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Assay Detail

CHEMBL4392267

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Binding
Inhibition of recombinant human C-terminal His-tagged soluble form of CD73 expressed in baculovirus infected Sf9 insect cells using [2,8-3H]AMP as substrate measured after 25 mins by scintillation counting method
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Structure-Activity Relationship of Purine and Pyrimidine Nucleotides as Ecto-5'-Nucleotidase (CD73) Inhibitors.
Junker A, Renn C, Dobelmann C, Namasivayam V, Jain S, Losenkova K, Irjala H, Duca S, Balasubramanian R, Chakraborty S, Börgel F, Zimmermann H, Yegutkin GG, Müller CE, Jacobson KA.
J Med Chem (2019) 62 : 3677 -3695
PubMed 30895781 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 8.07 8.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4483379 1 8.34
CHEMBL3606064 1 8.27
CHEMBL4443094 1 8.16
CHEMBL4443977 1 7.97
CHEMBL4551648 1 7.85
CHEMBL4470616 1 7.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4483379 Ki = 4.58 nM 8.34
CHEMBL3606064 Ki = 5.33 nM 8.27
CHEMBL4443094 Ki = 6.88 nM 8.16
CHEMBL4443977 Ki = 10.6 nM 7.97
CHEMBL4551648 Ki = 14.0 nM 7.85
CHEMBL4470616 Ki = 15.9 nM 7.80