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Literature summary for 3.1.1.4 extracted from

  • Boukli, L.; Touaibia, M.; Meddad-Belhabich, N.; Djimde, A.; Park, C.; Kim, J.; Yoon, J.; Lamouri, A.; Heymans, F.
    Design of new potent and selective secretory phospholipase A2 inhibitors. Part 5: Synthesis and biological activity of 1-alkyl-4-[4,5-dihydro-1,2,4-[4H]-oxadiazol-5-one-3-ylmethylbenz-4'-yl(oyl)] piperazines (2008), Bioorg. Med. Chem., 16, 1242-1253.
    View publication on PubMed
Search for more literature for 3.1.1.4

Cloned(Commentary)

Cloned (Comment) Organism
-
 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
3-(2-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]phenyl]ethyl)-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3-(2-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]phenyl]ethyl)-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
3-(3-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]phenyl]propyl)-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3-(3-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]phenyl]propyl)-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
3-[4-(4-hexadecylpiperazin-1-yl)benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3-[4-(4-hexadecylpiperazin-1-yl)benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
3-[4-(4-octadecylpiperazin-1-yl)benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3-[4-(4-octadecylpiperazin-1-yl)benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
3-[4-(4-tetradecylpiperazin-1-yl)benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3-[4-(4-tetradecylpiperazin-1-yl)benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
3-[4-(tetradecyloxy)benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3-[4-(tetradecyloxy)benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
3-[4-[(4-docosylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3-[4-[(4-docosylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
3-[4-[(4-hexadecylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3-[4-[(4-hexadecylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
3-[4-[(4-hexadecylpiperazin-1-yl)carbonyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3-[4-[(4-hexadecylpiperazin-1-yl)carbonyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
3-[4-[(4-hexadecylpiperazin-1-yl)methyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3-[4-[(4-hexadecylpiperazin-1-yl)methyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
3-[4-[(4-hexadecylpiperazin-1-yl)methyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3-[4-[(4-hexadecylpiperazin-1-yl)methyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
3-[4-[(4-icosylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3-[4-[(4-icosylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
3-[4-[(4-octadecylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3-[4-[(4-octadecylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
3-[4-[(4-octadecylpiperazin-1-yl)carbonyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3-[4-[(4-octadecylpiperazin-1-yl)carbonyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
3-[4-[(4-octadecylpiperazin-1-yl)methyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3-[4-[(4-octadecylpiperazin-1-yl)methyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
3-[4-[(4-octadecylpiperazin-1-yl)methyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3-[4-[(4-octadecylpiperazin-1-yl)methyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
3-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
3-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
3-[4-[(4-tetradecylpiperazin-1-yl)methyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3-[4-[(4-tetradecylpiperazin-1-yl)methyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
3-[4-[(4-tetradecylpiperazin-1-yl)methyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3-[4-[(4-tetradecylpiperazin-1-yl)methyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
LY311727
-
 Homo sapiens
LY311727
-
 Sus scrofa
additional information novel potent piperazinic derivatives that show improved anti-PLA2 activity with a high selectivity for human GIIA versus porcine GIB PLA2s compared to the reference compound of LY311727 and that are more active than reference compound II Homo sapiens
additional information novel potent piperazinic derivatives that show improved anti-PLA2 activity with a high selectivity for human GIIA versus porcine GIB PLA2s compared to the reference compound of LY311727 and that are more active than reference compound II Sus scrofa

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Sus scrofa
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
pancreas
-
 Sus scrofa
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1-palmitoyl-2-(10-pyrenyldecanoyl)-sn-glycero-3-phosphate + H2O
-
 Homo sapiens 10-pyrenyldecanoic acid + 1-palmitoyl-sn-glycero-3-phosphate
-
 ?
1-palmitoyl-2-(10-pyrenyldecanoyl)-sn-glycero-3-phosphate + H2O
-
 Sus scrofa 10-pyrenyldecanoic acid + 1-palmitoyl-sn-glycero-3-phosphate
-
 ?

