PD-1/PD-L1-IN-14 (compound 17) is a bifunctional inhibitor of PD-1/PD-L1 interactions, with an IC50 of 27.8 nM. PD-1/PD-L1-IN-14 (compound 17) inhibits PD-1/PD-L1 interactions and promotes dimerization, internalization, and degradation of PD-L1.

[D-Leu-4]-OB3 inhibits expressions of pro-inflammatory, proliferative and metastatic genes and PD-L1 expression. [D-Leu-4]-OB3 stimulates expression of pro-apoptotic genes.

Evixapodlin is a highly potent, small molecule human PD-1/PD-L1 protein-protein interaction inhibitor with IC50 of 0.213 nM, exhibits potential anticancer and antiviral activities.

PD-L1 inhibitor 4 is a small molecule inhibitor of PD-1/PD-L1 with SPR KD of 0.079 nM.PD-L1 inhibitor 4 exhibited substantially increased binding affinity to hPD-L1, as well as PD-1/PD-L1 inhibitory activity in physiological conditions.PD-L1 inhibitor 4 also showed a dose-dependent increase in IFN-γ secretion levels in a mixed lymphocyte reaction assay.

ZE132 is a potent and selective small-molecule inhibitor of PD-1/PD-L1 interaction with IC50 of <0.1 nM.ZE132 effectively inhibits the PD-1/PD-L1 interactions in vitro, and has a potent affinity to PD-L1.ZE132 shows robust anti-tumour effects in vivo, better than anti-PD-1 antibody.ZE132 treatment promotes cytotoxic T-cell tumour infiltration and induces IL-2 expression.ZE132 elicits strong inhibitory effects on the mRNA expression of TGF-β.

N2S2-CBMBC, an N2S2 bromo-benzyl ether derivative, acts as a ligand and use 99mTc-labelled complexes 99mTc-N2S2-CBMBC can be used as an imaging agent to be applied to the aspect of detecting PD-L1 expression, realize the real-time, comprehensive and convenient detection of the PD-L1 level of tumors, and overcome the defects of an immunohistochemical method.

HE-S2 is an antibody-drug conjugate triggering a potent antitumor immune response. HE-S2 acts by blocking the PD-1/PD-L1 interaction and activating the Toll-like receptor 7/8 (TLR7/8) signaling pathway. HE-S2 has remarkable antitumor activity.

PD-1/PD-L1-IN 6 (compound A13) is a potent PD-1/PD-L1 interaction inhibitor, with an IC50 of 132.8 nM. PD-1/PD-L1-IN 6 exhibits outstanding immunoregulatory activity. PD-1/PD-L1-IN 6 significantly elevates interferon-γ secretion in a Hep3B/OS-8/hPD-L1 and CD3 T cell co-culture model, without significant toxic effect. PD-1/PD-L1-IN 6 restores the immune response in a T cell-tumor co-culture model.

BMS-37 is a PD-1/PD-L1 immune checkpoint inhibitor. BMS-37 can be used as PD-L1 ligand to synthesize PROTAC molecules.

BMS135 is a small molecule h-PD1/h-PD-L1 interaction inhibitor with IC50 of 79.1 nM, bind specifically to hPD-L1 through a unique mode of action, induces the dimerization of hPD-L1.

BMS136 is a small molecule h-PD1/h-PD-L1 interaction inhibitor with IC50 of 96.7 nM, bind specifically to hPD-L1 through a unique mode of action, induces the dimerization of hPD-L1.

IMMH-010 (YPD-30) is an ester prodrug of YPD-29B, a high potent PD-L1 inhibitor (IC50=0.08 pM), YPD-30 is a potent PD-L1 inhibitor with IC50 of 45.2 nM in HTRF assays.

IMMH-010 maleate (YPD-30) is an ester prodrug of YPD-29B, a high potent PD-L1 inhibitor (IC50=0.08 pM), YPD-30 is a potent PD-L1 inhibitor with IC50 of 45.2 nM in HTRF assays.

MAX10181 (MAX-10181) is an orally active small molecule PD-L1 inhibitor, shows similar efficacy as Durvalumab in the head to head test of human PD-L1 knock-in MC38 cell line in human PD-1 knock-in mice.

YPD-29B is a potent, specific programmed cell death ligand 1 (PD-L1) inhibitor, effectively blocks the binding of PD-1 and PD-L1 with IC50 of 0.08 pM in HTRF protein-protein interaction assays.