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Assay Detail

CHEMBL646319

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

Binding
Binding affinity against adenosine A2 receptor using N-[3H]-ethyl adenosine-5-uronamide in rat striatal membranes
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Striatum
Subcellular Membrane
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Adenosine A2 receptor (CHEMBL2094117)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

8-Polycycloalkyl-1,3-dipropylxanthines as potent and selective antagonists for A1-adenosine receptors.
Shimada J, Suzuki F, Nonaka H, Ishii A.
J Med Chem (1992) 35 : 924 -930
PubMed 1548682 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 5.83 6.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL33722 1 6.42
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] 1 6.39
CHEMBL55839 1 6.19
CHEMBL113 CAFFEINE 4.0 1 4.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL33722 Ki = 381.0 nM 6.42
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] Ki = 410.0 nM 6.39
CHEMBL55839 Ki = 640.0 nM 6.19
CHEMBL113 CAFFEINE Ki = 48100.0 nM 4.32