. Author manuscript; available in PMC: 2017 Jun 7.

Published in final edited form as: Nature. 2016 Dec 7;540(7633):458–461. doi: 10.1038/nature20605

Extended Data Table 3.

Displacement of specific [³H]-INCB-3344 (5 nM) and [³H]-CCR2-RA (3 nM) binding from CCR2 constructs transiently expressed on CHO cells.

	[³H]-INCB-3344 displacement by INCB-3344	[³H]-INCB-3344 displacement by BMS-681	[³H]-CCR2-RA displacement by CCR2-RA-[R]	[³H]-CCR2-RA enhancement by BMS-681
Construct	pIC₅₀ ± S.E.M (IC₅₀, nM)			%Binding
WT CCR2	7.8 ± 0.0 (17)	8.1 ± 0.0 (8)	7.9 ± 0.0 (13)	134 ± 3%^a **
CCR2-T4L	8.1 ± 0.1* (8)	8.6 ± 0.1** (3)	8.2 ± 0.0** (6)	157 ± 13%^a ****

Values represent mean ± S.E.M of at three independent experiments performed in duplicate.

Percentage of [³H]-CCR2-RA (3 nM) binding in presence of BMS-681 (1 μM). Values higher than 100% represent binding enhancement compared to the 100% control without BMS-681.

Differences in pIC₅₀ values between constructs were analyzed using a Student’s t-test, with significant differences noted as follows: *p < 0.05, **p < 0.01.

Differences in %Binding in the absence (100%) and presence of BMS-681 were analyzed using a one-way ANOVA with Dunnett’s post-hoc test, with significant differences noted as follows: **p < 0.01, ****p < 0.0001.