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Assay Detail

CHEMBL868602

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Binding
Inhibition of rat brain homogenate AchE
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Acetylcholinesterase (CHEMBL3199)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and efficacy of 1-[bis(4-fluorophenyl)-methyl]piperazine derivatives for acetylcholinesterase inhibition, as a stimulant of central cholinergic neurotransmission in Alzheimer's disease.
Sadashiva CT, Narendra Sharath Chandra JN, Ponnappa KC, Veerabasappa Gowda T, Rangappa KS.
Bioorg Med Chem Lett (2006) 16 : 3932 -3936
PubMed 16735118 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.26 7.73

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL427232 1 7.73
CHEMBL211471 NEOSTIGMINE METHYLSULFATE 4.0 1 7.43
CHEMBL209392 1 7.43
CHEMBL211520 1 7.03
CHEMBL380050 1 6.70
CHEMBL209924 1 -
CHEMBL212162 1 -
CHEMBL212111 1 -
CHEMBL209863 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL427232 IC50 = 18.75 nM 7.73
CHEMBL211471 NEOSTIGMINE METHYLSULFATE IC50 = 37.5 nM 7.43
CHEMBL209392 IC50 = 37.5 nM 7.43
CHEMBL211520 IC50 = 93.75 nM 7.03
CHEMBL380050 IC50 = 200.0 nM 6.70
CHEMBL209924 IC50 - -
CHEMBL212162 IC50 - -
CHEMBL212111 IC50 - -
CHEMBL209863 IC50 - -