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Assay Detail

CHEMBL649872

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

Binding
Affinity for Adenosine A2 receptor determined by [3H]NECA binding to rat striatal membranes
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Striatum
Subcellular Membrane
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Adenosine A2 receptor (CHEMBL2094117)
Type PROTEIN FAMILY
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 5.52 7.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL477 ADENOSINE 4.0 1 7.43
CHEMBL1688963 ISOGUANOSINE 1 6.48
CHEMBL45891 1 6.44
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 6.33
CHEMBL607606 1 5.22
CHEMBL608168 1 5.12
CHEMBL608445 1 4.82
CHEMBL608747 1 4.82
CHEMBL607881 1 4.40
CHEMBL608742 1 4.10
CHEMBL608748 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL477 ADENOSINE Ki = 37.0 nM 7.43
CHEMBL1688963 ISOGUANOSINE Ki = 331.0 nM 6.48
CHEMBL45891 Ki = 363.0 nM 6.44
CHEMBL68738 N6-CYCLOPENTYLADENOSINE Ki = 462.0 nM 6.33
CHEMBL607606 Ki = 6000.0 nM 5.22
CHEMBL608168 Ki = 7500.0 nM 5.12
CHEMBL608445 Ki = 15000.0 nM 4.82
CHEMBL608747 Ki = 15000.0 nM 4.82
CHEMBL607881 Ki = 40000.0 nM 4.40
CHEMBL608742 Ki = 80000.0 nM 4.10
CHEMBL608748 Ki = 140000.0 nM -