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Assay Detail

CHEMBL641572

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

Binding
Binding affinity against H278D human adenosine A2A receptor stably transfected in CHO cells using [3H]- ZM-241385 as radioligand.
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Modeling the adenosine receptors: comparison of the binding domains of A2A agonists and antagonists.
Kim SK, Gao ZG, Van Rompaey P, Gross AS, Chen A, Van Calenbergh S, Jacobson KA.
J Med Chem (2003) 46 : 4847 -4859
PubMed 14584936 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 7.66 9.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL16687 CGS-15943 1 9.39
CHEMBL464859 NECA 1 7.72
CHEMBL144521 1 7.23
CHEMBL132629 1 7.06
CHEMBL129903 1 6.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL16687 CGS-15943 Ki = 0.41 nM 9.39
CHEMBL464859 NECA Ki = 19.1 nM 7.72
CHEMBL144521 Ki = 59.0 nM 7.23
CHEMBL132629 Ki = 87.0 nM 7.06
CHEMBL129903 Ki = 121.0 nM 6.92