Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4018931

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

Binding
Displacement of [125I]I-AB-MECA from human A3 adenosine receptor expressed in CHO cell membranes after 60 mins by gamma counting method
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Polypharmacology of N6-(3-Iodobenzyl)adenosine-5'-N-methyluronamide (IB-MECA) and Related A3 Adenosine Receptor Ligands: Peroxisome Proliferator Activated Receptor (PPAR) γ Partial Agonist and PPARδ Antagonist Activity Suggests Their Antidiabetic Potential.
Yu J, Ahn S, Kim HJ, Lee M, Ahn S, Kim J, Jin SH, Lee E, Kim G, Cheong JH, Jacobson KA, Jeong LS, Noh M.
J Med Chem (2017) 60 : 7459 -7475
PubMed 28799755 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 8.80 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL522152 1 9.52
CHEMBL200732 1 9.42
CHEMBL596042 1 9.38
CHEMBL594625 1 8.93
CHEMBL431733 NAMODENOSON 3.0 1 8.85
CHEMBL500569 1 8.82
CHEMBL387921 1 8.78
CHEMBL119709 IB-MECA 1 8.74
CHEMBL603424 1 8.67
CHEMBL596014 1 8.52
CHEMBL413686 1 8.38
CHEMBL227279 1 7.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL522152 Ki = 0.3 nM 9.52
CHEMBL200732 Ki = 0.38 nM 9.42
CHEMBL596042 Ki = 0.42 nM 9.38
CHEMBL594625 Ki = 1.17 nM 8.93
CHEMBL431733 NAMODENOSON Ki = 1.4 nM 8.85
CHEMBL500569 Ki = 1.5 nM 8.82
CHEMBL387921 Ki = 1.66 nM 8.78
CHEMBL119709 IB-MECA Ki = 1.8 nM 8.74
CHEMBL603424 Ki = 2.16 nM 8.67
CHEMBL596014 Ki = 3.03 nM 8.52
CHEMBL413686 Ki = 4.16 nM 8.38
CHEMBL227279 Ki = 25.8 nM 7.59