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Assay Detail

CHEMBL5161346

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

Binding
Inhibition of recombinant human AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured every 240 sec by Ellman's method
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Acetylcholinesterase (CHEMBL220)
Type SINGLE PROTEIN
Organism Homo sapiens

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 7.78 9.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2007996 1 9.13
CHEMBL5207628 1 8.71
CHEMBL5200047 1 8.57
CHEMBL5178885 1 7.89
CHEMBL5204900 1 7.84
CHEMBL292314 1 7.84
CHEMBL2021616 1 6.49
CHEMBL5188116 1 5.78
CHEMBL1668934 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2007996 IC50 = 0.74 nM 9.13
CHEMBL5207628 IC50 = 1.94 nM 8.71
CHEMBL5200047 IC50 = 2.71 nM 8.57
CHEMBL5178885 IC50 = 12.9 nM 7.89
CHEMBL5204900 IC50 = 14.5 nM 7.84
CHEMBL292314 IC50 = 14.5 nM 7.84
CHEMBL2021616 IC50 = 321.0 nM 6.49
CHEMBL5188116 IC50 = 1660.0 nM 5.78
CHEMBL1668934 IC50 = 115000.0 nM -