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Compound Detail

CHEMBL4093514

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CN1CCN(c2ccc(/C=C/c3cc(N4CCN(C)CC4)c4ccccc4[n+]3C)cc2)CC1.[I-]

Basic Information

ChEMBL ID CHEMBL4093514
Phase Preclinical
Structure Type MOL
InChI Key HDXJLMAVGSLTCE-UHFFFAOYSA-M
Parent Compound CHEMBL4116742
Active Moiety CHEMBL4116742
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

442.6
MW (Da)
3.34
ALogP
4
HBA
0
HBD
16.8
PSA (Ų)
0.58
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H36IN5
MW 569.54
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.49

Activity Summary

IC50 1 meas. best 5.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL220
IC50 5.6 5.6 2500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Acetylcholinesterase IC50 = 2500.0 nM 5.6 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