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Assay Detail

CHEMBL904692

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

Binding
Displacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cells
10
Total Activities
10
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

Discovery and characterization of 4'-(2-furyl)-N-pyridin-3-yl-4,5'-bipyrimidin-2'-amine (LAS38096), a potent, selective, and efficacious A2B adenosine receptor antagonist.
Vidal B, Nueda A, Esteve C, Domenech T, Benito S, Reinoso RF, Pont M, Calbet M, López R, Cadavid MI, Loza MI, Cárdenas A, Godessart N, Beleta J, Warrellow G, Ryder H.
J Med Chem (2007) 50 : 2732 -2736
PubMed 17469811 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 7.36 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL226238 1 7.80
CHEMBL375293 1 7.77
CHEMBL225972 1 7.62
CHEMBL438306 1 7.55
CHEMBL390600 1 7.47
CHEMBL226236 1 7.41
CHEMBL226237 1 7.16
CHEMBL389040 1 6.94
CHEMBL226188 1 6.94
CHEMBL225982 1 6.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL226238 Ki = 16.0 nM 7.80
CHEMBL375293 Ki = 17.0 nM 7.77
CHEMBL225972 Ki = 24.0 nM 7.62
CHEMBL438306 Ki = 28.0 nM 7.55
CHEMBL390600 Ki = 34.0 nM 7.47
CHEMBL226236 Ki = 39.0 nM 7.41
CHEMBL226237 Ki = 69.0 nM 7.16
CHEMBL389040 Ki = 115.0 nM 6.94
CHEMBL226188 Ki = 116.0 nM 6.94
CHEMBL225982 Ki = 119.0 nM 6.92