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Assay Detail

CHEMBL641886

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

Binding
Inhibitory concentration against rat brain acetylcholinesterase AChE
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Acetylcholinesterase (CHEMBL3199)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Acetylcholinesterase inhibitors: synthesis and structure-activity relationships of omega-[N-methyl-N-(3-alkylcarbamoyloxyphenyl)- methyl]aminoalkoxyheteroaryl derivatives.
Rampa A, Bisi A, Valenti P, Recanatini M, Cavalli A, Andrisano V, Cavrini V, Fin L, Buriani A, Giusti P.
J Med Chem (1998) 41 : 3976 -3986
PubMed 9767635 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 8.26 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL128471 1 9.22
CHEMBL340625 1 8.82
CHEMBL94 PHYSOSTIGMINE 3.0 1 8.70
CHEMBL440526 1 8.70
CHEMBL128202 1 8.40
CHEMBL340427 XANTHOSTIGMINE 1 7.70
CHEMBL128863 1 7.40
CHEMBL130918 1 7.16
CHEMBL131827 1 -
CHEMBL128260 1 -
CHEMBL337999 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL128471 IC50 = 0.6 nM 9.22
CHEMBL340625 IC50 = 1.5 nM 8.82
CHEMBL94 PHYSOSTIGMINE IC50 = 2.0 nM 8.70
CHEMBL440526 IC50 = 2.0 nM 8.70
CHEMBL128202 IC50 = 4.0 nM 8.40
CHEMBL340427 XANTHOSTIGMINE IC50 = 20.0 nM 7.70
CHEMBL128863 IC50 = 40.0 nM 7.40
CHEMBL130918 IC50 = 70.0 nM 7.16
CHEMBL131827 IC50 = 0.009 nM -
CHEMBL128260 IC50 > 1000.0 nM -
CHEMBL337999 IC50 > 100.0 nM -