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Assay Detail

CHEMBL1787618

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

Binding
Inhibition of electric eel AChE assessed as inhibition of acetylthiocholine chloride substrate hydrolysis incubated for 15 mins before substrate addition measured by spectrophotometry
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Acetylcholinesterase (CHEMBL4078)
Type SINGLE PROTEIN
Organism Electrophorus electricus

Publication

Synthesis and evaluation of heterobivalent tacrine derivatives as potential multi-functional anti-Alzheimer agents.
Luo W, Li YP, He Y, Huang SL, Li D, Gu LQ, Huang ZS.
Eur J Med Chem (2011) 46 : 2609 -2616
PubMed 21497959 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 7.67 8.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1783195 1 8.34
CHEMBL1783237 1 8.34
CHEMBL1783242 1 8.33
CHEMBL1783241 1 8.21
CHEMBL1783194 1 8.13
CHEMBL1783239 1 7.90
CHEMBL1783238 1 7.82
CHEMBL1783240 1 7.82
CHEMBL1783192 1 7.59
CHEMBL1783243 1 7.42
CHEMBL1783193 1 7.36
CHEMBL1783191 1 6.98
CHEMBL1677 TACRINE HYDROCHLORIDE 4.0 1 6.71
CHEMBL1783190 1 6.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1783195 IC50 = 4.55 nM 8.34
CHEMBL1783237 IC50 = 4.61 nM 8.34
CHEMBL1783242 IC50 = 4.7 nM 8.33
CHEMBL1783241 IC50 = 6.14 nM 8.21
CHEMBL1783194 IC50 = 7.48 nM 8.13
CHEMBL1783239 IC50 = 12.5 nM 7.90
CHEMBL1783238 IC50 = 15.1 nM 7.82
CHEMBL1783240 IC50 = 15.3 nM 7.82
CHEMBL1783192 IC50 = 25.6 nM 7.59
CHEMBL1783243 IC50 = 38.5 nM 7.42
CHEMBL1783193 IC50 = 43.6 nM 7.36
CHEMBL1783191 IC50 = 104.4 nM 6.98
CHEMBL1677 TACRINE HYDROCHLORIDE IC50 = 193.0 nM 6.71
CHEMBL1783190 IC50 = 365.2 nM 6.44