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Assay Detail

CHEMBL3375254

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

Binding
Inhibition of AChE (unknown origin)
4
Total Activities
4
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, biological evaluation, and crystal structure of a novel nanomolar selective butyrylcholinesterase inhibitor.
Brus B, Košak U, Turk S, Pišlar A, Coquelle N, Kos J, Stojan J, Colletier JP, Gobec S.
J Med Chem (2014) 57 : 8167 -8179
PubMed 25226236 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.24 6.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL95 TACRINE 4.0 1 6.72
CHEMBL1206 ETHOPROPAZINE 4.0 1 6.58
CHEMBL129837 4-ISOPROPYLPHENSERINE 1 6.12
CHEMBL636 RIVASTIGMINE 4.0 1 5.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL95 TACRINE IC50 = 190.0 nM 6.72
CHEMBL1206 ETHOPROPAZINE IC50 = 260.0 nM 6.58
CHEMBL129837 4-ISOPROPYLPHENSERINE IC50 = 750.0 nM 6.12
CHEMBL636 RIVASTIGMINE IC50 = 3030.0 nM 5.52