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Assay Detail

CHEMBL871476

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Binding
Inhibition of Torpedo californica AChE
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Torpedo californica
Confidence 9 — Direct single protein target
Curated By Expert

Target

Acetylcholinesterase (CHEMBL4780)
Type SINGLE PROTEIN
Organism Torpedo californica

Publication

Structural determinants of Torpedo californica acetylcholinesterase inhibition by the novel and orally active carbamate based anti-alzheimer drug ganstigmine (CHF-2819).
Bartolucci C, Siotto M, Ghidini E, Amari G, Bolzoni PT, Racchi M, Villetti G, Delcanale M, Lamba D.
J Med Chem (2006) 49 : 5051 -5058
PubMed 16913695 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.24 5.76

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL539874 GENESERINE 1 5.76
CHEMBL539623 1 5.39
CHEMBL541663 1 5.32
CHEMBL538602 1 5.29
CHEMBL539624 1 5.29
CHEMBL556603 1 5.12
CHEMBL558409 1 5.08
CHEMBL539875 1 5.07
CHEMBL539625 1 5.07
CHEMBL539873 1 5.01
CHEMBL538603 1 -
CHEMBL1201092 RIVASTIGMINE TARTRATE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL539874 GENESERINE IC50 = 1740.0 nM 5.76
CHEMBL539623 IC50 = 4040.0 nM 5.39
CHEMBL541663 IC50 = 4740.0 nM 5.32
CHEMBL538602 IC50 = 5130.0 nM 5.29
CHEMBL539624 IC50 = 5120.0 nM 5.29
CHEMBL556603 IC50 = 7610.0 nM 5.12
CHEMBL558409 IC50 = 8380.0 nM 5.08
CHEMBL539875 IC50 = 8440.0 nM 5.07
CHEMBL539625 IC50 = 8580.0 nM 5.07
CHEMBL539873 IC50 = 9800.0 nM 5.01
CHEMBL538603 IC50 = 186000.0 nM -
CHEMBL1201092 RIVASTIGMINE TARTRATE IC50 = 187200.0 nM -