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Assay Detail

CHEMBL643373

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

Binding
Inhibition of acetylcholinesterase.
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Acetylcholinesterase (CHEMBL220)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Imino 1,2,3,4-tetrahydrocyclopent[b]indole carbamates as dual inhibitors of acetylcholinesterase and monoamine oxidase
Fink DM, Palermo M, Bores GM, Huger FP, Kurys BE, Merriman MC, Olsen GE, Petko W, O'Malley GJ
Bioorg Med Chem Lett (1996) 6 : 625 -630
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.35 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL433041 EPTASTIGMINE 2.0 1 8.05
CHEMBL158946 1 7.22
CHEMBL160836 1 6.85
CHEMBL160219 1 6.80
CHEMBL155350 1 6.80
CHEMBL156861 1 6.75
CHEMBL155754 1 6.64
CHEMBL445916 1 6.64
CHEMBL157182 1 6.17
CHEMBL348607 1 5.50
CHEMBL156931 1 5.47
CHEMBL155863 1 5.42
CHEMBL156630 1 5.38
CHEMBL350464 1 5.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL433041 EPTASTIGMINE IC50 = 9.0 nM 8.05
CHEMBL158946 IC50 = 60.0 nM 7.22
CHEMBL160836 IC50 = 140.0 nM 6.85
CHEMBL160219 IC50 = 160.0 nM 6.80
CHEMBL155350 IC50 = 160.0 nM 6.80
CHEMBL156861 IC50 = 180.0 nM 6.75
CHEMBL155754 IC50 = 230.0 nM 6.64
CHEMBL445916 IC50 = 230.0 nM 6.64
CHEMBL157182 IC50 = 670.0 nM 6.17
CHEMBL348607 IC50 = 3170.0 nM 5.50
CHEMBL156931 IC50 = 3360.0 nM 5.47
CHEMBL155863 IC50 = 3840.0 nM 5.42
CHEMBL156630 IC50 = 4190.0 nM 5.38
CHEMBL350464 IC50 = 5680.0 nM 5.25