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Assay Detail

CHEMBL644774

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

Binding
Binding affinity at Adenosine A2 receptor in rat striatal membranes by [3H]-CGS- 21680 displacement.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Striatum
Subcellular Membrane
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adenosine A2 receptor (CHEMBL2094117)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists.
Karton Y, Jiang JL, Ji XD, Melman N, Olah ME, Stiles GL, Jacobson KA.
J Med Chem (1996) 39 : 2293 -2301
PubMed 8691424 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 4.80 6.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL309490 GALANGIN 1 6.01
CHEMBL76273 1 5.49
CHEMBL72862 1 5.48
CHEMBL275638 FLAVONE 2.0 1 5.46
CHEMBL75772 1 5.19
CHEMBL75590 1 4.94
CHEMBL28626 MORIN 1 4.76
CHEMBL75897 2'-HYDROXY-FLAVANONE 1 4.75
CHEMBL74975 1 4.60
CHEMBL74505 1 4.57
CHEMBL76874 1 4.47
CHEMBL74852 1 4.45
CHEMBL45176 VISNAGIN 1 4.37
CHEMBL75169 1 4.33
CHEMBL76128 1 4.31
CHEMBL309566 1 4.26
CHEMBL449090 1 4.20
CHEMBL78326 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL309490 GALANGIN Ki = 966.0 nM 6.01
CHEMBL76273 Ki = 3220.0 nM 5.49
CHEMBL72862 Ki = 3310.0 nM 5.48
CHEMBL275638 FLAVONE Ki = 3450.0 nM 5.46
CHEMBL75772 Ki = 6450.0 nM 5.19
CHEMBL75590 Ki = 11500.0 nM 4.94
CHEMBL28626 MORIN Ki = 17300.0 nM 4.76
CHEMBL75897 2'-HYDROXY-FLAVANONE Ki = 17600.0 nM 4.75
CHEMBL74975 Ki = 25100.0 nM 4.60
CHEMBL74505 Ki = 26800.0 nM 4.57
CHEMBL76874 Ki = 33800.0 nM 4.47
CHEMBL74852 Ki = 35600.0 nM 4.45
CHEMBL45176 VISNAGIN Ki = 42400.0 nM 4.37
CHEMBL75169 Ki = 46700.0 nM 4.33
CHEMBL76128 Ki = 49000.0 nM 4.31
CHEMBL309566 Ki = 54500.0 nM 4.26
CHEMBL449090 Ki = 63800.0 nM 4.20
CHEMBL78326 Ki = 167000.0 nM -