NPH16 is an orally active PD-1/PD-L1 inhibitor with an IC50 of 24.4 nM. NPH16 can promote HepG2 cell apoptosis. NPH16 shows excellent in vivo antitumor efficacy and favorable pharmacokinetic properties. NPH16 can be used for the study of liver cancer.

SCL-1 is an orally active anti-PD-1/PD-L1 inhibitor. SCL-1 can inhibit PD-1/PD-L1 binding. SCL-1 increases T cells, B cells and natural killer cells. SCL-1 exerts strong tumor growth inhibitory effects that were mediated by effector T-cell induction inside tumors and the up-regulated expression of long non-coding RNAs as neoantigens leading to cytotoxic T lymphocyte activation. SCL-1 can be used for the research of cancer, such as triple-negative breast cancer.

GJ19 is a PD-L1 inhibitor with an IC50 of 32.06 nM. GJ19 can effectively bind to human/murine PD-L1 protein with KD values of 171 and 290 nM, respectively. GJ19 concentration-dependently promotes HepG2 cell mortality in a co-culture model of HepG2/hPD-L1 and Jurkat T/hPD-1 cells. GJ19 effectively suppresses tumor growth in a B16-F10 melanoma mouse model. GJ19 can be used for the study of tumor immunotherapy.

XQ-P3 sodium is an aptamer that binds to PD-L1. XQ-P3 can inhibit the PD-1/PD-L1 interaction and restore the function of T cells to detect and attack tumor cells.

Cadapersen (RG6084) is an antisense oligonucleotide that induces the degradation of PD-L1 mRNA. It is used for the study of chronic hepatitis B (CHB).

Cadapersen sodium is an antisense oligonucleotide that induces the degradation of PD-L1 mRNA. It is used for the study of chronic hepatitis B (CHB).

LTB is a prodrug formed by coupling glycolysis inhibitor (Lonidamine) with PD1/PDL1 blocker (BMS-1) by thioketal linkage. LTB can further encapsulate photosensitizer chlorine e6 (Ce6)) to construct a co-delivery photodynamic nanoplatform (LTB-6 NPs) by self-assembly.

Lon-TK is a glycolysis inhibitor + linker conjugate of LTB. LTB is an intelligent responsive prodrug that connects Lonidamine (Lon) and a PD-L1 inhibitor (BMS-1) through a thioketal linker. It significantly inhibits the glycolytic metabolism of tumor cells and blocks the PD-1/PD-L1 immune escape pathway. Lon-TK shows potential for application in photodynamic-enhanced immunotherapy research.

D5B is a potent and selective PD-L1 inhibitor. D5B has been modified by DBCO. The EC50 of D5B degrading PD-L1 in 4T1 and B16-F10 tumor cells are 5.4 μM and 6.2 μM, respectively. D5B can block PD-L1/PD-1 interaction and has anti-tumor activity.

AB-3PRGD2 is a radiotherapeutic agent targeting integrin αvβ3. AB-3PRGD2 shows improved tumor uptake and prolonged tumor retention, leading to significantly enhanced tumor growth suppression. AB-3PRGD2 can remodel the tumor immune microenvironment by upregulating PD-L1 expression and increasing tumor-infiltrating CD8+ T cells.

CA-170, also known as AUPM170 and PD-1-IN-17, is a programmed cell death-1 (PD-1) inhibitor. PD-1-IN-17 was first reported in patent WO2015033301A1, (Compound 4), inhibits 92% splenocyte proliferation at 100 nM.

PD-1/PD-L1-IN-NP19 is a PD-1/PD-L1 inhibitor, with an IC50 of 12.5 nM for human PD-1/PD-L1 interaction. PD-1/PD-L1-IN-NP19 could activate the immune microenvironment in tumor, which may contribute to its antitumor effects.

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.

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.

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.

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.

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.

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.

PD-1/PD-L1-IN-23 is a potent and orally active inhibitor of PD-1/PD-L1. PD-1/PD-L1-IN-23 is an ester prodrug of L7. L7 is a benzo[c][1,2,5]oxadiazole derivative and biologically evaluated as inhibitors of PD-L1. PD-1/PD-L1-IN-23 displays significant antitumor effects in tumor models of syngeneic and PD-L1 humanized mice.

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

PD-1/PD-L1 inhibitor 2 is reported to prevent the interaction of PD-L1 with PD-1 with an IC50 value of 18 nM,a useful compound immunomodulator compound.

PD-1/PD-L1 inhibitor 1 is a PD-1/PD-L1 interaction inhibitor,IC50 values: 0.006-0.10 μM,a useful immunomodulator compound.

BMS-1166 is a potent PD-1/PD-L1 interaction inhibitor with an IC50 of 1.4 nM.

BMS-8 inhibits the PD-1/PD-L1 interaction with IC50 of 7.2 μM. BMS-8, binds directly to PD-L1 and induces formation of PD-L1 homodimers, which in turn prevents the interaction with PD-1[1].

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.

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.

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.

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.

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.

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.