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Assay Detail

CHEMBL641835

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

Binding
Displacement of [3H]DPCPX from Human Adenosine A2B 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 A2b (CHEMBL255)
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 6.65 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL332091 1 6.70
CHEMBL324735 1 6.65
CHEMBL118923 1 6.60
CHEMBL324512 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL332091 Ki = 200.0 nM 6.70
CHEMBL324735 Ki = 222.0 nM 6.65
CHEMBL118923 Ki = 250.0 nM 6.60
CHEMBL324512 Ki > 10000.0 nM -