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Assay Detail

CHEMBL861175

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Binding
Anticholinesterase activity against human plasma BChE
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cholinesterase (CHEMBL1914)
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 34 6.71 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL381926 1 8.70
CHEMBL204895 1 8.52
CHEMBL205340 1 8.40
CHEMBL205231 1 8.40
CHEMBL433041 EPTASTIGMINE 2.0 1 8.30
CHEMBL206642 1 7.89
CHEMBL204732 1 7.82
CHEMBL94 PHYSOSTIGMINE 3.0 1 7.80
CHEMBL382207 1 7.77
CHEMBL380830 1 7.64
CHEMBL205826 1 7.64
CHEMBL377283 1 7.55
CHEMBL636 RIVASTIGMINE 4.0 1 7.43
CHEMBL206237 1 7.40
CHEMBL95 TACRINE 4.0 1 7.33
CHEMBL129837 4-ISOPROPYLPHENSERINE 1 7.30
CHEMBL205321 1 7.27
CHEMBL205940 1 7.25
CHEMBL205967 1 6.92
CHEMBL494887 TETRAISOPROPYL PYROPHOSPHORAMIDE 1 6.01
CHEMBL381782 1 5.93
CHEMBL205895 1 5.81
CHEMBL54727 1 5.81
CHEMBL130458 TOLSERINE 1 5.71
CHEMBL382351 1 5.60
CHEMBL502 DONEPEZIL 4.0 1 5.38
CHEMBL383013 1 5.29
CHEMBL205335 1 5.29
CHEMBL659 GALANTAMINE 4.0 1 5.14
CHEMBL426674 1 4.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL381926 IC50 = 2.0 nM 8.70
CHEMBL204895 IC50 = 3.0 nM 8.52
CHEMBL205340 IC50 = 4.0 nM 8.40
CHEMBL205231 IC50 = 4.0 nM 8.40
CHEMBL433041 EPTASTIGMINE IC50 = 5.0 nM 8.30
CHEMBL206642 IC50 = 13.0 nM 7.89
CHEMBL204732 IC50 = 15.0 nM 7.82
CHEMBL94 PHYSOSTIGMINE IC50 = 16.0 nM 7.80
CHEMBL382207 IC50 = 17.0 nM 7.77
CHEMBL380830 IC50 = 23.0 nM 7.64
CHEMBL205826 IC50 = 23.0 nM 7.64
CHEMBL377283 IC50 = 28.0 nM 7.55
CHEMBL636 RIVASTIGMINE IC50 = 37.0 nM 7.43
CHEMBL206237 IC50 = 40.0 nM 7.40
CHEMBL95 TACRINE IC50 = 47.0 nM 7.33
CHEMBL129837 4-ISOPROPYLPHENSERINE IC50 = 50.0 nM 7.30
CHEMBL205321 IC50 = 54.0 nM 7.27
CHEMBL205940 IC50 = 56.0 nM 7.25
CHEMBL205967 IC50 = 120.0 nM 6.92
CHEMBL494887 TETRAISOPROPYL PYROPHOSPHORAMIDE IC50 = 980.0 nM 6.01
CHEMBL381782 IC50 = 1180.0 nM 5.93
CHEMBL205895 IC50 = 1560.0 nM 5.81
CHEMBL54727 IC50 = 1560.0 nM 5.81
CHEMBL130458 TOLSERINE IC50 = 1950.0 nM 5.71
CHEMBL382351 IC50 = 2490.0 nM 5.60
CHEMBL502 DONEPEZIL IC50 = 4150.0 nM 5.38
CHEMBL383013 IC50 = 5100.0 nM 5.29
CHEMBL205335 IC50 = 5100.0 nM 5.29
CHEMBL659 GALANTAMINE IC50 = 7300.0 nM 5.14
CHEMBL426674 IC50 = 11400.0 nM 4.94
CHEMBL206093 IC50 = 36400.0 nM 4.44
CHEMBL464538 IC50 = 48000.0 nM 4.32
CHEMBL378404 IC50 = 52000.0 nM 4.28
CHEMBL395280 HUPERZINE A IC50 > 10000.0 nM -