Table 3.

Preliminary SAR of compounds 57–61 (values were obtained from [75]).

Compd.	CRTH2 Binding (IC50 a)	Log D7.4	Rat Hep Clint b	Hum Mic Clint c	Agonism EOS Shape Change d	CRTH2 Ca2+ (IC50e)
57	18 nM	0.4	<4	6	IA	517 nM
58	316 nM		<3	5
59	10 nM	1.0	<3	11	IA
60	1.0 nM		<3	<3	IA	9 nM
61	0.3 nM	0.8	<3	<3	yes

^a Radiometric binding assay, n > 2 measurements. ^b Rat hepatocyte intrinsic clearance (µL/min/1 × 10⁶ cells). ^c Human liver microsomes intrinsic clearance (µL/min/mg). ^d Agonism in eosinophil shape change, IA refers to <10% response of DK-PGD₂. ^e Antagonism of PGD₂-mediated Ca²⁺ flux in human CHO cells, n > 2 measurements.