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Assay Detail

CHEMBL641070

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

Binding
Binding affinity for adenosine A1 receptor using [3H]PIA in rat brain cortical membrane
7
Total Activities
7
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 Expert

Target

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

Publication

Preparation, properties, reactions, and adenosine receptor affinities of sulfophenylxanthine nitrophenyl esters: toward the development of sulfonic acid prodrugs with peroral bioavailability.
Yan L, Müller CE.
J Med Chem (2004) 47 : 1031 -1043
PubMed 14761205 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.57 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL158507 1 8.00
CHEMBL274855 1 7.17
CHEMBL62350 8-PHENYL THEOPHYLLINE 1 7.05
CHEMBL418333 1 6.68
CHEMBL9069 1 6.58
CHEMBL275987 1 5.66
CHEMBL8488 1 4.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL158507 Ki = 10.0 nM 8.00
CHEMBL274855 Ki = 67.0 nM 7.17
CHEMBL62350 8-PHENYL THEOPHYLLINE Ki = 89.0 nM 7.05
CHEMBL418333 Ki = 210.0 nM 6.68
CHEMBL9069 Ki = 260.0 nM 6.58
CHEMBL275987 Ki = 2200.0 nM 5.66
CHEMBL8488 Ki = 14000.0 nM 4.85