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Assay Detail

CHEMBL641316

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

Binding
Displacement of specific [3H]-CGS- 21680 binding to adenosine A2A receptor in rat striatal membranes
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adenosine receptor A2a (CHEMBL302)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Methanocarba analogues of purine nucleosides as potent and selective adenosine receptor agonists.
Jacobson KA, Ji X, Li AH, Melman N, Siddiqui MA, Shin KJ, Marquez VE, Ravi RG.
J Med Chem (2000) 43 : 2196 -2203
PubMed 10841798 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 6.37 7.76

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL66393 1 7.76
CHEMBL477 ADENOSINE 4.0 1 7.52
CHEMBL307199 1 7.42
CHEMBL284969 1 6.22
CHEMBL417292 1 6.22
CHEMBL27809 1 6.13
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 6.07
CHEMBL49935 ARISTEROMYCIN 1 5.67
CHEMBL284216 1 5.47
CHEMBL27952 1 5.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL66393 Ki = 17.5 nM 7.76
CHEMBL477 ADENOSINE Ki = 30.0 nM 7.52
CHEMBL307199 Ki = 38.5 nM 7.42
CHEMBL284969 Ki = 605.0 nM 6.22
CHEMBL417292 Ki = 601.0 nM 6.22
CHEMBL27809 Ki = 732.0 nM 6.13
CHEMBL68738 N6-CYCLOPENTYLADENOSINE Ki = 857.0 nM 6.07
CHEMBL49935 ARISTEROMYCIN Ki = 2150.0 nM 5.67
CHEMBL284216 Ki = 3390.0 nM 5.47
CHEMBL27952 Ki = 6800.0 nM 5.17