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Assay Detail

CHEMBL5366374

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

Binding
Displacement of [125I]AB-MECA from rat A3AR transfected in CHO cell membrane assessed as inhibition constant incubated for 1 hr by gamma counter method
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type CHO
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Adenosine receptor A3 (CHEMBL3360)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Structure-Activity Relationship of Truncated 2,8-Disubstituted-Adenosine Derivatives as Dual A<sub>2A</sub>/A<sub>3</sub> Adenosine Receptor Antagonists and Their Cancer Immunotherapeutic Activity.
Kim G, Hou X, Byun WS, Kim G, Jarhad DB, Lee G, Hyun YE, Yu J, Lee CS, Qu S, Warnick E, Gao ZG, Kim JY, Ji S, Shin H, Choi JR, Jacobson KA, Lee HW, Lee SK, Jeong LS.
J Med Chem (2023) 66 : 12249 -12265
PubMed 37603705 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 9.14 9.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL200732 1 9.42
CHEMBL431733 NAMODENOSON 3.0 1 8.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL200732 Ki = 0.38 nM 9.42
CHEMBL431733 NAMODENOSON Ki = 1.4 nM 8.85