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Assay Detail

CHEMBL4353636

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Binding
Inhibition of electric eel AChE assessed as reduction in production of H202 using acetylcholine as substrate incubated for 15 mins followed by substrate addition by horse radish peroxidase/Amplex red reagent based fluorescence assay
22
Total Activities
22
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

Dipropargyl substituted diphenylpyrimidines as dual inhibitors of monoamine oxidase and acetylcholinesterase.
Kumar B, Kumar V, Prashar V, Saini S, Dwivedi AR, Bajaj B, Mehta D, Parkash J, Kumar V.
Eur J Med Chem (2019) 177 : 221 -234
PubMed 31151057 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 5.45 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL502 DONEPEZIL 4.0 1 7.52
CHEMBL4514270 1 5.87
CHEMBL4435127 1 5.76
CHEMBL4451426 1 5.75
CHEMBL4449439 1 5.74
CHEMBL4446207 1 5.59
CHEMBL4472217 1 5.36
CHEMBL4454141 1 5.34
CHEMBL4520073 1 5.29
CHEMBL4459207 1 5.23
CHEMBL4450296 1 5.23
CHEMBL4455144 1 5.20
CHEMBL4591817 1 5.17
CHEMBL4455630 1 5.16
CHEMBL4567714 1 5.16
CHEMBL4469654 1 5.16
CHEMBL4456862 1 5.15
CHEMBL4543829 1 5.14
CHEMBL4548899 1 5.12
CHEMBL4554961 1 5.09
CHEMBL8706 CLORGILINE 2.0 1 -
CHEMBL673 PARGYLINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL502 DONEPEZIL IC50 = 30.0 nM 7.52
CHEMBL4514270 IC50 = 1350.0 nM 5.87
CHEMBL4435127 IC50 = 1740.0 nM 5.76
CHEMBL4451426 IC50 = 1760.0 nM 5.75
CHEMBL4449439 IC50 = 1810.0 nM 5.74
CHEMBL4446207 IC50 = 2560.0 nM 5.59
CHEMBL4472217 IC50 = 4390.0 nM 5.36
CHEMBL4454141 IC50 = 4580.0 nM 5.34
CHEMBL4520073 IC50 = 5190.0 nM 5.29
CHEMBL4459207 IC50 = 5880.0 nM 5.23
CHEMBL4450296 IC50 = 5920.0 nM 5.23
CHEMBL4455144 IC50 = 6380.0 nM 5.20
CHEMBL4591817 IC50 = 6730.0 nM 5.17
CHEMBL4455630 IC50 = 6990.0 nM 5.16
CHEMBL4567714 IC50 = 6990.0 nM 5.16
CHEMBL4469654 IC50 = 6940.0 nM 5.16
CHEMBL4456862 IC50 = 7050.0 nM 5.15
CHEMBL4543829 IC50 = 7250.0 nM 5.14
CHEMBL4548899 IC50 = 7530.0 nM 5.12
CHEMBL4554961 IC50 = 8120.0 nM 5.09
CHEMBL8706 CLORGILINE IC50 - -
CHEMBL673 PARGYLINE IC50 - -