9a-(4-chlorobenzyl)-7-hydroxy-4-(4-(2-(piperidin-1-yl)ethoxy)phenyl)-1,2,9,9a-tetrahydro-3H-fluoren-3-one

Uses

CMP8, a selective ligand for estrogen receptor, binds to the mutant estrogen receptor ligand binding domain (ERLBD). CMP8 exhibits IC50 values of 29 nM , 41 nM, 1100 nM and 2200 nM for MGERα, MGRERα, hERα and hERβ, respectively[1][2].

in vivo

IC 50

MGERα: 29 nM (IC₅₀); MGRERα: 41 nM (IC₅₀); hERα: 1100 nM (IC₅₀); hERβ: 2200 nM (IC₅₀)

References

[1] Miyazaki Y, et al. Destabilizing domains derived from the human estrogen receptor. J Am Chem Soc. 2012 Mar 7;134(9):3942-5. DOI:10.1021/ja209933r
[2] Kinzel O, et al. A structure-guided approach to an orthogonal estrogen-receptor-based gene switch activated by ligands suitable for in vivo studies. J Med Chem. 2006 Sep 7;49(18):5404-7. DOI:10.1021/jm060516e
[3] PAOLA GALLINARI. A functionally orthogonal estrogen receptor-based transcription switch specifically induced by a nonsteroid synthetic ligand.[J]. Chemistry & biology, 2005, 12 8: 883-893. DOI: 10.1016/j.chembiol.2005.05.018