Proteins > Phenylethanolamine N-methyltransferase
Page last updated: 2024-08-07 15:53:53
Phenylethanolamine N-methyltransferase
A phenylethanolamine N-methyltransferase that is encoded in the genome of human. [PRO:DNx, UniProtKB:P11086]
Synonyms
PNMTase;
EC 2.1.1.28;
Noradrenaline N-methyltransferase
Research
Bioassay Publications (15)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 2 (13.33) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 12 (80.00) | 29.6817 |
| 2010's | 0 (0.00) | 24.3611 |
| 2020's | 1 (6.67) | 2.80 |
Compounds (16)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| 2,3-dichloro-alpha-methylbenzylamine | Homo sapiens (human) | Ki | 0.7433 | 3 | 3 |
| p-chloroamphetamine | Homo sapiens (human) | IC50 | 300.0000 | 1 | 2 |
| sk&f 29661 | Homo sapiens (human) | Ki | 33.1275 | 16 | 16 |
| 1,2,3,4-tetrahydroisoquinoline | Homo sapiens (human) | Ki | 8.1000 | 4 | 4 |
| 1-phenethylamine | Homo sapiens (human) | Ki | 830.0000 | 1 | 1 |
| exp561 | Homo sapiens (human) | Ki | 51.0000 | 1 | 1 |
| 1-phenethylamine, (s)-isomer | Homo sapiens (human) | Ki | 430.0000 | 1 | 1 |
| 2-aminobenzonorbornene | Homo sapiens (human) | Ki | 730.0000 | 1 | 1 |
| ly 134046 | Homo sapiens (human) | Ki | 546.8271 | 7 | 7 |
| 7,8-dichloro-1,2,3,4-tetrahydroisoquinoline | Homo sapiens (human) | IC50 | 2.5058 | 4 | 4 |
| 7,8-dichloro-1,2,3,4-tetrahydroisoquinoline | Homo sapiens (human) | Ki | 0.1961 | 14 | 14 |
| s-adenosylhomocysteine | Homo sapiens (human) | Ki | 14.0000 | 1 | 1 |
| 1-phenethylamine, (r)-isomer | Homo sapiens (human) | Ki | 4,800.0000 | 1 | 1 |
| 3-trifluoromethyl-7-bromo-1,2,3,4-tetrahydroisoquinoline | Homo sapiens (human) | Ki | 3.2000 | 2 | 2 |
| f21 | Homo sapiens (human) | Ki | 0.6100 | 1 | 1 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| s-adenosylmethionine | Homo sapiens (human) | Kd | 8.1000 | 6 | 6 |
Drugs with Other Measurements
Structural, mutagenic, and kinetic analysis of the binding of substrates and inhibitors of human phenylethanolamine N-methyltransferase.Journal of medicinal chemistry, , Nov-17, Volume: 48, Issue:23, 2005
Phenylethanolamine N-methyltransferase inhibition: re-evaluation of kinetic data.Bioorganic & medicinal chemistry letters, , Aug-16, Volume: 14, Issue:16, 2004
Phenylethanolamine N-methyltransferase kinetics: bovine versus recombinant human enzyme.Bioorganic & medicinal chemistry letters, , Jun-18, Volume: 11, Issue:12, 2001
Time-dependent inactivation of human phenylethanolamine N-methyltransferase by 7-isothiocyanatotetrahydroisoquinoline.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 19, Issue:4, 2009
Exploring the active site of phenylethanolamine N-methyltransferase with 1,2,3,4-tetrahydrobenz[h]isoquinoline inhibitors.Bioorganic & medicinal chemistry, , Feb-01, Volume: 15, Issue:3, 2007
Comparison of the binding of 3-fluoromethyl-7-sulfonyl-1,2,3,4-tetrahydroisoquinolines with their isosteric sulfonamides to the active site of phenylethanolamine N-methyltransferase.Journal of medicinal chemistry, , Sep-07, Volume: 49, Issue:18, 2006
Inhibitors of phenylethanolamine N-methyltransferase devoid of alpha2-adrenoceptor affinity.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 15, Issue:23, 2005
3-hydroxymethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline inhibitors of phenylethanolamine N-methyltransferase that display remarkable potency and selectivity.Journal of medicinal chemistry, , Jan-13, Volume: 48, Issue:1, 2005
Structural, mutagenic, and kinetic analysis of the binding of substrates and inhibitors of human phenylethanolamine N-methyltransferase.Journal of medicinal chemistry, , Nov-17, Volume: 48, Issue:23, 2005
Inhibitors of phenylethanolamine N-methyltransferase that are predicted to penetrate the blood-brain barrier: design, synthesis, and evaluation of 3-fluoromethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinolines that possess low affinity towJournal of medicinal chemistry, , Aug-26, Volume: 47, Issue:18, 2004
Phenylethanolamine N-methyltransferase inhibition: re-evaluation of kinetic data.Bioorganic & medicinal chemistry letters, , Aug-16, Volume: 14, Issue:16, 2004
Phenylethanolamine N-methyltransferase kinetics: bovine versus recombinant human enzyme.Bioorganic & medicinal chemistry letters, , Jun-18, Volume: 11, Issue:12, 2001
Exploring the active site of phenylethanolamine N-methyltransferase with 1,2,3,4-tetrahydrobenz[h]isoquinoline inhibitors.Bioorganic & medicinal chemistry, , Feb-01, Volume: 15, Issue:3, 2007
Comparison of the binding of 3-fluoromethyl-7-sulfonyl-1,2,3,4-tetrahydroisoquinolines with their isosteric sulfonamides to the active site of phenylethanolamine N-methyltransferase.Journal of medicinal chemistry, , Sep-07, Volume: 49, Issue:18, 2006
