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Assay Detail

CHEMBL874953

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

Functional
Inhibition of 100 nM NECA-stimulated cAMP production in CHO cells expressing human adenosine A2B receptor
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adenosine receptor A2b (CHEMBL255)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

New pyrrolo[2,1-f]purine-2,4-dione and imidazo[2,1-f]purine-2,4-dione derivatives as potent and selective human A3 adenosine receptor antagonists.
Baraldi PG, Preti D, Tabrizi MA, Fruttarolo F, Romagnoli R, Zaid NA, Moorman AR, Merighi S, Varani K, Borea PA.
J Med Chem (2005) 48 : 4697 -4701
PubMed 16000006 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.40 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL189904 1 6.40
CHEMBL371404 1 -
CHEMBL193130 1 -
CHEMBL434534 1 -
CHEMBL372026 1 -
CHEMBL188269 1 -
CHEMBL191421 1 -
CHEMBL364036 1 -
CHEMBL191414 1 -
CHEMBL188506 1 -
CHEMBL373090 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL189904 IC50 = 400.0 nM 6.40
CHEMBL371404 IC50 > 1000.0 nM -
CHEMBL193130 IC50 > 1000.0 nM -
CHEMBL434534 IC50 > 1000.0 nM -
CHEMBL372026 IC50 > 1000.0 nM -
CHEMBL188269 IC50 > 1000.0 nM -
CHEMBL191421 IC50 > 1000.0 nM -
CHEMBL364036 IC50 > 1000.0 nM -
CHEMBL191414 IC50 > 1000.0 nM -
CHEMBL188506 IC50 > 1000.0 nM -
CHEMBL373090 IC50 > 1000.0 nM -