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Assay Detail

CHEMBL641349

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

Binding
Affinity at Adenosine A2A receptor in rat striatal membranes by [3H]- CGS 21680 displacement.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Striatum
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Adenosine receptor A2a (CHEMBL302)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Interactions of flavonoids and other phytochemicals with adenosine receptors.
Ji XD, Melman N, Jacobson KA.
J Med Chem (1996) 39 : 781 -788
PubMed 8576921 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 5.03 6.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL309490 GALANGIN 1 6.01
CHEMBL283196 ALPHA-NAPHTHOFLAVONE 1 5.88
CHEMBL87496 1 5.87
CHEMBL276915 7-HYDROXYFLAVONE 1 5.57
CHEMBL348436 CIRSIMARITIN 1 5.52
CHEMBL275638 FLAVONE 2.0 1 5.46
CHEMBL16807 5-HYDROXYFLAVONE 1 5.21
CHEMBL293776 HISPIDULIN 1 5.19
CHEMBL349609 ARBORININE 1 5.19
CHEMBL75772 1 5.19
CHEMBL351246 1 5.16
CHEMBL50 QUERCETIN 3.0 1 5.16
CHEMBL28 APIGENIN 1 5.12
CHEMBL148826 1 4.55
CHEMBL165387 1 4.52
CHEMBL345778 1 4.45
CHEMBL74852 1 4.45
CHEMBL44 GENISTEIN 2.0 1 4.44
CHEMBL75169 1 4.33
CHEMBL149938 1 4.25
CHEMBL348920 1 4.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL309490 GALANGIN Ki = 966.0 nM 6.01
CHEMBL283196 ALPHA-NAPHTHOFLAVONE Ki = 1320.0 nM 5.88
CHEMBL87496 Ki = 1360.0 nM 5.87
CHEMBL276915 7-HYDROXYFLAVONE Ki = 2680.0 nM 5.57
CHEMBL348436 CIRSIMARITIN Ki = 3000.0 nM 5.52
CHEMBL275638 FLAVONE Ki = 3450.0 nM 5.46
CHEMBL16807 5-HYDROXYFLAVONE Ki = 6200.0 nM 5.21
CHEMBL293776 HISPIDULIN Ki = 6480.0 nM 5.19
CHEMBL349609 ARBORININE Ki = 6470.0 nM 5.19
CHEMBL75772 Ki = 6450.0 nM 5.19
CHEMBL351246 Ki = 6980.0 nM 5.16
CHEMBL50 QUERCETIN Ki = 6990.0 nM 5.16
CHEMBL28 APIGENIN Ki = 7580.0 nM 5.12
CHEMBL148826 Ki = 28000.0 nM 4.55
CHEMBL165387 Ki = 29900.0 nM 4.52
CHEMBL345778 Ki = 35400.0 nM 4.45
CHEMBL74852 Ki = 35600.0 nM 4.45
CHEMBL44 GENISTEIN Ki = 36000.0 nM 4.44
CHEMBL75169 Ki = 46700.0 nM 4.33
CHEMBL149938 Ki = 56500.0 nM 4.25
CHEMBL348920 Ki = 84000.0 nM 4.08