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Assay Detail

CHEMBL1100709

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

Binding
Inhibition of human plasma BChE after 5 mins by Ellman's method
18
Total Activities
18
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 and in vitro screening of symmetrical bispyridinium cholinesterase inhibitors bearing different connecting linkage-initial study for Myasthenia gravis implications.
Musilek K, Komloova M, Zavadova V, Holas O, Hrabinova M, Pohanka M, Dohnal V, Nachon F, Dolezal M, Dolezal M, Kuca K, Jung YS.
Bioorg Med Chem Lett (2010) 20 : 1763 -1766
PubMed 20138518 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.22 6.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1081810 1 6.10
CHEMBL54126 NEOSTIGMINE BROMIDE 2.0 1 6.10
CHEMBL225689 1 5.30
CHEMBL105742 1 5.22
CHEMBL430886 1 5.16
CHEMBL225688 1 4.54
CHEMBL1088155 1 4.11
CHEMBL812 PYRIDOSTIGMINE BROMIDE 4.0 1 -
CHEMBL1081126 1 -
CHEMBL1081125 1 -
CHEMBL1081124 1 -
CHEMBL1076550 1 -
CHEMBL1081613 1 -
CHEMBL1081449 1 -
CHEMBL1081448 1 -
CHEMBL389283 1 -
CHEMBL1088019 1 -
CHEMBL1088018 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1081810 IC50 = 800.0 nM 6.10
CHEMBL54126 NEOSTIGMINE BROMIDE IC50 = 800.0 nM 6.10
CHEMBL225689 IC50 = 5000.0 nM 5.30
CHEMBL105742 IC50 = 6000.0 nM 5.22
CHEMBL430886 IC50 = 7000.0 nM 5.16
CHEMBL225688 IC50 = 29000.0 nM 4.54
CHEMBL1088155 IC50 = 78000.0 nM 4.11
CHEMBL812 PYRIDOSTIGMINE BROMIDE IC50 = 16000000.0 nM -
CHEMBL1081126 IC50 = 529000.0 nM -
CHEMBL1081125 IC50 = 1380000.0 nM -
CHEMBL1081124 IC50 = 345000.0 nM -
CHEMBL1076550 IC50 = 1270000.0 nM -
CHEMBL1081613 IC50 = 541000.0 nM -
CHEMBL1081449 IC50 = 2360000.0 nM -
CHEMBL1081448 IC50 = 583000.0 nM -
CHEMBL389283 IC50 = 130000.0 nM -
CHEMBL1088019 IC50 = 120000.0 nM -
CHEMBL1088018 IC50 = 9800000.0 nM -