Mavorixafor is a chemokine (C-X-C motif) receptor 4 (CXCR4) antagonist (IC50 = 13 nM in a radioligand binding assay).1 It is selective for CXCR4 over chemokine (C-C motif) receptor 1 (CCR1), CCR2b, CCR4, CCR5, CXCR1, and CXCR2 (IC50s = >10 ?M for all). Mavorixafor reduces chemotaxis of CCRF-CEM T cells induced by chemokine (C-X-C motif) ligand 12 (CXCL12; IC50 = 19 nM).2 It inhibits fusion of CHO-K1 cells expressing gp120 to P4-P5 MAGI cells with an IC50 value of 1.5 nM. It decreases HIV-1 NL4.3 viral replication in MT-4 cells and isolated human peripheral blood mononuclear cells (PBMCs; IC50s = 2 and 9 nM, respectively).1
1.Skerlj, R.T., Bridger, G.J., Kaller, A., et al.Discovery of novel small molecule orally bioavailable C–X–C chemokine receptor 4 antagonists that are potent inhibitors of T-tropic (X4) HIV-1 replicationJ. Med. Chem.53(8)3376-3388(2010) 2.Mosi, R.M., Anastassova, V., Cox, J., et al.The molecular pharmacology of AMD11070: An orally bioavailable CXCR4 HIV entry inhibitorBiochem. Pharmacol.83(4)472-479(2012)