Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3375245

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

Binding
Inhibition of recombinant human BChE by Ellman 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

Cholinesterase (CHEMBL1914)
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 9 7.02 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL95 TACRINE 4.0 1 7.92
CHEMBL3338394 1 7.89
CHEMBL3338391 1 7.68
CHEMBL636 RIVASTIGMINE 4.0 1 7.52
CHEMBL129837 4-ISOPROPYLPHENSERINE 1 7.30
CHEMBL3338395 1 6.78
CHEMBL1206 ETHOPROPAZINE 4.0 1 6.52
CHEMBL3338392 1 5.87
CHEMBL3338393 1 5.67

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL95 TACRINE IC50 = 12.0 nM 7.92
CHEMBL3338394 IC50 = 13.0 nM 7.89
CHEMBL3338391 IC50 = 21.0 nM 7.68
CHEMBL636 RIVASTIGMINE IC50 = 30.0 nM 7.52
CHEMBL129837 4-ISOPROPYLPHENSERINE IC50 = 50.0 nM 7.30
CHEMBL3338395 IC50 = 166.0 nM 6.78
CHEMBL1206 ETHOPROPAZINE IC50 = 300.0 nM 6.52
CHEMBL3338392 IC50 = 1360.0 nM 5.87
CHEMBL3338393 IC50 = 2150.0 nM 5.67