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REV-ERB alpha has emerged as an important target for regulation of circadian rhythm and its associated physiology. Herein, we report on the optimization of a series of REV-ERB alpha agonists based on G5K4112 (1) for potency, selectivity, and bioavailability.(1) Potent REV-ERB alpha agonists 4, 10, 16, and 23 are detailed for their ability to suppress BMAL and IL-6 expression from human cells while also demonstrating excellent selectivity over LAR alpha. Amine 4 demonstrated in vivo bioavailability after either iv or oral dosing.
- circadian behaviour
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- 1 Finished
SMSdrug.net: Alignment Of Synthesis, Medicinal Chemistry And Strucrural Genomics To Accelerate Uk Drug Discovery: Network SMS-Drug
1/09/11 → 31/08/15