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Assay Detail

CHEMBL1042903

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

Binding
Displacement of [3H]CGS21680 from adenosine A2A receptor in rat brain striatal membrane after 60 mins
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Nucleoside-5'-monophosphates as prodrugs of adenosine A2A receptor agonists activated by ecto-5'-nucleotidase.
El-Tayeb A, Iqbal J, Behrenswerth A, Romio M, Schneider M, Zimmermann H, Schrader J, Müller CE.
J Med Chem (2009) 52 : 7669 -7677
PubMed 19580286 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 6.14 7.73

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL577036 1 7.73
CHEMBL568023 1 6.43
CHEMBL577915 1 6.27
CHEMBL577458 1 6.22
CHEMBL568009 1 6.15
CHEMBL576883 1 6.10
CHEMBL576838 1 5.96
CHEMBL578145 1 5.94
CHEMBL577902 1 5.87
CHEMBL578569 1 5.82
CHEMBL567801 1 5.61
CHEMBL578819 1 5.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL577036 Ki = 18.5 nM 7.73
CHEMBL568023 Ki = 372.0 nM 6.43
CHEMBL577915 Ki = 542.0 nM 6.27
CHEMBL577458 Ki = 606.0 nM 6.22
CHEMBL568009 Ki = 709.0 nM 6.15
CHEMBL576883 Ki = 793.0 nM 6.10
CHEMBL576838 Ki = 1100.0 nM 5.96
CHEMBL578145 Ki = 1160.0 nM 5.94
CHEMBL577902 Ki = 1350.0 nM 5.87
CHEMBL578569 Ki = 1520.0 nM 5.82
CHEMBL567801 Ki = 2480.0 nM 5.61
CHEMBL578819 Ki = 2900.0 nM 5.54