Synonyms

Synonyms Comment Organism
group IIA secretory PLA2
-
 Homo sapiens
group IIA secretory PLA2
-
 Sus scrofa
secretory phospholipase A2
-
 Homo sapiens
secretory phospholipase A2
-
 Sus scrofa
sPLA2 GIB
-
 Sus scrofa
sPLA2 GIIA
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00047
-
-
 Homo sapiens LY311727
0.0008
-
-
 Homo sapiens 3-[4-[(4-octadecylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.0011
-
-
 Homo sapiens 3-[4-[(4-octadecylpiperazin-1-yl)carbonyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
0.0022
-
-
 Homo sapiens 3-[4-[(4-octadecylpiperazin-1-yl)methyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.00271
-
-
 Homo sapiens 3-[4-(4-octadecylpiperazin-1-yl)benzyl]-1,2,4-oxadiazol-5(4H)-one
0.0035
-
-
 Homo sapiens 3-[4-(4-hexadecylpiperazin-1-yl)benzyl]-1,2,4-oxadiazol-5(4H)-one
0.004
-
-
 Homo sapiens 3-[4-[(4-hexadecylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.004
-
-
 Homo sapiens 3-[4-(tetradecyloxy)benzyl]-1,2,4-oxadiazol-5(4H)-one
0.0045
-
-
 Homo sapiens 3-[4-(4-tetradecylpiperazin-1-yl)benzyl]-1,2,4-oxadiazol-5(4H)-one
0.00508
-
-
 Homo sapiens 3-[4-[(4-octadecylpiperazin-1-yl)methyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
0.0053
-
-
 Homo sapiens 3-(3-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]phenyl]propyl)-1,2,4-oxadiazol-5(4H)-one
0.008
-
-
 Sus scrofa LY311727
0.009
-
-
 Homo sapiens 3-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.0187
-
-
 Homo sapiens 3-(2-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]phenyl]ethyl)-1,2,4-oxadiazol-5(4H)-one
0.1
-
-
 Homo sapiens 3-[4-[(4-tetradecylpiperazin-1-yl)methyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
0.1
-
-
 Sus scrofa 3-[4-[(4-tetradecylpiperazin-1-yl)methyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
0.1
-
-
 Homo sapiens 3-[4-[(4-hexadecylpiperazin-1-yl)methyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
0.1
-
-
 Sus scrofa 3-[4-[(4-hexadecylpiperazin-1-yl)methyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
0.1
-
-
 Sus scrofa 3-[4-[(4-octadecylpiperazin-1-yl)methyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
0.1
-
-
 Homo sapiens 3-[4-[(4-tetradecylpiperazin-1-yl)methyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.1
-
-
 Sus scrofa 3-[4-[(4-tetradecylpiperazin-1-yl)methyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.1
-
-
 Homo sapiens 3-[4-[(4-hexadecylpiperazin-1-yl)methyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.1
-
-
 Sus scrofa 3-[4-[(4-hexadecylpiperazin-1-yl)methyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.1
-
-
 Sus scrofa 3-[4-[(4-octadecylpiperazin-1-yl)methyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.1
-
-
 Homo sapiens 3-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
0.1
-
-
 Sus scrofa 3-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
0.1
-
-
 Homo sapiens 3-[4-[(4-hexadecylpiperazin-1-yl)carbonyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
0.1
-
-
 Sus scrofa 3-[4-[(4-hexadecylpiperazin-1-yl)carbonyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
0.1
-
-
 Sus scrofa 3-[4-[(4-octadecylpiperazin-1-yl)carbonyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
0.1
-
-
 Sus scrofa 3-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.1
-
-
 Sus scrofa 3-[4-[(4-hexadecylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.1
-
-
 Sus scrofa 3-[4-[(4-octadecylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.1
-
-
 Homo sapiens 3-[4-[(4-icosylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.1
-
-
 Sus scrofa 3-[4-[(4-icosylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.1
-
-
 Homo sapiens 3-[4-[(4-docosylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.1
-
-
 Sus scrofa 3-[4-[(4-docosylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
0.1
-
-
 Sus scrofa 3-[4-(4-tetradecylpiperazin-1-yl)benzyl]-1,2,4-oxadiazol-5(4H)-one
0.1
-
-
 Sus scrofa 3-[4-(4-hexadecylpiperazin-1-yl)benzyl]-1,2,4-oxadiazol-5(4H)-one
0.1
-
-
 Sus scrofa 3-[4-(4-octadecylpiperazin-1-yl)benzyl]-1,2,4-oxadiazol-5(4H)-one
0.1
-
-
 Sus scrofa 3-(2-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]phenyl]ethyl)-1,2,4-oxadiazol-5(4H)-one
0.1
-
-
 Sus scrofa 3-(3-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]phenyl]propyl)-1,2,4-oxadiazol-5(4H)-one
0.1
-
-
 Sus scrofa 3-[4-(tetradecyloxy)benzyl]-1,2,4-oxadiazol-5(4H)-one