Plerixafor is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM, respectively.

WZ811 is a small molecular and potency CXCR4 antagonist with EC50 of 0.3 nM.

AMD 3465 hexahydrobromide is a potent, selective CXCR4 antagonist and exhibits 8-fold higher affinity than AMD 3100 and inhibits SDF-1α-ligand binding (Ki = 41.7 nM).