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Assay Detail

CHEMBL4621698

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

Binding
Inhibition of human C-terminal Ig-Fc-tagged PD1 (Leu25 to Gln167 residues) expressed in HEK293 cells/human C-terminal epitope-His-tagged PDL1 (Phe19 to Arg238 residues) expressed in HEK293 cells protein-protein interaction preincubated for 15 mins with PDL1 followed by PD1 addition and measured after 15 mins by APC-labeled anti-His antibody/Eu-labeled anti-human IgG based HTRF assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 7 — Homologous single protein target
Curated By Autocuration

Publication

Discovery of Novel Resorcinol Dibenzyl Ethers Targeting the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Interaction as Potential Anticancer Agents.
Cheng B, Ren Y, Niu X, Wang W, Wang S, Tu Y, Liu S, Wang J, Yang D, Liao G, Chen J.
J Med Chem (2020) 63 : 8338 -8358
PubMed 32667799 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.55 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4646293 1 8.10
CHEMBL4648161 1 8.00
CHEMBL4639202 1 7.90
CHEMBL4638536 1 6.93
CHEMBL4099869 1 6.84
CHEMBL4643215 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4646293 IC50 = 7.9 nM 8.10
CHEMBL4648161 IC50 = 10.0 nM 8.00
CHEMBL4639202 IC50 = 12.5 nM 7.90
CHEMBL4638536 IC50 = 118.5 nM 6.93
CHEMBL4099869 IC50 = 146.0 nM 6.84
CHEMBL4643215 IC50 > 100.0 nM -