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Literature summary for 3.1.1.7 extracted from

  • Pietsch, M.; Gutschow, M.
    Synthesis of tricyclic 1,3-oxazin-4-ones and kinetic analysis of cholesterol esterase and acetylcholinesterase inhibition (2005), J. Med. Chem., 48, 8270-8288.
    View publication on PubMed
Search for more literature for 3.1.1.7

Cloned(Commentary)

Cloned (Comment) Organism
-
 Electrophorus electricus

Inhibitors

Inhibitors Comment Organism Structure
2-(dimethylamino)-7-ethyl-5,6,7,8-tetrahydro-4H-pyrido(4',3':4,5)thieno(2,3-d)(1,3)oxazin-4-one 50% inhibition at 0.011 mM Electrophorus electricus
2-(dimethylamino)-7-isobutyl-5,6,7,8-tetrahydro-4H-pyrido(4',3':4,5)thieno(2,3-d)(1,3)oxazin-4-one 50% inhibition at 0.00036 mM Electrophorus electricus
2-(dimethylamino)-7-methyl-5,6,7,8-tetrahydro-4H-pyrido(4',3':4,5)thieno(2,3-d)(1,3)oxazin-4-one 50% inhibition at 0.039 mM Electrophorus electricus
2-amino-7-benzyl-5,6,7,8-tetrahydro-4H-pyrido(4',3':4,5)thieno(2,3-d)(1,3)oxazin-4-one 50% inhibition at 0.0059 mM Electrophorus electricus
2-amino-7-benzyl-5,6,7,8-tetrahydro-4H-pyrido(4',3':4,5)thieno(2,3-d)(1,3)thiazin-4-one 50% inhibition at 0.0012 mM Electrophorus electricus
7-benzoyl-2-(dimethylamino)-5,6,7,8-tetrahydro-4H-pyrido(4',3':4,5)thieno(2,3-d)(1,3)oxazin-4-one 50% inhibition at 0.036 mM Electrophorus electricus
7-benzyl-2-((3,4-dimethoxybenzyl)(methyl)amino)-5,6,7,8-tetrahydro-4H-pyrido(4',3':4,5)thieno(2,3-d)(1,3)oxazin-4-one 50% inhibition at 0.00033 mM Electrophorus electricus
7-benzyl-2-(4-benzylpiperazin-1-yl)-5,6,7,8-tetrahydro-4H-pyrido(4',3':4,5)thieno(2,3-d)(1,3)oxazin-4-one 50% inhibition at 0.00132 mM Electrophorus electricus
7-benzyl-2-(benzyl(methyl)amino)-5,6,7,8-tetrahydro-4H-pyrido(4',3':4,5)thieno(2,3-d)(1,3)oxazin-4-one 50% inhibition at 0.00084 mM Electrophorus electricus
7-benzyl-2-(benzylamino)-5,6,7,8-tetrahydro-4H-pyrido(4',3':4,5)thieno(2,3-d)(1,3)oxazin-4-one 50% inhibition at 0.00286 mM Electrophorus electricus
7-benzyl-2-(benzylamino)-5,6,7,8-tetrahydro-4H-pyrido(4',3':4,5)thieno(2,3-d)(1,3)thiazin-4-one 50% inhibition at 0.0052 mM Electrophorus electricus
7-benzyl-2-(cyclohexylamino)-5,6,7,8-tetrahydro-4H-pyrido(4',3':4,5)thieno(2,3-d)(1,3)thiazin-4-one 50% inhibition at 0.00282 mM Electrophorus electricus
7-benzyl-2-(diethylamino)-5,6,7,8-tetrahydro-4H-pyrido(4',3':4,5)thieno(2,3-d)(1,3)oxazin-4-one 50% inhibition at 0.00208 mM Electrophorus electricus
7-benzyl-2-(dimethylamino)-5,6,7,8-tetrahydro-4H-pyrido(4',3':4,5)thieno(2,3-d)(1,3)oxazin-4-one 50% inhibition at 0.00089 mM Electrophorus electricus
7-benzyl-2-(isopropylamino)-5,6,7,8-tetrahydro-4H-pyrido(4',3':4,5)thieno(2,3-d)(1,3)oxazin-4-one 50% inhibition at 0.00074 mM Electrophorus electricus
7-benzyl-2-(isopropylamino)-5,6,7,8-tetrahydro-4H-pyrido(4',3':4,5)thieno(2,3-d)(1,3)thiazin-4-one 50% inhibition at 0.00058 mM Electrophorus electricus
7-benzyl-2-(phenylamino)-5,6,7,8-tetrahydro-4H-pyrido(4',3':4,5)thieno(2,3-d)(1,3)oxazin-4-one 50% inhibition at 0.00094 mM Electrophorus electricus
7-benzyl-2-(phenylamino)-5,6,7,8-tetrahydro-4H-pyrido(4',3':4,5)thieno(2,3-d)(1,3)thiazin-4-one 50% inhibition at 0.00103 mM Electrophorus electricus
7-benzyl-2-morpholin-4-yl-5,6,7,8-tetrahydro-4H-pyrido(4',3':4,5)thieno(2,3-d)(1,3)oxazin-4-one 50% inhibition at 0.00077 mM Electrophorus electricus
neostigmine bromide competitive Electrophorus electricus

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
67000
-
 gel filtration Electrophorus electricus

Organism

Organism UniProt Comment Textmining
Electrophorus electricus
-
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
proteolytic modification sequence contains a signal peptide Electrophorus electricus

Purification (Commentary)

Purification (Comment) Organism
-
 Electrophorus electricus

Subunits

Subunits Comment Organism
? enzyme exists as a mixture of 88 kDa dimers consisting of disulfide-linked 42- to 44-kDa polypeptides and a 42- to 44-kDa monomer, SDS-PAGE Electrophorus electricus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0031
-
 neostigmine bromide pH 7.0, 30°C, substrate acetylthiocholine Electrophorus electricus
0.0047
-
 neostigmine bromide pH 7.0, 30°C, substrate propionylthiocholine Electrophorus electricus