Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4675252

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

Binding
Inhibition of human CYP1A1 expressed in human HEK293 cells using 7-ethoxyresorufin as substrate preincubated for 30 mins followed by substrate additon and measured after 60 mins by fluorescence based assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Furanoflavones pongapin and lanceolatin B blocks the cell cycle and induce senescence in CYP1A1-overexpressing breast cancer cells.
Sharma R,Williams IS,Gatchie L,Sonawane VR,Chaudhuri B,Bharate SB
Bioorg Med Chem (2018) 26 : 6076 -6086
PubMed 30448188 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.42 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL577397 PONGAPIN 1 7.70
CHEMBL224157 LANCEOLATIN B 1 7.70
CHEMBL208484 KARANJIN 1 7.52
CHEMBL4763663 1 6.62
CHEMBL573847 OVALITENONE 1 6.32
CHEMBL4740121 1 6.31
CHEMBL458131 PONGAMOL 1 5.36
CHEMBL583961 PONGAGLABRONE 1 5.19
CHEMBL4793151 1 5.07
CHEMBL283196 ALPHA-NAPHTHOFLAVONE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL577397 PONGAPIN IC50 = 20.0 nM 7.70
CHEMBL224157 LANCEOLATIN B IC50 = 20.0 nM 7.70
CHEMBL208484 KARANJIN IC50 = 30.0 nM 7.52
CHEMBL4763663 IC50 = 240.0 nM 6.62
CHEMBL573847 OVALITENONE IC50 = 480.0 nM 6.32
CHEMBL4740121 IC50 = 490.0 nM 6.31
CHEMBL458131 PONGAMOL IC50 = 4400.0 nM 5.36
CHEMBL583961 PONGAGLABRONE IC50 = 6400.0 nM 5.19
CHEMBL4793151 IC50 = 8600.0 nM 5.07
CHEMBL283196 ALPHA-NAPHTHOFLAVONE IC50 > 10000.0 nM -