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Assay Detail

CHEMBL642726

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

Binding
Inhibition of acetylcholinesterase (AChE) in electric eel (type V-S) by modified radiometric assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Electrophorus electricus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Acetylcholinesterase (CHEMBL4078)
Type SINGLE PROTEIN
Organism Electrophorus electricus

Publication

The synthesis and in vitro acetylcholinesterase and butyrylcholinesterase inhibitory activity of tacrine (Cognex) derivaties
Gregor VE, Emmerling MR, Lee C, Moore CJ
Bioorg Med Chem Lett (1992) 2 : 861 -864
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.67 8.63

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL352500 1 8.63
CHEMBL292314 1 8.54
CHEMBL134057 1 8.35
CHEMBL368196 1 8.19
CHEMBL502 DONEPEZIL 4.0 1 8.04
CHEMBL95 TACRINE 4.0 1 8.03
CHEMBL431844 1 7.93
CHEMBL369661 1 7.44
CHEMBL62084 1 7.40
CHEMBL51934 VELNACRINE 2.0 1 7.22
CHEMBL172118 1 7.11
CHEMBL94 PHYSOSTIGMINE 3.0 1 6.56
CHEMBL355740 1 6.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL352500 IC50 = 2.33 nM 8.63
CHEMBL292314 IC50 = 2.87 nM 8.54
CHEMBL134057 IC50 = 4.43 nM 8.35
CHEMBL368196 IC50 = 6.52 nM 8.19
CHEMBL502 DONEPEZIL IC50 = 9.2 nM 8.04
CHEMBL95 TACRINE IC50 = 9.33 nM 8.03
CHEMBL431844 IC50 = 11.67 nM 7.93
CHEMBL369661 IC50 = 36.0 nM 7.44
CHEMBL62084 IC50 = 40.0 nM 7.40
CHEMBL51934 VELNACRINE IC50 = 59.83 nM 7.22
CHEMBL172118 IC50 = 77.7 nM 7.11
CHEMBL94 PHYSOSTIGMINE IC50 = 275.0 nM 6.56
CHEMBL355740 IC50 = 493.3 nM 6.31