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Assay Detail

CHEMBL636831

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Binding
In vitro inhibitory effect on rat Acetylcholinesterase
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Acetylcholinesterase (CHEMBL3199)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Flexible 1-[(2-aminoethoxy)alkyl]-3-ar(o)yl(thio)ureas as novel acetylcholinesterase inhibitors. Synthesis and biochemical evaluation.
Vidaluc JL, Calmel F, Bigg DC, Carilla E, Briley M.
J Med Chem (1995) 38 : 2969 -2973
PubMed 7636858 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 6.92 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL502 DONEPEZIL 4.0 1 8.77
CHEMBL100718 1 8.22
CHEMBL317541 1 7.89
CHEMBL100020 1 7.89
CHEMBL430679 1 7.82
CHEMBL431058 1 7.58
CHEMBL100819 1 7.52
CHEMBL101518 1 7.52
CHEMBL101940 1 7.26
CHEMBL95 TACRINE 4.0 1 7.20
CHEMBL102142 1 7.11
CHEMBL94 PHYSOSTIGMINE 3.0 1 7.10
CHEMBL100510 1 7.00
CHEMBL100334 1 6.92
CHEMBL101809 1 6.64
CHEMBL659 GALANTAMINE 4.0 1 6.27
CHEMBL101028 1 6.00
CHEMBL101155 1 5.96
CHEMBL99605 1 5.85
CHEMBL329518 1 5.82
CHEMBL101988 1 5.75
CHEMBL98497 1 5.64
CHEMBL99606 1 5.40
CHEMBL420827 1 -
CHEMBL329733 1 -
CHEMBL395280 HUPERZINE A 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL502 DONEPEZIL IC50 = 1.7 nM 8.77
CHEMBL100718 IC50 = 6.0 nM 8.22
CHEMBL317541 IC50 = 13.0 nM 7.89
CHEMBL100020 IC50 = 13.0 nM 7.89
CHEMBL430679 IC50 = 15.0 nM 7.82
CHEMBL431058 IC50 = 26.0 nM 7.58
CHEMBL100819 IC50 = 30.0 nM 7.52
CHEMBL101518 IC50 = 30.0 nM 7.52
CHEMBL101940 IC50 = 55.0 nM 7.26
CHEMBL95 TACRINE IC50 = 63.0 nM 7.20
CHEMBL102142 IC50 = 77.0 nM 7.11
CHEMBL94 PHYSOSTIGMINE IC50 = 80.0 nM 7.10
CHEMBL100510 IC50 = 100.0 nM 7.00
CHEMBL100334 IC50 = 120.0 nM 6.92
CHEMBL101809 IC50 = 230.0 nM 6.64
CHEMBL659 GALANTAMINE IC50 = 538.0 nM 6.27
CHEMBL101028 IC50 = 1000.0 nM 6.00
CHEMBL101155 IC50 = 1100.0 nM 5.96
CHEMBL99605 IC50 = 1400.0 nM 5.85
CHEMBL329518 IC50 = 1500.0 nM 5.82
CHEMBL101988 IC50 = 1800.0 nM 5.75
CHEMBL98497 IC50 = 2300.0 nM 5.64
CHEMBL99606 IC50 = 4000.0 nM 5.40
CHEMBL420827 IC50 > 10000.0 nM -
CHEMBL329733 IC50 > 10000.0 nM -
CHEMBL395280 HUPERZINE A IC50 - nM -