BMS-457 is a potent and selective CCR1 antagonist with binding IC50 of 0.8 nM, >1,000-fold selectivity against other CC family receptors.
BMS-457 displays single-digit nanomolar inhibition of chemotaxis induced by a number of CCR1 ligands, including MIP-1α( IC50=2.1 nM), Leukotactin-1 (IC50=4.4 nM), RANTES (IC50=1.0 nM), MPIF-1 (IC50=2.7 nM), and HCC-1 (IC50=4.0 nM).
BMS-457 blocks the ligand-stimulated upregulation of the β2-integrin CD11b in whole blood, with IC50 of 46 nM (MIP-1α) and 54 nM (LKN-1).
