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Compound Detail

CHEMBL4092048

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COc1cc2c(cc1OC)C(=O)C(Cc1cc[n+](Cc3cccc(Cl)c3)cc1C(N)=O)C2.[Br-]

Basic Information

ChEMBL ID CHEMBL4092048
Phase Preclinical
Structure Type MOL
InChI Key FIWPFDRVIPYHQB-UHFFFAOYSA-N
Parent Compound CHEMBL4116249
Active Moiety CHEMBL4116249
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

451.9
MW (Da)
3.39
ALogP
4
HBA
1
HBD
82.5
PSA (Ų)
0.56
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H24BrClN2O4
MW 531.83
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.01

Activity Summary

IC50 1 meas. best 7.39

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL220
IC50 7.39 7.39 41.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Acetylcholinesterase IC50 = 41.0 nM 7.39 Inhibition of AChE in human erythrocytes using acetylthiocholine iodide as subst... 28613859

Literature References

PubMed DOI Target Context # Activities
28613859 10.1021/acs.jmedchem.7b00702 Acetylcholinesterase 3
28613859 10.1021/acs.jmedchem.7b00702 Salmonella typhimurium 2
28613859 10.1021/acs.jmedchem.7b00702 Cholinesterase 1
28613859 10.1021/acs.jmedchem.7b00702 Amyloid-beta precursor protein 1
28613859 10.1021/acs.jmedchem.7b00702 No relevant target 1
28613859 10.1021/acs.jmedchem.7b00702 SH-SY5Y 1
28613859 10.1021/acs.jmedchem.7b00702 Mus musculus 1

Data from ChEMBL 36 via Core Engine