Proteins > Trace amine-associated receptor 1
Page last updated: 2024-08-08 00:11:06
Trace amine-associated receptor 1
A trace amine-associated receptor 1 that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q96RJ0]
Synonyms
TaR-1;
Trace amine receptor 1
Research
Bioassay Publications (8)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 1 (12.50) | 29.6817 |
| 2010's | 5 (62.50) | 24.3611 |
| 2020's | 2 (25.00) | 2.80 |
Compounds (28)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| tolazoline | Homo sapiens (human) | Ki | 1.6400 | 1 | 1 |
| st 1913 | Homo sapiens (human) | Ki | 0.5000 | 1 | 1 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| norepinephrine, (+,-)-isomer | Homo sapiens (human) | EC50 | 12.2000 | 1 | 1 |
| phenethylamine | Homo sapiens (human) | EC50 | 0.0950 | 4 | 4 |
| tryptamine | Homo sapiens (human) | EC50 | 2.2100 | 1 | 1 |
| 3-methoxytyramine | Homo sapiens (human) | EC50 | 0.3080 | 1 | 1 |
| o-methyltyramine | Homo sapiens (human) | EC50 | 5.9800 | 1 | 1 |
| phentermine | Homo sapiens (human) | EC50 | 5.4700 | 1 | 1 |
| tyramine | Homo sapiens (human) | EC50 | 0.5990 | 3 | 3 |
| dextroamphetamine | Homo sapiens (human) | EC50 | 0.6662 | 4 | 4 |
| methamphetamine | Homo sapiens (human) | EC50 | 1.4000 | 2 | 2 |
| 3-tyramine | Homo sapiens (human) | EC50 | 1.0395 | 2 | 2 |
| n-methylphenethylamine | Homo sapiens (human) | EC50 | 0.2627 | 3 | 3 |
| tranylcypromine | Homo sapiens (human) | EC50 | 1.5100 | 1 | 1 |
| 4-chlorophenylbiguanide | Homo sapiens (human) | EC50 | 10.0000 | 1 | 1 |
| n,n-dimethylphenylethylamine | Homo sapiens (human) | EC50 | 50.7450 | 2 | 2 |
| l-amphetamine | Homo sapiens (human) | EC50 | 1.0425 | 4 | 4 |
| 4-chlorophenethylamine | Homo sapiens (human) | EC50 | 2.8600 | 1 | 1 |
| 3,4-methylenedioxyphenethylamine | Homo sapiens (human) | EC50 | 5.0300 | 1 | 1 |
| 3-methoxy-4-hydroxyphenylethylamine | Homo sapiens (human) | EC50 | 1.4440 | 1 | 1 |
| 2-(2,5-dimethoxyphenyl)ethanamine | Homo sapiens (human) | EC50 | 2.0100 | 1 | 1 |
| 2-chloro-2-phenethylamine | Homo sapiens (human) | EC50 | 0.0770 | 1 | 1 |
| 2-(4-bromo-2,5-dimethoxyphenyl)ethylamine | Homo sapiens (human) | EC50 | 7.1900 | 1 | 1 |
| proguanil | Homo sapiens (human) | EC50 | 10.0000 | 1 | 1 |
| 3-iodothyronamine | Homo sapiens (human) | EC50 | 1.1417 | 3 | 3 |
| 2,5-dimethoxy-4-bromoamphetamine, (r)-isomer | Homo sapiens (human) | EC50 | 31.9400 | 1 | 1 |
| 2,5-dimethoxy-4-bromoamphetamine, (s)-isomer | Homo sapiens (human) | EC50 | 15.3400 | 1 | 1 |
| ro5166017 | Homo sapiens (human) | EC50 | 0.0590 | 1 | 1 |
Ulotaront: A TAAR1 Agonist for the Treatment of Schizophrenia.ACS medicinal chemistry letters, , Jan-13, Volume: 13, Issue:1, 2022
Rational design, chemical synthesis and biological evaluation of novel biguanides exploring species-specificity responsiveness of TAAR1 agonists.European journal of medicinal chemistry, , Feb-25, Volume: 146, 2018
Trace amine-associated receptor 1 is a stereoselective binding site for compounds in the amphetamine class.Bioorganic & medicinal chemistry, , Dec-01, Volume: 19, Issue:23, 2011
Structure-activity correlations for beta-phenethylamines at human trace amine receptor 1.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Ulotaront: A TAAR1 Agonist for the Treatment of Schizophrenia.ACS medicinal chemistry letters, , Jan-13, Volume: 13, Issue:1, 2022
The Alkaloids from Journal of natural products, , 08-27, Volume: 84, Issue:8, 2021
