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Assay Detail

CHEMBL995865

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

Binding
Displacement of [3H]ZM241385 from human recombinant adenosine A2A receptor expressed in CHO cells by liquid scintillation counting
5
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

N6-1,3-diphenylurea derivatives of 2-phenyl-9-benzyladenines and 8-azaadenines: synthesis and biological evaluation as allosteric modulators of A2A adenosine receptors.
Giorgi I, Biagi G, Bianucci AM, Borghini A, Livi O, Leonardi M, Pietra D, Calderone V, Martelli A.
Eur J Med Chem (2008) 43 : 1639 -1647
PubMed 18045744 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 5.62 5.89
EC50 2 4.91 5.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL492052 2 5.89
CHEMBL496984 1 5.72
CHEMBL496985 1 5.24
CHEMBL487497 1 4.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL492052 Ki = 1300.0 nM 5.89
CHEMBL496984 Ki = 1900.0 nM 5.72
CHEMBL496985 Ki = 5737.0 nM 5.24
CHEMBL492052 EC50 = 9740.0 nM 5.01
CHEMBL487497 EC50 = 16000.0 nM 4.80