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Assay Detail

CHEMBL4737367

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

Binding
Displacement of [3H]-ZM241385 from A2A receptor in rat brain corpora striata incubated for 70 mins by liquid scintillation counting method
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Design, synthesis and biological evaluation of Tozadenant analogues as adenosine A receptor ligands.
Renk DR,Skraban M,Bier D,Schulze A,Wabbals E,Wedekind F,Neumaier F,Neumaier B,Holschbach M
Eur J Med Chem (2021) 214 : 113214 -113214
PubMed 33548636 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 7.54 7.83

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4746388 1 7.83
CHEMBL2105747 TOZADENANT 3.0 1 7.73
CHEMBL4783723 1 7.72
CHEMBL4753657 1 7.69
CHEMBL4746896 1 6.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4746388 Ki = 14.9 nM 7.83
CHEMBL2105747 TOZADENANT Ki = 18.7 nM 7.73
CHEMBL4783723 Ki = 19.2 nM 7.72
CHEMBL4753657 Ki = 20.4 nM 7.69
CHEMBL4746896 Ki = 195.0 nM 6.71