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Assay Detail

CHEMBL4668688

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

Binding
Inhibition of CD73 in human CD8-positive T cells using AMP as substrate preincubated for 60 mins followed by substrate addition and measured after 2.5 hrs by PiColorLock gold reagent based colorimetric assay
3
Total Activities
3
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

Discovery of AB680: A Potent and Selective Inhibitor of CD73.
Lawson KV,Kalisiak J,Lindsey EA,Newcomb ET,Leleti MR,Debien L,Rosen BR,Miles DH,Sharif EU,Jeffrey JL,Tan JBL,Chen A,Zhao S,Xu G,Fu L,Jin L,Park TW,Berry W,Moschütz S,Scaletti E,Sträter N,Walker NP,Young SW,Walters MJ,Schindler U,Powers JP
J Med Chem (2020) 63 : 11448 -11468
PubMed 32614585 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 11.00 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4761506 1 11.00
CHEMBL4471306 QUEMLICLUSTAT 2.0 1 -
CHEMBL4743437 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4761506 IC50 = 0.01 nM 11.00
CHEMBL4471306 QUEMLICLUSTAT IC50 = 0.008 nM -
CHEMBL4743437 IC50 = 0.0027 nM -