Page last updated: 2024-08-07 12:43:38
Motilin receptor
A motilin receptor that is encoded in the genome of human. [PRO:DNx, UniProtKB:O43193]
Synonyms
G-protein coupled receptor 38
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 | 4 (50.00) | 29.6817 |
| 2010's | 3 (37.50) | 24.3611 |
| 2020's | 1 (12.50) | 2.80 |
Compounds (5)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| erythromycin | Homo sapiens (human) | Ki | 37.0000 | 1 | 1 |
| nitd 609 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
Drugs with Activation Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| yil 781 | Homo sapiens (human) | Activity | 1.0000 | 1 | 1 |
The role of the 4''-hydroxyl on motilin agonist potency in the 9-dihydroerythromycin series.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 21, Issue:12, 2011
9-Dihydroerythromycin ethers as motilin agonists--developing structure-activity relationships for potency and safety.Bioorganic & medicinal chemistry, , Nov-01, Volume: 18, Issue:21, 2010
Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate.Journal of medicinal chemistry, , Feb-26, Volume: 52, Issue:4, 2009
The discovery of biaryl carboxamides as novel small molecule agonists of the motilin receptor.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 18, Issue:24, 2008
Discovery of a potent and novel motilin agonist.Journal of medicinal chemistry, , Mar-25, Volume: 47, Issue:7, 2004
Discovery of DS-3801b, a non-macrolide GPR38 agonist with N-methylanilide structure.Bioorganic & medicinal chemistry letters, , 03-01, Volume: 59, 2022
Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate.Journal of medicinal chemistry, , Feb-26, Volume: 52, Issue:4, 2009
Discovery of DS-3801b, a non-macrolide GPR38 agonist with N-methylanilide structure.Bioorganic & medicinal chemistry letters, , 03-01, Volume: 59, 2022
Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate.Journal of medicinal chemistry, , Feb-26, Volume: 52, Issue:4, 2009
Enables
This protein enables 2 target(s):
| Target | Category | Definition |
|---|
| G protein-coupled peptide receptor activity | molecular function | Combining with a peptide 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:dph, GOC:tb] |
| 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] |
Located In
This protein is located in 2 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] |
| 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] |
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 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] |