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Urotensin-2 receptor
A urotensin-2 receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q9UKP6]
Synonyms
UR-2-R;
G-protein coupled receptor 14;
Urotensin II receptor;
UR-II-R
Research
Bioassay Publications (12)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 7 (58.33) | 29.6817 |
| 2010's | 5 (41.67) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (6)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| ici 199441 | Homo sapiens (human) | Ki | 4.0000 | 1 | 1 |
| act 058362 | Homo sapiens (human) | IC50 | 0.1213 | 3 | 3 |
| act 058362 | Homo sapiens (human) | Ki | 0.0410 | 1 | 1 |
| sb 657510 | Homo sapiens (human) | IC50 | 0.0330 | 2 | 2 |
| sb-706375 | Homo sapiens (human) | IC50 | 0.0093 | 3 | 3 |
| sb-706375 | Homo sapiens (human) | Ki | 0.0067 | 2 | 2 |
| urotensin ii | Homo sapiens (human) | Ki | 0.0043 | 2 | 2 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| ac 7954 | Homo sapiens (human) | EC50 | 0.7832 | 5 | 5 |
| urotensin ii | Homo sapiens (human) | EC50 | 0.0035 | 2 | 2 |
Urotensin-II receptor modulators as potential drugs.Journal of medicinal chemistry, , Apr-08, Volume: 53, Issue:7, 2010
Optimization of isochromanone based urotensin II receptor agonists.Bioorganic & medicinal chemistry, , Jul-01, Volume: 18, Issue:13, 2010
Novel and potent small-molecule urotensin II receptor agonists.Bioorganic & medicinal chemistry, , Jul-01, Volume: 17, Issue:13, 2009
Novel potent and efficacious nonpeptidic urotensin II receptor agonists.Journal of medicinal chemistry, , Apr-06, Volume: 49, Issue:7, 2006
Architecture of the human urotensin II receptor: comparison of the binding domains of peptide and non-peptide urotensin II agonists.Journal of medicinal chemistry, , Apr-07, Volume: 48, Issue:7, 2005
Deconstruction of sulfonamide inhibitors of the urotensin receptor (UT) and design and synthesis of benzylamine and benzylsulfone antagonists.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 23, Issue:7, 2013
Nonpeptide urotensin-II receptor antagonists: a new ligand class based on piperazino-phthalimide and piperazino-isoindolinone subunits.Journal of medicinal chemistry, , Dec-10, Volume: 52, Issue:23, 2009
Deconstruction of sulfonamide inhibitors of the urotensin receptor (UT) and design and synthesis of benzylamine and benzylsulfone antagonists.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 23, Issue:7, 2013
Nonpeptide urotensin-II receptor antagonists: a new ligand class based on piperazino-phthalimide and piperazino-isoindolinone subunits.Journal of medicinal chemistry, , Dec-10, Volume: 52, Issue:23, 2009
Sequence-derived three-dimensional pharmacophore models for G-protein-coupled receptors and their application in virtual screening.Journal of medicinal chemistry, , May-14, Volume: 52, Issue:9, 2009
Functional Selectivity Revealed by N-Methylation Scanning of Human Urotensin II and Related Peptides.Journal of medicinal chemistry, , 02-14, Volume: 62, Issue:3, 2019
Lead optimization of P5U and urantide: discovery of novel potent ligands at the urotensin-II receptor.Journal of medicinal chemistry, , Jul-24, Volume: 57, Issue:14, 2014
Further studies at neuropeptide s position 5: discovery of novel neuropeptide S receptor antagonists.Journal of medicinal chemistry, , Jul-09, Volume: 52, Issue:13, 2009
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] |
| urotensin II receptor activity | molecular function | Combining with urotensin II to initiate a change in cell activity. [GOC:mah, PMID:15102493] |
Located In
This protein is located in 2 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] |
| membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
Active In
This protein is active 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 5 target(s):
| Target | Category | Definition |
|---|
| signal transduction | biological process | The cellular process in which a signal is conveyed to trigger a change in the activity or state of a cell. Signal transduction begins with reception of a signal (e.g. a ligand binding to a receptor or receptor activation by a stimulus such as light), or for signal transduction in the absence of ligand, signal-withdrawal or the activity of a constitutively active receptor. Signal transduction ends with regulation of a downstream cellular process, e.g. regulation of transcription or regulation of a metabolic process. Signal transduction covers signaling from receptors located on the surface of the cell and signaling via molecules located within the cell. For signaling between cells, signal transduction is restricted to events at and within the receiving cell. [GOC:go_curators, GOC:mtg_signaling_feb11] |
| blood circulation | biological process | The flow of blood through the body of an animal, enabling the transport of nutrients to the tissues and the removal of waste products. [GOC:mtg_heart, ISBN:0192800825] |
| regulation of blood pressure | biological process | Any process that modulates the force with which blood travels through the circulatory system. The process is controlled by a balance of processes that increase pressure and decrease pressure. [GOC:dph, GOC:mtg_cardio, ISBN:0721643949] |
| blood vessel diameter maintenance | biological process | Any process that modulates the diameter of blood vessels. [GOC:pr] |
| neuropeptide signaling pathway | biological process | A G protein-coupled receptor signaling pathway initiated by a neuropeptide binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process. [GOC:mah, ISBN:0815316194] |