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Assay Detail

CHEMBL4670082

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

Binding
Inhibition of PD1-Tag2/PD-L1-Tag1 (unknown origin) protein-protein interaction preincubated for 15 mins followed by addition of anti-Tag1-Eu3+ and anti-Tag2-XL665 measured after 3 hrs by HTRF assay
9
Total Activities
9
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

Design and Discovery of Natural Cyclopeptide Skeleton Based Programmed Death Ligand 1 Inhibitor as Immune Modulator for Cancer Therapy.
Sun H,Chen D,Zhan S,Wu W,Xu H,Luo C,Su H,Feng Y,Shao W,Wan A,Zhou B,Wan G,Bu X
J Med Chem (2020) 63 : 11286 -11301
PubMed 32844651 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.36 6.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4099869 1 6.84
CHEMBL4793446 1 5.85
CHEMBL4763429 1 5.30
CHEMBL4781005 1 5.27
CHEMBL4740780 1 5.20
CHEMBL4793239 1 5.13
CHEMBL4782871 1 5.09
CHEMBL4789566 1 5.02
CHEMBL4776498 1 4.56

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4099869 IC50 = 146.0 nM 6.84
CHEMBL4793446 IC50 = 1420.0 nM 5.85
CHEMBL4763429 IC50 = 5020.0 nM 5.30
CHEMBL4781005 IC50 = 5370.0 nM 5.27
CHEMBL4740780 IC50 = 6350.0 nM 5.20
CHEMBL4793239 IC50 = 7420.0 nM 5.13
CHEMBL4782871 IC50 = 8100.0 nM 5.09
CHEMBL4789566 IC50 = 9630.0 nM 5.02
CHEMBL4776498 IC50 = 27500.0 nM 4.56