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Assay Detail

CHEMBL5042388

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

Binding
Displacement of [125I]I-AB-MECA from human adenosine A3 receptor expressed in HEK293 cells by radioligand binding assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Selective A<sub>3</sub> Adenosine Receptor Antagonist Radioligand for Human and Rodent Species.
Suresh RR, Gao ZG, Salmaso V, Chen E, Campbell RG, Poe RB, Liston TE, Jacobson KA.
ACS Med Chem Lett (2022) 13 : 623 -631
PubMed 35450351 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 8.41 9.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL119709 IB-MECA 1 9.43
CHEMBL88147 1 8.53
CHEMBL5073355 1 7.97
CHEMBL464859 NECA 1 7.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL119709 IB-MECA Ki = 0.37 nM 9.43
CHEMBL88147 Ki = 2.97 nM 8.53
CHEMBL5073355 Ki = 10.6 nM 7.97
CHEMBL464859 NECA Ki = 19.6 nM 7.71