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Assay Detail

CHEMBL881277

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

Binding
Binding affinity against adenosine A2A receptor of rat brain striatal membranes using [3H]CGS-21680
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Water-soluble phosphate prodrugs of 1-propargyl-8-styrylxanthine derivatives, A(2A)-selective adenosine receptor antagonists.
Sauer R, Maurinsh J, Reith U, Fülle F, Klotz KN, Müller CE.
J Med Chem (2000) 43 : 440 -448
PubMed 10669571 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.76 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL413079 1 8.10
CHEMBL136047 1 8.09
CHEMBL344857 1 7.92
CHEMBL138080 1 7.89
CHEMBL138396 1 7.68
CHEMBL138527 1 7.60
CHEMBL343175 1 7.41
CHEMBL139090 1 7.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL413079 Ki = 8.0 nM 8.10
CHEMBL136047 Ki = 8.2 nM 8.09
CHEMBL344857 Ki = 12.0 nM 7.92
CHEMBL138080 Ki = 13.0 nM 7.89
CHEMBL138396 Ki = 21.0 nM 7.68
CHEMBL138527 Ki = 25.0 nM 7.60
CHEMBL343175 Ki = 39.0 nM 7.41
CHEMBL139090 Ki = 42.0 nM 7.38