1675201-90-7

BMS-8 is a small molecule inhibitor of the protein-protein interaction between programmed death protein 1 (PD-1) and its ligand programmed cell death ligand 1 (PD-L1) with an IC₅₀ value of 146 nM in a homogeneous time-resolved fluorescence (HTRF) binding assay.

BMS-8 is inhibitor of the PD-1/PD-L1 interaction by inducing PD-L1 dimerization through PD-1 interacting surface, binding at a hydrophobic cavity formed upon PD-L1 dimerization.

[1] KATARZYNA GUZIK. 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-L1[J]. Journal of Medicinal Chemistry, 2017, 60 13: 5857-5867. DOI: 10.1021/acs.jmedchem.7b00293