Small molecule tertiary amines as agonists of the nuclear hormone receptor Rev-erbα

Abstract: The structure–activity relationship study of a small molecule Rev-erbα agonist is reported. The potency and efficacy of the agonists in a cell-based assay were optimized as compared to the initial lead. Modest mouse pharmacokinetics coupled with an improved in vitro profile make 12e a suitable in vivo probe to interrogate the functions of Rev-erbα in animal models of disease. [Copyright &y& Elsevier]

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