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Assay Detail

CHEMBL5317690

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of europium-labeled PD-1/biotinylated PD-L1 interaction (unknown origin) preincubated for 15 mins with PD-L1 followed by PD-1 addition and measured after 90 mins by TR-FRET assay
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Publication

Novel Small-Molecule PD-L1 Inhibitor Induces PD-L1 Internalization and Optimizes the Immune Microenvironment.
Sun C, Yin M, Cheng Y, Kuang Z, Liu X, Wang G, Wang X, Yuan K, Min W, Dong J, Hou Y, Hu L, Zhang G, Pei W, Wang L, Sun Y, Yu X, Xiao Y, Deng H, Yang P.
J Med Chem (2023) 66 : 2064 -2083
PubMed 36579489 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 41 6.21 8.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5398323 1 8.21
CHEMBL5419371 1 7.81
CHEMBL4089730 1 7.77
CHEMBL5398538 1 7.77
CHEMBL5419794 1 7.45
CHEMBL5426890 1 7.33
CHEMBL5393988 1 6.86
CHEMBL5408902 1 6.81
CHEMBL5440260 1 6.60
CHEMBL5429381 1 6.53
CHEMBL5421369 1 6.47
CHEMBL5426582 1 6.40
CHEMBL5414868 1 6.23
CHEMBL5410266 1 6.17
CHEMBL5423459 1 6.13
CHEMBL5437071 1 6.04
CHEMBL5407423 1 6.04
CHEMBL5404396 1 6.01
CHEMBL5437621 1 5.97
CHEMBL5401111 1 5.93
CHEMBL5410428 1 5.85
CHEMBL5431490 1 5.72
CHEMBL5423192 1 5.71
CHEMBL5420473 1 5.67
CHEMBL5440211 1 5.66
CHEMBL5425609 1 5.62
CHEMBL5424023 1 5.62
CHEMBL5404934 1 5.60
CHEMBL5423020 1 5.56
CHEMBL5429408 1 5.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5398323 IC50 = 6.1 nM 8.21
CHEMBL5419371 IC50 = 15.6 nM 7.81
CHEMBL5398538 IC50 = 16.9 nM 7.77
CHEMBL4089730 IC50 = 17.0 nM 7.77
CHEMBL5419794 IC50 = 35.9 nM 7.45
CHEMBL5426890 IC50 = 46.2 nM 7.33
CHEMBL5393988 IC50 = 138.8 nM 6.86
CHEMBL5408902 IC50 = 156.2 nM 6.81
CHEMBL5440260 IC50 = 249.4 nM 6.60
CHEMBL5429381 IC50 = 296.1 nM 6.53
CHEMBL5421369 IC50 = 342.3 nM 6.47
CHEMBL5426582 IC50 = 395.0 nM 6.40
CHEMBL5414868 IC50 = 590.0 nM 6.23
CHEMBL5410266 IC50 = 683.2 nM 6.17
CHEMBL5423459 IC50 = 744.9 nM 6.13
CHEMBL5437071 IC50 = 917.2 nM 6.04
CHEMBL5407423 IC50 = 912.1 nM 6.04
CHEMBL5404396 IC50 = 968.3 nM 6.01
CHEMBL5437621 IC50 = 1059.0 nM 5.97
CHEMBL5401111 IC50 = 1175.0 nM 5.93
CHEMBL5410428 IC50 = 1423.0 nM 5.85
CHEMBL5431490 IC50 = 1885.0 nM 5.72
CHEMBL5423192 IC50 = 1952.0 nM 5.71
CHEMBL5420473 IC50 = 2113.0 nM 5.67
CHEMBL5440211 IC50 = 2208.0 nM 5.66
CHEMBL5425609 IC50 = 2380.0 nM 5.62
CHEMBL5424023 IC50 = 2400.0 nM 5.62
CHEMBL5404934 IC50 = 2519.0 nM 5.60
CHEMBL5423020 IC50 = 2765.0 nM 5.56
CHEMBL5429408 IC50 = 3668.0 nM 5.44
CHEMBL5407051 IC50 = 3838.0 nM 5.42
CHEMBL5416067 IC50 = 4629.0 nM 5.33
CHEMBL5435306 IC50 = 5128.0 nM 5.29
CHEMBL5438458 IC50 = 5405.0 nM 5.27
CHEMBL5414269 IC50 = 6688.0 nM 5.17
CHEMBL5436142 IC50 > 10000.0 nM -
CHEMBL5438870 IC50 > 10000.0 nM -
CHEMBL5395885 IC50 > 10000.0 nM -
CHEMBL5432996 IC50 > 10000.0 nM -
CHEMBL5429195 IC50 > 10000.0 nM -
CHEMBL5423496 IC50 > 10000.0 nM -