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Assay Detail

CHEMBL4012876

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

Functional
Agonist activity at human adenosine receptor A2B expressed in CHO cell membranes assessed as forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by forskolin addition measured after 10 mins by liquid scintillation counter method
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adenosine receptor A2b (CHEMBL255)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The 1,2,4-Triazolo[4,3-a]pyrazin-3-one as a Versatile Scaffold for the Design of Potent Adenosine Human Receptor Antagonists. Structural Investigations to Target the A2A Receptor Subtype.
Falsini M, Squarcialupi L, Catarzi D, Varano F, Betti M, Dal Ben D, Marucci G, Buccioni M, Volpini R, De Vita T, Cavalli A, Colotta V.
J Med Chem (2017) 60 : 5772 -5790
PubMed 28590753 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 5.30 5.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL464859 NECA 1 5.82
CHEMBL487754 1 4.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL464859 NECA EC50 = 1510.0 nM 5.82
CHEMBL487754 EC50 = 16850.0 nM 4.77