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Assay Detail

CHEMBL645977

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
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 Expert

Target

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

Publication

Fluorosulfonyl- and bis-(beta-chloroethyl)amino-phenylamino functionalized pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine derivatives: irreversible antagonists at the human A3 adenosine receptor and molecular modeling studies.
Baraldi PG, Cacciari B, Moro S, Romagnoli R, Ji Xd, Jacobson KA, Gessi S, Borea PA, Spalluto G.
J Med Chem (2001) 44 : 2735 -2742
PubMed 11495585 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 6.35 6.61

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL65271 1 6.61
CHEMBL329791 1 6.58
CHEMBL330286 1 6.52
CHEMBL302765 1 5.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL65271 Ki = 245.0 nM 6.61
CHEMBL329791 Ki = 261.0 nM 6.58
CHEMBL330286 Ki = 303.0 nM 6.52
CHEMBL302765 Ki = 2056.0 nM 5.69