Synonyms: MRL871
Compound class:
Synthetic organic
Comment: MRL-871 is a negative allosteric modulator of the nuclear hormone receptor RORγt [1,3]. It binds to a site in the receptor's ligand binding domain that is distal to the canonical ortherosteric binding site.
Ligand Activity Visualisation ChartsThese 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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Immunopharmacology Comments |
RORγt is a master regulator of Th17 cells and affects the production of numerous cytokines (IL-17A, IL-17F, IL-22, IL-26, and GM-CSF). Orthosteric, and more recently, allosteric inhibitors of RORγt are being investigated as alternatives to anti-IL-17 antibody therapeutics (e.g. secukinumab, ixekizumab) for the treatment of autoimmune diseases that are driven by Th17 cytokines. |