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Assay Detail

CHEMBL640783

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

Binding
Affinity for Adenosine A1 receptor determined by [3H]N6-cyclohexyladenosine binding to rat brain membranes
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

High selectivity of novel isoguanosine analogues for the adenosine A1 receptor
Nair V, Fesbender AJ, Miller LP, Bruce JL
Bioorg Med Chem Lett (1991) 1 : 481 -486
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.48 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 9.22
CHEMBL45891 1 8.89
CHEMBL477 ADENOSINE 4.0 1 7.89
CHEMBL608168 1 7.72
CHEMBL607881 1 7.70
CHEMBL608742 1 7.46
CHEMBL608747 1 7.40
CHEMBL608445 1 7.26
CHEMBL607606 1 7.16
CHEMBL1688963 ISOGUANOSINE 1 7.03
CHEMBL608748 1 4.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL68738 N6-CYCLOPENTYLADENOSINE Ki = 0.6 nM 9.22
CHEMBL45891 Ki = 1.3 nM 8.89
CHEMBL477 ADENOSINE Ki = 12.8 nM 7.89
CHEMBL608168 Ki = 19.0 nM 7.72
CHEMBL607881 Ki = 20.0 nM 7.70
CHEMBL608742 Ki = 35.0 nM 7.46
CHEMBL608747 Ki = 40.0 nM 7.40
CHEMBL608445 Ki = 55.0 nM 7.26
CHEMBL607606 Ki = 70.0 nM 7.16
CHEMBL1688963 ISOGUANOSINE Ki = 94.0 nM 7.03
CHEMBL608748 Ki = 30000.0 nM 4.52