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Assay Detail

CHEMBL642125

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

Binding
Displacement of specific [3H]-CGS- 21680 binding at Adenosine A2A receptor in bovine striatal membranes.
19
Total Activities
19
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

Synthesis and structure-activity relationships of a new set of 2-arylpyrazolo[3,4-c]quinoline derivatives as adenosine receptor antagonists.
Colotta V, Catarzi D, Varano F, Cecchi L, Filacchioni G, Martini C, Trincavelli L, Lucacchini A.
J Med Chem (2000) 43 : 3118 -3124
PubMed 10956220 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 5.63 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL321441 1 7.30
CHEMBL419002 1 6.48
CHEMBL320805 1 6.48
CHEMBL106520 1 6.07
CHEMBL107414 1 5.92
CHEMBL107637 1 5.80
CHEMBL317270 1 5.66
CHEMBL320741 1 5.62
CHEMBL105913 1 5.43
CHEMBL107446 1 5.43
CHEMBL104115 1 5.42
CHEMBL104425 1 5.38
CHEMBL106986 1 5.30
CHEMBL107116 1 5.27
CHEMBL104177 1 5.24
CHEMBL322263 1 5.24
CHEMBL241987 1 5.07
CHEMBL104178 1 4.95
CHEMBL442005 1 4.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL321441 Ki = 49.5 nM 7.30
CHEMBL419002 Ki = 329.0 nM 6.48
CHEMBL320805 Ki = 331.0 nM 6.48
CHEMBL106520 Ki = 849.0 nM 6.07
CHEMBL107414 Ki = 1200.0 nM 5.92
CHEMBL107637 Ki = 1600.0 nM 5.80
CHEMBL317270 Ki = 2210.0 nM 5.66
CHEMBL320741 Ki = 2400.0 nM 5.62
CHEMBL105913 Ki = 3700.0 nM 5.43
CHEMBL107446 Ki = 3750.0 nM 5.43
CHEMBL104115 Ki = 3800.0 nM 5.42
CHEMBL104425 Ki = 4140.0 nM 5.38
CHEMBL106986 Ki = 5051.0 nM 5.30
CHEMBL107116 Ki = 5400.0 nM 5.27
CHEMBL104177 Ki = 5750.0 nM 5.24
CHEMBL322263 Ki = 5750.0 nM 5.24
CHEMBL241987 Ki = 8600.0 nM 5.07
CHEMBL104178 Ki = 11200.0 nM 4.95
CHEMBL442005 Ki = 11400.0 nM 4.94