Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1787217

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

Binding
Inhibition of Equine serum BChE using butyrylthiocholine iodide as a substrate after 20 mins by Ellman's assay
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Equus caballus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cholinesterase (CHEMBL5763)
Type SINGLE PROTEIN
Organism Equus caballus

Publication

Quinolizidinyl derivatives of bi- and tricyclic systems as potent inhibitors of acetyl- and butyrylcholinesterase with potential in Alzheimer's disease.
Tasso B, Catto M, Nicolotti O, Novelli F, Tonelli M, Giangreco I, Pisani L, Sparatore A, Boido V, Carotti A, Sparatore F.
Eur J Med Chem (2011) 46 : 2170 -2184
PubMed 21459491 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 45 5.82 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1782718 1 6.82
CHEMBL251940 PERICIAZINE 2.0 1 6.64
CHEMBL1782742 1 6.47
CHEMBL1782719 1 6.39
CHEMBL1782733 1 6.37
CHEMBL1782735 1 6.33
CHEMBL1782709 1 6.29
CHEMBL1782724 1 6.20
CHEMBL1782743 1 6.16
CHEMBL1206 ETHOPROPAZINE 4.0 1 6.14
CHEMBL1782737 1 6.13
CHEMBL1782736 1 6.12
CHEMBL1782730 1 6.08
CHEMBL1782739 1 6.07
CHEMBL1782741 1 6.06
CHEMBL1782714 1 6.06
CHEMBL1782738 1 6.05
CHEMBL1782721 1 6.03
CHEMBL1782720 1 6.02
CHEMBL1782713 1 5.96
CHEMBL1782725 1 5.96
CHEMBL1782734 1 5.92
CHEMBL1782715 1 5.85
CHEMBL1201342 METHIXENE 4.0 1 5.80
CHEMBL1782723 1 5.70
CHEMBL1782712 1 5.70
CHEMBL1782708 LUPINYLPHENOTHIAZINE 1 5.70
CHEMBL1782711 1 5.66
CHEMBL1782717 1 5.66
CHEMBL1782716 1 5.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1782718 IC50 = 150.0 nM 6.82
CHEMBL251940 PERICIAZINE IC50 = 230.0 nM 6.64
CHEMBL1782742 IC50 = 340.0 nM 6.47
CHEMBL1782719 IC50 = 410.0 nM 6.39
CHEMBL1782733 IC50 = 430.0 nM 6.37
CHEMBL1782735 IC50 = 470.0 nM 6.33
CHEMBL1782709 IC50 = 510.0 nM 6.29
CHEMBL1782724 IC50 = 630.0 nM 6.20
CHEMBL1782743 IC50 = 690.0 nM 6.16
CHEMBL1206 ETHOPROPAZINE IC50 = 720.0 nM 6.14
CHEMBL1782737 IC50 = 740.0 nM 6.13
CHEMBL1782736 IC50 = 750.0 nM 6.12
CHEMBL1782730 IC50 = 840.0 nM 6.08
CHEMBL1782739 IC50 = 860.0 nM 6.07
CHEMBL1782714 IC50 = 870.0 nM 6.06
CHEMBL1782741 IC50 = 870.0 nM 6.06
CHEMBL1782738 IC50 = 890.0 nM 6.05
CHEMBL1782721 IC50 = 930.0 nM 6.03
CHEMBL1782720 IC50 = 950.0 nM 6.02
CHEMBL1782713 IC50 = 1100.0 nM 5.96
CHEMBL1782725 IC50 = 1100.0 nM 5.96
CHEMBL1782734 IC50 = 1200.0 nM 5.92
CHEMBL1782715 IC50 = 1400.0 nM 5.85
CHEMBL1201342 METHIXENE IC50 = 1600.0 nM 5.80
CHEMBL1782723 IC50 = 2000.0 nM 5.70
CHEMBL1782712 IC50 = 2000.0 nM 5.70
CHEMBL1782708 LUPINYLPHENOTHIAZINE IC50 = 2000.0 nM 5.70
CHEMBL1782711 IC50 = 2200.0 nM 5.66
CHEMBL1782717 IC50 = 2200.0 nM 5.66
CHEMBL1782716 IC50 = 2200.0 nM 5.66
CHEMBL1782731 HOMOLUPINANOYLPHENOTHIAZINE IC50 = 3000.0 nM 5.52
CHEMBL609132 IC50 = 3000.0 nM 5.52
CHEMBL1782729 IC50 = 3300.0 nM 5.48
CHEMBL1782728 IC50 = 3800.0 nM 5.42
CHEMBL1782710 IC50 = 4000.0 nM 5.40
CHEMBL1782722 IC50 = 4200.0 nM 5.38
CHEMBL1782747 IC50 = 4300.0 nM 5.37
CHEMBL7568 QUINACRINE IC50 = 4500.0 nM 5.35
CHEMBL1782744 IC50 = 4700.0 nM 5.33
CHEMBL1782732 IC50 = 4800.0 nM 5.32
CHEMBL1782746 IC50 = 5400.0 nM 5.27
CHEMBL1782727 IC50 = 5500.0 nM 5.26
CHEMBL1782748 IC50 = 5800.0 nM 5.24
CHEMBL570 TRIFLUPROMAZINE IC50 = 7400.0 nM 5.13
CHEMBL1782726 IC50 = 8100.0 nM 5.09