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Assay Detail

CHEMBL5112963

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

Binding
Inhibition of human FASN enoyl reductase activity using crotonyl CoA as substrate assessed as inhibition of substrate hydrolysis measured every 1 min for 10 mins in the presence of NADPH by fluorescence based assay
2
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Fatty acid synthase (CHEMBL4158)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Therapeutic Activity of the Lansoprazole Metabolite 5-Hydroxy Lansoprazole Sulfide in Triple-Negative Breast Cancer by Inhibiting the Enoyl Reductase of Fatty Acid Synthase.
Beebe J, Josephraj S, Wang CJ, Danielson J, Cui Q, Huang C, Barlow L, Zhang RH, Zhang T, Nakshatri H, Dong Z, Li X, Liu JY, Zhang JT.
J Med Chem (2022) 65 : 13681 -13691
PubMed 36257066 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 5.77 5.77
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL480 LANSOPRAZOLE 4.0 1 5.77
CHEMBL5196605 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL480 LANSOPRAZOLE Ki = 1700.0 nM 5.77
CHEMBL5196605 Inhibition - % -