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Assay Detail

CHEMBL1671585

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

Binding
Dissociation constant for enzyme-inhibitor-substrate complex of human recombinant AChE by Lineweaver-Burk plot analysis
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Acetylcholinesterase (CHEMBL220)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Preparation and in vitro screening of symmetrical bis-isoquinolinium cholinesterase inhibitors bearing various connecting linkage--implications for early Myasthenia gravis treatment.
Musilek K, Komloova M, Holas O, Hrabinova M, Pohanka M, Dohnal V, Nachon F, Dolezal M, Dolezal M, Kuca K.
Eur J Med Chem (2011) 46 : 811 -818
PubMed 21236521 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 6.59 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1669479 AMBENONIUM DICHLORIDE 1 8.22
CHEMBL464538 1 7.30
CHEMBL1669494 1 6.12
CHEMBL1669486 1 6.01
CHEMBL1128 EDROPHONIUM CHLORIDE 4.0 1 5.32
CHEMBL1200970 ETHOPROPAZINE HYDROCHLORIDE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1669479 AMBENONIUM DICHLORIDE Ki = 6.0 nM 8.22
CHEMBL464538 Ki = 50.0 nM 7.30
CHEMBL1669494 Ki = 750.0 nM 6.12
CHEMBL1669486 Ki = 980.0 nM 6.01
CHEMBL1128 EDROPHONIUM CHLORIDE Ki = 4800.0 nM 5.32
CHEMBL1200970 ETHOPROPAZINE HYDROCHLORIDE Ki = 12100000.0 nM -