CCR2 is the receptor for the chemokine CCL2, known commonly as monocyte chemotactic protein-1 (MCP-1). INCB 3284 is a potent, selective, and orally bioavailable antagonist of monocyte chemotactic protein-1 binding to CCR2 (IC50 = 3.7 nM). For comparison, it has no significant inhibitor action at over 50 ion channels, transporters, GPCRs, and other chemokine receptors when tested at a concentration of 1 μM. INCB 3284 inhibits chemotaxis in vitro (IC50 = 4.7 nM) and displays acceptable oral bioavailability in mice, rats, dogs, monkeys, and chimpanzees.
