Small molecule tertiary amines as agonists of the nuclear hormone receptor Rev-erbα
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.
Shin, Youseung,Noel, Romain,Banerjee, Subhashis,Kojetin, Douglas,Song, Xinyi,He, Yuanjun,Lin, Li,Cameron, Michael D.,Burris, Thomas P.,Kamenecka, Theodore M.
p. 4413 - 4417
(2012/07/17)
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