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Assay Detail

CHEMBL859798

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

Binding
Anticholinesterase activity against human erythrocyte AChE
31
Total Activities
31
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

Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine.
Luo W, Yu QS, Kulkarni SS, Parrish DA, Holloway HW, Tweedie D, Shafferman A, Lahiri DK, Brossi A, Greig NH.
J Med Chem (2006) 49 : 2174 -2185
PubMed 16570913 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 6.75 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL130458 TOLSERINE 1 8.00
CHEMBL205895 1 7.89
CHEMBL464538 1 7.75
CHEMBL426674 1 7.70
CHEMBL433041 EPTASTIGMINE 2.0 1 7.66
CHEMBL502 DONEPEZIL 4.0 1 7.66
CHEMBL54727 1 7.66
CHEMBL205231 1 7.57
CHEMBL94 PHYSOSTIGMINE 3.0 1 7.55
CHEMBL206093 1 7.44
CHEMBL378404 1 7.42
CHEMBL395280 HUPERZINE A 2.0 1 7.33
CHEMBL205940 1 7.25
CHEMBL381926 1 7.09
CHEMBL205340 1 7.03
CHEMBL207777 1 7.01
CHEMBL204895 1 7.00
CHEMBL205335 1 6.85
CHEMBL95 TACRINE 4.0 1 6.72
CHEMBL377283 1 6.31
CHEMBL380830 1 6.21
CHEMBL129837 4-ISOPROPYLPHENSERINE 1 6.12
CHEMBL659 GALANTAMINE 4.0 1 6.10
CHEMBL205967 1 5.62
CHEMBL205321 1 5.46
CHEMBL382207 1 5.41
CHEMBL636 RIVASTIGMINE 4.0 1 5.38
CHEMBL381782 1 5.26
CHEMBL206237 1 5.17
CHEMBL382351 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL130458 TOLSERINE IC50 = 10.0 nM 8.00
CHEMBL205895 IC50 = 13.0 nM 7.89
CHEMBL464538 IC50 = 18.0 nM 7.75
CHEMBL426674 IC50 = 20.0 nM 7.70
CHEMBL433041 EPTASTIGMINE IC50 = 22.0 nM 7.66
CHEMBL502 DONEPEZIL IC50 = 22.0 nM 7.66
CHEMBL54727 IC50 = 22.0 nM 7.66
CHEMBL205231 IC50 = 27.0 nM 7.57
CHEMBL94 PHYSOSTIGMINE IC50 = 28.0 nM 7.55
CHEMBL206093 IC50 = 36.0 nM 7.44
CHEMBL378404 IC50 = 38.0 nM 7.42
CHEMBL395280 HUPERZINE A IC50 = 47.0 nM 7.33
CHEMBL205940 IC50 = 56.0 nM 7.25
CHEMBL381926 IC50 = 82.0 nM 7.09
CHEMBL205340 IC50 = 94.0 nM 7.03
CHEMBL207777 IC50 = 97.0 nM 7.01
CHEMBL204895 IC50 = 100.0 nM 7.00
CHEMBL205335 IC50 = 142.0 nM 6.85
CHEMBL95 TACRINE IC50 = 190.0 nM 6.72
CHEMBL377283 IC50 = 486.0 nM 6.31
CHEMBL380830 IC50 = 610.0 nM 6.21
CHEMBL129837 4-ISOPROPYLPHENSERINE IC50 = 760.0 nM 6.12
CHEMBL659 GALANTAMINE IC50 = 800.0 nM 6.10
CHEMBL205967 IC50 = 2420.0 nM 5.62
CHEMBL205321 IC50 = 3430.0 nM 5.46
CHEMBL382207 IC50 = 3860.0 nM 5.41
CHEMBL636 RIVASTIGMINE IC50 = 4150.0 nM 5.38
CHEMBL381782 IC50 = 5510.0 nM 5.26
CHEMBL206237 IC50 = 6700.0 nM 5.17
CHEMBL382351 IC50 = 9890.0 nM 5.00
CHEMBL494887 TETRAISOPROPYL PYROPHOSPHORAMIDE IC50 = 340000.0 nM -