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Assay Detail

CHEMBL641313

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

Binding
Displacement of [3H]-CGS- 21980 from Adenosine A2A receptor of rat striatal membranes
6
Total Activities
6
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

N6,5'-Disubstituted adenosine derivatives as partial agonists for the human adenosine A3 receptor.
van Tilburg EW, von Frijtag Drabbe Künzel J, de Groote M, Vollinga RC, Lorenzen A, IJzerman AP.
J Med Chem (1999) 42 : 1393 -1400
PubMed 10212125 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 5.10 6.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 6.24
CHEMBL477444 1 5.06
CHEMBL2113425 1 4.99
CHEMBL2113468 1 4.87
CHEMBL2113467 1 4.73
CHEMBL263643 1 4.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL68738 N6-CYCLOPENTYLADENOSINE Ki = 580.0 nM 6.24
CHEMBL477444 Ki = 8750.0 nM 5.06
CHEMBL2113425 Ki = 10250.0 nM 4.99
CHEMBL2113468 Ki = 13540.0 nM 4.87
CHEMBL2113467 Ki = 18780.0 nM 4.73
CHEMBL263643 Ki = 19010.0 nM 4.72