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Assay Detail

CHEMBL649056

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

Binding
Displacement of [3H]-MRE 3008-F20 from Human Adenosine A3 receptor expressed in HEK293 cells
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 Expert

Target

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

Publication

Synthesis, biological properties, and molecular modeling investigation of the first potent, selective, and water-soluble human A(3) adenosine receptor antagonist.
Maconi A, Pastorin G, Da Ros T, Spalluto G, Gao ZG, Jacobson KA, Baraldi PG, Cacciari B, Varani K, Moro S, Borea PA.
J Med Chem (2002) 45 : 3579 -3582
PubMed 12166930 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 9.70 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL118923 1 11.00
CHEMBL332091 1 10.40
CHEMBL324735 1 9.80
CHEMBL324512 1 7.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL118923 Ki = 0.01 nM 11.00
CHEMBL332091 Ki = 0.04 nM 10.40
CHEMBL324735 Ki = 0.16 nM 9.80
CHEMBL324512 Ki = 25.0 nM 7.60