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Assay Detail

CHEMBL641720

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

Binding
Displacement of specific [3H]PIA binding from adenosine A1 receptor in rat brain membranes.
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Subcellular Brain membranes
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Adenosine receptor A1 (CHEMBL318)
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 29 5.40 6.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL75772 1 6.29
CHEMBL87496 1 6.14
CHEMBL283196 ALPHA-NAPHTHOFLAVONE 1 6.11
CHEMBL309490 GALANGIN 1 6.06
CHEMBL356036 TETRAMETHYLKAEMPFEROL 1 5.97
CHEMBL348436 CIRSIMARITIN 1 5.92
CHEMBL168080 1 5.89
CHEMBL293776 HISPIDULIN 1 5.79
CHEMBL16807 5-HYDROXYFLAVONE 1 5.66
CHEMBL50 QUERCETIN 3.0 1 5.61
CHEMBL276915 7-HYDROXYFLAVONE 1 5.52
CHEMBL28 APIGENIN 1 5.52
CHEMBL351186 1 5.51
CHEMBL275638 FLAVONE 2.0 1 5.48
CHEMBL148826 1 5.47
CHEMBL44 GENISTEIN 2.0 1 5.30
CHEMBL351895 1 5.26
CHEMBL165387 1 5.15
CHEMBL351246 1 5.12
CHEMBL74852 1 5.09
CHEMBL26260 BETA-NAPHTHOFLAVONE 1 5.06
CHEMBL348920 1 5.05
CHEMBL149938 1 4.94
CHEMBL349609 ARBORININE 1 4.90
CHEMBL42639 1 4.77
CHEMBL345778 1 4.73
CHEMBL75169 1 4.56
CHEMBL439648 1 4.28
CHEMBL147199 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL75772 Ki = 509.0 nM 6.29
CHEMBL87496 Ki = 720.0 nM 6.14
CHEMBL283196 ALPHA-NAPHTHOFLAVONE Ki = 786.0 nM 6.11
CHEMBL309490 GALANGIN Ki = 863.0 nM 6.06
CHEMBL356036 TETRAMETHYLKAEMPFEROL Ki = 1070.0 nM 5.97
CHEMBL348436 CIRSIMARITIN Ki = 1200.0 nM 5.92
CHEMBL168080 Ki = 1290.0 nM 5.89
CHEMBL293776 HISPIDULIN Ki = 1610.0 nM 5.79
CHEMBL16807 5-HYDROXYFLAVONE Ki = 2170.0 nM 5.66
CHEMBL50 QUERCETIN Ki = 2470.0 nM 5.61
CHEMBL276915 7-HYDROXYFLAVONE Ki = 3030.0 nM 5.52
CHEMBL28 APIGENIN Ki = 3000.0 nM 5.52
CHEMBL351186 Ki = 3100.0 nM 5.51
CHEMBL275638 FLAVONE Ki = 3280.0 nM 5.48
CHEMBL148826 Ki = 3400.0 nM 5.47
CHEMBL44 GENISTEIN Ki = 5000.0 nM 5.30
CHEMBL351895 Ki = 5550.0 nM 5.26
CHEMBL165387 Ki = 7100.0 nM 5.15
CHEMBL351246 Ki = 7590.0 nM 5.12
CHEMBL74852 Ki = 8180.0 nM 5.09
CHEMBL26260 BETA-NAPHTHOFLAVONE Ki = 8800.0 nM 5.06
CHEMBL348920 Ki = 8890.0 nM 5.05
CHEMBL149938 Ki = 11600.0 nM 4.94
CHEMBL349609 ARBORININE Ki = 12700.0 nM 4.90
CHEMBL42639 Ki = 17000.0 nM 4.77
CHEMBL345778 Ki = 18800.0 nM 4.73
CHEMBL75169 Ki = 27600.0 nM 4.56
CHEMBL439648 Ki = 52500.0 nM 4.28
CHEMBL147199 Ki - nM -