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Assay Detail

CHEMBL1763500

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

Binding
Inhibition of human plasmatic BChE by modified Ellman's method
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cholinesterase (CHEMBL1914)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Preparation, in vitro screening and molecular modelling of symmetrical bis-quinolinium cholinesterase inhibitors--implications for early myasthenia gravis treatment.
Komloova M, Musilek K, Horova A, Holas O, Dohnal V, Gunn-Moore F, Kuca K.
Bioorg Med Chem Lett (2011) 21 : 2505 -2509
PubMed 21397501 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 5.63 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL225577 1 7.00
CHEMBL1762003 1 6.70
CHEMBL1761994 1 6.40
CHEMBL104387 1 6.40
CHEMBL105257 1 6.30
CHEMBL105017 1 6.22
CHEMBL1761995 1 6.16
CHEMBL1761999 1 6.10
CHEMBL1200970 ETHOPROPAZINE HYDROCHLORIDE 4.0 1 5.80
CHEMBL601410 1 5.30
CHEMBL1762000 1 5.22
CHEMBL1669479 AMBENONIUM DICHLORIDE 1 5.16
CHEMBL1761991 1 4.89
CHEMBL1762001 1 4.70
CHEMBL1761992 1 4.50
CHEMBL1761993 1 4.47
CHEMBL1761997 1 4.32
CHEMBL1761998 1 -
CHEMBL1128 EDROPHONIUM CHLORIDE 4.0 1 -
CHEMBL1761996 1 -
CHEMBL464538 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL225577 IC50 = 100.0 nM 7.00
CHEMBL1762003 IC50 = 200.0 nM 6.70
CHEMBL1761994 IC50 = 400.0 nM 6.40
CHEMBL104387 IC50 = 400.0 nM 6.40
CHEMBL105257 IC50 = 500.0 nM 6.30
CHEMBL105017 IC50 = 600.0 nM 6.22
CHEMBL1761995 IC50 = 700.0 nM 6.16
CHEMBL1761999 IC50 = 800.0 nM 6.10
CHEMBL1200970 ETHOPROPAZINE HYDROCHLORIDE IC50 = 1600.0 nM 5.80
CHEMBL601410 IC50 = 5000.0 nM 5.30
CHEMBL1762000 IC50 = 6000.0 nM 5.22
CHEMBL1669479 AMBENONIUM DICHLORIDE IC50 = 7000.0 nM 5.16
CHEMBL1761991 IC50 = 13000.0 nM 4.89
CHEMBL1762001 IC50 = 20000.0 nM 4.70
CHEMBL1761992 IC50 = 32000.0 nM 4.50
CHEMBL1761993 IC50 = 34000.0 nM 4.47
CHEMBL1761997 IC50 = 48000.0 nM 4.32
CHEMBL1761998 IC50 = 308000.0 nM -
CHEMBL1128 EDROPHONIUM CHLORIDE IC50 = 1370000.0 nM -
CHEMBL1761996 IC50 = 871000.0 nM -
CHEMBL464538 IC50 = 354000.0 nM -