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Literature summary 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

Cloned(Commentary)

EC Number Cloned (Comment) Organism
3.1.1.7
-
 Electrophorus electricus

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.1.1.7 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
3.1.1.7 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
3.1.1.7 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
3.1.1.7 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
3.1.1.7 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
3.1.1.7 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
3.1.1.7 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
3.1.1.7 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
3.1.1.7 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
3.1.1.7 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
3.1.1.7 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
3.1.1.7 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
3.1.1.7 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
3.1.1.7 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
3.1.1.7 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
3.1.1.7 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
3.1.1.7 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
3.1.1.7 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
3.1.1.7 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
3.1.1.7 neostigmine bromide competitive Electrophorus electricus
3.1.1.13 2-(diethylamino)-4H-(1)benzothieno(2,3-d)(1,3)oxazin-4-one
-
 Bos taurus
3.1.1.13 2-(diethylamino)-5,6-dimethyl-4H-thieno(2,3-d)(1,3)oxazin-4-one
-
 Bos taurus
3.1.1.13 2-(diethylamino)-5-isopropyl-4H-thieno(2,3-d)(1,3)oxazin-4-one
-
 Bos taurus
3.1.1.13 2-(diethylamino)-5-methyl-5,6,7,8-tetrahydro-4H-(1)benzothieno(2,3-d)(1,3)oxazin-4-one
-
 Bos taurus
3.1.1.13 2-(diethylamino)-6,7,8,9-tetrahydro-4H,5H-cyclohepta(4,5)thieno(2,3-d)(1,3)oxazin-4-one
-
 Bos taurus
3.1.1.13 2-(dimethylamino)-1,2,5,6,7,8-hexahydro-4H-(1)benzothieno(2,3-d)(1,3)oxazin-4-one
-
 Bos taurus
3.1.1.13 2-(dimethylamino)-1,5,6,7-tetrahydro-2H,4H-cyclopenta(4,5)thieno(2,3-d)(1,3)oxazin-4-one
-
 Bos taurus
3.1.1.13 2-(dimethylamino)-1,5,6,8-tetrahydro-2H,4H-thiopyrano(4',3':4,5)thieno(2,3-d)(1,3)oxazin-4-one
-
 Bos taurus
3.1.1.13 2-morpholin-4-yl-5,6,7,8-tetrahydro-4H-1-benzothieno(2,3-d)(1,3)oxazin-4-one
-
 Bos taurus

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.1.1.13 0.0065
-
 (25R)-3beta-hydroxycholest-5-en-27-oate pH 7.0 Bos taurus

Molecular Weight [Da]

EC Number Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
3.1.1.7 67000
-
 gel filtration Electrophorus electricus

Organism

EC Number Organism UniProt Comment Textmining
3.1.1.7 Electrophorus electricus
-
-
-
3.1.1.13 Bos taurus
-
-
-

Posttranslational Modification

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

Purification (Commentary)

EC Number Purification (Comment) Organism
3.1.1.7
-
 Electrophorus electricus

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.1.1.13 (25R)-3beta-hydroxycholest-5-en-27-oate + H2O
-
 Bos taurus ?
-
 ?
3.1.1.13 2-(dimethylamino)-1,5,6,7-tetrahydro-2H,4H-cyclopenta(4,5)thieno(2,3-d)(1,3)oxazin-4-one + H2O
-
 Bos taurus ?
-
 ?

Subunits

EC Number Subunits Comment Organism
3.1.1.7 ? 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]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.1.1.7 0.0031
-
 neostigmine bromide pH 7.0, 30°C, substrate acetylthiocholine Electrophorus electricus
3.1.1.7 0.0047
-
 neostigmine bromide pH 7.0, 30°C, substrate propionylthiocholine Electrophorus electricus
3.1.1.13 0.00063
-
 2-(dimethylamino)-1,5,6,7-tetrahydro-2H,4H-cyclopenta(4,5)thieno(2,3-d)(1,3)oxazin-4-one pH 7.0 Bos taurus
3.1.1.13 0.00164
-
 2-(diethylamino)-5-methyl-5,6,7,8-tetrahydro-4H-(1)benzothieno(2,3-d)(1,3)oxazin-4-one pH 7.0 Bos taurus
3.1.1.13 0.00215
-
 2-(dimethylamino)-1,2,5,6,7,8-hexahydro-4H-(1)benzothieno(2,3-d)(1,3)oxazin-4-one pH 7.0 Bos taurus
3.1.1.13 0.0043
-
 2-(diethylamino)-5,6-dimethyl-4H-thieno(2,3-d)(1,3)oxazin-4-one pH 7.0 Bos taurus
3.1.1.13 0.0057
-
 2-morpholin-4-yl-5,6,7,8-tetrahydro-4H-1-benzothieno(2,3-d)(1,3)oxazin-4-one pH 7.0 Bos taurus
3.1.1.13 0.00576
-
 2-(dimethylamino)-1,5,6,8-tetrahydro-2H,4H-thiopyrano(4',3':4,5)thieno(2,3-d)(1,3)oxazin-4-one pH 7.0 Bos taurus
3.1.1.13 0.006
-
 2-(diethylamino)-6,7,8,9-tetrahydro-4H,5H-cyclohepta(4,5)thieno(2,3-d)(1,3)oxazin-4-one pH 7.0 Bos taurus
3.1.1.13 0.0064
-
 2-(diethylamino)-5-isopropyl-4H-thieno(2,3-d)(1,3)oxazin-4-one pH 7.0 Bos taurus
3.1.1.13 0.0075
-
 2-(diethylamino)-4H-(1)benzothieno(2,3-d)(1,3)oxazin-4-one pH 7.0 Bos taurus