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Assay Detail

CHEMBL638320

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

Binding
Displacement of [3H]-CGS- 21680 from Adenosine A2 receptor of rat striatal membranes
13
Total Activities
12
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

New base-altered adenosine analogues: Synthesis and affinity at adenosine A1 and A2A receptors
Ha SB, Melman N, Jacobson KA, Nair V
Bioorg Med Chem Lett (1997) 7 : 3085 -3090
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 5.55 6.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL321536 1 6.41
CHEMBL88439 1 6.33
CHEMBL610971 1 6.31
CHEMBL423315 1 6.03
CHEMBL611882 1 5.87
CHEMBL313306 1 5.72
CHEMBL104580 2 5.55
CHEMBL236757 1 5.13
CHEMBL610970 1 5.06
CHEMBL612197 1 4.98
CHEMBL607753 1 4.71
CHEMBL608330 1 4.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL321536 Ki = 390.0 nM 6.41
CHEMBL88439 Ki = 470.0 nM 6.33
CHEMBL610971 Ki = 492.0 nM 6.31
CHEMBL423315 Ki = 936.0 nM 6.03
CHEMBL611882 Ki = 1360.0 nM 5.87
CHEMBL313306 Ki = 1900.0 nM 5.72
CHEMBL104580 Ki = 2800.0 nM 5.55
CHEMBL104580 Ki = 2800.0 nM 5.55
CHEMBL236757 Ki = 7340.0 nM 5.13
CHEMBL610970 Ki = 8630.0 nM 5.06
CHEMBL612197 Ki = 10400.0 nM 4.98
CHEMBL607753 Ki = 19400.0 nM 4.71
CHEMBL608330 Ki = 30300.0 nM 4.52