Proteins > Melanin-concentrating hormone receptor 1
Page last updated: 2024-08-07 17:23:26
Melanin-concentrating hormone receptor 1
A melanin-concentrating hormone receptor 1 that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q99705]
Synonyms
MCH receptor 1;
MCH-R1;
MCHR-1;
G-protein coupled receptor 24;
MCH-1R;
MCH1R;
MCHR;
SLC-1;
Somatostatin receptor-like protein
Research
Bioassay Publications (16)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 9 (56.25) | 29.6817 |
2010's | 7 (43.75) | 24.3611 |
2020's | 0 (0.00) | 2.80 |
Compounds (7)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
snap7941 | Homo sapiens (human) | Kd | 0.0006 | 1 | 1 |
Drugs with Other Measurements
Dihydropyrrolopyrazol-6-one MCHR1 antagonists for the treatment of obesity: Insights on in vivo efficacy from a novel FLIPR assay setup.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 25, Issue:14, 2015
Synthesis and SAR of 4-aryl-1-(indazol-5-yl)pyridin-2(1H)ones as MCH-1 antagonists for the treatment of obesity.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 20, Issue:23, 2010
Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: in vitro profiling and in vivo evaluation.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 19, Issue:21, 2009
Novel approach for chemotype hopping based on annotated databases of chemically feasible fragments and a prospective case study: new melanin concentrating hormone antagonists.Journal of medicinal chemistry, , Apr-09, Volume: 52, Issue:7, 2009
The discovery and optimization of pyrimidinone-containing MCH R1 antagonists.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 16, Issue:18, 2006
Discovery of novel phenylpyridone derivatives as potent and selective MCH1R antagonists.Bioorganic & medicinal chemistry, , Jan-15, Volume: 19, Issue:2, 2011
Melanin-concentrating hormone receptor 1 antagonists: synthesis, structure-activity relationship, docking studies, and biological evaluation of 2,3,4,5-tetrahydro-1H-3-benzazepine derivatives.Bioorganic & medicinal chemistry, , Nov-01, Volume: 19, Issue:21, 2011
Discovery, synthesis, and structure-activity relationship of 6-aminomethyl-7,8-dihydronaphthalenes as human melanin-concentrating hormone receptor 1 antagonists.Bioorganic & medicinal chemistry, , Sep-15, Volume: 19, Issue:18, 2011
Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: in vitro profiling and in vivo evaluation.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 19, Issue:21, 2009
Novel approach for chemotype hopping based on annotated databases of chemically feasible fragments and a prospective case study: new melanin concentrating hormone antagonists.Journal of medicinal chemistry, , Apr-09, Volume: 52, Issue:7, 2009
Design and synthesis of novel hydantoin-containing melanin-concentrating hormone receptor antagonists.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 17, Issue:13, 2007
Bis(aminopyrrolidine)-derived ureas (APUs) as potent MCH1 receptor antagonists.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 15, Issue:4, 2005
Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 2.Bioorganic & medicinal chemistry letters, , Oct-04, Volume: 14, Issue:19, 2004
A virtual screening approach to finding novel and potent antagonists at the melanin-concentrating hormone 1 receptor.Journal of medicinal chemistry, , Jul-29, Volume: 47, Issue:16, 2004
Identification of a new small molecule chemotype of Melanin Concentrating Hormone Receptor-1 antagonists using pharmacophore-based virtual screening.Bioorganic & medicinal chemistry letters, , 12-15, Volume: 29, Issue:24, 2019
Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: in vitro profiling and in vivo evaluation.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 19, Issue:21, 2009
Lead optimization of 4-(dimethylamino)quinazolines, potent and selective antagonists for the melanin-concentrating hormone receptor 1.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 15, Issue:17, 2005
Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: in vitro profiling and in vivo evaluation.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 19, Issue:21, 2009
Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 2.Bioorganic & medicinal chemistry letters, , Oct-04, Volume: 14, Issue:19, 2004
Enables
This protein enables 6 target(s):
Target | Category | Definition |
signaling receptor binding | molecular function | Binding to one or more specific sites on a receptor molecule, a macromolecule that undergoes combination with a hormone, neurotransmitter, drug or intracellular messenger to initiate a change in cell function. [GOC:bf, GOC:ceb, ISBN:0198506732] |
neuropeptide receptor activity | molecular function | Combining with a neuropeptide to initiate a change in cell activity. [GOC:ai] |
melanin-concentrating hormone receptor activity | molecular function | Combining with the cyclic peptide hormone melanin-concentrating hormone to initiate a change in cell activity. [GOC:mah] |
hormone binding | molecular function | Binding to an hormone, a naturally occurring substance secreted by specialized cells that affect the metabolism or behavior of cells possessing functional receptors for the hormone. Hormones may be produced by the same, or different, cell as express the receptor. [GOC:jl] |
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] |
neuropeptide binding | molecular function | Interacting selectively and non-covalently and stoichiometrically with neuropeptides, peptides with direct synaptic effects (peptide neurotransmitters) or indirect modulatory effects on the nervous system (peptide neuromodulators). [http://www.wormbook.org/chapters/www_neuropeptides/neuropeptides.html] |
Located In
This protein is located in 4 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] |
cilium | cellular component | A specialized eukaryotic organelle that consists of a filiform extrusion of the cell surface and of some cytoplasmic parts. Each cilium is largely bounded by an extrusion of the cytoplasmic (plasma) membrane, and contains a regular longitudinal array of microtubules, anchored to a basal body. [GOC:cilia, GOC:curators, GOC:kmv, GOC:vw, ISBN:0198547684, PMID:16824949, PMID:17009929, PMID:20144998] |
ciliary membrane | cellular component | The portion of the plasma membrane surrounding a cilium. [GOC:cilia, GOC:dph, GOC:rph] |
non-motile cilium | cellular component | A cilium which may have a variable array of axonemal microtubules but does not contain molecular motors. [GOC:cilia, GOC:dgh, GOC:kmv, PMID:17009929, PMID:20144998, PMID:22118931] |
Active In
This protein is active in 2 target(s):
Target | Category | Definition |
neuron projection | cellular component | A prolongation or process extending from a nerve cell, e.g. an axon or dendrite. [GOC:jl, http://www.cogsci.princeton.edu/~wn/] |
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 8 target(s):
Target | Category | Definition |
generation of precursor metabolites and energy | biological process | The chemical reactions and pathways resulting in the formation of precursor metabolites, substances from which energy is derived, and any process involved in the liberation of energy from these substances. [GOC:jl] |
cell surface receptor signaling pathway | biological process | The series of molecular signals initiated by an extracellular ligand binding to a receptor located on the cell surface. The pathway ends with regulation of a downstream cellular process, e.g. transcription. [GOC:signaling] |
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] |
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the inhibition of adenylyl cyclase activity and a subsequent decrease in the intracellular concentration of cyclic AMP (cAMP). [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194] |
positive regulation of cytosolic calcium ion concentration | biological process | Any process that increases the concentration of calcium ions in the cytosol. [GOC:ai] |
feeding behavior | biological process | Behavior associated with the intake of food. [GOC:mah] |
positive regulation of calcium ion transport | biological process | Any process that activates or increases the frequency, rate or extent of the directed movement of calcium ions into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. [GOC:ai] |
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] |