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Literature summary 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

Cloned(Commentary)

EC Number Cloned (Comment) Organism
3.1.1.4
-
 Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.1.1.4 3-(2-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]phenyl]ethyl)-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3.1.1.4 3-(2-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]phenyl]ethyl)-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
3.1.1.4 3-(3-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]phenyl]propyl)-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3.1.1.4 3-(3-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]phenyl]propyl)-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
3.1.1.4 3-[4-(4-hexadecylpiperazin-1-yl)benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3.1.1.4 3-[4-(4-hexadecylpiperazin-1-yl)benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
3.1.1.4 3-[4-(4-octadecylpiperazin-1-yl)benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3.1.1.4 3-[4-(4-octadecylpiperazin-1-yl)benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
3.1.1.4 3-[4-(4-tetradecylpiperazin-1-yl)benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3.1.1.4 3-[4-(4-tetradecylpiperazin-1-yl)benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
3.1.1.4 3-[4-(tetradecyloxy)benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3.1.1.4 3-[4-(tetradecyloxy)benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
3.1.1.4 3-[4-[(4-docosylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3.1.1.4 3-[4-[(4-docosylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
3.1.1.4 3-[4-[(4-hexadecylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3.1.1.4 3-[4-[(4-hexadecylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
3.1.1.4 3-[4-[(4-hexadecylpiperazin-1-yl)carbonyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3.1.1.4 3-[4-[(4-hexadecylpiperazin-1-yl)carbonyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
3.1.1.4 3-[4-[(4-hexadecylpiperazin-1-yl)methyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3.1.1.4 3-[4-[(4-hexadecylpiperazin-1-yl)methyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
3.1.1.4 3-[4-[(4-hexadecylpiperazin-1-yl)methyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3.1.1.4 3-[4-[(4-hexadecylpiperazin-1-yl)methyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
3.1.1.4 3-[4-[(4-icosylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3.1.1.4 3-[4-[(4-icosylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
3.1.1.4 3-[4-[(4-octadecylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3.1.1.4 3-[4-[(4-octadecylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
3.1.1.4 3-[4-[(4-octadecylpiperazin-1-yl)carbonyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3.1.1.4 3-[4-[(4-octadecylpiperazin-1-yl)carbonyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
3.1.1.4 3-[4-[(4-octadecylpiperazin-1-yl)methyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3.1.1.4 3-[4-[(4-octadecylpiperazin-1-yl)methyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
3.1.1.4 3-[4-[(4-octadecylpiperazin-1-yl)methyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3.1.1.4 3-[4-[(4-octadecylpiperazin-1-yl)methyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
3.1.1.4 3-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3.1.1.4 3-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
3.1.1.4 3-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3.1.1.4 3-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
3.1.1.4 3-[4-[(4-tetradecylpiperazin-1-yl)methyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3.1.1.4 3-[4-[(4-tetradecylpiperazin-1-yl)methyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
3.1.1.4 3-[4-[(4-tetradecylpiperazin-1-yl)methyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
-
 Homo sapiens
3.1.1.4 3-[4-[(4-tetradecylpiperazin-1-yl)methyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
-
 Sus scrofa
3.1.1.4 LY311727
-
 Homo sapiens
3.1.1.4 LY311727
-
 Sus scrofa
3.1.1.4 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
3.1.1.4 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

EC Number Organism UniProt Comment Textmining
3.1.1.4 Homo sapiens
-
-
-
3.1.1.4 Sus scrofa
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.1.1.4 pancreas
-
 Sus scrofa
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.1.1.4 1-palmitoyl-2-(10-pyrenyldecanoyl)-sn-glycero-3-phosphate + H2O
-
 Homo sapiens 10-pyrenyldecanoic acid + 1-palmitoyl-sn-glycero-3-phosphate
-
 ?
3.1.1.4 1-palmitoyl-2-(10-pyrenyldecanoyl)-sn-glycero-3-phosphate + H2O
-
 Sus scrofa 10-pyrenyldecanoic acid + 1-palmitoyl-sn-glycero-3-phosphate
-
 ?

