CP-481715 is a potent and selective CCR1 antagonist with Ki of 9.2 nM and IC50 of 74 nM, lacks intrinsic agonist activity.
CP-481715 displays >100-fold selectiveity over a panel of GPCRs including related chemokine receptors.
CP-481715 fully blocks the ability of CCL3 and CCL5 to stimulate receptor signaling (calcium mobilization, IC50=71 nM), monocyte chemotaxis, IC50= 55 nM, and MMP 9 release, IC50= 54 nM).
CP-481715 inhibits cell infiltration and inflammatory responses in human CCR1 transgenic mice.
