Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 56, Issue 11, Pages 4729-4737Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm400458q
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Funding
- EPSRC
- EPSRC [EP/H031111/1, EP/H031111/2, EP/I037253/1, EP/I037229/1] Funding Source: UKRI
- MRC [G0601556] Funding Source: UKRI
- Academy of Medical Sciences (AMS) [AMS-SGCL7-Blaikley] Funding Source: researchfish
- Engineering and Physical Sciences Research Council [EP/I037253/1, EP/I037229/1, EP/H031111/2, EP/H031111/1] Funding Source: researchfish
- Medical Research Council [G0601556] Funding Source: researchfish
- National Institute for Health Research [CL-2011-06-501] Funding Source: researchfish
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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.
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