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Compound Detail

CHEMBL4086383

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COc1cc(/C=C/c2cc(N3CCN(C)CC3)c3ccccc3[n+]2C)ccc1N1CCN(C)CC1.[I-]

Basic Information

ChEMBL ID CHEMBL4086383
Phase Preclinical
Structure Type MOL
InChI Key TXLZPXNCLOPJPI-UHFFFAOYSA-M
Parent Compound CHEMBL4117678
Active Moiety CHEMBL4117678
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

472.7
MW (Da)
3.35
ALogP
5
HBA
0
HBD
26.1
PSA (Ų)
0.53
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H38IN5O
MW 599.56
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -0.35

Activity Summary

IC50 1 meas. best 5.38

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL220
IC50 5.38 5.38 4200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Acetylcholinesterase IC50 = 4200.0 nM 5.38 Inhibition of human erythrocyte AChE using acetylthiocholine chloride as substra... 28242549

Literature References

PubMed DOI Target Context # Activities
28242549 10.1016/j.ejmech.2017.02.042 No relevant target 2
28242549 10.1016/j.ejmech.2017.02.042 Acetylcholinesterase 2
28242549 10.1016/j.ejmech.2017.02.042 Cholinesterase 2
28242549 10.1016/j.ejmech.2017.02.042 Amyloid-beta precursor protein 1

Data from ChEMBL 36 via Core Engine