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Assay Detail

CHEMBL5041876

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Binding
Inhibition of human soluble CD73 assessed as inhibition constant
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Structure-Activity Relationship of 3-Methylcytidine-5'-α,β-methylenediphosphates as CD73 Inhibitors.
Scortichini M, Idris RM, Moschütz S, Keim A, Salmaso V, Dobelmann C, Oliva P, Losenkova K, Irjala H, Vaittinen S, Sandholm J, Yegutkin GG, Sträter N, Junker A, Müller CE, Jacobson KA.
J Med Chem (2022) 65 : 2409 -2433
PubMed 35080883 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 8.56 9.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5081267 1 9.36
CHEMBL5083600 1 9.36
CHEMBL5074970 1 9.29
CHEMBL5078828 1 9.20
CHEMBL5080841 1 9.17
CHEMBL5086866 1 9.07
CHEMBL5076916 1 9.05
CHEMBL5084248 1 8.97
CHEMBL5081442 1 8.94
CHEMBL5081604 1 8.90
CHEMBL5079813 1 8.80
CHEMBL5094601 1 8.79
CHEMBL5076275 1 8.75
CHEMBL5089752 1 8.75
CHEMBL5076684 1 8.60
CHEMBL5070874 1 8.58
CHEMBL5093165 1 8.46
CHEMBL5092522 1 7.85
CHEMBL5077925 1 7.23
CHEMBL5083016 1 7.15
CHEMBL3606064 1 5.59
CHEMBL5075093 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5081267 Ki = 0.436 nM 9.36
CHEMBL5083600 Ki = 0.441 nM 9.36
CHEMBL5074970 Ki = 0.511 nM 9.29
CHEMBL5078828 Ki = 0.626 nM 9.20
CHEMBL5080841 Ki = 0.673 nM 9.17
CHEMBL5086866 Ki = 0.848 nM 9.07
CHEMBL5076916 Ki = 0.894 nM 9.05
CHEMBL5084248 Ki = 1.08 nM 8.97
CHEMBL5081442 Ki = 1.14 nM 8.94
CHEMBL5081604 Ki = 1.27 nM 8.90
CHEMBL5079813 Ki = 1.58 nM 8.80
CHEMBL5094601 Ki = 1.63 nM 8.79
CHEMBL5076275 Ki = 1.76 nM 8.75
CHEMBL5089752 Ki = 1.78 nM 8.75
CHEMBL5076684 Ki = 2.51 nM 8.60
CHEMBL5070874 Ki = 2.613 nM 8.58
CHEMBL5093165 Ki = 3.5 nM 8.46
CHEMBL5092522 Ki = 14.1 nM 7.85
CHEMBL5077925 Ki = 59.2 nM 7.23
CHEMBL5083016 Ki = 71.5 nM 7.15
CHEMBL3606064 Ki = 2540.0 nM 5.59
CHEMBL5075093 Ki > 50000.0 nM -