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Assay Detail

CHEMBL641337

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

Binding
Binding affinity in membrane of CHO cell stably expressing recombinant human Adenosine A3 receptor in the presence of GTPgammaS using [3H]8-ethyl-4-methyl-2-phenyl-(8R)-4,5,7,8-tetrahydro-1H-imidazo[2,1-i]-purin-5-one as radioligand
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Structural determinants of A(3) adenosine receptor activation: nucleoside ligands at the agonist/antagonist boundary.
Gao ZG, Kim SK, Biadatti T, Chen W, Lee K, Barak D, Kim SG, Johnson CR, Jacobson KA.
J Med Chem (2002) 45 : 4471 -4484
PubMed 12238926 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 8.16 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL88147 1 8.92
CHEMBL307199 1 8.41
CHEMBL342873 1 8.40
CHEMBL344187 1 7.62
CHEMBL284969 1 7.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL88147 Ki = 1.2 nM 8.92
CHEMBL307199 Ki = 3.9 nM 8.41
CHEMBL342873 Ki = 4.0 nM 8.40
CHEMBL344187 Ki = 24.0 nM 7.62
CHEMBL284969 Ki = 34.0 nM 7.47