Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORγ/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity.
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Gong H, et al. Among authors: sack js.
Bioorg Med Chem Lett. 2018 Jan 15;28(2):85-93. doi: 10.1016/j.bmcl.2017.12.006. Epub 2017 Dec 5.
Bioorg Med Chem Lett. 2018.
PMID: 29233651
Pharmacodynamic (PD) data for compound 35 in an IL-23 induced IL-17 mouse model is discussed along with the implications of a high Y(max) in the PXR assay for long term preclinical pharmacokinetic (PK) studies....
Pharmacodynamic (PD) data for compound 35 in an IL-23 induced IL-17 mouse model is discussed along with the implications of a high Y(max) in …