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Assay Detail

CHEMBL641298

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Binding
Binding affinity for adenosine A2A receptor as displacement of [3H]-CGS- 21680 from rat striatal membranes at 10e-4 M
4
Total Activities
4
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

Structure-activity relationships and molecular modeling of 3, 5-diacyl-2,4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists.
Li AH, Moro S, Melman N, Ji XD, Jacobson KA.
J Med Chem (1998) 41 : 3186 -3201
PubMed 9703464 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 6.76 7.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL119709 IB-MECA 1 7.25
CHEMBL133566 1 6.71
CHEMBL431733 NAMODENOSON 3.0 1 6.33
CHEMBL265096 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL119709 IB-MECA Ki = 56.0 nM 7.25
CHEMBL133566 Ki = 197.0 nM 6.71
CHEMBL431733 NAMODENOSON Ki = 470.0 nM 6.33
CHEMBL265096 Ki > 100000.0 nM -