Table 3.

Structure–activity relationship exploration and metabolic stability in liver microsomes of amines and sulfur‐substituted compounds.

Compound	Y	PR transactivation assay		Metabolic stability assay
		IC50 [nm]	Efficacy [%]	F max Human [%]	F max Rat [%]
14		0.50	100	n.d.	n.d.
15		8.0	100	98	100
16		3.5	100	57	88
17		0.01	100	31	34
18 (vilaprisan)		0.09	100	94	87
19		0.9	100	75	69