tethered chemerin 9   Click here for help

GtoPdb Ligand ID: 9784

Immunopharmacology Ligand
Compound class: Peptide or derivative
Comment: This is a synthetic peptide designed as a long-acting CMKLR1 agonist. The construct tethers the potent chemerin receptor agonist chemerin C-terminal peptide to the outer surface of the cell membrane, in juxtaposition to the receptor [1].
Structural and sequence details are:
1-56 TNFα type II transmembrane domain
57-78 repetitive glycine-asparagine linker
79-88 myc epitope tag
89-99 repetitive glycine-asparagine linker
100-108 chemerin C-terminal peptide at the carboxy terminal of the construct [1-2].
In vivo delivery is achieved by lipidating the chemerin nonapeptide portion of the construct [1].
The potent chemoattractant mediating effects of CMKLR1 has lead to the development of chemerin agonists as candidate therapeutics to improve resolution of inflammation, particularly as has been established in asthma models [3].
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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.

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Bioactivity Comments
The binding affinity of this peptide to CMKLR1 was not determined in [1], but it it unlikely to differ significantly from the affinity published in [5] for the isolated nonapeptide, chemerin (149-157).
Selectivity at GPCRs
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
chemerin receptor 1 Hs Agonist Agonist ~8.3 pIC50 - 1,4
⤷ pIC50 ~8.3 (IC50 ~5.5x10-9 M) [1,4]
Description: Binding affinity in a radioligand displacement assay using membranes prepared from chemerinR-expressing CHO-K1 cells and 125I-YHSFFFPGQFAFS as tracer.