Phenylethanolamine N-methyltransferase kinetics: bovine versus recombinant human enzyme.Bioorganic & medicinal chemistry letters, , Jun-18, Volume: 11, Issue:12, 2001
Structural, mutagenic, and kinetic analysis of the binding of substrates and inhibitors of human phenylethanolamine N-methyltransferase.Journal of medicinal chemistry, , Nov-17, Volume: 48, Issue:23, 2005
Phenylethanolamine N-methyltransferase inhibition: re-evaluation of kinetic data.Bioorganic & medicinal chemistry letters, , Aug-16, Volume: 14, Issue:16, 2004
Phenylethanolamine N-methyltransferase kinetics: bovine versus recombinant human enzyme.Bioorganic & medicinal chemistry letters, , Jun-18, Volume: 11, Issue:12, 2001
Recent developments in fragment-based drug discovery.Journal of medicinal chemistry, , Jul-10, Volume: 51, Issue:13, 2008
Exploring the active site of phenylethanolamine N-methyltransferase with 1,2,3,4-tetrahydrobenz[h]isoquinoline inhibitors.Bioorganic & medicinal chemistry, , Feb-01, Volume: 15, Issue:3, 2007
Comparison of the binding of 3-fluoromethyl-7-sulfonyl-1,2,3,4-tetrahydroisoquinolines with their isosteric sulfonamides to the active site of phenylethanolamine N-methyltransferase.Journal of medicinal chemistry, , Sep-07, Volume: 49, Issue:18, 2006
Inhibitors of phenylethanolamine N-methyltransferase devoid of alpha2-adrenoceptor affinity.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 15, Issue:23, 2005
Structural, mutagenic, and kinetic analysis of the binding of substrates and inhibitors of human phenylethanolamine N-methyltransferase.Journal of medicinal chemistry, , Nov-17, Volume: 48, Issue:23, 2005
3-hydroxymethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline inhibitors of phenylethanolamine N-methyltransferase that display remarkable potency and selectivity.Journal of medicinal chemistry, , Jan-13, Volume: 48, Issue:1, 2005
Inhibitors of phenylethanolamine N-methyltransferase that are predicted to penetrate the blood-brain barrier: design, synthesis, and evaluation of 3-fluoromethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinolines that possess low affinity towJournal of medicinal chemistry, , Aug-26, Volume: 47, Issue:18, 2004
Phenylethanolamine N-methyltransferase inhibition: re-evaluation of kinetic data.Bioorganic & medicinal chemistry letters, , Aug-16, Volume: 14, Issue:16, 2004
Phenylethanolamine N-methyltransferase kinetics: bovine versus recombinant human enzyme.Bioorganic & medicinal chemistry letters, , Jun-18, Volume: 11, Issue:12, 2001
Inhibitors of phenylethanolamine N-methyltransferase and epinephrine biosynthesis. 3. Bis[tetrahydroisoquinoline]s.Journal of medicinal chemistry, , Volume: 24, Issue:6, 1981
Inhibitors of phenylethanolamine N-methyltransferase and epinephrine biosynthesis. 1. Chloro-substituted 1,2,3,4-tetrahydroisoquinolines.Journal of medicinal chemistry, , Volume: 23, Issue:5, 1980
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.Bioorganic & medicinal chemistry, , Jan-01, Volume: 16, Issue:1, 2008
Inhibitors of phenylethanolamine N-methyltransferase devoid of alpha2-adrenoceptor affinity.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 15, Issue:23, 2005
Enables
This protein enables 2 target(s):
| Target | Category | Definition |
|---|
| phenylethanolamine N-methyltransferase activity | molecular function | Catalysis of the reaction: S-adenosyl-L-methionine + phenylethanolamine = S-adenosyl-L-homocysteine + N-methylphenylethanolamine. [EC:2.1.1.28] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
Located In
This protein is located in 1 target(s):
| Target | Category | Definition |
|---|
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
Involved In
This protein is involved in 3 target(s):
| Target | Category | Definition |
|---|
| methylation | biological process | The process in which a methyl group is covalently attached to a molecule. [GOC:mah] |
| epinephrine biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of epinephrine, a hormone produced by the medulla of the adrenal glands that increases heart activity, improves the power and prolongs the action of muscles, and increases the rate and depth of breathing. It is synthesized by the methylation of norepinephrine. [GOC:jl, ISBN:0192801023, ISBN:0198506732] |
| catecholamine biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of any of a group of physiologically important biogenic amines that possess a catechol (3,4-dihydroxyphenyl) nucleus and are derivatives of 3,4-dihydroxyphenylethylamine. [GOC:jl, ISBN:0198506732] |