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Literature summary 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

EC Number Inhibitors Comment Organism Structure
3.1.4.4 4-(4-(2-(3-methoxyphenyl)benzo[b]thiophen-3-yl)phenoxy)-N,N-dimethylethan-1-amine
-
 Homo sapiens
3.1.4.4 4-(4-(2-(3-methoxyphenyl)benzo[b]thiophen-3-yl)phenoxy)-N,N-dimethylethan-1-amine
-
 Pseudomonas aeruginosa
3.1.4.4 desketoraloxifene
-
 Homo sapiens
3.1.4.4 desketoraloxifene
-
 Pseudomonas aeruginosa
3.1.4.54 4-(4-(2-(3-methoxyphenyl)benzo[b]thiophen-3-yl)phenoxy)-N,N-dimethylethan-1-amine compound additionally inhibits human phospholipases Pld1 and Pld2 and Pseudomonas aeruginosa PldA Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
3.1.4.4 Homo sapiens
-
-
-
3.1.4.4 Pseudomonas aeruginosa
-
-
-
3.1.4.54 Homo sapiens
-
-
-

Source Tissue

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

Substrates and Products (Substrate)

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

Synonyms

EC Number Synonyms Comment Organism
3.1.4.4 PLD1
-
 Homo sapiens
3.1.4.4 PLD2
-
 Homo sapiens
3.1.4.4 PldA
-
 Pseudomonas aeruginosa
3.1.4.54 NAPE-PLD
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.1.4.4 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
3.1.4.4 0.0026
-
 isoform PLD2, cellular assay, pH 7.5, 37°C Homo sapiens desketoraloxifene
3.1.4.4 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
3.1.4.4 0.0061
-
 isoform PLD1, cellular assay, pH 7.5, 37°C Homo sapiens desketoraloxifene
3.1.4.4 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
3.1.4.4 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
3.1.4.4 0.0099
-
 substrate presented in liposome, pH 7.5, 37°C Pseudomonas aeruginosa desketoraloxifene
3.1.4.4 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
3.1.4.4 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
3.1.4.54 0.067
-
 pH 7.5, 37°C Homo sapiens 4-(4-(2-(3-methoxyphenyl)benzo[b]thiophen-3-yl)phenoxy)-N,N-dimethylethan-1-amine