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Assay Detail

CHEMBL1780345

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

ADMET
Inhibition of CYP1A1 EROD activity assessed as inhibition of deethylation of 7-ethoxyresorufin to resorufin
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Cytochrome P450 1A1 (CHEMBL2231)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Comparative CYP1A1 and CYP1B1 substrate and inhibitor profile of dietary flavonoids.
Androutsopoulos VP, Papakyriakou A, Vourloumis D, Spandidos DA.
Bioorg Med Chem (2011) 19 : 2842 -2849
PubMed 21482471 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 6.46 7.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL117 CHRYSIN 1 7.38
CHEMBL243664 ACACETIN 1 7.35
CHEMBL90568 DIOSMETIN 1 7.05
CHEMBL487402 EUPATORIN 1 6.68
CHEMBL164 MYRICETIN 1 6.43
CHEMBL28 APIGENIN 1 6.41
CHEMBL124885 1 6.20
CHEMBL50 QUERCETIN 3.0 1 6.18
CHEMBL150 KAEMPFEROL 1.0 1 6.12
CHEMBL151 LUTEOLIN 2.0 1 6.05
CHEMBL8260 BAICALEIN 2.0 1 5.91
CHEMBL55415 SCUTELLAREIN 1 5.79
CHEMBL210635 GENKWANIN 1 -
CHEMBL72637 CIRSILIOL 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL117 CHRYSIN Ki = 42.0 nM 7.38
CHEMBL243664 ACACETIN Ki = 45.0 nM 7.35
CHEMBL90568 DIOSMETIN Ki = 89.0 nM 7.05
CHEMBL487402 EUPATORIN Ki = 210.0 nM 6.68
CHEMBL164 MYRICETIN Ki = 370.0 nM 6.43
CHEMBL28 APIGENIN Ki = 390.0 nM 6.41
CHEMBL124885 Ki = 630.0 nM 6.20
CHEMBL50 QUERCETIN Ki = 660.0 nM 6.18
CHEMBL150 KAEMPFEROL Ki = 750.0 nM 6.12
CHEMBL151 LUTEOLIN Ki = 890.0 nM 6.05
CHEMBL8260 BAICALEIN Ki = 1220.0 nM 5.91
CHEMBL55415 SCUTELLAREIN Ki = 1640.0 nM 5.79
CHEMBL210635 GENKWANIN Ki > 2340.0 nM -
CHEMBL72637 CIRSILIOL Ki > 800.0 nM -