(1,2,4-oxadiazol-5(4H)-one)
0.05
-
pH 7.5, isozyme hGIB sPLA2 Sus scrofa 3-O-[4-(4,5-dihydro-5-oxo-1,2,4-4H-oxadiazol-3-yl)phenyl]-2-O-tetradecyl-1-O-triphenylmethylglycerol
0.0578
-
pH 7.5, isozyme hGIB sPLA2 Sus scrofa 3,3'-[[3-(tetradecyloxy)propane-1,2-diyl]bis(oxybenzene-4,1-diylethane-2,1-diyl)]bis(1,2,4-oxadiazol-5(4H)-one)
0.0636
-
pH 7.5, isozyme hGIB sPLA2 Sus scrofa 3,3'-[[3-(tetradecyloxy)propane-1,2-diyl]bis(oxybenzene-4,1-diylmethanediyl)]bis(1,2,4-oxadiazol-5(4H)-one)
0.1
-
above, pH 7.5, isozyme hGIB sPLA2 Sus scrofa 3,3'-[[2-(tetradecyloxy)propane-1,3-diyl]bis(oxybenzene-4,1-diylmethanediyl)]bis(1,2,4-oxadiazol-5(4H)-one)
0.1
-
above, pH 7.5, isozyme hGIB sPLA2 Sus scrofa 3,3'-[[2-(pentyloxy)propane-1,3-diyl]bis(oxybenzene-4,1-diylethane-2,1-diyl)]bis(1,2,4-oxadiazol-5(4H)-one)
0.1
-
pH 7.5, isozyme hGIB sPLA2 Sus scrofa 3-[4-[3-(decyloxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.1
-
pH 7.5, isozyme hGIB sPLA2 Homo sapiens 3-[4-[3-(4-methylphenoxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.1
-
pH 7.5, isozyme hGIB sPLA2 Sus scrofa 3-[4-[3-(pentyloxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.1
-
pH 7.5, isozyme hGV sPLA2 Homo sapiens 3-[4-[3-(4-methylphenoxy)-2-(tetradecyloxy)propoxy]benzyl]-1,2,4-oxadiazol-5(4H)-one