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Assay Detail

CHEMBL648803

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

Binding
Binding affinity against Adenosine A2 receptor using [3H]NECA with 50 nM CPA in rat striatal brain membranes
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adenosine A2 receptor (CHEMBL2094117)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

N6-bicycloalkyladenosines with unusually high potency and selectivity for the adenosine A1 receptor.
Trivedi BK, Bridges AJ, Patt WC, Priebe SR, Bruns RF.
J Med Chem (1989) 32 : 8 -11
PubMed 2909748 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 5.87 6.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 6.33
CHEMBL2112184 1 6.21
CHEMBL489640 1 6.12
CHEMBL2112183 1 6.01
CHEMBL2112182 1 5.86
CHEMBL477444 1 5.73
CHEMBL3038256 1 5.68
CHEMBL3038259 1 5.52
CHEMBL3038260 1 5.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL68738 N6-CYCLOPENTYLADENOSINE Ki = 462.0 nM 6.33
CHEMBL2112184 Ki = 610.0 nM 6.21
CHEMBL489640 Ki = 750.0 nM 6.12
CHEMBL2112183 Ki = 970.0 nM 6.01
CHEMBL2112182 Ki = 1390.0 nM 5.86
CHEMBL477444 Ki = 1870.0 nM 5.73
CHEMBL3038256 Ki = 2100.0 nM 5.68
CHEMBL3038259 Ki = 3000.0 nM 5.52
CHEMBL3038260 Ki = 3900.0 nM 5.41