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Compound class: Synthetic organic
Comment: SR1001 is a synthetic retinoic-acid-receptor-related orphan receptor (ROR) modulator . Its interaction with the ligand binding sites of RORα and RORγt induces conformational changes in these receptors that alter co-activator/co-repressor binding affinity, and which lead to suppression of the receptors' transcriptional activity. Chemically SR1001 is a derivative of the liver X receptor ligand T0901317, which has been shown to act as an inverse agonist of RORα and RORγ .
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.✖
|SR1001 has high affinity for both RORα and RORγt. It suppresses Th17 cell differentiation and production of Th17 cytokines in vitro and in vivo, and reduces clinical severity of autoimmune disease in a mouse multiple scelrosis model .|