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Assay Detail

CHEMBL4048079

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

Binding
Inhibition of rat serum BChE using butyrylthiocholine chloride as substrate incubated for 15 mins by Ellman's method
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Butyrylcholinesterase (CHEMBL3403)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design, synthesis and biological evaluation of phthalimide-alkylamine derivatives as balanced multifunctional cholinesterase and monoamine oxidase-B inhibitors for the treatment of Alzheimer's disease.
Sang Z, Wang K, Wang H, Yu L, Wang H, Ma Q, Ye M, Han X, Liu W.
Bioorg Med Chem Lett (2017) 27 : 5053 -5059
PubMed 29033232 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 4.77 5.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4075667 1 5.66
CHEMBL502 DONEPEZIL 4.0 1 5.36
CHEMBL4064598 1 5.28
CHEMBL3547159 1 5.08
CHEMBL4096975 1 5.04
CHEMBL4066908 1 5.03
CHEMBL4104552 1 4.88
CHEMBL4091683 1 4.88
CHEMBL4086653 1 4.83
CHEMBL4089264 1 4.83
CHEMBL4066677 1 4.80
CHEMBL4081393 1 4.79
CHEMBL4080466 1 4.79
CHEMBL4077879 1 4.79
CHEMBL4085625 1 4.75
CHEMBL4096963 1 4.74
CHEMBL4069776 1 4.72
CHEMBL3547058 1 4.68
CHEMBL4099414 1 4.65
CHEMBL4094393 1 4.64
CHEMBL4066289 1 4.58
CHEMBL4091015 1 4.56
CHEMBL4070797 1 4.55
CHEMBL4061108 1 4.49
CHEMBL4086843 1 4.48
CHEMBL4089274 1 4.41
CHEMBL4061100 1 4.37
CHEMBL4104698 1 4.35
CHEMBL4076402 1 4.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4075667 IC50 = 2200.0 nM 5.66
CHEMBL502 DONEPEZIL IC50 = 4420.0 nM 5.36
CHEMBL4064598 IC50 = 5300.0 nM 5.28
CHEMBL3547159 IC50 = 8400.0 nM 5.08
CHEMBL4096975 IC50 = 9100.0 nM 5.04
CHEMBL4066908 IC50 = 9400.0 nM 5.03
CHEMBL4104552 IC50 = 13200.0 nM 4.88
CHEMBL4091683 IC50 = 13300.0 nM 4.88
CHEMBL4086653 IC50 = 14800.0 nM 4.83
CHEMBL4089264 IC50 = 14900.0 nM 4.83
CHEMBL4066677 IC50 = 15900.0 nM 4.80
CHEMBL4081393 IC50 = 16200.0 nM 4.79
CHEMBL4080466 IC50 = 16300.0 nM 4.79
CHEMBL4077879 IC50 = 16100.0 nM 4.79
CHEMBL4085625 IC50 = 17900.0 nM 4.75
CHEMBL4096963 IC50 = 18100.0 nM 4.74
CHEMBL4069776 IC50 = 18900.0 nM 4.72
CHEMBL3547058 IC50 = 20700.0 nM 4.68
CHEMBL4099414 IC50 = 22500.0 nM 4.65
CHEMBL4094393 IC50 = 22800.0 nM 4.64
CHEMBL4066289 IC50 = 26200.0 nM 4.58
CHEMBL4091015 IC50 = 27700.0 nM 4.56
CHEMBL4070797 IC50 = 27900.0 nM 4.55
CHEMBL4061108 IC50 = 32400.0 nM 4.49
CHEMBL4086843 IC50 = 32900.0 nM 4.48
CHEMBL4089274 IC50 = 39000.0 nM 4.41
CHEMBL4061100 IC50 = 42900.0 nM 4.37
CHEMBL4104698 IC50 = 44400.0 nM 4.35
CHEMBL4076402 IC50 = 58500.0 nM 4.23