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Assay Detail

CHEMBL642327

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

Binding
Inhibition of binding to membranes from HEK293 cells expressing human Adenosine A2 receptor
5
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 5 — Multiple protein complex / RNA
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 6.55 6.97

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL52333 ROLOFYLLINE 3.0 1 6.97
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] 1 6.80
CHEMBL298474 3 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL52333 ROLOFYLLINE Ki = 108.0 nM 6.97
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] Ki = 157.0 nM 6.80
CHEMBL298474 Ki = 201.0 nM 6.70
CHEMBL298474 Ki = 475.0 nM 6.32
CHEMBL298474 Ki = 1100.0 nM 5.96