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Assay Detail

CHEMBL1074290

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

Binding
Displacement of [3H]DPCPX from adenosine A1 receptor in rat brain cortical membrane in presence of 100 uM GTP
3
Total Activities
3
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 A1 (CHEMBL318)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

2-Amino-5-benzoyl-4-phenylthiazoles: Development of potent and selective adenosine A1 receptor antagonists.
Scheiff AB, Yerande SG, El-Tayeb A, Li W, Inamdar GS, Vasu KK, Sudarsanam V, Müller CE.
Bioorg Med Chem (2010) 18 : 2195 -2203
PubMed 20188574 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.33 7.65

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL592679 1 7.65
CHEMBL591710 1 7.54
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 6.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL592679 IC50 = 22.3 nM 7.65
CHEMBL591710 IC50 = 28.8 nM 7.54
CHEMBL68738 N6-CYCLOPENTYLADENOSINE IC50 = 154.0 nM 6.81