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Literature summary extracted from

  • Grunewald, G.L.; Seim, M.R.; Bhat, S.R.; Wilson, M.E.; Criscione, K.R.
    Synthesis of 4,5,6,7-tetrahydrothieno[3,2-c]pyridines and comparison with their isosteric 1,2,3,4-tetrahydroisoquinolines as inhibitors of phenylethanolamine N-methyltransferase (2008), Bioorg. Med. Chem., 16, 542-559.
    View publication on PubMedView publication on EuropePMC

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.1.1.28 (6R)-6-methyl-2-nitro-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
 Homo sapiens
2.1.1.28 (6R)-6-methyl-4,5,6,7-tetrahydrothieno[3,2-c]pyridine-2-carbonitrile
-
 Homo sapiens
2.1.1.28 (6S)-6-methyl-2-nitro-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
 Homo sapiens
2.1.1.28 (6S)-6-methyl-4,5,6,7-tetrahydrothieno[3,2-c]pyridine-2-carbonitrile
-
 Homo sapiens
2.1.1.28 1,2,3,4-tetrahydroisoquinoline
-
 Homo sapiens
2.1.1.28 1,2,3,4-tetrahydroisoquinoline-7-sulfonamide
-
 Homo sapiens
2.1.1.28 1-(4,5,6,7-tetrahydrothieno[3,2-c]pyridin-2-yl)ethanone
-
 Homo sapiens
2.1.1.28 1-phenylmethanamine
-
 Homo sapiens
2.1.1.28 1-thiophen-2-ylmethanamine
-
 Homo sapiens
2.1.1.28 1-thiophen-3-ylmethanamine
-
 Homo sapiens
2.1.1.28 2-bromo-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
 Homo sapiens
2.1.1.28 2-bromo-6-(trifluoromethyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
 Homo sapiens
2.1.1.28 2-methyl-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
 Homo sapiens
2.1.1.28 2-nitro-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
 Homo sapiens
2.1.1.28 2-phenylethanamine
-
 Homo sapiens
2.1.1.28 2-Phenylethylamine
-
 Homo sapiens
2.1.1.28 2-thiophen-2-ylethanamine
-
 Homo sapiens
2.1.1.28 3-(trifluoromethyl)-1,2,3,4-tetrahydro[1]benzothieno[3,2-c]pyridine
-
 Homo sapiens
2.1.1.28 3-methyl-1,2,3,4-tetrahydroisoquinoline
-
 Homo sapiens
2.1.1.28 3-methyl-1,2,3,4-tetrahydro[1]benzothieno[3,2-c]pyridine
-
 Homo sapiens
2.1.1.28 3-methyl-7-nitro-1,2,3,4-tetrahydroisoquinoline
-
 Homo sapiens
2.1.1.28 3-Phenylpropylamine
-
 Homo sapiens
2.1.1.28 3-thienylmethylamine inhibits the enzyme and is selective toward the alpha2-adrenoceptor Homo sapiens
2.1.1.28 4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
 Homo sapiens
2.1.1.28 4,5,6,7-tetrahydrothieno[3,2-c]pyridine-2-carbonitrile
-
 Homo sapiens
2.1.1.28 4,5,6,7-tetrahydrothieno[3,2-c]pyridine-2-carboxamide
-
 Homo sapiens
2.1.1.28 6-(trifluoromethyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
 Homo sapiens
2.1.1.28 6-methyl-2-nitro-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
 Homo sapiens
2.1.1.28 6-methyl-4,5,6,7-tetrahydrothieno[3,2-c]pyridine
-
 Homo sapiens
2.1.1.28 6-methyl-4,5,6,7-tetrahydrothieno[3,2-c]pyridine-2-carbonitrile
-
 Homo sapiens
2.1.1.28 7,8-dichloro-1,2,3,4-tetrahydroisoquinoline
-
 Homo sapiens
2.1.1.28 7-bromo-1,2,3,4-tetrahydroisoquinoline
-
 Homo sapiens
2.1.1.28 7-bromo-3-methyl-1,2,3,4-tetrahydroisoquinoline
-
 Homo sapiens
2.1.1.28 7-nitro-1,2,3,4-tetrahydroisoquinoline
-
 Homo sapiens
2.1.1.28 benzylamine
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.1.1.28 S-adenosyl-L-methionine + norepinephrine Homo sapiens terminal step in epinephrine biosynthesis S-adenosyl-L-homocysteine + epinephrine
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.1.1.28 Homo sapiens
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.1.1.28 S-adenosyl-L-methionine + norepinephrine
-
 Homo sapiens S-adenosyl-L-homocysteine + epinephrine
-
 ?
