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Compound Detail

CHEMBL4165327

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COc1cc2c(cc1OC)C(=O)C(Cc1cc[n+](Cc3ccccc3)cc1Br)C2.[Br-]

Basic Information

ChEMBL ID CHEMBL4165327
Phase Preclinical
Structure Type MOL
InChI Key HJANHZWEMNJHRA-UHFFFAOYSA-M
Parent Compound CHEMBL4299916
Active Moiety CHEMBL4299916
3
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

453.4
MW (Da)
4.40
ALogP
3
HBA
0
HBD
39.4
PSA (Ų)
0.52
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H23Br2NO3
MW 533.26
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness 0.40

Activity Summary

IC50 4 meas. best 9.44

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL220
IC50 9.44 9.44 0.4 2
Acetylcholinesterase
CHEMBL4078
IC50 9.44 9.44 0.4 1
Cholinesterase
CHEMBL5763
IC50 5.75 5.75 1790.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29324339 10.1016/j.ejmech.2017.12.084 Acetylcholinesterase 2
29324339 10.1016/j.ejmech.2017.12.084 Cholinesterase 1
29324339 10.1016/j.ejmech.2017.12.084 Unchecked 1
31437780 10.1016/j.ejmech.2019.111613 Acetylcholinesterase 1
37515920 10.1016/j.ejmech.2023.115670 Acetylcholinesterase 1

Data from ChEMBL 36 via Core Engine