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Assay Detail

CHEMBL640528

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

Binding
[3H]NECA saturation binding in CHO cells expressing human recombinant A2A adenosine receptor
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

Adenosine receptor A2a (CHEMBL251)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Introduction of alkynyl chains on C-8 of adenosine led to very selective antagonists of the A(3) adenosine receptor.
Volpini R, Costanzi S, Lambertucci C, Vittori S, Klotz K, Lorenzen A, Cristalli G.
Bioorg Med Chem Lett (2001) 11 : 1931 -1934
PubMed 11459663 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.08 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL464859 NECA 1 7.70
CHEMBL61259 1 6.22
CHEMBL3350496 1 4.33
CHEMBL2181966 1 -
CHEMBL3350497 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL464859 NECA Ki = 20.0 nM 7.70
CHEMBL61259 Ki = 600.0 nM 6.22
CHEMBL3350496 Ki = 46600.0 nM 4.33
CHEMBL2181966 Ki > 100000.0 nM -
CHEMBL3350497 Ki > 100000.0 nM -