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Assay Detail

CHEMBL4682742

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

Binding
Displacement of [3H]DPCPX from rat brain cortical membrane A1AR in presence of 100 uM of GTP by scintillation counting analysis
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Cortex
Subcellular Cell membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Adenosine receptor A1 (CHEMBL318)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Substituted 4-phenylthiazoles: Development of potent and selective A, A and dual A/A adenosine receptor antagonists.
Abdelrahman A,Yerande SG,Namasivayam V,Klapschinski TA,Alnouri MW,El-Tayeb A,Müller CE
Eur J Med Chem (2020) 186 : 111879 -111879
PubMed 31780082 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 9.00 10.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4797181 1 10.12
CHEMBL4796077 1 10.08
CHEMBL4764086 1 10.01
CHEMBL4784975 1 8.50
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 6.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4797181 IC50 = 0.0763 nM 10.12
CHEMBL4796077 IC50 = 0.084 nM 10.08
CHEMBL4764086 IC50 = 0.0981 nM 10.01
CHEMBL4784975 IC50 = 3.14 nM 8.50
CHEMBL68738 N6-CYCLOPENTYLADENOSINE IC50 = 537.6 nM 6.27