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Assay Detail

CHEMBL2345138

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Binding
Inhibition of electric eel AChE using acetylcholine iodide as substrate after 10 mins by Ellman method
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Electrophorus electricus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Acetylcholinesterase (CHEMBL4078)
Type SINGLE PROTEIN
Organism Electrophorus electricus

Publication

Synthesis and biological evaluation of 1,3,4-thiadiazole analogues as novel AChE and BuChE inhibitors.
Skrzypek A, Matysiak J, Niewiadomy A, Bajda M, Szymański P.
Eur J Med Chem (2013) 62 : 311 -319
PubMed 23376249 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 5.95 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2337271 DONEPEZIL HYDROCHLORIDE MONOHYDRATE 1 7.70
CHEMBL54126 NEOSTIGMINE BROMIDE 2.0 1 7.30
CHEMBL396226 1 7.22
CHEMBL2337278 1 7.05
CHEMBL2337272 1 6.80
CHEMBL2337264 1 6.77
CHEMBL2337265 1 6.72
CHEMBL2337269 1 6.17
CHEMBL2337273 1 5.97
CHEMBL2337263 1 5.81
CHEMBL2337274 1 5.81
CHEMBL2337267 1 5.76
CHEMBL2337280 1 5.73
CHEMBL243254 1 5.72
CHEMBL2337268 1 5.67
CHEMBL2337261 1 5.66
CHEMBL2337266 1 4.72
CHEMBL2337262 1 4.71
CHEMBL2337270 1 4.68
CHEMBL2337279 1 4.57
CHEMBL2337277 1 4.34
CHEMBL2337275 1 -
CHEMBL2337276 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2337271 DONEPEZIL HYDROCHLORIDE MONOHYDRATE IC50 = 20.0 nM 7.70
CHEMBL54126 NEOSTIGMINE BROMIDE IC50 = 50.0 nM 7.30
CHEMBL396226 IC50 = 60.0 nM 7.22
CHEMBL2337278 IC50 = 90.0 nM 7.05
CHEMBL2337272 IC50 = 160.0 nM 6.80
CHEMBL2337264 IC50 = 170.0 nM 6.77
CHEMBL2337265 IC50 = 190.0 nM 6.72
CHEMBL2337269 IC50 = 670.0 nM 6.17
CHEMBL2337273 IC50 = 1070.0 nM 5.97
CHEMBL2337263 IC50 = 1560.0 nM 5.81
CHEMBL2337274 IC50 = 1550.0 nM 5.81
CHEMBL2337267 IC50 = 1730.0 nM 5.76
CHEMBL2337280 IC50 = 1870.0 nM 5.73
CHEMBL243254 IC50 = 1890.0 nM 5.72
CHEMBL2337268 IC50 = 2120.0 nM 5.67
CHEMBL2337261 IC50 = 2180.0 nM 5.66
CHEMBL2337266 IC50 = 19210.0 nM 4.72
CHEMBL2337262 IC50 = 19340.0 nM 4.71
CHEMBL2337270 IC50 = 20860.0 nM 4.68
CHEMBL2337279 IC50 = 26700.0 nM 4.57
CHEMBL2337277 IC50 = 45260.0 nM 4.34
CHEMBL2337275 IC50 = 128420.0 nM -
CHEMBL2337276 IC50 = 112010.0 nM -