2.1.1.28 S-adenosyl-L-methionine + norepinephrine terminal step in epinephrine biosynthesis Homo sapiens S-adenosyl-L-homocysteine + epinephrine
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.1.1.28 PNMT
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.1.1.28 37
-
 assay at Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.1.1.28 8
-
 assay at Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
2.1.1.28 S-adenosyl-L-methionine
-
 Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.1.1.28 0.0000031
-
 7,8-dichloro-1,2,3,4-tetrahydroisoquinoline pH 8.0, 37°C Homo sapiens
2.1.1.28 0.000017
-
 7-bromo-3-methyl-1,2,3,4-tetrahydroisoquinoline pH 8.0, 37°C Homo sapiens
2.1.1.28 0.000056
-
 7-bromo-1,2,3,4-tetrahydroisoquinoline pH 8.0, 37°C Homo sapiens
2.1.1.28 0.000067
-
 3-methyl-1,2,3,4-tetrahydro[1]benzothieno[3,2-c]pyridine pH 8.0, 37°C Homo sapiens
2.1.1.28 0.000072
-
 3-methyl-7-nitro-1,2,3,4-tetrahydroisoquinoline pH 8.0, 37°C Homo sapiens
2.1.1.28 0.00012
-
 7-nitro-1,2,3,4-tetrahydroisoquinoline pH 8.0, 37°C Homo sapiens
2.1.1.28 0.00028
-
 1,2,3,4-tetrahydroisoquinoline-7-sulfonamide pH 8.0, 37°C Homo sapiens
2.1.1.28 0.00031
-
 (6S)-6-methyl-2-nitro-4,5,6,7-tetrahydrothieno[3,2-c]pyridine S-isomer, pH 8.0, 37°C Homo sapiens
2.1.1.28 0.00073
-
 2-bromo-6-(trifluoromethyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine pH 8.0, 37°C Homo sapiens
2.1.1.28 0.0012
-
 2-bromo-4,5,6,7-tetrahydrothieno[3,2-c]pyridine pH 8.0, 37°C Homo sapiens
2.1.1.28 0.0014
-
 3-methyl-1,2,3,4-tetrahydroisoquinoline pH 8.0, 37°C Homo sapiens
2.1.1.28 0.0026
-
 2-nitro-4,5,6,7-tetrahydrothieno[3,2-c]pyridine pH 8.0, 37°C Homo sapiens
2.1.1.28 0.0033
-
 (6S)-6-methyl-4,5,6,7-tetrahydrothieno[3,2-c]pyridine-2-carbonitrile S-isomer, pH 8.0, 37°C Homo sapiens
2.1.1.28 0.0058
-
 1,2,3,4-tetrahydroisoquinoline pH 8.0, 37°C Homo sapiens
2.1.1.28 0.0058
-
 6-methyl-4,5,6,7-tetrahydrothieno[3,2-c]pyridine pH 8.0, 37°C Homo sapiens
2.1.1.28 0.0096
-
 (6R)-6-methyl-2-nitro-4,5,6,7-tetrahydrothieno[3,2-c]pyridine R-isomer, pH 8.0, 37°C Homo sapiens
2.1.1.28 0.015
-
 4,5,6,7-tetrahydrothieno[3,2-c]pyridine-2-carbonitrile pH 8.0, 37°C Homo sapiens
2.1.1.28 0.017
-
 3-(trifluoromethyl)-1,2,3,4-tetrahydro[1]benzothieno[3,2-c]pyridine pH 8.0, 37°C Homo sapiens
2.1.1.28 0.021
-
 2-bromo-6-(trifluoromethyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine pH 8.0, 37°C Homo sapiens
2.1.1.28 0.025
-
 2-methyl-4,5,6,7-tetrahydrothieno[3,2-c]pyridine pH 8.0, 37°C Homo sapiens
2.1.1.28 0.037
-
 4,5,6,7-tetrahydrothieno[3,2-c]pyridine pH 8.0, 37°C Homo sapiens
2.1.1.28 0.04
-
 6-(trifluoromethyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine pH 8.0, 37°C Homo sapiens
2.1.1.28 0.061
-
 1-(4,5,6,7-tetrahydrothieno[3,2-c]pyridin-2-yl)ethanone pH 8.0, 37°C Homo sapiens
2.1.1.28 0.1
-
 4,5,6,7-tetrahydrothieno[3,2-c]pyridine-2-carboxamide pH 8.0, 37°C Homo sapiens
2.1.1.28 0.11
-
 1-thiophen-3-ylmethanamine pH 8.0, 37°C Homo sapiens
2.1.1.28 0.15
-
 (6R)-6-methyl-4,5,6,7-tetrahydrothieno[3,2-c]pyridine-2-carbonitrile R-isomer, pH 8.0, 37°C Homo sapiens
2.1.1.28 0.17
-
 benzylamine pH 8.0, 37°C Homo sapiens
2.1.1.28 0.22
-
 2-Phenylethylamine pH 8.0, 37°C Homo sapiens
2.1.1.28 0.3
-
 2-thiophen-2-ylethanamine pH 8.0, 37°C Homo sapiens
2.1.1.28 0.45
-
 1-thiophen-2-ylmethanamine pH 8.0, 37°C Homo sapiens