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Assay Detail

CHEMBL5240496

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

Binding
Inhibition of equine BChE using acetylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition and measured after 30 mins by DTNB reagent based Ellman's method
16
Total Activities
16
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

Multitargeting approaches to cognitive impairment: Synthesis of aryl-alkylpiperazines and assessment at cholinesterases, histamine H<sub>3</sub> and dopamine D<sub>3</sub> receptors.
Aranha CMSQ, Reiner-Link D, Leitzbach LR, Lopes FB, Stark H, Fernandes JPS.
Bioorg Med Chem (2023) 78 : 117132 -117132
PubMed 36542960 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 4.53 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL278020 NEOSTIGMINE 4.0 1 6.80
CHEMBL4069293 1 4.78
CHEMBL5280702 1 4.58
CHEMBL5289654 1 4.39
CHEMBL5270151 1 4.36
CHEMBL4293814 1 4.27
CHEMBL5283987 1 4.24
CHEMBL5276899 1 4.23
CHEMBL5267271 1 4.11
CHEMBL5265920 1 4.07
CHEMBL5278711 1 4.01
CHEMBL5289468 1 -
CHEMBL5282002 1 -
CHEMBL5276588 1 -
CHEMBL5270288 1 -
CHEMBL5287235 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL278020 NEOSTIGMINE IC50 = 160.0 nM 6.80
CHEMBL4069293 IC50 = 16700.0 nM 4.78
CHEMBL5280702 IC50 = 26300.0 nM 4.58
CHEMBL5289654 IC50 = 40700.0 nM 4.39
CHEMBL5270151 IC50 = 43700.0 nM 4.36
CHEMBL4293814 IC50 = 53700.0 nM 4.27
CHEMBL5283987 IC50 = 57500.0 nM 4.24
CHEMBL5276899 IC50 = 58900.0 nM 4.23
CHEMBL5267271 IC50 = 78500.0 nM 4.11
CHEMBL5265920 IC50 = 85100.0 nM 4.07
CHEMBL5278711 IC50 = 97700.0 nM 4.01
CHEMBL5289468 IC50 - -
CHEMBL5282002 IC50 - -
CHEMBL5276588 IC50 - -
CHEMBL5270288 IC50 - -
CHEMBL5287235 IC50 - -