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Assay Detail

CHEMBL1696017

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 CHO cells at 10 uM
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of New Human A(2A) Adenosine Receptor Agonists: Design, Synthesis, and Binding Mode of Truncated 2-Hexynyl-4'-thioadenosine.
Hou X, Kim HO, Alexander V, Kim K, Choi S, Park SG, Lee JH, Yoo LS, Gao ZG, Jacobson KA, Jeong LS.
ACS Med Chem Lett (2010) 1 : 516 -520
PubMed 21286238 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 7.78 8.78

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL387921 1 8.78
CHEMBL1688378 1 7.93
CHEMBL1688379 1 7.88
CHEMBL1688380 1 7.70
CHEMBL1688381 1 6.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL387921 Ki = 1.66 nM 8.78
CHEMBL1688378 Ki = 11.8 nM 7.93
CHEMBL1688379 Ki = 13.2 nM 7.88
CHEMBL1688380 Ki = 20.0 nM 7.70
CHEMBL1688381 Ki = 259.0 nM 6.59