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. Author manuscript; available in PMC: 2016 May 12.
Published in final edited form as: Nat Rev Drug Discov. 2014 Mar;13(3):197–216. doi: 10.1038/nrd4100

Figure 5. Development of selective ROR ligands.

Figure 5

Following a screen of known nuclear receptor ligands against the entire nuclear receptor superfamily, the liver X receptor (LXR) agonist T0901317 was identified as a retinoic acid receptor-related orphan receptor (ROR) ligand. T0901317 has substantial promiscuity against other nuclear receptors. Various alterations in the structure led to the discovery of an agonist of RORα and RORγ (SR1078), an inverse agonist of RORα and RORγ (SR1001), and a RORγ-selective inverse agonist (SR2211). FXR, farnesoid X receptor; PXR, pregnane X receptor.