Identification and structure activity relationships of quinoline tertiary alcohol modulators of RORγt

Add time:09/10/2019    Source:sciencedirect.com

A high-throughput screen of the ligand binding domain of the nuclear receptor retinoic acid-related orphan receptor gamma t (RORγt) employing a thermal shift assay yielded a quinoline tertiary alcohol hit. Optimization of the 2-, 3- and 4-positions of the quinoline core using structure-activity relationships and structure-based drug design methods led to the discovery of a series of modulators with improved RORγt inhibitory potency and inverse agonism properties.

We also recommend Trading Suppliers and Manufacturers of 4,6-DICHLORO-2-(TRIFLUOROMETHYL)QUINOLINE (cas 18706-33-7). Pls Click Website Link as below: cas 18706-33-7 suppliers

Prev:Short notePhotoinduced synthesis of quinoline derivatives catalyzed by organic photocatalyst at room temperature
Next:Synthesis, characterization and pharmacological activities of 2-[4-cyano-(3-trifluoromethyl)phenyl amino)]-4-(4-quinoline/coumarin-4-yloxy)-6-(fluoropiperazinyl)-s-triazines)