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Assay Detail

CHEMBL644952

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

Binding
Binding affinity against human adenosine A3 receptor expressed on HEK293 cells using [125I]I-AB-MECA
6
Total Activities
6
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

New, non-adenosine, high-potency agonists for the human adenosine A2B receptor with an improved selectivity profile compared to the reference agonist N-ethylcarboxamidoadenosine.
Beukers MW, Chang LC, von Frijtag Drabbe Künzel JK, Mulder-Krieger T, Spanjersberg RF, Brussee J, IJzerman AP.
J Med Chem (2004) 47 : 3707 -3709
PubMed 15239649 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.12 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL464859 NECA 1 7.96
CHEMBL122396 1 7.62
CHEMBL125979 1 7.13
CHEMBL122806 1 6.98
CHEMBL124345 1 6.77
CHEMBL122622 1 6.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL464859 NECA Ki = 11.0 nM 7.96
CHEMBL122396 Ki = 24.0 nM 7.62
CHEMBL125979 Ki = 74.0 nM 7.13
CHEMBL122806 Ki = 104.0 nM 6.98
CHEMBL124345 Ki = 171.0 nM 6.77
CHEMBL122622 Ki = 538.0 nM 6.27