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Assay Detail

CHEMBL684541

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

Functional
In vitro reversal of vecuronium-induced neuromuscular block in guinea pig hemi-diaphragm.
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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
EC50 22 6.41 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL86863 1 7.92
CHEMBL87273 1 7.72
CHEMBL245079 HUPERZINE B 1 7.72
CHEMBL502 DONEPEZIL 4.0 1 7.37
CHEMBL87344 1 7.05
CHEMBL314989 1 7.00
CHEMBL87632 1 7.00
CHEMBL315385 1 6.48
CHEMBL87014 1 6.37
CHEMBL87823 1 6.28
CHEMBL85404 1 6.20
CHEMBL87623 1 6.05
CHEMBL659 GALANTAMINE 4.0 1 5.96
CHEMBL75013 ZANAPEZIL 2.0 1 5.94
CHEMBL87883 1 5.84
CHEMBL432376 1 5.80
CHEMBL313231 1 5.77
CHEMBL87955 1 5.73
CHEMBL313778 1 5.57
CHEMBL313234 1 4.36
CHEMBL86031 1 -
CHEMBL611808 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL86863 EC50 = 12.0 nM 7.92
CHEMBL87273 EC50 = 19.0 nM 7.72
CHEMBL245079 HUPERZINE B EC50 = 19.0 nM 7.72
CHEMBL502 DONEPEZIL EC50 = 43.0 nM 7.37
CHEMBL87344 EC50 = 90.0 nM 7.05
CHEMBL314989 EC50 = 100.0 nM 7.00
CHEMBL87632 EC50 = 100.0 nM 7.00
CHEMBL315385 EC50 = 331.0 nM 6.48
CHEMBL87014 EC50 = 430.0 nM 6.37
CHEMBL87823 EC50 = 530.0 nM 6.28
CHEMBL85404 EC50 = 630.0 nM 6.20
CHEMBL87623 EC50 = 890.0 nM 6.05
CHEMBL659 GALANTAMINE EC50 = 1100.0 nM 5.96
CHEMBL75013 ZANAPEZIL EC50 = 1140.0 nM 5.94
CHEMBL87883 EC50 = 1440.0 nM 5.84
CHEMBL432376 EC50 = 1600.0 nM 5.80
CHEMBL313231 EC50 = 1700.0 nM 5.77
CHEMBL87955 EC50 = 1880.0 nM 5.73
CHEMBL313778 EC50 = 2700.0 nM 5.57
CHEMBL313234 EC50 = 43500.0 nM 4.36
CHEMBL86031 EC50 > 3000.0 nM -
CHEMBL611808 EC50 > 10000.0 nM -