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Assay Detail

CHEMBL646439

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

Binding
Displacement of [125 I]AB-MECA from Adenosine A3 receptor expressed in HEK cells
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Chiral resolution and stereospecificity of 6-phenyl-4-phenylethynyl- 1,4-dihydropyridines as selective A(3) adenosine receptor antagonists.
Jiang J, Li AH, Jang SY, Chang L, Melman N, Moro S, Ji X, Lobkovsky EB, Clardy JC, Jacobson KA.
J Med Chem (1999) 42 : 3055 -3065
PubMed 10447949 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 6.44 7.67

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL321579 1 7.67
CHEMBL89852 1 7.65
CHEMBL315458 1 7.12
CHEMBL315984 1 6.96
CHEMBL431232 1 6.37
CHEMBL103433 1 6.12
CHEMBL104198 1 5.88
CHEMBL105672 1 5.56
CHEMBL283013 1 4.63

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL321579 Ki = 21.3 nM 7.67
CHEMBL89852 Ki = 22.2 nM 7.65
CHEMBL315458 Ki = 75.0 nM 7.12
CHEMBL315984 Ki = 110.0 nM 6.96
CHEMBL431232 Ki = 426.0 nM 6.37
CHEMBL103433 Ki = 750.0 nM 6.12
CHEMBL104198 Ki = 1310.0 nM 5.88
CHEMBL105672 Ki = 2770.0 nM 5.56
CHEMBL283013 Ki = 23500.0 nM 4.63