Table 1.

Kinetic characterization of [³H]INCB3344 and 15a in membranes of CHO cells transiently expressing murine CCR2 (mCCR2).

	[3H]INCB3344 (hCCR2b*)	15a (hCCR2b†)
KRI‡	1.0 (1.0)	1.6 (1.7)
k on (nM−1 min−1)	0.030 ± 0.003 (0.054)	0.007 ± 0.001 (0.008)
k off (min−1)	0.227 ± 0.031 (0.013)	0.051 ± 0.008 (0.0014)
K D § (nM)	7.6 ± 1.3 (0.23)	7.4 ± 1.5 (0.175)
RT|| (min)	4.4 ± 0.6 (76)	19.7 ± 3.1 (714)

Values are means ± S.E.M of three separate experiments performed in duplicate.

^*Values of [³H]INCB3344 for hCCR2b were taken from Vilums et al. ²⁵.

^†Values of 15a for hCCR2b were taken from Vilums et al. ²⁴.

^‡Kinetic rate index (KRI) = B_t1/B_t2 (see Materials and Methods).

^§ K _D = k _off/k _on.

^||RT = 1/k _off.