Table 3.

CCR1 binding and activation parameters for CCL2/CCL7 chimeras

Binding inhibition constants are reported as pIC₅₀ values (−log₁₀ of the IC₅₀; in m) ± S.E. Potency values for receptor activation are reported as pEC₅₀ values (−log₁₀ of the EC₅₀; in m) ± S.E. The corresponding IC₅₀ and EC₅₀ values (in nm) are in parentheses. Maximal effects (E_max) are reported as normalized values; the maximal response used for normalization was CCL7 (1 μm) for βArr and GPA assays, forskolin (10 μm) for the cAMP assay, and FBS (10%) for the pERK assay. CCL7 was used as a reference in each assay for statistical analysis. ND, values that could not be determined from the data. *, p < 0.05; **, p < 0.01; ***, p < 0.001.

	CCR1 binding, pIC50	β-Arrestin-2 assay		GPA assay (αi2)		cAMP assay		pERK assay
		pEC50	Emax	pEC50	Emax	pEC50	Emax	pEC50	Emax
	m	m		m		m		m
CCL2	7.2 ± 0.2 (57)***	7.8 ± 0.3 (17)	58.6 ± 8**	<6.5 (>300)	ND	<6.5 (>300)	ND	6.9 ± 0.1 (130)***	24.2 ± 2***
CCL2-722	8.0 ± 0.1 (9.3)***	7.8 ± 0.2 (14)	72.1 ± 6	<6.5 (>300)	ND	6.9 ± 0.2 (277)**	38.4 ± 5	7.6 ± 0.2 (24)*	33.7 ± 2*
CCL2-272	9.0 ± 0.1 (1.0)	7.8 ± 0.1 (16)	70.5 ± 4	<6.5 (>300)	ND	7.3 ± 0.1 (54)	42.5 ± 3	7.7 ± 0.2 (22)	31.4 ± 2**
CCL2-227	7.2 ± 0.1 (63)***	<7.0 (>300)	ND	<6.5 (>300)	ND	<6.5 (>300)	ND	7.0 ± 0.1 (110)***	27.1 ± 2***
CCL2-777	9.8 ± 0.1 (0.2)***	8.3 ± 0.1 (5.6)	107.0 ± 6	7.3 ± 0.1 (45.9)	93.6 ± 4	7.6 ± 0.1 (26)	49.5 ± 3	7.8 ± 0.1 (15)	37.8 ± 2
CCL7	9.0 ± 0.1 (1.0)	8.3 ± 0.1 (5.2)	97.8 ± 5	7.4 ± 0.1 (35.7)	105.5 ± 5	7.9 ± 0.2 (14)	44.2 ± 3	8.2 ± 0.2 (6.0)	43.7 ± 2
CCL7-277	8.1 ± 0.1 (7.2)***	8.2 ± 0.2 (6.7)	76.5 ± 6	<6.5 (>300)	ND	7.5 ± 0.2 (33)	37.9 ± 3	7.2 ± 0.2 (64)***	32.3 ± 3**
CCL7-727	7.8 ± 0.1 (16)***	8.2 ± 0.2 (6.8)	82.6 ± 6	<6.5 (>300)	ND	7.2 ± 0.1 (62)*	39.7 ± 3	7.6 ± 0.1 (24)*	40.5 ± 1
CCL7-772	8.5 ± 0.2 (3.4)*	8.7 ± 0.2 (2.0)	97.4 ± 7	7.6 ± 0.1 (27.1)	90.4 ± 11	7.9 ± 0.1 (14)	50.3 ± 2	8.2 ± 0.1 (6.8)	50.2 ± 2
CCL7-222	7.2 ± 0.1 (61)***	ND	ND	<6.5 (>300)	ND	<6.5 (>300)	ND	6.5 ± 0.1 (350)***	22.1 ± 3***