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Assay Detail

CHEMBL1176720

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

Binding
Inhibition of human plasma BChE pretreated for 30 mins by Ellman technique
16
Total Activities
16
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

Long-acting anticholinesterases for myasthenia gravis: synthesis and activities of quaternary phenylcarbamates of neostigmine, pyridostigmine and physostigmine.
Yu QS, Holloway HW, Luo W, Lahiri DK, Brossi A, Greig NH.
Bioorg Med Chem (2010) 18 : 4687 -4693
PubMed 20627738 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.60 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54577 1 8.22
CHEMBL94 PHYSOSTIGMINE 3.0 1 7.80
CHEMBL1173624 1 7.37
CHEMBL417915 1 7.29
CHEMBL1173090 1 7.29
CHEMBL211471 NEOSTIGMINE METHYLSULFATE 4.0 1 7.22
CHEMBL1173604 1 6.89
CHEMBL1172913 1 6.85
CHEMBL1173605 1 6.68
CHEMBL1173603 1 6.26
CHEMBL812 PYRIDOSTIGMINE BROMIDE 4.0 1 6.05
CHEMBL54727 1 5.81
CHEMBL300143 1 5.71
CHEMBL1171854 1 4.75
CHEMBL1172830 1 4.75
CHEMBL1173543 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54577 IC50 = 6.0 nM 8.22
CHEMBL94 PHYSOSTIGMINE IC50 = 16.0 nM 7.80
CHEMBL1173624 IC50 = 43.0 nM 7.37
CHEMBL417915 IC50 = 51.0 nM 7.29
CHEMBL1173090 IC50 = 51.0 nM 7.29
CHEMBL211471 NEOSTIGMINE METHYLSULFATE IC50 = 60.0 nM 7.22
CHEMBL1173604 IC50 = 130.0 nM 6.89
CHEMBL1172913 IC50 = 140.0 nM 6.85
CHEMBL1173605 IC50 = 210.0 nM 6.68
CHEMBL1173603 IC50 = 550.0 nM 6.26
CHEMBL812 PYRIDOSTIGMINE BROMIDE IC50 = 900.0 nM 6.05
CHEMBL54727 IC50 = 1560.0 nM 5.81
CHEMBL300143 IC50 = 1950.0 nM 5.71
CHEMBL1171854 IC50 = 18000.0 nM 4.75
CHEMBL1172830 IC50 = 18000.0 nM 4.75
CHEMBL1173543 IC50 > 30000.0 nM -