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Assay Detail

CHEMBL645002

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Functional
In vitro inhibitory activity against human acetylcholinesterase
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Acetylcholinesterase (CHEMBL220)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Syntheses and anticholinesterase activity of tetrahydrobenzazepine carbamates.
Chen YL, Liston D, Nielsen J, Chapin D, Dunaiskis A, Hedberg K, Ives J, Johnson J, Jones S.
J Med Chem (1994) 37 : 1996 -2000
PubMed 8027982 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.94 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL413765 1 7.70
CHEMBL61274 1 7.14
CHEMBL433041 EPTASTIGMINE 2.0 1 6.96
CHEMBL413549 1 6.90
CHEMBL94 PHYSOSTIGMINE 3.0 1 6.89
CHEMBL64633 1 6.88
CHEMBL64529 1 6.84
CHEMBL302168 1 6.80
CHEMBL60379 1 6.77
CHEMBL292421 1 6.77
CHEMBL60380 1 6.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL413765 IC50 = 20.0 nM 7.70
CHEMBL61274 IC50 = 72.0 nM 7.14
CHEMBL433041 EPTASTIGMINE IC50 = 110.0 nM 6.96
CHEMBL413549 IC50 = 125.0 nM 6.90
CHEMBL94 PHYSOSTIGMINE IC50 = 128.0 nM 6.89
CHEMBL64633 IC50 = 133.0 nM 6.88
CHEMBL64529 IC50 = 143.0 nM 6.84
CHEMBL302168 IC50 = 159.0 nM 6.80
CHEMBL60379 IC50 = 171.0 nM 6.77
CHEMBL292421 IC50 = 169.0 nM 6.77
CHEMBL60380 IC50 = 206.0 nM 6.69