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Assay Detail

CHEMBL644119

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

Binding
In vitro inhibition of human recombinant AChE.
15
Total Activities
15
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

Quaternary salts of E2020 analogues as acetylcholinesterase inhibitors for the reversal of neuromuscular block.
Clark JK, Cowley P, Muir AW, Palin R, Pow E, Prosser AB, Taylor R, Zhang MQ.
Bioorg Med Chem Lett (2002) 12 : 2565 -2568
PubMed 12182861 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.34 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL87273 1 8.10
CHEMBL87344 1 7.77
CHEMBL502 DONEPEZIL 4.0 1 7.75
CHEMBL87014 1 7.66
CHEMBL314989 1 7.60
CHEMBL87823 1 7.30
CHEMBL86835 1 7.18
CHEMBL86031 1 7.00
CHEMBL432376 1 6.92
CHEMBL313582 1 6.86
CHEMBL313231 1 6.62
CHEMBL659 GALANTAMINE 4.0 1 -
CHEMBL315385 1 -
CHEMBL85404 1 -
CHEMBL611808 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL87273 IC50 = 8.0 nM 8.10
CHEMBL87344 IC50 = 17.0 nM 7.77
CHEMBL502 DONEPEZIL IC50 = 18.0 nM 7.75
CHEMBL87014 IC50 = 22.0 nM 7.66
CHEMBL314989 IC50 = 25.0 nM 7.60
CHEMBL87823 IC50 = 50.0 nM 7.30
CHEMBL86835 IC50 = 66.0 nM 7.18
CHEMBL86031 IC50 = 100.0 nM 7.00
CHEMBL432376 IC50 = 120.0 nM 6.92
CHEMBL313582 IC50 = 139.0 nM 6.86
CHEMBL313231 IC50 = 240.0 nM 6.62
CHEMBL659 GALANTAMINE IC50 ~ 500.0 nM -
CHEMBL315385 IC50 < 500.0 nM -
CHEMBL85404 IC50 ~ 500.0 nM -
CHEMBL611808 IC50 > 100000.0 nM -