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Assay Detail

CHEMBL664326

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

Binding
Inhibition of recombinant human Cytochrome P450 19A1
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Aromatase (CHEMBL1978)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Fluorine substitution can block CYP3A4 metabolism-dependent inhibition: identification of (S)-N-[1-(4-fluoro-3- morpholin-4-ylphenyl)ethyl]-3- (4-fluorophenyl)acrylamide as an orally bioavailable KCNQ2 opener devoid of CYP3A4 metabolism-dependent inhibition.
Wu YJ, Davis CD, Dworetzky S, Fitzpatrick WC, Harden D, He H, Knox RJ, Newton AE, Philip T, Polson C, Sivarao DV, Sun LQ, Tertyshnikova S, Weaver D, Yeola S, Zoeckler M, Sinz MW.
J Med Chem (2003) 46 : 3778 -3781
PubMed 12930139 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 4.89 4.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL317935 1 4.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL317935 IC50 = 13000.0 nM 4.89