| S8549 |
AUNP-12
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AUNP-12 (Aur-012, Aurigene-012, Aurigene NP-12), a new immune checkpoint modulator, is an inhibitor of the PD-1 pathway.
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Acta Pharm Sin B, 2024, 14(1):350-364
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Carcinogenesis, 2022, bgac043
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Molecules, 2019, 24(15)
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| S8275 |
Tomivosertib (eFT508)
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Tomivosertib (eFT-508) is a potent and selective MNK1/2 inhibitor with IC50s of 2.4 nM and 1 nM, respectively. It potentially results in decreased tumour cell proliferation and tumour growth. Tomivosertib (eFT-508) inhibits eIF4E phosphorylation and dramatically downregulates PD-L1 protein abundance.
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Nat Commun, 2025, 16(1):7853
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Nat Commun, 2024, 15(1):9755
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J Clin Invest, 2024, 134(16)e168393
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| S7912 |
BMS-202
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BMS202 is a small-molecule PD-1/PD-L1 interaction inhibitor with IC50 of 18 nM.
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Front Immunol, 2025, 16:1529710
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Front Oncol, 2025, 15:1590095
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Front Oncol, 2025, 15:1572040
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| S7911 |
BMS-1
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BMS-1 is a small-molecule inhibitor of PD-1/PD-L1 interaction with IC50 of 6 nM.
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Theranostics, 2025, 15(9):3924-3942
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J Med Chem, 2024, 67(5):4036-4062
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PLoS Comput Biol, 2024, 20(11):e1012284
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| S8158 |
PD-1/PD-L1 Inhibitor 3
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PD-1/PD-L1 Inhibitor 3 (Programmed Death-1/Programmed Death-Ligand 1 Inhibitor 3) is a Macrocyclic inhibitor of PD-1/PD-L1 interaction with IC50 of 5.6 nM
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ACS Appl Mater Interfaces, 2024, 16(18):22839-49
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J Med Chem, 2024, 67(5):4036-4062
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Front Oncol, 2024, 14:1536406
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| S8859 |
BMS-1166
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BMS-1166 is a novel and potent small molecule inhibitor of the PD-1/PD-L1 interaction with an IC50 of 1.4 nM.
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Mater Today Bio, 2025, 32:101801
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Int J Mol Sci, 2025, 26(14)6876
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iScience, 2024, 27(7):110243
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| S0094 |
SR 0987
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SR 0987, a SR 1078 analog, is an agonist for T cell-specific RORγ (RORγt) with EC50 of 800 nM. This compound represses PD-1, produces IL17 and is potential for the treatment of cancer.
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Evid Based Complement Alternat Med, 2022, 2022:8315503.
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| S9863 |
INCB086550
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INCB086550 (PD-1/PD-L1-IN-8) is a potent PD-1/PD-L1 inhibitor, with an IC50 <= 10 nM. This compound binds to PD-L1 and interrupts its interaction with PD-1 and also induces PD-L1 dimerization and internalisation.
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In Vivo, 2025, 39(1):80-95
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| E1322 |
GS-4224
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GS-4224 (Evixapodlin, PD-1/PD-L1-IN 7) is an inhibitor of human PD-1/PD-L1 protein/protein interaction with an IC50 of 0.213 nM. It enhances IFN-γ and Granzyme B Production in chronic hepatitis B (CHB) CD8+ T Cells and CD4+ T Cells. It exhibits anticancer and antiviral functions.
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| S8473 |
CA-170 (AUPM-170)
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CA-170 (AUPM-170, PD-1-IN-1) is a potent and orally available inhibitor of the immune checkpoint regulatory proteins PD-L1 (programmed cell death ligand-1) and VISTA (V-domain immunoglobulin (Ig) suppressor of T-cell activation). This compound exhibits anti-tumour efficacy.
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