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Assay Detail

CHEMBL875789

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

Binding
In vitro inhibitory activity against human AchE (Acetylcholinesterase)
22
Total Activities
17
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

Syntheses, resolution, and structure-activity relationships of potent acetylcholinesterase inhibitors: 8-carbaphysostigmine analogues.
Chen YL, Nielsen J, Hedberg K, Dunaiskis A, Jones S, Russo L, Johnson J, Ives J, Liston D.
J Med Chem (1992) 35 : 1429 -1434
PubMed 1573636 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.64 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL34222 3 7.70
CHEMBL416586 3 7.44
CHEMBL286690 1 7.16
CHEMBL284938 1 7.11
CHEMBL433041 EPTASTIGMINE 2.0 1 6.96
CHEMBL32966 1 6.94
CHEMBL94 PHYSOSTIGMINE 3.0 1 6.89
CHEMBL32964 1 6.81
CHEMBL33161 1 6.75
CHEMBL284369 1 6.68
CHEMBL287691 1 6.60
CHEMBL32543 2 6.29
CHEMBL33098 1 6.20
CHEMBL33727 1 5.97
CHEMBL33173 1 5.88
CHEMBL32653 1 5.66
CHEMBL34002 1 4.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL34222 IC50 = 20.0 nM 7.70
CHEMBL416586 IC50 = 36.0 nM 7.44
CHEMBL34222 IC50 = 45.0 nM 7.35
CHEMBL416586 IC50 = 58.0 nM 7.24
CHEMBL286690 IC50 = 69.0 nM 7.16
CHEMBL284938 IC50 = 77.0 nM 7.11
CHEMBL433041 EPTASTIGMINE IC50 = 110.0 nM 6.96
CHEMBL32966 IC50 = 114.0 nM 6.94
CHEMBL94 PHYSOSTIGMINE IC50 = 128.0 nM 6.89
CHEMBL32964 IC50 = 154.0 nM 6.81
CHEMBL33161 IC50 = 176.0 nM 6.75
CHEMBL416586 IC50 = 211.0 nM 6.68
CHEMBL284369 IC50 = 208.0 nM 6.68
CHEMBL34222 IC50 = 233.0 nM 6.63
CHEMBL287691 IC50 = 253.0 nM 6.60
CHEMBL32543 IC50 = 518.0 nM 6.29
CHEMBL32543 IC50 = 546.0 nM 6.26
CHEMBL33098 IC50 = 629.0 nM 6.20
CHEMBL33727 IC50 = 1076.0 nM 5.97
CHEMBL33173 IC50 = 1330.0 nM 5.88
CHEMBL32653 IC50 = 2192.0 nM 5.66
CHEMBL34002 IC50 = 12487.0 nM 4.90