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Assay Detail

CHEMBL5165091

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

Binding
Binding affinity towards His-tagged recombinant human PD-L1 measured by MST dimerization binding assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Programmed cell death 1 ligand 1 (CHEMBL3580522)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pyrazolones as inhibitors of immune checkpoint blocking the PD-1/PD-L1 interaction.
Le Biannic R, Magnez R, Klupsch F, Leleu-Chavain N, Thiroux B, Tardy M, El Bouazzati H, Dezitter X, Renault N, Vergoten G, Bailly C, Quesnel B, Thuru X, Millet R.
Eur J Med Chem (2022) 236 : 114343 -114343
PubMed 35429911 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 6 7.92 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5207924 1 9.15
CHEMBL5171729 1 8.70
CHEMBL5194957 1 7.62
CHEMBL4089730 1 7.43
CHEMBL5176505 1 7.34
CHEMBL374252 1 7.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5207924 Kd = 0.7 nM 9.15
CHEMBL5171729 Kd = 2.0 nM 8.70
CHEMBL5194957 Kd = 24.0 nM 7.62
CHEMBL4089730 Kd = 37.0 nM 7.43
CHEMBL5176505 Kd = 46.0 nM 7.34
CHEMBL374252 Kd = 53.0 nM 7.28