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

CHEMBL4018932

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

Binding
Displacement of [3H]CCPA from human A1 receptor expressed in CHO cell membranes after 60 mins by gamma counting method
10
Total Activities
10
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 A1 (CHEMBL226)
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 10 7.08 8.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL596042 1 8.27
CHEMBL596014 1 8.03
CHEMBL522152 1 7.70
CHEMBL594625 1 7.63
CHEMBL119709 IB-MECA 1 7.29
CHEMBL603424 1 6.80
CHEMBL200732 1 6.71
CHEMBL431733 NAMODENOSON 3.0 1 6.65
CHEMBL500569 1 6.07
CHEMBL413686 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL596042 Ki = 5.4 nM 8.27
CHEMBL596014 Ki = 9.27 nM 8.03
CHEMBL522152 Ki = 20.2 nM 7.70
CHEMBL594625 Ki = 23.6 nM 7.63
CHEMBL119709 IB-MECA Ki = 51.2 nM 7.29
CHEMBL603424 Ki = 159.0 nM 6.80
CHEMBL200732 Ki = 193.0 nM 6.71
CHEMBL431733 NAMODENOSON Ki = 222.0 nM 6.65
CHEMBL500569 Ki = 860.0 nM 6.07
CHEMBL413686 Ki = 2490.0 nM 5.60