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Assay Detail

CHEMBL641565

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

Binding
Inhibitory potency against acetylcholinesterase (AChE) of rat cortex homogenate with ethopropazine as BChE inhibitor
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Acetylcholinesterase (CHEMBL3199)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Potent, easily synthesized huperzine A-tacrine hybrid acetylcholinesterase inhibitors.
Carlier PR, Du DM, Han Y, Liu J, Pang YP.
Bioorg Med Chem Lett (1999) 9 : 2335 -2338
PubMed 10476864 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.40 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL32823 1 8.82
CHEMBL76658 1 8.06
CHEMBL77374 1 7.58
CHEMBL74607 1 7.44
CHEMBL1202834 1 7.43
CHEMBL1202835 1 7.37
CHEMBL1202836 1 7.28
CHEMBL76659 1 6.95
CHEMBL395280 HUPERZINE A 2.0 1 6.94
CHEMBL1202837 1 6.91
CHEMBL95 TACRINE 4.0 1 6.65

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL32823 IC50 = 1.5 nM 8.82
CHEMBL76658 IC50 = 8.8 nM 8.06
CHEMBL77374 IC50 = 26.2 nM 7.58
CHEMBL74607 IC50 = 36.3 nM 7.44
CHEMBL1202834 IC50 = 37.1 nM 7.43
CHEMBL1202835 IC50 = 42.6 nM 7.37
CHEMBL1202836 IC50 = 53.1 nM 7.28
CHEMBL76659 IC50 = 112.0 nM 6.95
CHEMBL395280 HUPERZINE A IC50 = 114.0 nM 6.94
CHEMBL1202837 IC50 = 122.0 nM 6.91
CHEMBL95 TACRINE IC50 = 223.0 nM 6.65