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Assay Detail

CHEMBL649879

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

Binding
Binding affinity against Adenosine A2 receptor using N-[3H]-ethyladenosin-5''-uronamide in rat striatal membranes
8
Total Activities
8
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 8 5.69 6.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL172950 1 6.25
CHEMBL321507 1 6.07
CHEMBL157655 1 5.62
CHEMBL1355736 THEOPHYLLINE 4.0 1 4.80
CHEMBL173327 1 -
CHEMBL173102 1 -
CHEMBL320147 1 -
CHEMBL368276 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL172950 Ki = 560.0 nM 6.25
CHEMBL321507 Ki = 850.0 nM 6.07
CHEMBL157655 Ki = 2400.0 nM 5.62
CHEMBL1355736 THEOPHYLLINE Ki = 16000.0 nM 4.80
CHEMBL173327 Ki > 10000.0 nM -
CHEMBL173102 Ki > 10000.0 nM -
CHEMBL320147 Ki > 100000.0 nM -
CHEMBL368276 Ki > 100000.0 nM -