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Assay Detail

CHEMBL641990

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

Binding
Binding affinity for Adenosine A2 receptor from Guinea pig membranes
5
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adenosine A2 receptor (CHEMBL2094257)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Synthesis and biological evaluation of the enantiomers of the potent and selective A1-adenosine antagonist 1,3-dipropyl-8-[2-(5,6-epoxynorbonyl)]-xanthine.
Pfister JR, Belardinelli L, Lee G, Lum RT, Milner P, Stanley WC, Linden J, Baker SP, Schreiner G.
J Med Chem (1997) 40 : 1773 -1778
PubMed 9191953 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.42 6.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL52333 ROLOFYLLINE 3.0 1 6.64
CHEMBL298474 3 6.60
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL52333 ROLOFYLLINE Ki = 230.0 nM 6.64
CHEMBL298474 Ki = 250.0 nM 6.60
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] Ki = 320.0 nM 6.50
CHEMBL298474 Ki = 465.0 nM 6.33
CHEMBL298474 Ki = 930.0 nM 6.03