- Advanced search
- Immuno Portal
- Malaria Portal
Synonyms: BIM-22493 | Imcivree® | IRC-022493 | RM-493
setmelanotide is an approved drug (FDA (2020), EMA (2021))
Compound class: Peptide or derivative
Comment: Setmelanotide is an agonist of melanocortin receptors, with approximately 20-fold selectivity for the melanocortin 4 receptor subtype . Chemically it is an eight-amino-acid cyclic peptide, that is able to cross the blood-brain barrier when administered peripherally. Setmelanotide offers anti-obesity potential.
The INN record documents the sequence as N2-acetyl-L-arginyl-L-cysteinyl-D-alanyl-L-histidyl-D-phenylalanyl-L-arginyl-L-tryptophyl-L-cysteinamide, cyclic (2-8)-disulfide.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
|EC50 values for cAMP production in vitro vs. human melanocortin receptors are MC4R (0.27mM), MC3R (5.3nM), MC1R (5.8nM), and rat MC4R (0.28nM) .|
|Selectivity at GPCRs|
|Key to terms and symbols||Click column headers to sort|