INCB10820 (PF-4178903) is a potent, selective, orally bioavailable dual CCR2 and CCR5 antagonist with binding IC50 of 3.0 nM and 5.3 nM, respectively.
INCB10820 displays an IC50 of 4.3 nM in CCR5 chemotaxis functional assay.
INCB10820 is active against mouse, rat and cynomolgus monkey CCR2 with binding IC50 of 2.8, 2.9 and 4.6 nM, respectively, but inactive against canine CCR2, also is active against mouse and cynomolgus monkey CCR5 with IC50 of 71 and 4.0 nM, respectively.
