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Literature summary for 2.1.1.28 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
Search for more literature for 2.1.1.28

Inhibitors

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

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
PNMT
-
 Homo sapiens

Temperature Optimum [°C]

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

pH Optimum

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

Cofactor

Cofactor Comment Organism Structure
S-adenosyl-L-methionine
-
 Homo sapiens

Ki Value [mM]

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