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Assay Detail

CHEMBL5628215

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

Binding
Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured after 5 mins by Ellman's method
8
Total Activities
8
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

Synthesis, computational and experimental pharmacological studies for (thio)ether-triazine 5-HT<sub>6</sub>R ligands with noticeable action on AChE/BChE and chalcogen-dependent intrinsic activity in search for new class of drugs against Alzheimer's disease.
Czarnota-Łydka K, Sudoł-Tałaj S, Kucwaj-Brysz K, Kurczab R, Satała G, de Candia M, Samarelli F, Altomare CD, Carocci A, Barbarossa A, Żesławska E, Głuch-Lutwin M, Mordyl B, Kubacka M, Wilczyńska-Zawal N, Jastrzębska-Więsek M, Partyka A, Khan N, Więcek M, Nitek W, Honkisz-Orzechowska E, Latacz G, Wesołowska A, Carrieri A, Handzlik J.
Eur J Med Chem (2023) 259 : 115695 -115695
PubMed 37567058 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.53 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL95 TACRINE 4.0 1 7.60
CHEMBL4873127 1 6.30
CHEMBL502 DONEPEZIL 4.0 1 5.56
CHEMBL5632197 1 5.01
CHEMBL5632758 1 5.00
CHEMBL5632000 1 5.00
CHEMBL5633074 1 4.92
CHEMBL5631952 1 4.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL95 TACRINE IC50 = 25.0 nM 7.60
CHEMBL4873127 IC50 = 500.0 nM 6.30
CHEMBL502 DONEPEZIL IC50 = 2750.0 nM 5.56
CHEMBL5632197 IC50 = 9800.0 nM 5.01
CHEMBL5632758 IC50 = 9950.0 nM 5.00
CHEMBL5632000 IC50 = 10000.0 nM 5.00
CHEMBL5633074 IC50 = 12100.0 nM 4.92
CHEMBL5631952 IC50 = 15000.0 nM 4.82