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Assay Detail

CHEMBL642017

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

Binding
Displacement of specific [125I]AB-MECA binding at rat Adenosine A3 receptor stably expressed in CHO cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

Adenosine receptor A3 (CHEMBL3360)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis, CoMFA analysis, and receptor docking of 3,5-diacyl-2, 4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists.
Li AH, Moro S, Forsyth N, Melman N, Ji XD, Jacobson KA.
J Med Chem (1999) 42 : 706 -721
PubMed 10052977 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 6.23 6.95

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL111545 1 6.95
CHEMBL162630 1 6.81
CHEMBL111086 1 6.74
CHEMBL321845 1 6.39
CHEMBL2112931 1 6.30
CHEMBL422184 1 6.29
CHEMBL164321 1 6.22
CHEMBL164210 1 6.05
CHEMBL89852 1 5.85
CHEMBL348766 1 5.59
CHEMBL440720 1 5.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL111545 Ki = 113.0 nM 6.95
CHEMBL162630 Ki = 156.0 nM 6.81
CHEMBL111086 Ki = 183.0 nM 6.74
CHEMBL321845 Ki = 410.0 nM 6.39
CHEMBL2112931 Ki = 495.0 nM 6.30
CHEMBL422184 Ki = 512.0 nM 6.29
CHEMBL164321 Ki = 600.0 nM 6.22
CHEMBL164210 Ki = 900.0 nM 6.05
CHEMBL89852 Ki = 1420.0 nM 5.85
CHEMBL348766 Ki = 2580.0 nM 5.59
CHEMBL440720 Ki = 4260.0 nM 5.37