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Assay Detail

CHEMBL646486

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

Binding
Binding of Adenosine A2 receptor in whole rat brain membrane using [3H]CHA as a Radioligand
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

A novel synthesis of xanthines: support for a new binding mode for xanthines with respect to adenosine at adenosine receptors.
Peet NP, Lentz NL, Meng EC, Dudley MW, Ogden AM, Demeter DA, Weintraub HJ, Bey P.
J Med Chem (1990) 33 : 3127 -3130
PubMed 2258897 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.31 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 8.96
CHEMBL45891 1 8.62
CHEMBL106265 8-CYCLOPENTYLTHEOPHYLLINE 1 8.41
CHEMBL321505 1 8.33
CHEMBL62350 8-PHENYL THEOPHYLLINE 1 7.68
CHEMBL262083 N6-PHENYLADENOSINE 1 6.96
CHEMBL262984 1 6.80
CHEMBL388757 N6-BENZYLADENOSINE 1 6.46
CHEMBL337073 1 6.19
CHEMBL340019 1 6.07
CHEMBL1355736 THEOPHYLLINE 4.0 1 5.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL68738 N6-CYCLOPENTYLADENOSINE Ki = 1.1 nM 8.96
CHEMBL45891 Ki = 2.4 nM 8.62
CHEMBL106265 8-CYCLOPENTYLTHEOPHYLLINE Ki = 3.9 nM 8.41
CHEMBL321505 Ki = 4.7 nM 8.33
CHEMBL62350 8-PHENYL THEOPHYLLINE Ki = 20.9 nM 7.68
CHEMBL262083 N6-PHENYLADENOSINE Ki = 110.0 nM 6.96
CHEMBL262984 Ki = 157.0 nM 6.80
CHEMBL388757 N6-BENZYLADENOSINE Ki = 350.0 nM 6.46
CHEMBL337073 Ki = 644.0 nM 6.19
CHEMBL340019 Ki = 848.0 nM 6.07
CHEMBL1355736 THEOPHYLLINE Ki = 1310.0 nM 5.88