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Literature summary for 3.1.4.4 extracted from

  • Scott, S.; Spencer, C.; OReilly, M.; Brown, K.; Lavieri, R.; Cho, C.; Jung, D.; Larock, R.; Brown, H.; Lindsley, C.
    Discovery of desketoraloxifene analogues as inhibitors of mammalian, Pseudomonas aeruginosa, and NAPE phospholipase D enzymes (2015), ACS Chem. Biol., 10, 421-432 .
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
4-(4-(2-(3-methoxyphenyl)benzo[b]thiophen-3-yl)phenoxy)-N,N-dimethylethan-1-amine
-
Homo sapiens
4-(4-(2-(3-methoxyphenyl)benzo[b]thiophen-3-yl)phenoxy)-N,N-dimethylethan-1-amine
-
Pseudomonas aeruginosa
desketoraloxifene
-
Homo sapiens
desketoraloxifene
-
Pseudomonas aeruginosa

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Pseudomonas aeruginosa
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
Calu-1 cell
-
Homo sapiens
-
HEK-293 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
dipalmitoylphosphatidylcholine + H2O
-
Homo sapiens choline + dipalmitoylphosphatidate
-
?
dipalmitoylphosphatidylcholine + H2O
-
Pseudomonas aeruginosa choline + dipalmitoylphosphatidate
-
?

Synonyms

Synonyms Comment Organism
PLD1
-
Homo sapiens
PLD2
-
Homo sapiens
PldA
-
Pseudomonas aeruginosa

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0026
-
isofom PLD1, cellular assay, pH 7.5, 37°C Homo sapiens 4-(4-(2-(3-methoxyphenyl)benzo[b]thiophen-3-yl)phenoxy)-N,N-dimethylethan-1-amine
0.0026
-
isoform PLD2, cellular assay, pH 7.5, 37°C Homo sapiens desketoraloxifene
0.0047
-
isofom PLD1, recombinant protein, pH 7.5, 37°C Homo sapiens 4-(4-(2-(3-methoxyphenyl)benzo[b]thiophen-3-yl)phenoxy)-N,N-dimethylethan-1-amine
0.0061
-
isoform PLD1, cellular assay, pH 7.5, 37°C Homo sapiens desketoraloxifene
0.0071
-
isofom PLD2, recombinant protein, pH 7.5, 37°C Homo sapiens 4-(4-(2-(3-methoxyphenyl)benzo[b]thiophen-3-yl)phenoxy)-N,N-dimethylethan-1-amine
0.0075
-
monomeric substrate, pH 7.5, 37°C Pseudomonas aeruginosa 4-(4-(2-(3-methoxyphenyl)benzo[b]thiophen-3-yl)phenoxy)-N,N-dimethylethan-1-amine
0.0099
-
substrate presented in liposome, pH 7.5, 37°C Pseudomonas aeruginosa desketoraloxifene
0.0161
-
substrate presented in liposome, pH 7.5, 37°C Pseudomonas aeruginosa 4-(4-(2-(3-methoxyphenyl)benzo[b]thiophen-3-yl)phenoxy)-N,N-dimethylethan-1-amine
0.02
-
isofom PLD2, cellular assay, pH 7.5, 37°C Homo sapiens 4-(4-(2-(3-methoxyphenyl)benzo[b]thiophen-3-yl)phenoxy)-N,N-dimethylethan-1-amine