Table 1.

SAR439859 in vitro properties.

Assay descriptionERα transcriptionERβ transcriptionMCF7 ERαMCF7MCF7 (Y537S)MCF7 (D538G)
luciferaseluciferasedegradationcell viabilitycell viabilitycell viability
CompoundsIC50 (nmol/L)IC50 (nmol/L)DC50 (nmol/L)Dmax (%)IC50 (nmol/L)Emax (%)IC50 (nmol/L)Emax (%)IC50 (nmol/L)Emax (%)
SAR4398591.88.40.4981.16410.079.81.070.1
4-OH-Tamoxifen0.90.5NANA4.25320.161.46.551.8
Fulvestrant0.50.90.2980.3652.976.70.6568.1
  • Abbreviation: NA, not applicable.