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Assay Detail

CHEMBL4011336

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

Binding
Displacement of [125I]N6-(4-amino-3-iodobenzyl)adenosine-5'-N-methyluronamide from mouse A3AR expressed in HEK293T cells pre-incubated for 10 mins before radioligand addition and measured 90 mins after radioligand addition by micro beta scintillation counting analysis relative to control
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Adenosine receptor A3 (CHEMBL1075269)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters.
Tosh DK, Janowsky A, Eshleman AJ, Warnick E, Gao ZG, Chen Z, Gizewski E, Auchampach JA, Salvemini D, Jacobson KA.
J Med Chem (2017) 60 : 3109 -3123
PubMed 28319392 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.18 7.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4092411 1 7.47
CHEMBL4086593 1 6.22
CHEMBL4090355 1 5.93
CHEMBL4097426 1 5.75
CHEMBL4105127 1 5.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4092411 Ki = 34.0 nM 7.47
CHEMBL4086593 Ki = 597.0 nM 6.22
CHEMBL4090355 Ki = 1170.0 nM 5.93
CHEMBL4097426 Ki = 1800.0 nM 5.75
CHEMBL4105127 Ki = 2810.0 nM 5.55