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Assay Detail

CHEMBL874440

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

Binding
Inhibitory concentration against human erythrocyte Acetylcholinesterase
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Acetylcholinesterase (CHEMBL220)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel anticholinesterases based on the molecular skeletons of furobenzofuran and methanobenzodioxepine.
Luo W, Yu QS, Zhan M, Parrish D, Deschamps JR, Kulkarni SS, Holloway HW, Alley GM, Lahiri DK, Brossi A, Greig NH.
J Med Chem (2005) 48 : 986 -994
PubMed 15715468 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.84 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL300143 1 8.00
CHEMBL362049 1 7.89
CHEMBL433041 EPTASTIGMINE 2.0 1 7.66
CHEMBL74926 PHENSERINE 1 7.66
CHEMBL502 DONEPEZIL 4.0 1 7.66
CHEMBL178770 1 7.64
CHEMBL362444 1 7.57
CHEMBL94 PHYSOSTIGMINE 3.0 1 7.55
CHEMBL395280 HUPERZINE A 2.0 1 7.33
CHEMBL178294 1 7.25
CHEMBL367795 1 7.09
CHEMBL361409 1 7.03
CHEMBL539624 1 6.90
CHEMBL95 TACRINE 4.0 1 6.72
CHEMBL369554 1 6.44
CHEMBL417915 1 6.12
CHEMBL659 GALANTAMINE 4.0 1 6.10
CHEMBL362704 1 6.08
CHEMBL179320 1 5.58
CHEMBL178132 1 5.41
CHEMBL636 RIVASTIGMINE 4.0 1 5.38
CHEMBL178792 1 5.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL300143 IC50 = 10.0 nM 8.00
CHEMBL362049 IC50 = 13.0 nM 7.89
CHEMBL433041 EPTASTIGMINE IC50 = 22.0 nM 7.66
CHEMBL74926 PHENSERINE IC50 = 22.0 nM 7.66
CHEMBL502 DONEPEZIL IC50 = 22.0 nM 7.66
CHEMBL178770 IC50 = 23.0 nM 7.64
CHEMBL362444 IC50 = 27.0 nM 7.57
CHEMBL94 PHYSOSTIGMINE IC50 = 28.0 nM 7.55
CHEMBL395280 HUPERZINE A IC50 = 47.0 nM 7.33
CHEMBL178294 IC50 = 56.0 nM 7.25
CHEMBL367795 IC50 = 82.0 nM 7.09
CHEMBL361409 IC50 = 94.0 nM 7.03
CHEMBL539624 IC50 = 125.0 nM 6.90
CHEMBL95 TACRINE IC50 = 190.0 nM 6.72
CHEMBL369554 IC50 = 360.0 nM 6.44
CHEMBL417915 IC50 = 760.0 nM 6.12
CHEMBL659 GALANTAMINE IC50 = 800.0 nM 6.10
CHEMBL362704 IC50 = 830.0 nM 6.08
CHEMBL179320 IC50 = 2650.0 nM 5.58
CHEMBL178132 IC50 = 3860.0 nM 5.41
CHEMBL636 RIVASTIGMINE IC50 = 4150.0 nM 5.38
CHEMBL178792 IC50 = 4300.0 nM 5.37