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Assay Detail

CHEMBL642124

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

Binding
Binding affinity towards Adenosine A2A receptor of bovine striatal membrane using [3H]-CGS- at 20 uM
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Adenosine receptor A2a (CHEMBL251)
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 9 7.19 8.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL274274 1 8.19
CHEMBL416537 1 7.84
CHEMBL416354 1 7.73
CHEMBL278197 1 7.31
CHEMBL279870 1 7.18
CHEMBL16643 1 7.14
CHEMBL273578 1 7.07
CHEMBL16416 1 6.42
CHEMBL274267 1 5.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL274274 Ki = 6.5 nM 8.19
CHEMBL416537 Ki = 14.6 nM 7.84
CHEMBL416354 Ki = 18.7 nM 7.73
CHEMBL278197 Ki = 49.0 nM 7.31
CHEMBL279870 Ki = 66.0 nM 7.18
CHEMBL16643 Ki = 72.0 nM 7.14
CHEMBL273578 Ki = 85.8 nM 7.07
CHEMBL16416 Ki = 376.0 nM 6.42
CHEMBL274267 Ki = 1370.0 nM 5.86