BMS-1001 is a potent inhibitor of PD-1/PD-L1 interaction(IC50 : 2.25 nM, in a homogenous time-resolved fluorescence binding assay).

The small-molecule inhibitors of the PD-1/PD-L1 interaction, BMS-1001 , ?bind to human PD-L1 and block its interaction with PD-1, when tested on isolated proteins.?The compounds present low toxicity towards tested cell lines and block the interaction of soluble PD-L1 with the cell surface-expressed PD-1.?BMS-1001 alleviate the inhibitory effect of the soluble PD-L1 on the T-cell receptor-mediated activation of T-lymphocytes.?Moreover, the compounds were effective in attenuating the inhibitory effect of the cell surface-associated PD-L1.