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Assay Detail

CHEMBL644388

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

Binding
Binding affinity towards human adenosine A3 receptor expressed in HEK293 cells using [125I]AB-MECA at 1 uM
3
Total Activities
3
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 A3 (CHEMBL256)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

1,2,4-Triazolo[4,3-a]quinoxalin-1-one: a versatile tool for the synthesis of potent and selective adenosine receptor antagonists.
Colotta V, Catarzi D, Varano F, Cecchi L, Filacchioni G, Martini C, Trincavelli L, Lucacchini A.
J Med Chem (2000) 43 : 1158 -1164
PubMed 10737748 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 5.32 5.99

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL16010 1 5.99
CHEMBL106265 8-CYCLOPENTYLTHEOPHYLLINE 1 5.89
CHEMBL1355736 THEOPHYLLINE 4.0 1 4.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL16010 Ki = 1020.0 nM 5.99
CHEMBL106265 8-CYCLOPENTYLTHEOPHYLLINE Ki = 1300.0 nM 5.89
CHEMBL1355736 THEOPHYLLINE Ki = 86000.0 nM 4.07