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Assay Detail

CHEMBL638447

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Binding
Inhibitory activity on Acetylcholinesterase (AChE) from human erythrocytes
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Acetylcholinesterase (CHEMBL220)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationships of methoctramine-related polyamines as muscular nicotinic receptor noncompetitive antagonists. 3. Effect of inserting the tetraamine backbone into a macrocyclic structure.
Bolognesi ML, Bixel MG, Marucci G, Bartolini M, Krauss M, Angeli P, Antonello A, Rosini M, Tumiatti V, Hucho F, Melchiorre C.
J Med Chem (2002) 45 : 3286 -3295
PubMed 12109912 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.27 6.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL11805 CAPROCTAMINE 1 6.77
CHEMBL324975 1 5.85
CHEMBL327100 1 5.47
CHEMBL27673 METHOCTRAMINE 1 5.27
CHEMBL325740 1 5.21
CHEMBL326308 1 4.80
CHEMBL323655 1 4.48
CHEMBL110045 1 4.27
CHEMBL325505 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL11805 CAPROCTAMINE IC50 = 169.82 nM 6.77
CHEMBL324975 IC50 = 1412.54 nM 5.85
CHEMBL327100 IC50 = 3388.44 nM 5.47
CHEMBL27673 METHOCTRAMINE IC50 = 5370.32 nM 5.27
CHEMBL325740 IC50 = 6165.95 nM 5.21
CHEMBL326308 IC50 = 15848.93 nM 4.80
CHEMBL323655 IC50 = 33113.11 nM 4.48
CHEMBL110045 IC50 = 53703.18 nM 4.27
CHEMBL325505 IC50 = 104712.85 nM -