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Assay Detail

CHEMBL636823

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

Binding
Inhibitory activity against acetylcholinesterase in rat brain
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Acetylcholinesterase (CHEMBL3199)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Acetylcholinesterase inhibition by fused dihydroquinazoline compounds
Jaen JC, Gregor VE, Lee C, Davis R, Emmerling M
Bioorg Med Chem Lett (1996) 6 : 737 -742
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.38 7.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL395280 HUPERZINE A 2.0 1 7.03
CHEMBL95 TACRINE 4.0 1 6.70
CHEMBL433041 EPTASTIGMINE 2.0 1 6.22
CHEMBL659 GALANTAMINE 4.0 1 5.75
CHEMBL445130 1 5.72
CHEMBL161880 1 5.32
CHEMBL165726 1 5.03
CHEMBL165304 1 4.82
CHEMBL349977 1 4.79
CHEMBL355821 1 4.75
CHEMBL166194 1 4.45
CHEMBL162734 1 4.00
CHEMBL163362 1 -
CHEMBL165292 1 -
CHEMBL166359 1 -
CHEMBL350496 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL395280 HUPERZINE A IC50 = 94.0 nM 7.03
CHEMBL95 TACRINE IC50 = 200.0 nM 6.70
CHEMBL433041 EPTASTIGMINE IC50 = 600.0 nM 6.22
CHEMBL659 GALANTAMINE IC50 = 1760.0 nM 5.75
CHEMBL445130 IC50 = 1900.0 nM 5.72
CHEMBL161880 IC50 = 4750.0 nM 5.32
CHEMBL165726 IC50 = 9300.0 nM 5.03
CHEMBL165304 IC50 = 15000.0 nM 4.82
CHEMBL349977 IC50 = 16400.0 nM 4.79
CHEMBL355821 IC50 = 18000.0 nM 4.75
CHEMBL166194 IC50 = 35900.0 nM 4.45
CHEMBL162734 IC50 = 100000.0 nM 4.00
CHEMBL163362 IC50 > 100000.0 nM -
CHEMBL165292 IC50 > 100000.0 nM -
CHEMBL166359 IC50 > 100000.0 nM -
CHEMBL350496 IC50 > 100000.0 nM -