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Assay Detail

CHEMBL4675240

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

Binding
Inhibition of human CYP1A1 expressed in HEK293 cells assessed as reduction in CYP1A1 mediated B[alpha]P-7,8- dihydrodiol induced-toxicity by measuring EC50 at 3 times of IC50 concentration by MTT assay (Rvb = 1.4 +/ 0.4 uM)
3
Total Activities
3
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
EC50 3 4.89 4.99

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL458131 PONGAMOL 1 4.99
CHEMBL224157 LANCEOLATIN B 1 4.84
CHEMBL577397 PONGAPIN 1 4.83

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL458131 PONGAMOL EC50 = 10200.0 nM 4.99
CHEMBL224157 LANCEOLATIN B EC50 = 14400.0 nM 4.84
CHEMBL577397 PONGAPIN EC50 = 14800.0 nM 4.83