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Assay Detail

CHEMBL5316662

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

Binding
Inhibition of cell surface anchored CD73 (unknown origin) expressed in human SK-MEL-28 cells incubated for 30 mins by malachite green assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type SK-MEL-28
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of a Series of Potent, Selective, and Orally Bioavailable Nucleoside Inhibitors of CD73 That Demonstrates <i>In Vivo</i> Antitumor Activity.
Li J, Chen L, Billedeau RJ, Stanton TF, Chiang JTP, Lee CC, Li W, Steggerda S, Emberley E, Gross M, Bhupathi D, Che X, Chen J, Dang R, Huang T, Ma Y, MacKinnon A, Makkouk A, Marguier G, Neou S, Sotirovska N, Spurlock S, Zhang J, Zhang W, van Zandt M, Yuan L, Savoy J, Parlati F, Sjogren EB.
J Med Chem (2023) 66 : 345 -370
PubMed 36529947 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.84 9.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5423436 1 9.68
CHEMBL5393743 1 8.55
CHEMBL5404019 1 6.77
CHEMBL5402847 1 6.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5423436 IC50 = 0.21 nM 9.68
CHEMBL5393743 IC50 = 2.8 nM 8.55
CHEMBL5404019 IC50 = 169.0 nM 6.77
CHEMBL5402847 IC50 = 434.0 nM 6.36