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Assay Detail

CHEMBL5161348

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

Binding
Inhibition of recombinant mouse sEH using CMNPC as substrate preincubated for 5 mins followed by substrate addition and measured every 30 sec for 10 mins for by fluorescence based assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Bifunctional epoxide hydrolase 2 (CHEMBL4140)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery and In Vivo Proof of Concept of a Highly Potent Dual Inhibitor of Soluble Epoxide Hydrolase and Acetylcholinesterase for the Treatment of Alzheimer's Disease.
Codony S, Pont C, Griñán-Ferré C, Di Pede-Mattatelli A, Calvó-Tusell C, Feixas F, Osuna S, Jarné-Ferrer J, Naldi M, Bartolini M, Loza MI, Brea J, Pérez B, Bartra C, Sanfeliu C, Juárez-Jiménez J, Morisseau C, Hammock BD, Pallàs M, Vázquez S, Muñoz-Torrero D.
J Med Chem (2022) 65 : 4909 -4925
PubMed 35271276 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.87 8.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1668934 1 8.55
CHEMBL5204900 1 7.92
CHEMBL5188116 1 7.84
CHEMBL5200047 1 7.82
CHEMBL5178885 1 7.65
CHEMBL5207628 1 7.46
CHEMBL292314 1 -
CHEMBL2007996 1 -
CHEMBL2021616 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1668934 IC50 = 2.8 nM 8.55
CHEMBL5204900 IC50 = 12.1 nM 7.92
CHEMBL5188116 IC50 = 14.5 nM 7.84
CHEMBL5200047 IC50 = 15.0 nM 7.82
CHEMBL5178885 IC50 = 22.3 nM 7.65
CHEMBL5207628 IC50 = 34.3 nM 7.46
CHEMBL292314 IC50 > 50000.0 nM -
CHEMBL2007996 IC50 > 50000.0 nM -
CHEMBL2021616 IC50 > 50000.0 nM -