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Literature summary extracted from

  • Grunewald, G.L.; Dahanukar, V.H.; Jalluri, R.K.; Criscione, K.R.
    Synthesis, biochemical evaluation, and classical and three-dimensional quantitative structure-activity relationship studies of 7-substituted-1,2,3,4-tetrahydroisoquinolines and their relative affinities toward phenylethanolamine N-methyltransferase and the a2-adrenoceptor (1999), J. Med. Chem., 42, 118-134.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.1.1.28 1,2,3,4-tetrahydroisoquinoline-7-carboxylic acid
-
 Bos taurus
2.1.1.28 7-acetamido-1,2,3,4-tetrahydroisoquinoline
-
 Bos taurus
2.1.1.28 7-allylsulfonyl-1,2,3,4-tetrahydrosioquinoline
-
 Bos taurus
2.1.1.28 7-aminocarbonyl-1,2,3,4-tetrahydroisoquinoline
-
 Bos taurus
2.1.1.28 7-aminomethyl-1,2,3,4-tetrahydroisoquinoline dihydrochloride
-
 Bos taurus
2.1.1.28 7-benzoyl-1,2,3,4-tetrahydroisoquinoline
-
 Bos taurus
2.1.1.28 7-benzyl-1,2,3,4-tetrahydroisoquinoline
-
 Bos taurus
2.1.1.28 7-bromo-N-triphenylmethyl-1,2,3,4-tetrahydroisoquinoline
-
 Bos taurus
2.1.1.28 7-hydroxymethyl-1,2,3,4-tetrahydroisoquinoline oxalate
-
 Bos taurus
2.1.1.28 7-iodo-1,2,3,4-tetrahydroisoquinoline
-
 Bos taurus
2.1.1.28 7-methoxycarbonyl-1,2,3,4-tetrahydroisoquinoline
-
 Bos taurus
2.1.1.28 7-methylsulfinyl-1,2,3,4-tetrahydroisoquinoline
-
 Bos taurus
2.1.1.28 7-methylsulfonyl-1,2,3,4-tetrahydroisoquinoline
-
 Bos taurus
2.1.1.28 7-methylthio-1,2,3,4-tetrahydroisoquinoline
-
 Bos taurus
2.1.1.28 7-phenylsulfonyl-1,2,3,4-tetrahydroisoquinoline
-
 Bos taurus
2.1.1.28 7-trichloromethylsulfonyl-1,2,3,4-tetrahydroisoquinoline
-
 Bos taurus
2.1.1.28 7-trifluoroacetyl-1,2,3,4-tetrahydroisoquinoline
-
 Bos taurus
2.1.1.28 7-trifluoromethyl-1,2,3,4-tetrahydroisoquinoline
-
 Bos taurus
2.1.1.28 additional information 7-substituted-1,2,3,4-tetrahydroisoquinolines are potent inhibitors, unfortunately, most of these compounds also exhibit a strong affinity for the alpha2-adrenoreceptor Bos taurus

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.1.1.28 additional information Bos taurus enzyme is involved in biosynthesis of epinephrine ?
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.1.1.28 Bos taurus
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.1.1.28 adrenal medulla
-
 Bos taurus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.1.1.28 additional information enzyme is involved in biosynthesis of epinephrine Bos taurus ?
-
 ?

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.1.1.28 0.00018
-
 7-trifluoromethyl-1,2,3,4-tetrahydroisoquinoline
-
 Bos taurus
2.1.1.28 0.00029
-
 7-bromo-N-triphenylmethyl-1,2,3,4-tetrahydroisoquinoline
-
 Bos taurus
2.1.1.28 0.00037
-
 7-iodo-1,2,3,4-tetrahydroisoquinoline
-
 Bos taurus
2.1.1.28 0.00061
-
 7-methylthio-1,2,3,4-tetrahydroisoquinoline
-
 Bos taurus
2.1.1.28 0.0013
-
 7-methylsulfonyl-1,2,3,4-tetrahydroisoquinoline
-
 Bos taurus
2.1.1.28 0.0013
-
 7-trichloromethylsulfonyl-1,2,3,4-tetrahydroisoquinoline
-
 Bos taurus
2.1.1.28 0.0029
-
 7-benzoyl-1,2,3,4-tetrahydroisoquinoline
-
 Bos taurus
2.1.1.28 0.0057
-
 7-trifluoroacetyl-1,2,3,4-tetrahydroisoquinoline
-
 Bos taurus
2.1.1.28 0.0067
-
 7-methoxycarbonyl-1,2,3,4-tetrahydroisoquinoline
-
 Bos taurus
2.1.1.28 0.0098
-
 7-allylsulfonyl-1,2,3,4-tetrahydrosioquinoline
-
 Bos taurus
2.1.1.28 0.011
-
 7-hydroxymethyl-1,2,3,4-tetrahydroisoquinoline oxalate
-
 Bos taurus
2.1.1.28 0.014
-
 7-phenylsulfonyl-1,2,3,4-tetrahydroisoquinoline
-
 Bos taurus
2.1.1.28 0.045
-
 7-methylsulfinyl-1,2,3,4-tetrahydroisoquinoline
-
 Bos taurus
2.1.1.28 0.061
-
 7-benzyl-1,2,3,4-tetrahydroisoquinoline
-
 Bos taurus
2.1.1.28 0.064
-
 7-aminocarbonyl-1,2,3,4-tetrahydroisoquinoline
-
 Bos taurus
2.1.1.28 0.19
-
 7-acetamido-1,2,3,4-tetrahydroisoquinoline
-
 Bos taurus
2.1.1.28 0.47
-
 1,2,3,4-tetrahydroisoquinoline-7-carboxylic acid
-
 Bos taurus
2.1.1.28 1.9
-
 7-aminomethyl-1,2,3,4-tetrahydroisoquinoline dihydrochloride
-
 Bos taurus