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Assay Detail

CHEMBL5526129

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

Binding
Positive allosteric modulation of human A3 adenosine receptor transfected in HEK293 cell membranes assessed as potentiation of 5-(2-chloro-6-((3-iodobenzyl)amino)-9H-purin-9-yl)-3,4-dihydroxy-N-methyltetrahydrofuran-2-carboxamide induced [35S]GTP-gammaS binding by measuring agonist EC50 at 1 uM pretreated for 1 hr followed by agonist addition and measured after 2 hrs by liquid scintillation counting method (Rvb = 39.3 nM)
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Lipid Trolling to Optimize A<sub>3</sub> Adenosine Receptor-Positive Allosteric Modulators (PAMs).
Pradhan B, Pavan M, Fisher CL, Salmaso V, Wan TC, Keyes RF, Rollison N, Suresh RR, Kumar TS, Gao ZG, Smith BC, Auchampach JA, Jacobson KA.
J Med Chem (2024) 67 : 12221 -12247
PubMed 38959401 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 8.11 8.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5565378 1 8.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5565378 EC50 = 7.69 nM 8.11