BMS 1166 is an inhibitor of the protein-protein interaction between programmed cell death 1 (PD-1) and its ligand PD-L1 that has an IC50 value of 1.4 nM in a homologous time-resolved fluorescence (HTRF) assay.1 It increases the activation of Jurkat cells expressing PD-1 in co-culture with CHO cells expressing PD-L1 (EC50 = 276 nM in a reporter assay).2
1.Guzik, K., Zak, K.M., Grudnik, P., et al.Small-molecule inhibitors of the programmed cell death-1/programmed death-ligand 1 (PD-1/PD-L1) interaction via transiently induced protein states and dimerization of PD-L1J. Med. Chem.60(13)5857-5867(2017) 2.Skalniak, L., Zak, K.M., Guzik, K., et al.Small-molecule inhibitors of PD-1/PD-L1 immune checkpoint alleviate the PD-L1-induced exhaustion of T-cellsOncotarget8(42)72167-72181(2017)