Synonyms

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

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.1.1.4 0.00047
-
-
 Homo sapiens LY311727
3.1.1.4 0.0008
-
-
 Homo sapiens 3-[4-[(4-octadecylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
3.1.1.4 0.0011
-
-
 Homo sapiens 3-[4-[(4-octadecylpiperazin-1-yl)carbonyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
3.1.1.4 0.0022
-
-
 Homo sapiens 3-[4-[(4-octadecylpiperazin-1-yl)methyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
3.1.1.4 0.00271
-
-
 Homo sapiens 3-[4-(4-octadecylpiperazin-1-yl)benzyl]-1,2,4-oxadiazol-5(4H)-one
3.1.1.4 0.0035
-
-
 Homo sapiens 3-[4-(4-hexadecylpiperazin-1-yl)benzyl]-1,2,4-oxadiazol-5(4H)-one
3.1.1.4 0.004
-
-
 Homo sapiens 3-[4-[(4-hexadecylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
3.1.1.4 0.004
-
-
 Homo sapiens 3-[4-(tetradecyloxy)benzyl]-1,2,4-oxadiazol-5(4H)-one
3.1.1.4 0.0045
-
-
 Homo sapiens 3-[4-(4-tetradecylpiperazin-1-yl)benzyl]-1,2,4-oxadiazol-5(4H)-one
3.1.1.4 0.00508
-
-
 Homo sapiens 3-[4-[(4-octadecylpiperazin-1-yl)methyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
3.1.1.4 0.0053
-
-
 Homo sapiens 3-(3-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]phenyl]propyl)-1,2,4-oxadiazol-5(4H)-one
3.1.1.4 0.008
-
-
 Sus scrofa LY311727
3.1.1.4 0.009
-
-
 Homo sapiens 3-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
3.1.1.4 0.0187
-
-
 Homo sapiens 3-(2-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]phenyl]ethyl)-1,2,4-oxadiazol-5(4H)-one
3.1.1.4 0.1
-
-
 Homo sapiens 3-[4-[(4-tetradecylpiperazin-1-yl)methyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
3.1.1.4 0.1
-
-
 Sus scrofa 3-[4-[(4-tetradecylpiperazin-1-yl)methyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
3.1.1.4 0.1
-
-
 Homo sapiens 3-[4-[(4-hexadecylpiperazin-1-yl)methyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
3.1.1.4 0.1
-
-
 Sus scrofa 3-[4-[(4-hexadecylpiperazin-1-yl)methyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
3.1.1.4 0.1
-
-
 Sus scrofa 3-[4-[(4-octadecylpiperazin-1-yl)methyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
3.1.1.4 0.1
-
-
 Homo sapiens 3-[4-[(4-tetradecylpiperazin-1-yl)methyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
3.1.1.4 0.1
-
-
 Sus scrofa 3-[4-[(4-tetradecylpiperazin-1-yl)methyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
3.1.1.4 0.1
-
-
 Homo sapiens 3-[4-[(4-hexadecylpiperazin-1-yl)methyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
3.1.1.4 0.1
-
-
 Sus scrofa 3-[4-[(4-hexadecylpiperazin-1-yl)methyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
3.1.1.4 0.1
-
-
 Sus scrofa 3-[4-[(4-octadecylpiperazin-1-yl)methyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
3.1.1.4 0.1
-
-
 Homo sapiens 3-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
3.1.1.4 0.1
-
-
 Sus scrofa 3-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
3.1.1.4 0.1
-
-
 Homo sapiens 3-[4-[(4-hexadecylpiperazin-1-yl)carbonyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
3.1.1.4 0.1
-
-
 Sus scrofa 3-[4-[(4-hexadecylpiperazin-1-yl)carbonyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
3.1.1.4 0.1
-
-
 Sus scrofa 3-[4-[(4-octadecylpiperazin-1-yl)carbonyl]phenyl]-1,2,4-oxadiazol-5(4H)-one
3.1.1.4 0.1
-
-
 Sus scrofa 3-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
3.1.1.4 0.1
-
-
 Sus scrofa 3-[4-[(4-hexadecylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
3.1.1.4 0.1
-
-
 Sus scrofa 3-[4-[(4-octadecylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
3.1.1.4 0.1
-
-
 Homo sapiens 3-[4-[(4-icosylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
3.1.1.4 0.1
-
-
 Sus scrofa 3-[4-[(4-icosylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
3.1.1.4 0.1
-
-
 Homo sapiens 3-[4-[(4-docosylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
3.1.1.4 0.1
-
-
 Sus scrofa 3-[4-[(4-docosylpiperazin-1-yl)carbonyl]benzyl]-1,2,4-oxadiazol-5(4H)-one
3.1.1.4 0.1
-
-
 Sus scrofa 3-[4-(4-tetradecylpiperazin-1-yl)benzyl]-1,2,4-oxadiazol-5(4H)-one
3.1.1.4 0.1
-
-
 Sus scrofa 3-[4-(4-hexadecylpiperazin-1-yl)benzyl]-1,2,4-oxadiazol-5(4H)-one
3.1.1.4 0.1
-
-
 Sus scrofa 3-[4-(4-octadecylpiperazin-1-yl)benzyl]-1,2,4-oxadiazol-5(4H)-one
3.1.1.4 0.1
-
-
 Sus scrofa 3-(2-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]phenyl]ethyl)-1,2,4-oxadiazol-5(4H)-one
3.1.1.4 0.1
-
-
 Sus scrofa 3-(3-[4-[(4-tetradecylpiperazin-1-yl)carbonyl]phenyl]propyl)-1,2,4-oxadiazol-5(4H)-one
3.1.1.4 0.1
-
-
 Sus scrofa 3-[4-(tetradecyloxy)benzyl]-1,2,4-oxadiazol-5(4H)-one