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Assay Detail

CHEMBL3419481

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

Binding
Binding affinity to human adenosine A2A receptor
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Adenosine receptor A2a (CHEMBL251)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and biological evaluation of novel 2-((2-(4-(substituted)phenylpiperazin-1-yl)ethyl)amino)-5'-N-ethylcarboxamidoadenosines as potent and selective agonists of the A2A adenosine receptor.
Preti D, Baraldi PG, Saponaro G, Romagnoli R, Aghazadeh Tabrizi M, Baraldi S, Cosconati S, Bruno A, Novellino E, Vincenzi F, Ravani A, Borea PA, Varani K.
J Med Chem (2015) 58 : 3253 -3267
PubMed 25780876 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 7.42 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1950649 APADENOSON 3.0 1 9.30
CHEMBL1096896 UK432097 2.0 1 8.40
CHEMBL1950554 BINODENOSON 3.0 1 6.57
CHEMBL317052 REGADENOSON ANHYDROUS 4.0 1 6.54
CHEMBL1950553 SONEDENOSON 2.0 1 6.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1950649 APADENOSON Ki = 0.5 nM 9.30
CHEMBL1096896 UK432097 Ki = 4.0 nM 8.40
CHEMBL1950554 BINODENOSON Ki = 270.0 nM 6.57
CHEMBL317052 REGADENOSON ANHYDROUS Ki = 290.0 nM 6.54
CHEMBL1950553 SONEDENOSON Ki = 490.0 nM 6.31