CMP8

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]. IC50 & Target: IC50: 29 nM (MGERα) , 41 nM (MGRERα), 1100 nM (hERα), 2200 nM (hERβ)^[1][2]. In Vivo: CMP8 (Compound 20h) is dosed in male Balb-c mice (4 mg/kg, ip). The plasma concentration after 4 h is 1.5-fold its EC₅₀ in mammalian cells with a C_max of 0.5 µM after 30 min^[1][2].