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Literature summary for 3.1.4.54 extracted from

  • Castellani, B.; Diamanti, E.; Pizzirani, D.; Tardia, P.; Maccesi, M.; Realini, N.; Magotti, P.; Garau, G.; Bakkum, T.; Rivara, S.; Mor, M.; Piomelli, D.
    Synthesis and characterization of the first inhibitor of N-acylphosphatidylethanolamine phospholipase D (NAPE-PLD) (2017), Chem. Commun. (Camb.), 53, 12814-12817 .
    View publication on PubMedView publication on EuropePMC
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Protein Variants

Protein Variants Comment Organism
Q320A decrease in catalytic activity Homo sapiens
Q320S decrease in catalytic activity Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2,4-dioxo-N-[4-(4-pyridyl)phenyl]-1H-quinazoline-6-sulfonamide reversible uncompetitive inhibitor, compound binds via a reversible mechanism to the enzyme's zinc center. Compound is not inhibitory to carbonic anhydrase II, neutral endopeptidase and angiotensin-converting enzyme Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q6IQ20
-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0367
-
 mutant Q320S, pH not specified in the publication, temperature not specified in the publication Homo sapiens 2,4-dioxo-N-[4-(4-pyridyl)phenyl]-1H-quinazoline-6-sulfonamide
0.0462
-
 wild-type, pH not specified in the publication, temperature not specified in the publication Homo sapiens 2,4-dioxo-N-[4-(4-pyridyl)phenyl]-1H-quinazoline-6-sulfonamide
0.0892
-
 mutant Q320A, pH not specified in the publication, temperature not specified in the publication Homo sapiens 2,4-dioxo-N-[4-(4-pyridyl)phenyl]-1H-quinazoline-6-sulfonamide