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Assay Detail

CHEMBL638609

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

Binding
In vitro inhibitory concentration against acetylcholinesterase (AChE) obtained from mouse brain homogenate.
49
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Acetylcholinesterase (CHEMBL3198)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Synthesis and structure-activity relationships of acetylcholinesterase inhibitors: 1-benzyl-4-(2-phthalimidoethyl)piperidine and related derivatives.
Sugimoto H, Tsuchiya Y, Sugumi H, Higurashi K, Karibe N, Iimura Y, Sasaki A, Araki S, Yamanishi Y, Yamatsu K.
J Med Chem (1992) 35 : 4542 -4548
PubMed 1469686 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 49 7.09 9.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL542744 1 9.25
CHEMBL94 PHYSOSTIGMINE 3.0 1 9.16
CHEMBL138107 1 8.92
CHEMBL140228 1 8.66
CHEMBL140999 1 8.62
CHEMBL433678 1 8.55
CHEMBL342413 1 8.38
CHEMBL138552 1 8.35
CHEMBL126354 1 8.27
CHEMBL140770 1 8.10
CHEMBL139353 1 8.06
CHEMBL141001 1 8.05
CHEMBL138442 1 7.96
CHEMBL105874 1 7.90
CHEMBL141276 1 7.89
CHEMBL140106 1 7.89
CHEMBL140990 1 7.77
CHEMBL140737 1 7.75
CHEMBL141042 1 7.64
CHEMBL106891 1 7.52
CHEMBL55312 1 7.46
CHEMBL127527 1 7.34
CHEMBL340672 1 7.28
CHEMBL141167 1 7.19
CHEMBL340621 1 7.19
CHEMBL95 TACRINE 4.0 1 7.09
CHEMBL333909 1 7.01
CHEMBL141352 1 6.97
CHEMBL56470 1 6.77
CHEMBL340609 1 6.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL542744 IC50 = 0.56 nM 9.25
CHEMBL94 PHYSOSTIGMINE IC50 = 0.69 nM 9.16
CHEMBL138107 IC50 = 1.2 nM 8.92
CHEMBL140228 IC50 = 2.2 nM 8.66
CHEMBL140999 IC50 = 2.4 nM 8.62
CHEMBL433678 IC50 = 2.8 nM 8.55
CHEMBL342413 IC50 = 4.2 nM 8.38
CHEMBL138552 IC50 = 4.5 nM 8.35
CHEMBL126354 IC50 = 5.4 nM 8.27
CHEMBL140770 IC50 = 8.0 nM 8.10
CHEMBL139353 IC50 = 8.8 nM 8.06
CHEMBL141001 IC50 = 9.0 nM 8.05
CHEMBL138442 IC50 = 11.0 nM 7.96
CHEMBL105874 IC50 = 12.5 nM 7.90
CHEMBL140106 IC50 = 13.0 nM 7.89
CHEMBL141276 IC50 = 13.0 nM 7.89
CHEMBL140990 IC50 = 17.0 nM 7.77
CHEMBL140737 IC50 = 18.0 nM 7.75
CHEMBL141042 IC50 = 23.0 nM 7.64
CHEMBL106891 IC50 = 30.0 nM 7.52
CHEMBL55312 IC50 = 35.0 nM 7.46
CHEMBL127527 IC50 = 46.0 nM 7.34
CHEMBL340672 IC50 = 52.0 nM 7.28
CHEMBL340621 IC50 = 64.0 nM 7.19
CHEMBL141167 IC50 = 65.0 nM 7.19
CHEMBL95 TACRINE IC50 = 81.0 nM 7.09
CHEMBL333909 IC50 = 98.0 nM 7.01
CHEMBL141352 IC50 = 108.0 nM 6.97
CHEMBL56470 IC50 = 170.0 nM 6.77
CHEMBL340609 IC50 = 205.0 nM 6.69
CHEMBL123909 IC50 = 240.0 nM 6.62
CHEMBL141515 IC50 = 270.0 nM 6.57
CHEMBL141622 IC50 = 340.0 nM 6.47
CHEMBL336686 IC50 = 440.0 nM 6.36
CHEMBL55014 IC50 = 560.0 nM 6.25
CHEMBL141873 IC50 = 590.0 nM 6.23
CHEMBL125578 IC50 = 660.0 nM 6.18
CHEMBL141801 IC50 = 700.0 nM 6.16
CHEMBL141810 IC50 = 800.0 nM 6.10
CHEMBL141853 IC50 = 830.0 nM 6.08
CHEMBL142014 IC50 = 1000.0 nM 6.00
CHEMBL141203 IC50 = 1100.0 nM 5.96
CHEMBL140328 IC50 = 1200.0 nM 5.92
CHEMBL142013 IC50 = 1600.0 nM 5.80
CHEMBL326868 IC50 = 3000.0 nM 5.52
CHEMBL140948 IC50 = 6800.0 nM 5.17
CHEMBL140769 IC50 = 9400.0 nM 5.03
CHEMBL140936 IC50 = 12000.0 nM 4.92
CHEMBL419184 IC50 = 27000.0 nM 4.57