Table 8.

In vitro target profile of Compound 3.

	Radioligand competition binding	Functional antagonism
GPCR	% Inhibition at 10 µM	IC50 (µM)	Kb (µM)	Fold selectivity over the human B2 receptor*
V1a	84	9.1	0.31	1,292
CRF1	74	10	3.6	15,000
TP	62	3.6	0.51	2,125
NK1	83	17	2.4	10,000
NK2	21	–	–	–
NK3	6.1	17	1.6	6,667
EP1	80	–	–	–

*Relative to the K_b at the human B₂ receptor (0.24 nM).