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Assay Detail

CHEMBL4729976

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

Binding
Inhibition of CD73 in human CD8+ T-cells assessed as reduction in AMP-induced ADO expression preincubated for 15 mins followed by AMP addition and measured after 1 hr by LC-MS/MS analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CD8-positive T cell
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5'-nucleotidase (CHEMBL5957)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Orally Bioavailable Small-Molecule CD73 Inhibitor (OP-5244) Reverses Immunosuppression through Blockade of Adenosine Production.
Du X,Moore J,Blank BR,Eksterowicz J,Sutimantanapi D,Yuen N,Metzger T,Chan B,Huang T,Chen X,Chen Y,Duong F,Kong W,Chang JH,Sun J,Zavorotinskaya T,Ye Q,Junttila MR,Ndubaku C,Friedman LS,Fantin VR,Sun D
J Med Chem (2020) 63 : 10433 -10459
PubMed 32865411 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 9.66 9.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4764985 1 9.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4764985 EC50 = 0.22 nM 9.66