2. Academic Validation
  3. Small molecule tertiary amines as agonists of the nuclear hormone receptor Rev-erbα

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

  • Bioorg Med Chem Lett. 2012 Jul 1;22(13):4413-7. doi: 10.1016/j.bmcl.2012.04.126.
Youseung Shin 1,  Romain Noel,  Subhashis Banerjee,  Douglas Kojetin,  Xinyi Song,  Yuanjun He,  Li Lin,  Michael D Cameron,  Thomas P Burris,  Theodore M Kamenecka
Affiliations

Affiliation

  • 1 Department of Molecular Therapeutics and Translational Research Institute, The Scripps Research Institute, Scripps Florida, 130 Scripps Way #A2A, Jupiter, FL 33458, USA.
PMID: 22633688 DOI: 10.1016/j.bmcl.2012.04.126
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.

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