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Compound Detail

CHEMBL5208725

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c1cc2c(cc1OCCCN1CCCCC1)CN1CCCCC1=N2

Basic Information

ChEMBL ID CHEMBL5208725
Phase Preclinical
Structure Type MOL
InChI Key WHVZYWOSAKGOJG-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

327.5
MW (Da)
3.97
ALogP
4
HBA
0
HBD
28.1
PSA (Ų)
0.77
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H29N3O
MW 327.47
Aromatic Rings 1
Heavy Atoms 24
NP-Likeness -0.70

Activity Summary

IC50 3 meas. best 8.18

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cholinesterase
CHEMBL5763
IC50 8.18 8.18 6.5 1
Acetylcholinesterase
CHEMBL4078
IC50 7.48 7.48 33.3 1
Acetylcholinesterase
CHEMBL220
IC50 6.65 6.65 225.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cholinesterase IC50 = 6.55 nM 8.18 Inhibition of equine serum BuChE 34742016
Acetylcholinesterase IC50 = 33.3 nM 7.48 Inhibition of electric eel AChE 34742016
Acetylcholinesterase IC50 = 225.0 nM 6.65 Inhibition of human AChE 34742016

Literature References

PubMed DOI Target Context # Activities
34742016 10.1016/j.ejmech.2021.113949 Acetylcholinesterase 2
34742016 10.1016/j.ejmech.2021.113949 Cholinesterase 1
34742016 10.1016/j.ejmech.2021.113949 Unchecked 1

Data from ChEMBL 36 via Core Engine