Table 3.

Curve-fitting parameters for CCL3-mediated receptor internalization, chemotaxis and β-arrestin translocation

	AZD4818	BX471	CCX354	CP481715	MLN-3897	PS899877
pIC50 for CCL3-mediated CCR1 internalizationa	6.91 ± 0.24 n = 4	6.87 ± 1.34 n = 2	6.08 ± 2.39 n = 2	NC	6.07 ± 0.55 n = 3	6.68 ± 0.20 n = 2
pIC50 for CCL3-mediated chemotaxisb	8.96 ± 0.71 n = 3	8.49 ± 0.36 n = 4	9.06 ± 0.51 n = 4	7.56 ± 0.14 n = 4	9.2 ± 0.10 n = 3	8.32 ± 0.32 n = 3
pkB for β-arrestin translocationc	8.58 ± 0.59 n = 4	9.15 ± 0.51 n = 7	6.93 ± 0.04 n = 2	8.26 ± 0.98 n = 4	7.74 ± 0.44 n = 8	8.86 ± 0.21 n = 2

The table summarizes the curve parameters of the six CCR1 antagonists analysed. For CCR1 internalization and chemotaxis, the results provided are the pIC₅₀ mean ± SE for the noted number of independent experiments. In the case of CCR1 internalization ∼10 0000 events were examined for each experiment. For chemotaxis each point was performed in quadruplicate and the number of cells that migrated spontaneously to the chemotaxis buffer was subtracted. The chemotactic index was then determined by dividing the number of migrated cells in the presence of the antagonist by the number of cells that migrated spontaneously to CCL3. Non-linear regression analysis was performed using GraphPad Prism (version 6.0). For β-arrestin translocation the results provided are the mean equilibrium dissociation constant (pkB) ± SEM (Christopoulos and Kenakin, 2002) for the noted number of independent experiments, each being performed in triplicate. NC indicates a curve could not be generated.

^aValues obtained with baseline constrained to 1.0 and maximum set to be greater than 2.0.

^bValues obtained with baseline constrained to 1.0.

^cValues obtained with no constraints on the baseline or maxima of concentration–response curves.