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Assay Detail

CHEMBL883650

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

Binding
Binding affinity towards human Adenosine A2b receptor expressed in HEK293 cells using 5 nM [3H]DPCPX
7
Total Activities
7
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

2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
Minetti P, Tinti MO, Carminati P, Castorina M, Di Cesare MA, Di Serio S, Gallo G, Ghirardi O, Giorgi F, Giorgi L, Piersanti G, Bartoccini F, Tarzia G.
J Med Chem (2005) 48 : 6887 -6896
PubMed 16250647 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.89 8.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL68500 ALLOXAZINE 1 8.42
CHEMBL198942 1 7.75
CHEMBL197682 1 6.85
CHEMBL196258 1 6.82
CHEMBL197669 ST1535 1.0 1 6.45
CHEMBL198200 1 6.29
CHEMBL196259 1 5.63

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL68500 ALLOXAZINE Ki = 3.8 nM 8.42
CHEMBL198942 Ki = 18.0 nM 7.75
CHEMBL197682 Ki = 140.0 nM 6.85
CHEMBL196258 Ki = 153.0 nM 6.82
CHEMBL197669 ST1535 Ki = 352.3 nM 6.45
CHEMBL198200 Ki = 518.0 nM 6.29
CHEMBL196259 Ki = 2330.0 nM 5.63