. 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 4.

Observed association and dissociation rate constants of [³H]-CCR2-RA (7 nM) on membranes from CHO cells transiently expressing WT CCR2 and CCR2-T4L, in the absence or presence of 1 μM BMS-681.

	CHO-CCR2		CHO-CCR2-T4L
	Control	+1 μM BMS-681	Control	+1 μM BMS-681
k_obs(min⁻¹)	0.031 ± 0.002	0.038 ± 0.003*	0.015 ± 0.003	0.015 ± 0.001
%B/B_control^a	100 ± 0.0	135 ± 2.0****	100 ± 0.0	162 ± 8.4**
k_off,fast (min⁻¹)	0.089 ± 0.015	0.069 ± 0.012*	0.077 ± 0.013	0.049 ± 0.003^b
k_off,slow (min⁻¹)	0.016 ± 0.005	0.012 ± 0.004	0.010 ± 0.003	0.049 ± 0.003^b
%fast	70 ± 10	71 ± 11	69 ±8	N/A^b

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

% B/B_control represents the % of maximum binding in absence (B_control) or presence (B) of BMS-681 (1 μM).

For CHO-CCR2-T4L only, dissociation kinetics of [³H]CCR2-RA (7 nM) in presence of BMS-681 (1 μM) fitted best with a monophasic exponential decay model, resulting in a single k_off value, as shown in the table. Thus for CHO-CCR2-T4L, the statistical significance between k_off measurements with and without BMS-681 could not be calculated.

Statistical significance was analyzed using a Student’s t-test, with significant differences versus control noted as follows: *p < 0.05, **p < 0.01, ****p<0.0001