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Assay Detail

CHEMBL643496

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

Binding
Binding affinity against human adenosine A1 receptor expressed in CHO cells using [3H]DPCPX
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adenosine receptor A1 (CHEMBL226)
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 5 8.48 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL125979 1 8.70
CHEMBL124345 1 8.62
CHEMBL122622 1 8.59
CHEMBL122806 1 8.36
CHEMBL122396 1 8.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL125979 Ki = 2.0 nM 8.70
CHEMBL124345 Ki = 2.4 nM 8.62
CHEMBL122622 Ki = 2.6 nM 8.59
CHEMBL122806 Ki = 4.4 nM 8.36
CHEMBL122396 Ki = 7.0 nM 8.15