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Assay Detail

CHEMBL3606141

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

Binding
Inhibition of equine serum BChE pre-incubated for 5 mins before butyrylthiocholineiodide substrate addition by Ellman's method
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Equus caballus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cholinesterase (CHEMBL5763)
Type SINGLE PROTEIN
Organism Equus caballus

Publication

Discovery of new acetylcholinesterase inhibitors with small core structures through shape-based virtual screening.
Chen Y, Liu ZL, Fu TM, Li W, Xu XL, Sun HP.
Bioorg Med Chem Lett (2015) 25 : 3442 -3446
PubMed 26212777 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.61 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL130880 IPIDACRINE 2.0 1 7.16
CHEMBL3605836 1 6.96
CHEMBL3605838 1 6.48
CHEMBL1531257 1 6.34
CHEMBL95 TACRINE 4.0 1 6.09
CHEMBL283841 1 5.65
CHEMBL1616296 1 5.05
CHEMBL1617348 1 4.80
CHEMBL226970 1 4.51
CHEMBL1478435 1 4.44
CHEMBL3605837 1 4.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL130880 IPIDACRINE IC50 = 70.0 nM 7.16
CHEMBL3605836 IC50 = 110.0 nM 6.96
CHEMBL3605838 IC50 = 330.0 nM 6.48
CHEMBL1531257 IC50 = 460.0 nM 6.34
CHEMBL95 TACRINE IC50 = 820.0 nM 6.09
CHEMBL283841 IC50 = 2250.0 nM 5.65
CHEMBL1616296 IC50 = 8920.0 nM 5.05
CHEMBL1617348 IC50 = 15940.0 nM 4.80
CHEMBL226970 IC50 = 30680.0 nM 4.51
CHEMBL1478435 IC50 = 36150.0 nM 4.44
CHEMBL3605837 IC50 = 60910.0 nM 4.21