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Assay Detail

CHEMBL4187638

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

Binding
Inhibition of FAAH in mouse brain microsomes using OMP substrate by fluorescence based assay
7
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Tissue Brain
Subcellular microsomes
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Fatty-acid amide hydrolase 1 (CHEMBL3455)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Identification and optimization of soluble epoxide hydrolase inhibitors with dual potency towards fatty acid amide hydrolase.
Kodani SD, Bhakta S, Hwang SH, Pakhomova S, Newcomer ME, Morisseau C, Hammock BD.
Bioorg Med Chem Lett (2018) 28 : 762 -768
PubMed 29366648 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.77 7.96
Inhibition 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL184238 URB-597 1.0 2 7.96
CHEMBL4204424 2 7.92
CHEMBL4216368 1 6.46
CHEMBL4215208 1 6.29
CHEMBL2397148 1 5.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL184238 URB-597 IC50 = 11.0 nM 7.96
CHEMBL4204424 IC50 = 12.0 nM 7.92
CHEMBL4216368 IC50 = 350.0 nM 6.46
CHEMBL4215208 IC50 = 510.0 nM 6.29
CHEMBL2397148 IC50 = 6300.0 nM 5.20
CHEMBL4204424 Inhibition > 80.0 % -
CHEMBL184238 URB-597 Inhibition > 80.0 % -