CYP3A4 Inhibition Assay Service

CYP3A4 for compound screening and profiling assay using luminescence-based method to measure cytochrome P450 enzyme activity.

Target Overview
CAT#

CYP3A4

Enzyme

Human CYP3A4 + P450 Reductase microsomes

Synonym

CYP3A4, cytochrome P450 subfamily IIIA polypeptide 4

Scientific Information

P08684 (https://www.uniprot.org/uniprotkb/P08684/entry)

Assay Properties
Substrate

P450-Glo™ proluciferin Substrate

Reaction

RH + O₂ + NADPH + H⁺ = ROH + H₂O + oxidized [NADPH—hemoprotein reductase]

Readout

Enzymatic activity

Reference Compound IC50s
Compound IC50 (nM)
Ketoconazole 4.6
Verapamil 6810
Montelukast 1730
Tranylcypromine >10000
Cimetidine >10000
Screening Location

Malvern, PA, USA

Further Information

More information can be found on our website CYP450 Inhibition Assay Services.

Reference compound IC50 for CYP3A4