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Assay Detail

CHEMBL639638

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Binding
Inhibition of (R)-N6-([3H]-phenylisopropyl) adenosine binding to adenosine A1 receptor from rat cortical membranes
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

(E)-1,3-dialkyl-7-methyl-8-(3,4,5-trimethoxystyryl)xanthines: potent and selective adenosine A2 antagonists.
Shimada J, Suzuki F, Nonaka H, Ishii A, Ichikawa S.
J Med Chem (1992) 35 : 2342 -2345
PubMed 1613758 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.57 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] 1 9.05
CHEMBL273094 XANTHINE AMINE CONGENER 1 8.92
CHEMBL22099 1 5.64
CHEMBL1355736 THEOPHYLLINE 4.0 1 4.89
CHEMBL113 CAFFEINE 4.0 1 4.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] Ki = 0.9 nM 9.05
CHEMBL273094 XANTHINE AMINE CONGENER Ki = 1.2 nM 8.92
CHEMBL22099 Ki = 2300.0 nM 5.64
CHEMBL1355736 THEOPHYLLINE Ki = 13000.0 nM 4.89
CHEMBL113 CAFFEINE Ki = 44000.0 nM 4.36