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Assay Detail

CHEMBL4017391

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

Binding
Binding affinity to His-tagged PD-L1 (unknown origin) assessed as reduction in PD-L1/PD1-Ig interaction preincubated with PD-L1 for 15 mins followed by addition of PD1-Ig measured after 15 mins by HTRF assay
7
Total Activities
7
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

Small-Molecule Inhibitors of the Programmed Cell Death-1/Programmed Death-Ligand 1 (PD-1/PD-L1) Interaction via Transiently Induced Protein States and Dimerization of PD-L1.
Guzik K, Zak KM, Grudnik P, Magiera K, Musielak B, Törner R, Skalniak L, Dömling A, Dubin G, Holak TA.
J Med Chem (2017) 60 : 5857 -5867
PubMed 28613862 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.95 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4071326 1 8.85
CHEMBL4084368 1 8.65
CHEMBL4081869 1 8.22
CHEMBL4061613 1 8.22
CHEMBL4089730 1 7.75
CHEMBL4062686 1 7.10
CHEMBL4099869 1 6.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4071326 IC50 = 1.4 nM 8.85
CHEMBL4084368 IC50 = 2.25 nM 8.65
CHEMBL4081869 IC50 = 6.0 nM 8.22
CHEMBL4061613 IC50 = 6.0 nM 8.22
CHEMBL4089730 IC50 = 18.0 nM 7.75
CHEMBL4062686 IC50 = 80.0 nM 7.10
CHEMBL4099869 IC50 = 146.0 nM 6.84