TABLE 3

CRTh2 antagonist human whole-blood (WBSC) and isolated cellular (ISC) shape-change potency values plus protein binding and physicochemical descriptors clogP, logD_7.4, and logK_IAM

Data are mean ± S.E.M. for three or more experiments.

CRTh2 Antagonist	cLogP	Log D_7.4^a	log K_IAM7.4^b	% Human Plasma Protein Unbound^c	WBSC IC₅₀	ISC IC₅₀
					nM	nM
QAW039	2.26	0.65	1.12	7.8	0.44 ± 0.19	0.40 ± 0.04
QAV680	1.15	−0.34	0.55	21.4	31.0 ± 1.0	5.0 ± 1.0
AZD-1981	4.79	1.19	1.77	1.8	13.10 ± 4.03	2.21 ± 0.87
OC-459	4.57	1.32	1.91	0.5	422.5 ± 155.9	6.4 ± 1.4
BI-671800	4.58	1.65	1.95	0.4	104.9 ± 35.3	1.87 ± 0.88
Ramatroban	3.97	1.34	1.89	2.7	195 ± 75.4	11.4 ± 1.9
Setipiprant	4.28	1.35	1.88	0.4	>500	10.7 ± 1.7

↵^a Determined by high-performance liquid chromatography (HPLC) column method (Kerns et al., 2003).
↵^b Determined by HPLC column method (Valko et al., 2000).
↵^c Determined by equilibrium dialysis (Banker et al., 2003).