TABLE 2

A summary of data from competitive binding experiments

Displacement of ¹²⁵I-CCL2 from cells expressing WT CCR2 and selected CCR2 point mutants, with increasing concentrations of unlabelled CCL2, TAK-779, or Teijin compound 1. The data are representative of three experiments. Data are presented as mean ± S.E.

Construct	CCL2 Displacement			TAK-779 Displacement			Teijin Compound 1 Displacement
Construct		IC₅₀	Log IC₅₀	IC₅₀	Log IC₅₀	IC₅₀	Log IC₅₀
	nM	M	nM	M	nM	M
WT CCR2	9.60	−8.02 ± 0.07	49.30	−7.307 ± 0.39	405.51	−6.392 ± 0.09
Y49A^1.39	N.S.B.	N.S.B.	N.S.B.	N.S.B.	N.S.B.	N.S.B.
W98A^2.60	N.S.B.	N.S.B.	N.S.B.	N.S.B.	N.S.B.	N.S.B.
Y120A^3.32	N.S.B.	N.S.B.	N.S.B.	N.S.B.	N.S.B.	N.S.B.
H121A^3.33	4.18	−8.38 ± 0.03	19.90	−7.70 ± 0.04	1127.20	−5.948 ± 0.43
I263A^6.55	3.18	−8.50 ± 0.04	12.85	−7.89 ± 0.03	787.05	−6.104 ± 0.13
E291Q^7.39	N.S.B.	N.S.B.	N.S.B.	N.S.B.	N.S.B.	N.S.B.
T292V^7.40	9.18	−8.04 ± 0.12	663.74	−6.178 ± 9.34	N.O.D.	N.O.D.

N.S.B., no specific binding (i.e., at a 1000-fold excess of unlabeled CCL2, less than 50% displacement of ¹²⁵I-CCL2 was observed). N.O.D., no observable displacement (i.e., at ≥1000-fold excess of antagonist, less than 50% displacement of ¹²⁵I-CCL2 was observed).