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Assay Detail

CHEMBL4180913

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

Binding
Inhibition of rat brain AChE using acetylthiocholine iodide as substrate by spectroscopic method
18
Total Activities
18
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

Acetylcholinesterase (CHEMBL3199)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Exploration of multi-target potential of chromen-4-one based compounds in Alzheimer's disease: Design, synthesis and biological evaluations.
Singh M, Kaur M, Singh N, Silakari O.
Bioorg Med Chem (2017) 25 : 6273 -6285
PubMed 29089261 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.74 8.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4217941 1 8.23
CHEMBL4207594 1 8.21
CHEMBL4208825 1 8.19
CHEMBL4213552 1 8.17
CHEMBL4214058 1 8.11
CHEMBL4204793 1 8.08
CHEMBL502 DONEPEZIL 4.0 1 7.90
CHEMBL4209658 1 7.87
CHEMBL4207152 1 7.81
CHEMBL4218884 1 7.78
CHEMBL4210581 1 7.76
CHEMBL16751 1 7.46
CHEMBL345778 1 7.43
CHEMBL485247 1 7.36
CHEMBL4205720 1 7.32
CHEMBL4216881 1 7.24
CHEMBL4203490 1 7.18
CHEMBL4218485 1 7.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4217941 IC50 = 5.87 nM 8.23
CHEMBL4207594 IC50 = 6.12 nM 8.21
CHEMBL4208825 IC50 = 6.48 nM 8.19
CHEMBL4213552 IC50 = 6.77 nM 8.17
CHEMBL4214058 IC50 = 7.7 nM 8.11
CHEMBL4204793 IC50 = 8.25 nM 8.08
CHEMBL502 DONEPEZIL IC50 = 12.7 nM 7.90
CHEMBL4209658 IC50 = 13.53 nM 7.87
CHEMBL4207152 IC50 = 15.6 nM 7.81
CHEMBL4218884 IC50 = 16.5 nM 7.78
CHEMBL4210581 IC50 = 17.3 nM 7.76
CHEMBL16751 IC50 = 35.0 nM 7.46
CHEMBL345778 IC50 = 37.3 nM 7.43
CHEMBL485247 IC50 = 44.2 nM 7.36
CHEMBL4205720 IC50 = 48.12 nM 7.32
CHEMBL4216881 IC50 = 57.2 nM 7.24
CHEMBL4203490 IC50 = 65.7 nM 7.18
CHEMBL4218485 IC50 = 67.2 nM 7.17