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Assay Detail

CHEMBL1936218

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

Binding
Displacement of [3H]-DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Pyrrolo- and pyrazolo-[3,4-e][1,2,4]triazolo[1,5-c]pyrimidines as adenosine receptor antagonists.
Baraldi PG, Saponaro G, Aghazadeh Tabrizi M, Baraldi S, Romagnoli R, Moorman AR, Varani K, Borea PA, Preti D.
Bioorg Med Chem (2012) 20 : 1046 -1059
PubMed 22204739 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 6.19 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL332091 1 6.70
CHEMBL302765 1 5.68
CHEMBL17127 SCH-58261 1 -
CHEMBL17121 SCH-63390 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL332091 Ki = 200.0 nM 6.70
CHEMBL302765 Ki = 2100.0 nM 5.68
CHEMBL17127 SCH-58261 Ki > 10000.0 nM -
CHEMBL17121 SCH-63390 Ki > 10000.0 nM -