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Assay Detail

CHEMBL870058

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

Binding
Displacement of [125I]I-AB-MECA from human adenosine A3 receptor Q167E mutant expressed in COS7 cells
7
Total Activities
7
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 Expert

Target

Adenosine receptor A3 (CHEMBL256)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Orthogonal activation of the reengineered A3 adenosine receptor (neoceptor) using tailored nucleoside agonists.
Gao ZG, Duong HT, Sonina T, Kim SK, Van Rompaey P, Van Calenbergh S, Mamedova L, Kim HO, Kim MJ, Kim AY, Liang BT, Jeong LS, Jacobson KA.
J Med Chem (2006) 49 : 2689 -2702
PubMed 16640329 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 5.69 6.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL382812 1 6.24
CHEMBL208475 1 5.14
CHEMBL377071 1 -
CHEMBL382194 1 -
CHEMBL378069 1 -
CHEMBL144521 1 -
CHEMBL207610 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL382812 Ki = 570.0 nM 6.24
CHEMBL208475 Ki = 7200.0 nM 5.14
CHEMBL377071 Ki - -
CHEMBL382194 Ki > 100000.0 nM -
CHEMBL378069 Ki > 10000.0 nM -
CHEMBL144521 Ki > 10000.0 nM -
CHEMBL207610 Ki > 10000.0 nM -