Page last updated: 2024-08-07 12:43:58
Orexin receptor type 1
An orexin/hypocretin receptor type 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:O43613]
Synonyms
Ox-1-R;
Ox1-R;
Ox1R;
Hypocretin receptor type 1
Research
Bioassay Publications (29)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 5 (17.24) | 29.6817 |
2010's | 20 (68.97) | 24.3611 |
2020's | 4 (13.79) | 2.80 |
Compounds (16)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
sb 408124 | Homo sapiens (human) | Kd | 0.0269 | 1 | 1 |
sb674042 | Homo sapiens (human) | Kd | 0.0051 | 1 | 1 |
oroxin b | Homo sapiens (human) | EC50 | 1.2504 | 2 | 2 |
orexin-a | Homo sapiens (human) | EC50 | 0.0101 | 3 | 3 |
Drugs with Other Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
sr141716 | Homo sapiens (human) | Ke | 6.6670 | 3 | 3 |
sb 334867-a | Homo sapiens (human) | Ke | 0.0450 | 1 | 1 |
gsk 1059865 | Homo sapiens (human) | Kb | 0.0016 | 1 | 1 |
Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis.Journal of medicinal chemistry, , 02-27, Volume: 63, Issue:4, 2020
Selective orexin receptor antagonists.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 23, Issue:17, 2013
Biomedical application of orexin/hypocretin receptor ligands in neuroscience.Journal of medicinal chemistry, , Feb-26, Volume: 52, Issue:4, 2009
Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis.Journal of medicinal chemistry, , 02-27, Volume: 63, Issue:4, 2020
Substituted Azabicyclo[2.2.1]heptanes as Selective Orexin-1 Antagonists: Discovery of JNJ-54717793.ACS medicinal chemistry letters, , Oct-08, Volume: 11, Issue:10, 2020
Imidazopyridine-based selective and multifunctional ligands of biological targets associated with psychiatric and neurodegenerative diseases.European journal of medicinal chemistry, , Nov-01, Volume: 181, 2019
Discovery of highly potent and selective orexin 1 receptor antagonists (1-SORAs) suitable for in vivo interrogation of orexin 1 receptor pharmacology.Bioorganic & medicinal chemistry letters, , 12-01, Volume: 26, Issue:23, 2016
Pharmacophore Model To Discover OX1 and OX2 Orexin Receptor Ligands.Journal of medicinal chemistry, , Sep-22, Volume: 59, Issue:18, 2016
Disubstituted piperidines as potent orexin (hypocretin) receptor antagonists.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 22, Issue:12, 2012
Diaryl urea analogues of SB-334867 as orexin-1 receptor antagonists.Bioorganic & medicinal chemistry letters, , May-15, Volume: 21, Issue:10, 2011
Structure-Based Discovery of Novel Ligands for the Orexin 2 Receptor.Journal of medicinal chemistry, , 10-08, Volume: 63, Issue:19, 2020
Novel Octahydropyrrolo[3,4-c]pyrroles Are Selective Orexin-2 Antagonists: SAR Leading to a Clinical Candidate.Journal of medicinal chemistry, , Jul-23, Volume: 58, Issue:14, 2015
Selective orexin receptor antagonists.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 23, Issue:17, 2013
Biomedical application of orexin/hypocretin receptor ligands in neuroscience.Journal of medicinal chemistry, , Feb-26, Volume: 52, Issue:4, 2009
Novel substituted 4-phenyl-[1,3]dioxanes: potent and selective orexin receptor 2 (OX(2)R) antagonists.Bioorganic & medicinal chemistry letters, , Aug-16, Volume: 14, Issue:16, 2004
Structure-Based Discovery of Novel Ligands for the Orexin 2 Receptor.Journal of medicinal chemistry, , 10-08, Volume: 63, Issue:19, 2020
Selective orexin receptor antagonists.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 23, Issue:17, 2013
Biomedical application of orexin/hypocretin receptor ligands in neuroscience.Journal of medicinal chemistry, , Feb-26, Volume: 52, Issue:4, 2009
Selective orexin receptor antagonists.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 23, Issue:17, 2013
Biomedical application of orexin/hypocretin receptor ligands in neuroscience.Journal of medicinal chemistry, , Feb-26, Volume: 52, Issue:4, 2009
N-acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline: the first orexin-2 receptor selective non-peptidic antagonist.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 13, Issue:24, 2003
Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia.Journal of medicinal chemistry, , Jan-28, Volume: 59, Issue:2, 2016
Selective orexin receptor antagonists.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 23, Issue:17, 2013
Substituted tetrahydroisoquinolines as selective antagonists for the orexin 1 receptor.Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
Structure-activity relationship studies and sleep-promoting activity of novel 1-chloro-5,6,7,8-tetrahydroimidazo[1,5-a]pyrazine derivatives as dual orexin receptor antagonists. Part 2.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 23, Issue:13, 2013
Biomedical application of orexin/hypocretin receptor ligands in neuroscience.Journal of medicinal chemistry, , Feb-26, Volume: 52, Issue:4, 2009
Structure-Based Discovery of Novel Ligands for the Orexin 2 Receptor.Journal of medicinal chemistry, , 10-08, Volume: 63, Issue:19, 2020
Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis.Journal of medicinal chemistry, , 02-27, Volume: 63, Issue:4, 2020
Discovery of novel substituted octahydropyrrolo[3,4-c]pyrroles as dual orexin receptor antagonists for insomnia treatment.Bioorganic & medicinal chemistry letters, , 03-15, Volume: 27, Issue:6, 2017
Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia.Journal of medicinal chemistry, , Jan-28, Volume: 59, Issue:2, 2016
Discovery of dual orexin receptor antagonists with rat sleep efficacy enabled by expansion of the acetonitrile-assisted/diphosgene-mediated 2,4-dichloropyrimidine synthesis.Bioorganic & medicinal chemistry letters, , May-01, Volume: 24, Issue:9, 2014
Selective orexin receptor antagonists.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 23, Issue:17, 2013
Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia.Journal of medicinal chemistry, , Jul-22, Volume: 53, Issue:14, 2010
Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis.Journal of medicinal chemistry, , 02-27, Volume: 63, Issue:4, 2020
Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia.Journal of medicinal chemistry, , Jan-28, Volume: 59, Issue:2, 2016
Discovery of piperidine ethers as selective orexin receptor antagonists (SORAs) inspired by filorexant.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 25, Issue:3, 2015
Recent trends in orexin research--2010 to 2015.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 25, Issue:15, 2015
Selective orexin receptor antagonists.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 23, Issue:17, 2013
Selective orexin receptor antagonists.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 23, Issue:17, 2013
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 21, Issue:18, 2011
2-Methyl-3-furanyl-4H-1,2,4-triazol-3-ylthioamides: a new class of selective orexin 2 antagonists.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 20, Issue:22, 2010
Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis.Journal of medicinal chemistry, , 02-27, Volume: 63, Issue:4, 2020
Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia.Journal of medicinal chemistry, , Jan-28, Volume: 59, Issue:2, 2016
Recent trends in orexin research--2010 to 2015.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 25, Issue:15, 2015
[no title available]Bioorganic & medicinal chemistry letters, , 03-15, Volume: 60, 2022
Development of an orexin-2 receptor selective agonist, [Ala(11), D-Leu(15)]orexin-B.Bioorganic & medicinal chemistry letters, , Jan-06, Volume: 13, Issue:1, 2003
Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis.Journal of medicinal chemistry, , 02-27, Volume: 63, Issue:4, 2020
Selective orexin receptor antagonists.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 23, Issue:17, 2013
Substituted Azabicyclo[2.2.1]heptanes as Selective Orexin-1 Antagonists: Discovery of JNJ-54717793.ACS medicinal chemistry letters, , Oct-08, Volume: 11, Issue:10, 2020
Recent trends in orexin research--2010 to 2015.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 25, Issue:15, 2015
Substituted tetrahydroisoquinolines as selective antagonists for the orexin 1 receptor.Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
Selective orexin receptor antagonists.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 23, Issue:17, 2013
[no title available]Bioorganic & medicinal chemistry letters, , 03-15, Volume: 60, 2022
Truncated Orexin Peptides: Structure-Activity Relationship Studies.ACS medicinal chemistry letters, , Dec-12, Volume: 4, Issue:12, 2013
Substituted tetrahydroisoquinolines as selective antagonists for the orexin 1 receptor.Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
Structure-activity analysis of truncated orexin-A analogues at the orexin-1 receptor.Bioorganic & medicinal chemistry letters, , Mar-12, Volume: 11, Issue:5, 2001
Enables
This protein enables 5 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] |
protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
orexin receptor activity | molecular function | Combining with orexin to initiate a change in cell activity. [GOC:ai] |
peptide hormone binding | molecular function | Binding to a peptide with hormonal activity in animals. [GOC:jl, ISBN:0198506732] |
peptide binding | molecular function | Binding to a peptide, an organic compound comprising two or more amino acids linked by peptide bonds. [GOC:jl] |
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] |
synapse | cellular component | The junction between an axon of one neuron and a dendrite of another neuron, a muscle fiber or a glial cell. As the axon approaches the synapse it enlarges into a specialized structure, the presynaptic terminal bouton, which contains mitochondria and synaptic vesicles. At the tip of the terminal bouton is the presynaptic membrane; facing it, and separated from it by a minute cleft (the synaptic cleft) is a specialized area of membrane on the receiving cell, known as the postsynaptic membrane. In response to the arrival of nerve impulses, the presynaptic terminal bouton secretes molecules of neurotransmitters into the synaptic cleft. These diffuse across the cleft and transmit the signal to the postsynaptic membrane. [GOC:aruk, ISBN:0198506732, PMID:24619342, PMID:29383328, PMID:31998110] |
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 6 target(s):
Target | Category | Definition |
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] |
chemical synaptic transmission | biological process | The vesicular release of classical neurotransmitter molecules from a presynapse, across a chemical synapse, the subsequent activation of neurotransmitter receptors at the postsynapse of a target cell (neuron, muscle, or secretory cell) and the effects of this activation on the postsynaptic membrane potential and ionic composition of the postsynaptic cytosol. This process encompasses both spontaneous and evoked release of neurotransmitter and all parts of synaptic vesicle exocytosis. Evoked transmission starts with the arrival of an action potential at the presynapse. [GOC:jl, MeSH:D009435] |
feeding behavior | biological process | Behavior associated with the intake of food. [GOC:mah] |
regulation of cytosolic calcium ion concentration | biological process | Any process involved in the maintenance of an internal steady state of calcium ions within the cytosol of a cell or between the cytosol and its surroundings. [GOC:ai, GOC:mah, GOC:rph] |
positive regulation of ERK1 and ERK2 cascade | biological process | Any process that activates or increases the frequency, rate or extent of signal transduction mediated by the ERK1 and ERK2 cascade. [GOC:mah] |
cellular response to hormone stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a hormone stimulus. [GOC:mah] |