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Compound class: Synthetic organic
Comment: Probe 1.1 is a biased agonist for the κ opioid receptor . The compound was designed to preferentially bias KOR activation towards G protein signaling with minimal effects on βarrestin2 recruitment and downstream ERK1/2 activation.
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.✖
1. Zhou L, Lovell KM, Frankowski KJ, Slauson SR, Phillips AM, Streicher JM, Stahl E, Schmid CL, Hodder P, Madoux F et al.. (2013)
Development of functionally selective, small molecule agonists at kappa opioid receptors.
J. Biol. Chem., 288 (51): 36703-16. [PMID:24187130]