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Assay Detail

CHEMBL3090249

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

Binding
Inhibition of human recombinant ecto-5'-nucleotidase expressed in african green monkey COS7 cells using adenosine monophosphate as substrate preincubated for 10 mins before substrate addition measured after 10 mins by capillary electrophoresis
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type COS-7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Identification of sulfonic acids as efficient ecto-5'-nucleotidase inhibitors.
Iqbal J, Saeed A, Raza R, Matin A, Hameed A, Furtmann N, Lecka J, Sévigny J, Bajorath J.
Eur J Med Chem (2013) 70 : 685 -691
PubMed 24215819 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 4.81 5.88

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3087995 1 5.88
CHEMBL3088000 1 5.21
CHEMBL1566888 1 5.09
CHEMBL1339340 1 4.87
CHEMBL60494 1 4.66
CHEMBL3087996 1 4.52
CHEMBL3087999 1 4.39
CHEMBL68253 SULFAMATE 1 4.38
CHEMBL3087998 1 4.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3087995 IC50 = 1320.0 nM 5.88
CHEMBL3088000 IC50 = 6100.0 nM 5.21
CHEMBL1566888 IC50 = 8200.0 nM 5.09
CHEMBL1339340 IC50 = 13500.0 nM 4.87
CHEMBL60494 IC50 = 21800.0 nM 4.66
CHEMBL3087996 IC50 = 30500.0 nM 4.52
CHEMBL3087999 IC50 = 41000.0 nM 4.39
CHEMBL68253 SULFAMATE IC50 = 42100.0 nM 4.38
CHEMBL3087998 IC50 = 47600.0 nM 4.32