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Assay Detail

CHEMBL641001

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

Binding
Inhibition of photolabeling of 34 kDa polypeptide in adenosine A1 receptor
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adenosine receptor A1 (CHEMBL318)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Photoaffinity labeling adenosine A1 receptors with an antagonist 125I-labeled aryl azide derivative of 8-phenylxanthine.
Earl CQ, Patel A, Craig RH, Daluge SM, Linden J.
J Med Chem (1988) 31 : 752 -756
PubMed 3351851 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.85 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL351481 1 7.80
CHEMBL605469 1 6.37
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 4.96
CHEMBL464859 NECA 1 4.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL351481 IC50 = 16.0 nM 7.80
CHEMBL605469 IC50 = 430.0 nM 6.37
CHEMBL68738 N6-CYCLOPENTYLADENOSINE IC50 = 11000.0 nM 4.96
CHEMBL464859 NECA IC50 = 52000.0 nM 4.28