Structure-activity correlations for beta-phenethylamines at human trace amine receptor 1.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Trace amine-associated receptor 1 is a stereoselective binding site for compounds in the amphetamine class.Bioorganic & medicinal chemistry, , Dec-01, Volume: 19, Issue:23, 2011
Structure-activity correlations for beta-phenethylamines at human trace amine receptor 1.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Ulotaront: A TAAR1 Agonist for the Treatment of Schizophrenia.ACS medicinal chemistry letters, , Jan-13, Volume: 13, Issue:1, 2022
Structure-activity correlations for beta-phenethylamines at human trace amine receptor 1.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Ulotaront: A TAAR1 Agonist for the Treatment of Schizophrenia.ACS medicinal chemistry letters, , Jan-13, Volume: 13, Issue:1, 2022
Structure-activity correlations for beta-phenethylamines at human trace amine receptor 1.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Trace amine-associated receptor 1 is a stereoselective binding site for compounds in the amphetamine class.Bioorganic & medicinal chemistry, , Dec-01, Volume: 19, Issue:23, 2011
Structure-activity correlations for beta-phenethylamines at human trace amine receptor 1.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Ulotaront: A TAAR1 Agonist for the Treatment of Schizophrenia.ACS medicinal chemistry letters, , Jan-13, Volume: 13, Issue:1, 2022
Novel biguanide-based derivatives scouted as TAAR1 agonists: Synthesis, biological evaluation, ADME prediction and molecular docking studies.European journal of medicinal chemistry, , Feb-15, Volume: 127, 2017
Trace amine-associated receptor 1 is a stereoselective binding site for compounds in the amphetamine class.Bioorganic & medicinal chemistry, , Dec-01, Volume: 19, Issue:23, 2011
Enables
This protein enables 2 target(s):
| Target | Category | Definition |
|---|
| G protein-coupled receptor activity | molecular function | Combining with an extracellular signal and transmitting the signal across the membrane by activating an associated G-protein; promotes the exchange of GDP for GTP on the alpha subunit of a heterotrimeric G-protein complex. [GOC:bf, http://www.iuphar-db.org, Wikipedia:GPCR] |
| trace-amine receptor activity | molecular function | Combining with a trace amine to initiate a change in cell activity. Trace amines are biogenic amines that are synthesized from aromatic amino acids and are substrates for monoamine oxidase, and are therefore detectable only at trace levels in mammals. [GOC:mah, PMID:19325074] |
Located In
This protein is located in 1 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
Involved In
This protein is involved in 1 target(s):
| Target | Category | Definition |
|---|
| G protein-coupled receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to its receptor, in which the activated receptor promotes the exchange of GDP for GTP on the alpha-subunit of an associated heterotrimeric G-protein complex. The GTP-bound activated alpha-G-protein then dissociates from the beta- and gamma-subunits to further transmit the signal within the cell. The pathway begins with receptor-ligand interaction, and ends with regulation of a downstream cellular process. The pathway can start from the plasma membrane, Golgi or nuclear membrane. [GOC:bf, GOC:mah, PMID:16902576, PMID:24568158, Wikipedia:G_protein-coupled_receptor] |