R3(BΔ23-27)R/I5 chimeric peptide   Click here for help

GtoPdb Ligand ID: 3907

Compound class: Peptide or derivative
Comment: Synthetic chimeric peptide consisting of the A chain of human INSL5 linked via cysteine bonds to a synthetic analogue of the human relaxin 3 B chain. The two subunit components are linked by disulphide bonds between cysteine residues. The sequence of the relaxin 3 component is shown via the link in the structure tab; for the sequence of the other subunit see INSL5 (A chain).
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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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View interactive charts of activity data across species
References
1. Haugaard-Kedström LM, Shabanpoor F, Hossain MA, Clark RJ, Ryan PJ, Craik DJ, Gundlach AL, Wade JD, Bathgate RA, Rosengren KJ. (2011)
Design, synthesis, and characterization of a single-chain peptide antagonist for the relaxin-3 receptor RXFP3.
J Am Chem Soc, 133 (13): 4965-74. [PMID:21384867]
2. Kocan M, Sarwar M, Hossain MA, Wade JD, Summers RJ. (2014)
Signalling profiles of H3 relaxin, H2 relaxin and R3(BΔ23-27)R/I5 acting at the relaxin family peptide receptor 3 (RXFP3).
Br J Pharmacol, 171 (11): 2827-41. [PMID:24641548]
3. Kristensson L, Mayer G, Ploj K, Wetterlund M, Arlbrandt S, Björquist A, Wissing BM, Castaldo M, Larsson N. (2015)
Partial agonist activity of R3(BΔ23-27)R/I5 at RXFP3--investigation of in vivo and in vitro pharmacology.
Eur J Pharmacol, 747: 123-31. [PMID:25496752]
4. Kuei C, Sutton S, Bonaventure P, Pudiak C, Shelton J, Zhu J, Nepomuceno D, Wu J, Chen J, Kamme F et al.. (2007)
R3(BDelta23 27)R/I5 chimeric peptide, a selective antagonist for GPCR135 and GPCR142 over relaxin receptor LGR7: in vitro and in vivo characterization.
J Biol Chem, 282 (35): 25425-35. [PMID:17606621]