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Assay Detail

CHEMBL644649

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

Binding
Binding affinity against Q89D human adenosine A2A receptor expressed in CHO cells using [3H]- ZM-241385
6
Total Activities
6
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

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 6 8.24 9.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL16687 CGS-15943 1 9.46
CHEMBL464859 NECA 1 8.82
CHEMBL129903 1 8.44
CHEMBL132629 1 8.19
CHEMBL302376 1 7.28
CHEMBL144521 1 7.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL16687 CGS-15943 Ki = 0.35 nM 9.46
CHEMBL464859 NECA Ki = 1.5 nM 8.82
CHEMBL129903 Ki = 3.6 nM 8.44
CHEMBL132629 Ki = 6.4 nM 8.19
CHEMBL302376 Ki = 52.0 nM 7.28
CHEMBL144521 Ki = 58.0 nM 7.24