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Assay Detail

CHEMBL641435

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Functional
Antagonist activity against rat adenosine A3 receptor using [125I]I-AB-MECA or [125 I]IABA
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) adenosine receptors.
Kim YC, Ji X, Melman N, Linden J, Jacobson KA.
J Med Chem (2000) 43 : 1165 -1172
PubMed 10737749 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 4.83 5.56

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL17123 1 5.56
CHEMBL16997 1 4.82
CHEMBL27041 1 4.12
CHEMBL16724 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL17123 Ki = 2750.0 nM 5.56
CHEMBL16997 Ki = 15000.0 nM 4.82
CHEMBL27041 Ki = 75700.0 nM 4.12
CHEMBL16724 Ki = 173000.0 nM -